PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 11779033-14 2001 In accordance with this finding, indapamide (5 x 10(-4) M) caused a 95% to 99% decrease in the early elevation of c-fos expression as evaluated by northern blot analysis of mRNA induced after serum addition. Indapamide 33-43 Fos proto-oncogene, AP-1 transcription factor subunit Homo sapiens 114-119 9346894-2 1997 It is the primary receptor for the immunosuppressant actions of the drug FK506 in whose presence FKBP12 binds to and inhibits calcineurin, disrupting interleukin formation in lymphocytes. Tacrolimus 73-78 FKBP prolyl isomerase 1A Homo sapiens 97-103 9346894-4 1997 We now report that FKBP12 binds the IP3R at residues 1400-1401, a leucyl-prolyl dipeptide epitope that structurally resembles FK506. Tacrolimus 126-131 FKBP prolyl isomerase 1A Homo sapiens 19-25 9346894-4 1997 We now report that FKBP12 binds the IP3R at residues 1400-1401, a leucyl-prolyl dipeptide epitope that structurally resembles FK506. Tacrolimus 126-131 inositol 1,4,5-trisphosphate receptor type 3 Homo sapiens 36-40 9346894-6 1997 We propose that FK506 promotes an FKBP12-calcineurin interaction by mimicking structurally similar dipeptide epitopes present within proteins that use FKBP12 to anchor calcineurin to the appropriate physiologic substrates. Tacrolimus 16-21 FKBP prolyl isomerase 1A Homo sapiens 34-40 9346894-6 1997 We propose that FK506 promotes an FKBP12-calcineurin interaction by mimicking structurally similar dipeptide epitopes present within proteins that use FKBP12 to anchor calcineurin to the appropriate physiologic substrates. Tacrolimus 16-21 FKBP prolyl isomerase 1A Homo sapiens 151-157 9355847-8 1997 The associated changes in the expression of CD11c, CD29, and CD31 were also significantly altered by FK506. Tacrolimus 101-106 integrin subunit alpha X Homo sapiens 44-49 9355847-8 1997 The associated changes in the expression of CD11c, CD29, and CD31 were also significantly altered by FK506. Tacrolimus 101-106 integrin subunit beta 1 Homo sapiens 51-55 9355847-8 1997 The associated changes in the expression of CD11c, CD29, and CD31 were also significantly altered by FK506. Tacrolimus 101-106 platelet and endothelial cell adhesion molecule 1 Homo sapiens 61-65 9349985-3 1997 The effects of cyclosporine A (CsA), tacrolimus (FK506), and dexamethasone (DEX) on cytokine-induced production of interleukin (IL)-8 in a human colonic cancer cell line (HT-29) were examined. Tacrolimus 49-54 C-X-C motif chemokine ligand 8 Homo sapiens 115-133 9336339-4 1997 The expression of interferon-gamma mRNA in reverse transcriptase-polymerase chain reaction in the ear was inhibited by FK-506 and cyclosporin A. Tacrolimus 119-125 interferon gamma Mus musculus 18-34 9336339-6 1997 Contrary to the above in vivo findings, the immunosuppressors, FK-506 and cyclosporin A, inhibited the production of interferon-gamma and interleukin-2 by cultured Th1 cells (1E10.H2 cells) and of interleukin-4 and -5 by Th2 cells (D10.G4.1 cells) in vitro. Tacrolimus 63-69 interferon gamma Mus musculus 117-133 9336339-6 1997 Contrary to the above in vivo findings, the immunosuppressors, FK-506 and cyclosporin A, inhibited the production of interferon-gamma and interleukin-2 by cultured Th1 cells (1E10.H2 cells) and of interleukin-4 and -5 by Th2 cells (D10.G4.1 cells) in vitro. Tacrolimus 63-69 interleukin 2 Mus musculus 138-151 9336339-6 1997 Contrary to the above in vivo findings, the immunosuppressors, FK-506 and cyclosporin A, inhibited the production of interferon-gamma and interleukin-2 by cultured Th1 cells (1E10.H2 cells) and of interleukin-4 and -5 by Th2 cells (D10.G4.1 cells) in vitro. Tacrolimus 63-69 negative elongation factor complex member C/D, Th1l Mus musculus 164-167 9336339-6 1997 Contrary to the above in vivo findings, the immunosuppressors, FK-506 and cyclosporin A, inhibited the production of interferon-gamma and interleukin-2 by cultured Th1 cells (1E10.H2 cells) and of interleukin-4 and -5 by Th2 cells (D10.G4.1 cells) in vitro. Tacrolimus 63-69 interleukin 4 Mus musculus 197-217 9336339-6 1997 Contrary to the above in vivo findings, the immunosuppressors, FK-506 and cyclosporin A, inhibited the production of interferon-gamma and interleukin-2 by cultured Th1 cells (1E10.H2 cells) and of interleukin-4 and -5 by Th2 cells (D10.G4.1 cells) in vitro. Tacrolimus 63-69 heart and neural crest derivatives expressed 2 Mus musculus 221-224 9336339-7 1997 These results indicated that FK-506 and cyclosporin A selectively inhibited the Th1 cell-mediated contact dermatitis and potentiated the Th2 cell-mediated IgE antibody production in vivo. Tacrolimus 29-35 negative elongation factor complex member C/D, Th1l Mus musculus 80-83 9336339-7 1997 These results indicated that FK-506 and cyclosporin A selectively inhibited the Th1 cell-mediated contact dermatitis and potentiated the Th2 cell-mediated IgE antibody production in vivo. Tacrolimus 29-35 heart and neural crest derivatives expressed 2 Mus musculus 137-140 9336339-9 1997 However, because FK-506 and cyclosporin A inhibited the production of cytokines by both Th1 and Th2 cells in vitro and these two immunosuppressors showed higher selectivity toward inhibiting Th1 cell-mediated reactions by limitations in vivo experiments. Tacrolimus 17-23 negative elongation factor complex member C/D, Th1l Mus musculus 88-91 9336339-9 1997 However, because FK-506 and cyclosporin A inhibited the production of cytokines by both Th1 and Th2 cells in vitro and these two immunosuppressors showed higher selectivity toward inhibiting Th1 cell-mediated reactions by limitations in vivo experiments. Tacrolimus 17-23 heart and neural crest derivatives expressed 2 Mus musculus 96-99 9336339-9 1997 However, because FK-506 and cyclosporin A inhibited the production of cytokines by both Th1 and Th2 cells in vitro and these two immunosuppressors showed higher selectivity toward inhibiting Th1 cell-mediated reactions by limitations in vivo experiments. Tacrolimus 17-23 negative elongation factor complex member C/D, Th1l Mus musculus 191-194 9349628-0 1997 Inhibition of CREB- and cAMP response element-mediated gene transcription by the immunosuppressive drugs cyclosporin A and FK506 in T cells. Tacrolimus 123-128 cAMP responsive element binding protein 1 Homo sapiens 14-18 9349628-1 1997 The clinically important immunosuppressant drugs cyclosporin A and FK506 (tacrolimus) inhibit in T-cells calcineurin phosphatase activity and nuclear translocation of the cytosolic component of the transcription factor nuclear factor of activated T-cells (NF-ATc) that is involved in the induction of early genes during T-cell activation. Tacrolimus 67-72 nuclear factor of activated T cells 1 Homo sapiens 256-262 9349628-1 1997 The clinically important immunosuppressant drugs cyclosporin A and FK506 (tacrolimus) inhibit in T-cells calcineurin phosphatase activity and nuclear translocation of the cytosolic component of the transcription factor nuclear factor of activated T-cells (NF-ATc) that is involved in the induction of early genes during T-cell activation. Tacrolimus 74-84 nuclear factor of activated T cells 1 Homo sapiens 256-262 9295299-10 1997 The immunosuppressants cyclosporin A and FK506 abolish calcineurin-mediated induction of CTF-1 activity. Tacrolimus 41-46 cardiotrophin 1 Mus musculus 89-94 10837558-1 1997 The objective of this section is to evaluate the contributions of hepatic metabolism, intestinal metabolism and intestinal p-glycoprotein to the pharmacokinetics of orally administered cyclosporine and tacrolimus. Tacrolimus 202-212 ATP binding cassette subfamily B member 1 Homo sapiens 123-137 10837558-2 1997 Cyclosporine and tacrolimus are metabolized primarily by cytochrome P450 3A4 (CYP3A4) in the liver and small intestine. Tacrolimus 17-27 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 57-76 10837558-2 1997 Cyclosporine and tacrolimus are metabolized primarily by cytochrome P450 3A4 (CYP3A4) in the liver and small intestine. Tacrolimus 17-27 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 78-84 10837558-4 1997 Cyclosporine and tacrolimus are also substrates for p-glycoprotein, which acts as a counter-transport pump, actively transporting cyclosporine and tacrolimus back into the intestinal lumen. Tacrolimus 17-27 ATP binding cassette subfamily B member 1 Homo sapiens 52-66 10837558-4 1997 Cyclosporine and tacrolimus are also substrates for p-glycoprotein, which acts as a counter-transport pump, actively transporting cyclosporine and tacrolimus back into the intestinal lumen. Tacrolimus 147-157 ATP binding cassette subfamily B member 1 Homo sapiens 52-66 10837558-14 1997 It seems that compounds that alter (either induce or inhibit) CYP3A4 and/or p-glycoprotein will alter the oral pharmacokinetics of cyclosporine and tacrolimus. Tacrolimus 148-158 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 62-68 10837558-14 1997 It seems that compounds that alter (either induce or inhibit) CYP3A4 and/or p-glycoprotein will alter the oral pharmacokinetics of cyclosporine and tacrolimus. Tacrolimus 148-158 ATP binding cassette subfamily B member 1 Homo sapiens 76-90 9344552-1 1997 The immunosuppressant drugs FK506 and cyclosporin A inhibit T-cell proliferation via a common mechanism: calcineurin inhibition following binding to their respective binding proteins, the peptidyl prolyl isomerases FKBP-12 and cyclophilin A. Tacrolimus 28-33 FKBP prolyl isomerase 1A Rattus norvegicus 215-222 9344552-1 1997 The immunosuppressant drugs FK506 and cyclosporin A inhibit T-cell proliferation via a common mechanism: calcineurin inhibition following binding to their respective binding proteins, the peptidyl prolyl isomerases FKBP-12 and cyclophilin A. Tacrolimus 28-33 peptidylprolyl isomerase A Rattus norvegicus 227-240 9349628-3 1997 Previous studies in pancreatic islet cell lines have shown that cyclosporin A and FK506 through inhibition of calcineurin interfere also with the function of the transcription factor cAMP response element binding protein (CREB) that is activated by cAMP and calcium signals and binds to cAMP/calcium response elements (CRE). Tacrolimus 82-87 cAMP responsive element binding protein 1 Homo sapiens 183-220 9349628-3 1997 Previous studies in pancreatic islet cell lines have shown that cyclosporin A and FK506 through inhibition of calcineurin interfere also with the function of the transcription factor cAMP response element binding protein (CREB) that is activated by cAMP and calcium signals and binds to cAMP/calcium response elements (CRE). Tacrolimus 82-87 cAMP responsive element binding protein 1 Homo sapiens 222-226 9349628-4 1997 By transient expression of CRE-reporter genes or GAL4-CREB fusion proteins, the present study shows that inhibition of CREB/CRE-directed transcription by cyclosporin A and FK506 occurs in a great variety of cell types including in cell lines derived from tissues in which adverse effects of the immunosuppressants develop. Tacrolimus 172-177 galectin 4 Homo sapiens 49-53 9349628-4 1997 By transient expression of CRE-reporter genes or GAL4-CREB fusion proteins, the present study shows that inhibition of CREB/CRE-directed transcription by cyclosporin A and FK506 occurs in a great variety of cell types including in cell lines derived from tissues in which adverse effects of the immunosuppressants develop. Tacrolimus 172-177 cAMP responsive element binding protein 1 Homo sapiens 54-58 9349628-4 1997 By transient expression of CRE-reporter genes or GAL4-CREB fusion proteins, the present study shows that inhibition of CREB/CRE-directed transcription by cyclosporin A and FK506 occurs in a great variety of cell types including in cell lines derived from tissues in which adverse effects of the immunosuppressants develop. Tacrolimus 172-177 cAMP responsive element binding protein 1 Homo sapiens 119-123 9349628-6 1997 When taken together with recent evidence for an essential role of CREB in T-cell activation and proliferation, the present results suggest that inhibition of CREB/CRE-directed transcription may be a molecular mechanism of the immunosuppressive effect of cyclosporin A and FK506. Tacrolimus 272-277 cAMP responsive element binding protein 1 Homo sapiens 158-162 9396011-9 1997 By influencing phosphorylation of neuronal nitric oxide synthase, FKBP12 regulates nitric oxide formation, which is reduced by FK506. Tacrolimus 127-132 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 66-72 9325011-4 1997 The dependence on Ca2+ in the induction of GM-CSF, but not of apoptosis, was further confirmed by the inhibition of TNF- or IL-1-induced cytokine production by cyclosporin A or FK506, drugs that block the Ca2+/calmodulin-dependent protein Ser/Thr phosphatase calcineurin. Tacrolimus 177-182 colony stimulating factor 2 Rattus norvegicus 43-49 9325011-4 1997 The dependence on Ca2+ in the induction of GM-CSF, but not of apoptosis, was further confirmed by the inhibition of TNF- or IL-1-induced cytokine production by cyclosporin A or FK506, drugs that block the Ca2+/calmodulin-dependent protein Ser/Thr phosphatase calcineurin. Tacrolimus 177-182 tumor necrosis factor Rattus norvegicus 116-119 9268302-5 1997 In Jurkat cells, TLiSA1/PTA1 mRNA and surface protein expression is greatly stimulated by treatment of the cells with phorbol ester, but the T cell proliferative signal of phorbol ester and ionophore combined greatly reduces or abrogates this response, and this suppressive effect of the ionophore is not reversed by incorporating FK506 to inhibit calcineurin. Tacrolimus 331-336 CD226 molecule Homo sapiens 17-23 9292524-6 1997 The results showed that IL-3 was induced by calcium ionophore and that the IL-3 induced by Fc gammaRIII stimulation was blocked by EGTA or FK506, but not by staurosporine (protein kinase C [PKC] inhibitor), indicating the important role of calcium-calcineurin in this system. Tacrolimus 139-144 interleukin 3 Mus musculus 75-79 9292524-6 1997 The results showed that IL-3 was induced by calcium ionophore and that the IL-3 induced by Fc gammaRIII stimulation was blocked by EGTA or FK506, but not by staurosporine (protein kinase C [PKC] inhibitor), indicating the important role of calcium-calcineurin in this system. Tacrolimus 139-144 Fc receptor, IgG, low affinity III Mus musculus 91-103 9268302-5 1997 In Jurkat cells, TLiSA1/PTA1 mRNA and surface protein expression is greatly stimulated by treatment of the cells with phorbol ester, but the T cell proliferative signal of phorbol ester and ionophore combined greatly reduces or abrogates this response, and this suppressive effect of the ionophore is not reversed by incorporating FK506 to inhibit calcineurin. Tacrolimus 331-336 CD226 molecule Homo sapiens 24-28 9271313-3 1997 We investigated the mechanisms controlling IL-5 messenger RNA (mRNA) expression in human T-lymphocytes in the presence of CsA or FK506. Tacrolimus 129-134 interleukin 5 Homo sapiens 43-47 9271313-7 1997 CsA and FK506 strongly inhibited cellular IL-5 mRNA expression in response to phytohemagglutinin (PHA), or to phorbol myristate acetate (PMA), and/or calcium ionophore. Tacrolimus 8-13 interleukin 5 Homo sapiens 42-46 9271313-0 1997 Cyclosporin A and FK506 reduce interleukin-5 mRNA abundance by inhibiting gene transcription. Tacrolimus 18-23 interleukin 5 Homo sapiens 31-44 9271313-9 1997 Nuclear run-on assays done with either 7-day cultured PBMC or HSB-2 cells demonstrated striking inhibition of IL-5 gene transcription by both CsA and FK506 at levels reflecting the degree of reduction of total cellular IL-5 mRNA abundance. Tacrolimus 150-155 interleukin 5 Homo sapiens 110-114 9271313-9 1997 Nuclear run-on assays done with either 7-day cultured PBMC or HSB-2 cells demonstrated striking inhibition of IL-5 gene transcription by both CsA and FK506 at levels reflecting the degree of reduction of total cellular IL-5 mRNA abundance. Tacrolimus 150-155 interleukin 5 Homo sapiens 219-223 9271313-11 1997 Thus, the inhibitory effect of CsA and FK506 on cellular IL-5 mRNA expression can be explained by inhibition of the rate of IL-5 gene transcription. Tacrolimus 39-44 interleukin 5 Homo sapiens 57-61 9271313-11 1997 Thus, the inhibitory effect of CsA and FK506 on cellular IL-5 mRNA expression can be explained by inhibition of the rate of IL-5 gene transcription. Tacrolimus 39-44 interleukin 5 Homo sapiens 124-128 9252447-6 1997 Rapamycin potently blocked both the basal and the CCK-stimulated p70s6k activity, and this inhibition was reversed by an excess of FK-506. Tacrolimus 131-137 cholecystokinin Rattus norvegicus 50-53 9304807-2 1997 FK-506 non-competitively inhibited the aniline p-hydroxylase, p-nitroanisole O-demethylase and lidocaine N-deethylase activities of cytochrome P-450-linked monooxygenase systems, these activities being mainly catalyzed by cytochromes P-450 CYP2E1, CYP2C11 and CYP3A4, respectively, and the Ki values of the activities for FK-506 were determined to be 605, 491 and 97 microM, respectively. Tacrolimus 0-6 cytochrome P450, subfamily 2, polypeptide 11 Rattus norvegicus 248-255 9246018-1 1997 OBJECTIVE: To quantitate the effect of ketoconazole, an azole antifungal agent and potent inhibitor of CYP3A4 and P-glycoprotein, on the bioavailability of tacrolimus, a substrate of the CYP3A system and of P-glycoprotein. Tacrolimus 156-166 ATP binding cassette subfamily B member 1 Homo sapiens 114-128 9246018-1 1997 OBJECTIVE: To quantitate the effect of ketoconazole, an azole antifungal agent and potent inhibitor of CYP3A4 and P-glycoprotein, on the bioavailability of tacrolimus, a substrate of the CYP3A system and of P-glycoprotein. Tacrolimus 156-166 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 103-108 9246018-1 1997 OBJECTIVE: To quantitate the effect of ketoconazole, an azole antifungal agent and potent inhibitor of CYP3A4 and P-glycoprotein, on the bioavailability of tacrolimus, a substrate of the CYP3A system and of P-glycoprotein. Tacrolimus 156-166 ATP binding cassette subfamily B member 1 Homo sapiens 207-221 9247567-2 1997 Inhibition of T cell activation by the immunosuppressants cyclosporin A (CsA) and FK506 exerts a suppressive effect on the induction of these NF-kappa B-controlled cytokine promoters. Tacrolimus 82-87 nuclear factor kappa B subunit 1 Homo sapiens 142-152 9223178-0 1997 Mean field analysis of FKBP12 complexes with FK506 and rapamycin: implications for a role of crystallographic water molecules in molecular recognition and specificity. Tacrolimus 45-50 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 23-29 9223178-1 1997 Mean field analysis of FKBP12 complexes with FK506 and rapamycin has been performed by using structures obtained from molecular docking simulations on a simple, yet robust molecular recognition energy landscape. Tacrolimus 45-50 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 23-29 9223178-4 1997 The stability gap in the FKBP12-FK506 system is determined by two critical water molecules from the effector region that participate in a network of specific hydrogen bond interactions. Tacrolimus 32-37 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 25-31 9223178-5 1997 This interaction pattern protects the integrity and precision of the composite ligand-protein effector surface in the binary FKBP12-FK506 complex and is preserved in the crystal structure of the FKBP12-FK506-calcineurin ternary complex. Tacrolimus 132-137 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 125-131 9223178-5 1997 This interaction pattern protects the integrity and precision of the composite ligand-protein effector surface in the binary FKBP12-FK506 complex and is preserved in the crystal structure of the FKBP12-FK506-calcineurin ternary complex. Tacrolimus 132-137 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 195-201 9223178-5 1997 This interaction pattern protects the integrity and precision of the composite ligand-protein effector surface in the binary FKBP12-FK506 complex and is preserved in the crystal structure of the FKBP12-FK506-calcineurin ternary complex. Tacrolimus 202-207 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 125-131 9223178-5 1997 This interaction pattern protects the integrity and precision of the composite ligand-protein effector surface in the binary FKBP12-FK506 complex and is preserved in the crystal structure of the FKBP12-FK506-calcineurin ternary complex. Tacrolimus 202-207 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 195-201 9233699-9 1997 However, local expression of IgM, C3 and T helper 1 cytokines, serum antibodies of IgG and IgM, and delayed-type hypersensitivity were suppressed in the anti-LFA-1 mAb- plus FK506-treated group. Tacrolimus 174-179 immunoglobulin heavy constant mu Mus musculus 29-32 9233699-9 1997 However, local expression of IgM, C3 and T helper 1 cytokines, serum antibodies of IgG and IgM, and delayed-type hypersensitivity were suppressed in the anti-LFA-1 mAb- plus FK506-treated group. Tacrolimus 174-179 immunoglobulin heavy constant mu Mus musculus 91-94 9233699-9 1997 However, local expression of IgM, C3 and T helper 1 cytokines, serum antibodies of IgG and IgM, and delayed-type hypersensitivity were suppressed in the anti-LFA-1 mAb- plus FK506-treated group. Tacrolimus 174-179 integrin alpha L Mus musculus 158-163 9199340-7 1997 Similar to the upregulation of IL-2 secretion, the transcriptional upregulation of the RE/AP composite element by CD28 is FK506 insensitive. Tacrolimus 122-127 CD28 molecule Homo sapiens 114-118 9195923-0 1997 Protein phosphatase 5 is a major component of glucocorticoid receptor.hsp90 complexes with properties of an FK506-binding immunophilin. Tacrolimus 108-113 nuclear receptor subfamily 3 group C member 1 Homo sapiens 46-69 9195923-0 1997 Protein phosphatase 5 is a major component of glucocorticoid receptor.hsp90 complexes with properties of an FK506-binding immunophilin. Tacrolimus 108-113 heat shock protein 90 alpha family class A member 1 Homo sapiens 70-75 9195923-2 1997 The immunophilin, which can be of the FK506- or cyclosporin A-binding class, binds to hsp90 via its tetratricopeptide repeat (TPR) domain, and different receptor heterocomplexes exist depending upon which immunophilin occupies the TPR-binding region of hsp90. Tacrolimus 38-43 heat shock protein 90 alpha family class A member 1 Homo sapiens 86-91 9195923-7 1997 Approximately one-half of the GR.hsp90 heterocomplexes in L cell cytosol contains an immunophilin with high affinity FK506 binding activity, such as FKBP51 or FKBP52, and approximately 35% contains PP5. Tacrolimus 117-122 nuclear receptor subfamily 3 group C member 1 Homo sapiens 30-32 9195923-7 1997 Approximately one-half of the GR.hsp90 heterocomplexes in L cell cytosol contains an immunophilin with high affinity FK506 binding activity, such as FKBP51 or FKBP52, and approximately 35% contains PP5. Tacrolimus 117-122 heat shock protein 90 alpha family class A member 1 Homo sapiens 33-38 9195923-11 1997 Of the 9 residues in this portion of FKBP52 involved in high affinity interactions with FK506, 3 residues are retained and 4 have homologous substitutions in PP5. Tacrolimus 88-93 FKBP prolyl isomerase 4 Homo sapiens 37-43 9195923-12 1997 Although immunoadsorbed PP5 did not bind [3H]FK506, we found that both rabbit PP5 in reticulocyte lysate and purified rat PP5 were specifically retained by an FK506 affinity matrix. Tacrolimus 159-164 protein phosphatase 5 catalytic subunit Homo sapiens 78-81 9195923-12 1997 Although immunoadsorbed PP5 did not bind [3H]FK506, we found that both rabbit PP5 in reticulocyte lysate and purified rat PP5 were specifically retained by an FK506 affinity matrix. Tacrolimus 159-164 protein phosphatase 5, catalytic subunit Rattus norvegicus 78-81 9195923-13 1997 Thus, we propose that PP5 possesses properties of an immunophilin with low affinity FK506 binding activity and that it determines a major portion of the native GR heterocomplexes in L cell cytosol. Tacrolimus 84-89 protein phosphatase 5 catalytic subunit Homo sapiens 22-25 9190906-2 1997 Furthermore we show that IL-10 production by human T cell lines, such as IFN-gamma and IL-2, is inhibited by the immunosuppressive drugs cyclosporin A and FK506. Tacrolimus 155-160 interleukin 10 Homo sapiens 25-30 9190906-2 1997 Furthermore we show that IL-10 production by human T cell lines, such as IFN-gamma and IL-2, is inhibited by the immunosuppressive drugs cyclosporin A and FK506. Tacrolimus 155-160 interferon gamma Homo sapiens 73-82 9190906-2 1997 Furthermore we show that IL-10 production by human T cell lines, such as IFN-gamma and IL-2, is inhibited by the immunosuppressive drugs cyclosporin A and FK506. Tacrolimus 155-160 interleukin 2 Homo sapiens 87-91 9182928-4 1997 RESULTS: Interleukin-2 production was suppressed in patients treated with tacrolimus. Tacrolimus 74-84 interleukin 2 Homo sapiens 9-22 9304807-3 1997 The inhibition of cytochrome P-450-linked monooxygenase systems by FK-506 seemed to involve the direct inhibition of cytochromes P-450 because the NADPH-cytochrome c reductase and NADPH-ferricyanide reductase activities of NADPH-cytochrome P-450 reductase were not affected by the presence of 1 mM FK-506 at all. Tacrolimus 67-73 cytochrome p450 oxidoreductase Rattus norvegicus 223-255 9154824-7 1997 FK-506, another ligand of FKBP12 affecting the phosphatase calcineurin, did not antagonize but shared the effect of rapamycin. Tacrolimus 0-6 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 26-32 9182723-6 1997 These St-induced effects were inhibited by pretreatment with FK506, indicating that CaN activity was required for the observed effects on NFATp. Tacrolimus 61-66 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 2 Mus musculus 138-143 9145907-3 1997 Disruption of the association between immunophilin FKBP12 and Ry1R with FK 506 or rapamycin completely eliminates PCB 95-enhanced binding of [3H]ryanodine (IC50 approximately 35 microM) to Ry1R and PCB 95-induced release of Ca2+ from actively loaded SR vesicles (IC50 approximately 11 microM), demonstrating a FKBP12-dependent mechanism. Tacrolimus 72-78 FKBP prolyl isomerase 1A Homo sapiens 38-57 9145907-4 1997 FK 506 selectively eliminates PCB 95-induced Ca2+ release from SR because Ry1R maintains responsiveness to caffeine and Ca2+. Tacrolimus 0-6 pyruvate carboxylase Homo sapiens 30-33 9145907-9 1997 The actions of PCB 95 on SR-loading capacity are additive with those of FK 506. Tacrolimus 72-78 pyruvate carboxylase Homo sapiens 15-18 9111057-4 1997 One of the ligand-dependent clones, ARA9, encodes a novel 330-amino acid protein with regions of amino acid sequence similarity to the 52-kDa FK506-binding protein known to be associated with the glucocorticoid receptor. Tacrolimus 142-147 aryl hydrocarbon receptor interacting protein Homo sapiens 36-40 9111057-4 1997 One of the ligand-dependent clones, ARA9, encodes a novel 330-amino acid protein with regions of amino acid sequence similarity to the 52-kDa FK506-binding protein known to be associated with the glucocorticoid receptor. Tacrolimus 142-147 nuclear receptor subfamily 3 group C member 1 Homo sapiens 196-219 9103428-0 1997 IL-2-induced IL-5 synthesis, but not proliferation, of human CD4+ T cells is suppressed by FK506. Tacrolimus 91-96 interleukin 2 Homo sapiens 0-4 9103428-0 1997 IL-2-induced IL-5 synthesis, but not proliferation, of human CD4+ T cells is suppressed by FK506. Tacrolimus 91-96 interleukin 5 Homo sapiens 13-17 9103428-0 1997 IL-2-induced IL-5 synthesis, but not proliferation, of human CD4+ T cells is suppressed by FK506. Tacrolimus 91-96 CD4 molecule Homo sapiens 61-64 9103428-2 1997 Immunosuppressant FK506 suppressed IL-5 synthesis of T cells activated through TCR in a dose-dependent manner. Tacrolimus 18-23 interleukin 5 Homo sapiens 35-39 9103428-3 1997 IL-5 gene transcription and protein synthesis were also induced in the same T cell clones upon stimulation with IL-2 and were suppressed by FK506 in a dose response similar to that induced by TCR stimulation. Tacrolimus 140-145 interleukin 5 Homo sapiens 0-4 9103428-5 1997 Human IL-5 promoter/enhancer-luciferase gene construct transfected to T cell clones was transcribed upon either TCR or IL-2 stimulation and was clearly down-regulated by FK506, indicating that the approximately 500-bp human IL-5 gene segment located 5" upstream of the coding region contained FK506-sensitive enhancer elements. Tacrolimus 170-175 interleukin 5 Homo sapiens 6-10 9103428-5 1997 Human IL-5 promoter/enhancer-luciferase gene construct transfected to T cell clones was transcribed upon either TCR or IL-2 stimulation and was clearly down-regulated by FK506, indicating that the approximately 500-bp human IL-5 gene segment located 5" upstream of the coding region contained FK506-sensitive enhancer elements. Tacrolimus 170-175 interleukin 5 Homo sapiens 224-228 9103428-5 1997 Human IL-5 promoter/enhancer-luciferase gene construct transfected to T cell clones was transcribed upon either TCR or IL-2 stimulation and was clearly down-regulated by FK506, indicating that the approximately 500-bp human IL-5 gene segment located 5" upstream of the coding region contained FK506-sensitive enhancer elements. Tacrolimus 293-298 interleukin 5 Homo sapiens 6-10 9103428-5 1997 Human IL-5 promoter/enhancer-luciferase gene construct transfected to T cell clones was transcribed upon either TCR or IL-2 stimulation and was clearly down-regulated by FK506, indicating that the approximately 500-bp human IL-5 gene segment located 5" upstream of the coding region contained FK506-sensitive enhancer elements. Tacrolimus 293-298 interleukin 5 Homo sapiens 224-228 9103428-6 1997 Our present findings clearly indicate that FK506-sensitive signaling molecules are involved in T cell IL-5 production induced by both TCR and IL-2 stimulation and suggest that IL-2 receptor signal leading to IL-5 gene transcription is transduced by a unique FK506-sensitive pathway other than the Ca2+-dependent signal transduction pathway, such as the calcineurin-NF-AT system. Tacrolimus 43-48 interleukin 5 Homo sapiens 102-106 9103428-6 1997 Our present findings clearly indicate that FK506-sensitive signaling molecules are involved in T cell IL-5 production induced by both TCR and IL-2 stimulation and suggest that IL-2 receptor signal leading to IL-5 gene transcription is transduced by a unique FK506-sensitive pathway other than the Ca2+-dependent signal transduction pathway, such as the calcineurin-NF-AT system. Tacrolimus 43-48 interleukin 2 Homo sapiens 142-146 9103428-6 1997 Our present findings clearly indicate that FK506-sensitive signaling molecules are involved in T cell IL-5 production induced by both TCR and IL-2 stimulation and suggest that IL-2 receptor signal leading to IL-5 gene transcription is transduced by a unique FK506-sensitive pathway other than the Ca2+-dependent signal transduction pathway, such as the calcineurin-NF-AT system. Tacrolimus 43-48 interleukin 2 Homo sapiens 176-180 9103428-6 1997 Our present findings clearly indicate that FK506-sensitive signaling molecules are involved in T cell IL-5 production induced by both TCR and IL-2 stimulation and suggest that IL-2 receptor signal leading to IL-5 gene transcription is transduced by a unique FK506-sensitive pathway other than the Ca2+-dependent signal transduction pathway, such as the calcineurin-NF-AT system. Tacrolimus 43-48 interleukin 5 Homo sapiens 208-212 9103428-6 1997 Our present findings clearly indicate that FK506-sensitive signaling molecules are involved in T cell IL-5 production induced by both TCR and IL-2 stimulation and suggest that IL-2 receptor signal leading to IL-5 gene transcription is transduced by a unique FK506-sensitive pathway other than the Ca2+-dependent signal transduction pathway, such as the calcineurin-NF-AT system. Tacrolimus 258-263 interleukin 2 Homo sapiens 176-180 9103428-6 1997 Our present findings clearly indicate that FK506-sensitive signaling molecules are involved in T cell IL-5 production induced by both TCR and IL-2 stimulation and suggest that IL-2 receptor signal leading to IL-5 gene transcription is transduced by a unique FK506-sensitive pathway other than the Ca2+-dependent signal transduction pathway, such as the calcineurin-NF-AT system. Tacrolimus 258-263 interleukin 5 Homo sapiens 208-212 9112351-2 1997 BACKGROUND: Tacrolimus (FK506), a macrolide molecule that potently inhibits the expression of interleukin 2 by T lymphocytes, represents a potential major advance in the management of rejection following solid-organ transplantation. Tacrolimus 24-29 interleukin 2 Homo sapiens 94-107 9147322-8 1997 Inhibition of FKBP by the immunosuppressants FK506 or rapamycin increased the duration of spontaneous or depolarization-evoked Ca2+ sparks 6- to 7-fold. Tacrolimus 45-50 carbonic anhydrase 2 Rattus norvegicus 127-130 9147322-11 1997 FK506 potentiated and prolonged electrically stimulated [Ca2+]i transients and contractions, but did not affect the amplitude and kinetics of the L-type Ca2+ channel current. Tacrolimus 0-5 carbonic anhydrase 2 Rattus norvegicus 57-60 9147322-13 1997 In planar lipid bilayers, FK506 (15 microM) prolonged approximately 7-fold the mean open lifetime of reconstituted single RyRs, induced the appearance of long-lasting subconductance states, and markedly slowed the spontaneous decay of RyR activity elicited by fast and sustained Ca2+ stimuli. Tacrolimus 26-31 ryanodine receptor 2 Rattus norvegicus 122-125 9147322-13 1997 In planar lipid bilayers, FK506 (15 microM) prolonged approximately 7-fold the mean open lifetime of reconstituted single RyRs, induced the appearance of long-lasting subconductance states, and markedly slowed the spontaneous decay of RyR activity elicited by fast and sustained Ca2+ stimuli. Tacrolimus 26-31 carbonic anhydrase 2 Rattus norvegicus 279-282 9169521-6 1997 Synaptic potentiation induced by FK-506 was significantly attenuated by co-injecting BAPTA, heparin/dantrolene (inhibitors of intracellular Ca2+ release), a CaM-binding peptide, or CaM-KII/PKC pseudosubstrate peptides. Tacrolimus 33-39 carbonic anhydrase 2 Rattus norvegicus 140-143 9165550-0 1997 Time-dependent disposition of tacrolimus and its effect on endothelin-1 in liver allograft recipients. Tacrolimus 30-40 endothelin 1 Homo sapiens 59-71 9165550-1 1997 STUDY OBJECTIVE: To characterize a time-dependent disposition of oral tacrolimus and its relationship with plasma endothelin-1 concentrations. Tacrolimus 70-80 endothelin 1 Homo sapiens 114-126 9145907-3 1997 Disruption of the association between immunophilin FKBP12 and Ry1R with FK 506 or rapamycin completely eliminates PCB 95-enhanced binding of [3H]ryanodine (IC50 approximately 35 microM) to Ry1R and PCB 95-induced release of Ca2+ from actively loaded SR vesicles (IC50 approximately 11 microM), demonstrating a FKBP12-dependent mechanism. Tacrolimus 72-78 pyruvate carboxylase Homo sapiens 114-117 9145907-3 1997 Disruption of the association between immunophilin FKBP12 and Ry1R with FK 506 or rapamycin completely eliminates PCB 95-enhanced binding of [3H]ryanodine (IC50 approximately 35 microM) to Ry1R and PCB 95-induced release of Ca2+ from actively loaded SR vesicles (IC50 approximately 11 microM), demonstrating a FKBP12-dependent mechanism. Tacrolimus 72-78 FKBP prolyl isomerase 1A Homo sapiens 51-57 9045922-4 1997 Blocking the IL-2 pathway by cyclosporin A, FK506, rapamycin, anti-IL-2 or CD25 antibodies, prevented the development of sensitivity to apoptosis. Tacrolimus 44-49 interleukin 2 Homo sapiens 13-17 9113492-8 1997 Cyclosporin and tacrolimus cause post-transplant diabetes mellitus by a number of mechanisms, including decreased insulin secretion, increased insulin resistance or a direct toxic effect on the beta cell. Tacrolimus 16-26 insulin Homo sapiens 114-121 9104801-0 1997 Extremely high serum level of IgE during immunosuppressive therapy: paradoxical effect of cyclosporine A and tacrolimus. Tacrolimus 109-119 immunoglobulin heavy constant epsilon Homo sapiens 30-33 9104801-1 1997 A case of X-linked autoimmune enteropathy was successfully treated with cyclosporine A (CsA) or tacrolimus (FK506) and developed extremely high serum levels of IgE during the immunosuppressive therapy. Tacrolimus 108-113 immunoglobulin heavy constant epsilon Homo sapiens 160-163 9104801-2 1997 Serum IgE levels increased from 190 to 1,000-2,500 IU/ml with CsA therapy and as high as 80,000 IU/ml with subsequent FK506 therapy. Tacrolimus 118-123 immunoglobulin heavy constant epsilon Homo sapiens 6-9 9104801-4 1997 Thereafter, serum IgE levels progressively decreased in parallel with a reduced dosage of FK506. Tacrolimus 90-95 immunoglobulin heavy constant epsilon Homo sapiens 18-21 9101372-19 1997 BGP levels were significantly increased in the CsA (p < 0.01) and FK506 (p < 0.001) groups on day 28. Tacrolimus 69-74 bone gamma-carboxyglutamate protein Rattus norvegicus 0-3 9143223-0 1997 Calcineurin inhibitor, FK506, prevents reduction in the binding capacity of cyclic AMP-dependent protein kinase in ischemic gerbil brain. Tacrolimus 23-28 calcineurin binding protein 1 Homo sapiens 0-21 9143223-7 1997 In the ischemia group of gerbils, FK506 prevented any significant reduction of cAMP binding in the hippocampus CA1 and cerebral cortices on the ischemic side, whereas it exerted no significant influence on the cAMP binding of the nonischemic side. Tacrolimus 34-39 carbonic anhydrase 1 Homo sapiens 111-114 9103242-9 1997 Blocking the resulting damage of this inflammatory reaction with anti-LFA-1 in animals also treated with FK506, a powerful immunosuppressant for gene therapy, largely increased the long-term transgene expression compared with mice only treated with FK506. Tacrolimus 105-110 integrin alpha L Mus musculus 70-75 9103242-9 1997 Blocking the resulting damage of this inflammatory reaction with anti-LFA-1 in animals also treated with FK506, a powerful immunosuppressant for gene therapy, largely increased the long-term transgene expression compared with mice only treated with FK506. Tacrolimus 249-254 integrin alpha L Mus musculus 70-75 9096348-3 1997 FK1012 is used as a pharmacological mediator of dimerization to bring together FK506 binding domains, taken from the endogenous protein FKBP12. Tacrolimus 79-84 FKBP prolyl isomerase 1A pseudogene 3 Homo sapiens 136-142 9178371-2 1997 The in vitro metabolism of tacrolimus (TAC, FK 506) was investigated in the liver microsomes prepared from normal rats as well as rats treated with dexamethasone (DEX) and rifampin (RIF). Tacrolimus 27-37 tachykinin precursor 3 Rattus norvegicus 39-42 9125197-5 1997 The 51.2 kDa protein encoded by this gene shares 87% identity to murine FKBP51 and demonstrates a similar IC50 value for the FK506-mediated inhibition of calcineurin phosphatase in vitro. Tacrolimus 125-130 FK506 binding protein 5 Mus musculus 72-78 9113092-0 1997 Decrease in kidney calbindin-D 28kDa as a possible mechanism mediating cyclosporine A- and FK-506-induced calciuria and tubular mineralization. Tacrolimus 91-97 calbindin 1 Rattus norvegicus 19-33 9127694-0 1997 Identification of a 37 kDa tacrolimus, sirolimus and cyclosporine binding immunophilin possessing glyceraldehyde 3-phosphate dehydrogenase activity isolated from the Jurkat T cell line. Tacrolimus 27-37 glyceraldehyde-3-phosphate dehydrogenase Homo sapiens 98-138 9127694-1 1997 OBJECTIVE: The isolation and partial characterization of a 37 kDa minor immunophilin from the Jurkat cell line which binds to cyclosporine (CsA), Tacrolimus (FK506) and Sirolimus (RAPA). Tacrolimus 158-163 transcriptional regulating factor 1 Homo sapiens 180-184 9032415-6 1997 The assay is very sensitive and selective for immunosuppressive compounds inhibiting IL-2 gene expression such as cyclosporine (CsA) and FK506, their active metabolites and derivatives, but not for others such as rapamycin. Tacrolimus 137-142 interleukin 2 Homo sapiens 85-89 9013543-4 1997 cADPR as well as FK506 bound to FK506-binding protein 12.6 (FKBP12.6), which we also found occurs naturally in islet microsomes. Tacrolimus 17-22 FKBP prolyl isomerase 1B Homo sapiens 32-58 9013543-4 1997 cADPR as well as FK506 bound to FK506-binding protein 12.6 (FKBP12.6), which we also found occurs naturally in islet microsomes. Tacrolimus 17-22 FKBP prolyl isomerase 1B Homo sapiens 60-68 9061187-0 1997 Modeling the interaction between FK506 and FKBP12: a mechanism for formation of the calcineurin inhibitory complex. Tacrolimus 33-38 FKBP prolyl isomerase 1A pseudogene 3 Homo sapiens 43-49 9061187-1 1997 FK506 is a naturally occurring immunosuppressant whose mode of action involves formation of an initial complex with the cytosolic protein FKBP12. Tacrolimus 0-5 FKBP prolyl isomerase 1A pseudogene 3 Homo sapiens 138-144 9061187-7 1997 Comparison of the structure of Z-Arg32-ascomycin in water with structures of FK506 bound to FKBP12 indicate that the conformation of the pipecolate region is conserved during the binding process. Tacrolimus 77-82 FKBP prolyl isomerase 1A pseudogene 3 Homo sapiens 92-98 9061187-10 1997 From computer models and molecular dynamics simulations of interactions between FK506 and FKBP12 we suggest that the conformational changes observed in bound FK506 are induced by the interaction between the 80"s loop of FKBP12 and the pyranose ring of FKBP12. Tacrolimus 80-85 FKBP prolyl isomerase 1A pseudogene 3 Homo sapiens 90-96 9061187-10 1997 From computer models and molecular dynamics simulations of interactions between FK506 and FKBP12 we suggest that the conformational changes observed in bound FK506 are induced by the interaction between the 80"s loop of FKBP12 and the pyranose ring of FKBP12. Tacrolimus 80-85 FKBP prolyl isomerase 1A pseudogene 3 Homo sapiens 220-226 9061187-10 1997 From computer models and molecular dynamics simulations of interactions between FK506 and FKBP12 we suggest that the conformational changes observed in bound FK506 are induced by the interaction between the 80"s loop of FKBP12 and the pyranose ring of FKBP12. Tacrolimus 80-85 FKBP prolyl isomerase 1A pseudogene 3 Homo sapiens 220-226 9061187-10 1997 From computer models and molecular dynamics simulations of interactions between FK506 and FKBP12 we suggest that the conformational changes observed in bound FK506 are induced by the interaction between the 80"s loop of FKBP12 and the pyranose ring of FKBP12. Tacrolimus 158-163 FKBP prolyl isomerase 1A pseudogene 3 Homo sapiens 90-96 9061187-10 1997 From computer models and molecular dynamics simulations of interactions between FK506 and FKBP12 we suggest that the conformational changes observed in bound FK506 are induced by the interaction between the 80"s loop of FKBP12 and the pyranose ring of FKBP12. Tacrolimus 158-163 FKBP prolyl isomerase 1A pseudogene 3 Homo sapiens 220-226 9061187-10 1997 From computer models and molecular dynamics simulations of interactions between FK506 and FKBP12 we suggest that the conformational changes observed in bound FK506 are induced by the interaction between the 80"s loop of FKBP12 and the pyranose ring of FKBP12. Tacrolimus 158-163 FKBP prolyl isomerase 1A pseudogene 3 Homo sapiens 220-226 9080295-7 1997 FK506 also suppressed anti-H alpha 125-147 and anti-rat AChR antibody production accompanied by a decrease in the antigen-specific T cell response against H alpha 125-147. Tacrolimus 0-5 cholinergic receptor nicotinic alpha 2 subunit Rattus norvegicus 56-60 9112351-2 1997 BACKGROUND: Tacrolimus (FK506), a macrolide molecule that potently inhibits the expression of interleukin 2 by T lymphocytes, represents a potential major advance in the management of rejection following solid-organ transplantation. Tacrolimus 12-22 interleukin 2 Homo sapiens 94-107 9016789-2 1997 FK506, in contrast, had no effect on DEX-induced apoptosis; moreover, an excess of FK506 reversed the potentiation of apoptosis by RAP, indicating that RAP exerts its effects through binding to FKBP. Tacrolimus 83-88 regulatory associated protein of MTOR, complex 1 Mus musculus 131-134 9123208-0 1997 Impaired T-cell IL-10 secretion and CD4 helper function in liver transplant patients treated with tacrolimus. Tacrolimus 98-108 interleukin 10 Homo sapiens 16-21 9123208-0 1997 Impaired T-cell IL-10 secretion and CD4 helper function in liver transplant patients treated with tacrolimus. Tacrolimus 98-108 CD4 molecule Homo sapiens 36-39 9123209-0 1997 High-dose cellular IL-10 exacerbates rejection and reverses effects of cyclosporine and tacrolimus in Mouse cardiac transplantation. Tacrolimus 88-98 interleukin 10 Mus musculus 19-24 9016789-2 1997 FK506, in contrast, had no effect on DEX-induced apoptosis; moreover, an excess of FK506 reversed the potentiation of apoptosis by RAP, indicating that RAP exerts its effects through binding to FKBP. Tacrolimus 83-88 regulatory associated protein of MTOR, complex 1 Mus musculus 152-155 9016789-2 1997 FK506, in contrast, had no effect on DEX-induced apoptosis; moreover, an excess of FK506 reversed the potentiation of apoptosis by RAP, indicating that RAP exerts its effects through binding to FKBP. Tacrolimus 83-88 FK506 binding protein 1a Mus musculus 194-198 9016789-5 1997 The reduction of JNK activity by RAP was reversed by the addition of an excess of FK506. Tacrolimus 82-87 mitogen-activated protein kinase 8 Mus musculus 17-20 9016789-5 1997 The reduction of JNK activity by RAP was reversed by the addition of an excess of FK506. Tacrolimus 82-87 regulatory associated protein of MTOR, complex 1 Mus musculus 33-36 9209689-0 1997 Implication of CYP 3A in the toxicity of cyclosporin G (CsG), cyclosporin A (CsA) and FK506 on rat hepatocytes in primary culture. Tacrolimus 86-91 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 15-21 9209689-1 1997 FK506, cyclosporin A (CsA), and its structural analog cyclosporin G (CsG) are immunosuppressant drugs mainly metabolized by hepatic cytochrome P-450 3A (CYP 3A) oxygenase. Tacrolimus 0-5 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 132-151 9209689-1 1997 FK506, cyclosporin A (CsA), and its structural analog cyclosporin G (CsG) are immunosuppressant drugs mainly metabolized by hepatic cytochrome P-450 3A (CYP 3A) oxygenase. Tacrolimus 0-5 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 153-159 9209689-12 1997 Our results show that the toxicity of the three drugs in rat hepatocytes is dependent on CYP 3A induction: increased for FK506, decreased for CsA and CsG. Tacrolimus 121-126 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 89-95 9117088-7 1997 The antigen-induced interleukin (IL)-5 formation in the BALF and serum was inhibited by FK-506 by 75% in both instances. Tacrolimus 88-94 interleukin 5 Mus musculus 20-38 9051292-4 1997 The effect on ODC was specific for the intracellular signalling pathway leading to activation of p70S6k, as the immunosuppressant FK 506 was without effect on ODC activity. Tacrolimus 130-136 ornithine decarboxylase 1 Rattus norvegicus 14-17 9051292-4 1997 The effect on ODC was specific for the intracellular signalling pathway leading to activation of p70S6k, as the immunosuppressant FK 506 was without effect on ODC activity. Tacrolimus 130-136 ribosomal protein S6 kinase B1 Rattus norvegicus 97-103 9117088-13 1997 These findings indicate that antigen-induced in vivo IL-5 release and eosinophil, but not T-cell, infiltration into the bronchial lumen of sensitized BP2 mice are targets for the anti-allergic activities of FK-506. Tacrolimus 207-213 interleukin 5 Mus musculus 53-57 8955134-3 1996 FKBP59 and FKBP12 belong to the large family of immunophilins that bind the macrolide immunosuppressant drugs FK506 and rapamycin. Tacrolimus 110-115 FKBP prolyl isomerase 4 Homo sapiens 0-6 8955134-3 1996 FKBP59 and FKBP12 belong to the large family of immunophilins that bind the macrolide immunosuppressant drugs FK506 and rapamycin. Tacrolimus 110-115 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 11-17 8955134-10 1996 The formation of the complexes between FKBP59 or FKBP12 and FAP48 is prevented by FK506 and rapamycin in a dose-dependent manner. Tacrolimus 82-87 FKBP prolyl isomerase 4 Homo sapiens 39-45 8955134-10 1996 The formation of the complexes between FKBP59 or FKBP12 and FAP48 is prevented by FK506 and rapamycin in a dose-dependent manner. Tacrolimus 82-87 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 49-55 8955134-10 1996 The formation of the complexes between FKBP59 or FKBP12 and FAP48 is prevented by FK506 and rapamycin in a dose-dependent manner. Tacrolimus 82-87 glomulin, FKBP associated protein Homo sapiens 60-65 8981925-0 1996 Effects of tacrolimus (FK506) on human insulin gene expression, insulin mRNA levels, and insulin secretion in HIT-T15 cells. Tacrolimus 23-28 insulin Homo sapiens 39-46 8994885-1 1996 Recently, two structures of the Ser/Thr phosphorylase calcineurin in complex with FK506 and its cognate immunophilin, FKBP12, have been reported, both solved by small pharmaceutical companies focused on structure-based drug design. Tacrolimus 82-87 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 118-124 8981925-2 1996 Regulation of insulin gene expression in the beta cell may also involve Ca2+-signaling pathways and FK506 has been associated with insulin-requiring diabetes mellitus during clinical use. Tacrolimus 100-105 insulin Homo sapiens 14-21 8981925-3 1996 The purpose of this study was to characterize the effects of FK506 on human insulin gene transcription, insulin mRNA levels, and insulin secretion using as a model the HIT-T15 beta cell line. Tacrolimus 61-66 insulin Homo sapiens 76-83 8981925-5 1996 Decreased insulin secretion in the presence of FK506 was also accompanied by a dose-dependent decrease in HIT cell insulin content, insulin mRNA levels, and expression of a human insulin promoter-chloramphenicol acetyl transferase (CAT) reporter gene. Tacrolimus 47-52 insulin Homo sapiens 10-17 8981925-5 1996 Decreased insulin secretion in the presence of FK506 was also accompanied by a dose-dependent decrease in HIT cell insulin content, insulin mRNA levels, and expression of a human insulin promoter-chloramphenicol acetyl transferase (CAT) reporter gene. Tacrolimus 47-52 insulin Homo sapiens 115-122 8981925-5 1996 Decreased insulin secretion in the presence of FK506 was also accompanied by a dose-dependent decrease in HIT cell insulin content, insulin mRNA levels, and expression of a human insulin promoter-chloramphenicol acetyl transferase (CAT) reporter gene. Tacrolimus 47-52 insulin Homo sapiens 115-122 8981925-6 1996 FK506 decreased HIT cell expression of the human insulin promoter-CAT reporter gene by 40% in the presence of both low (0.4 mM) at high (20 mM) glucose concentrations. Tacrolimus 0-5 insulin Homo sapiens 49-56 8981925-8 1996 These findings suggest that FK506 may have direct effects to reversibly inhibit insulin gene transcription, leading to a decline in insulin mRNA levels, insulin synthesis, and ultimately insulin secretion. Tacrolimus 28-33 insulin Homo sapiens 80-87 8981925-8 1996 These findings suggest that FK506 may have direct effects to reversibly inhibit insulin gene transcription, leading to a decline in insulin mRNA levels, insulin synthesis, and ultimately insulin secretion. Tacrolimus 28-33 insulin Homo sapiens 132-139 8981925-8 1996 These findings suggest that FK506 may have direct effects to reversibly inhibit insulin gene transcription, leading to a decline in insulin mRNA levels, insulin synthesis, and ultimately insulin secretion. Tacrolimus 28-33 insulin Homo sapiens 132-139 8981925-8 1996 These findings suggest that FK506 may have direct effects to reversibly inhibit insulin gene transcription, leading to a decline in insulin mRNA levels, insulin synthesis, and ultimately insulin secretion. Tacrolimus 28-33 insulin Homo sapiens 132-139 8971291-12 1996 Water immersion stress increased gastric mucosal IL-1 beta and IL-2 contents 6 h after stress treatment, and these increases were prevented by FK506. Tacrolimus 143-148 interleukin 1 beta Rattus norvegicus 49-58 8971291-12 1996 Water immersion stress increased gastric mucosal IL-1 beta and IL-2 contents 6 h after stress treatment, and these increases were prevented by FK506. Tacrolimus 143-148 interleukin 2 Rattus norvegicus 63-67 8939643-3 1996 The immunosuppressants cyclosporin A and FK506, when complexed with immunophilins, inactivate the protein phosphatase calcineurin, resulting in the inhibition of interleukin-2 gene activation. Tacrolimus 41-46 interleukin 2 Homo sapiens 162-175 8906804-4 1996 Interference with the IL-2 pathway was achieved by 1) inhibition of cytokine synthesis using cyclosporin A or FK506, 2) neutralization of IL-2 by anti-IL-2 Ab, 3) inhibition of binding to IL-2R by CD25 mAb, and 4) blocking of IL-2R signaling by rapamycin. Tacrolimus 110-115 interleukin 2 Homo sapiens 22-26 8974006-3 1996 NFAT acts at the antigen receptor response element-2 (ARRE-2) sequence in the IL-2 enhancer and is the nuclear target of T cell stimulation signals and the immunosuppressant drugs cyclosporine and FK506, which are potent inhibitors of IL-2 gene transcription. Tacrolimus 197-202 interleukin 2 Homo sapiens 78-82 8974006-3 1996 NFAT acts at the antigen receptor response element-2 (ARRE-2) sequence in the IL-2 enhancer and is the nuclear target of T cell stimulation signals and the immunosuppressant drugs cyclosporine and FK506, which are potent inhibitors of IL-2 gene transcription. Tacrolimus 197-202 interleukin 2 Homo sapiens 235-239 8946659-1 1996 In a prospective study, we evaluated a novel enzyme-linked immunosorbent assay (ELISA) (Pro-Trac) for determining tacrolimus (FK 506) concentrations in whole blood. Tacrolimus 114-124 T cell receptor alpha constant Homo sapiens 92-96 8946659-1 1996 In a prospective study, we evaluated a novel enzyme-linked immunosorbent assay (ELISA) (Pro-Trac) for determining tacrolimus (FK 506) concentrations in whole blood. Tacrolimus 126-132 T cell receptor alpha constant Homo sapiens 92-96 8946659-8 1996 We conclude that if assay precision in the upper range is improved, the Pro-Trac ELISA might be a valuable alternative to the MEIA for therapeutic drug monitoring of tacrolimus. Tacrolimus 166-176 T cell receptor alpha constant Homo sapiens 76-80 8962237-0 1996 Decreased Fas antigen expression of cultured hepatocytes with FK 506. Tacrolimus 62-68 Fas cell surface death receptor Homo sapiens 10-21 8906804-6 1996 While the addition of rIL-2 reversed the inhibitory effect of cyclosporin A and FK506, the addition of rIL-4, rIL-7, or rIFN-gamma did not, although these cytokines induced progression into the S phase of the cell cycle. Tacrolimus 80-85 interleukin 2 Rattus norvegicus 22-27 8906215-5 1996 Cyclosporin A, FK-506, and cyclophosphamide clearly inhibited the antigen-induced increase of IL-5 and eosinophils in BALF. Tacrolimus 15-21 interleukin 5 Mus musculus 94-98 8917502-7 1996 Using this system, we screened a Jurkat cDNA library fused to the transcriptional activation domain in yeast expressing the hormone binding domain of rat glucocorticoid receptor-LexA DNA binding domain fusion protein in the presence of dexamethasone-FK506 heterodimer. Tacrolimus 250-255 nuclear receptor subfamily 3, group C, member 1 Rattus norvegicus 154-177 8986461-1 1996 FK-506 (Tacrolimus) has been shown to block T cell proliferation in vitro by inhibiting the generation of several lymphokines, especially interleukin (IL)-2, but little direct evidence is available to support the view that the immunosuppressive effects of FK-506 in vivo are mediated by a similar inhibition of lymphokine cascade. Tacrolimus 0-6 interleukin 2 Mus musculus 138-156 8986461-1 1996 FK-506 (Tacrolimus) has been shown to block T cell proliferation in vitro by inhibiting the generation of several lymphokines, especially interleukin (IL)-2, but little direct evidence is available to support the view that the immunosuppressive effects of FK-506 in vivo are mediated by a similar inhibition of lymphokine cascade. Tacrolimus 8-18 interleukin 2 Mus musculus 138-156 8986461-6 1996 In contrast to the effects of FK-506 on IL-2 and IFN-gamma productions in MLN, IL-1 and tumor necrosis factor-alpha in the intestinal wall, which were enhanced by H. nana infection, were not completely decreased as a result of 10.0 mg/kg FK-506 treatment. Tacrolimus 30-36 interleukin 2 Mus musculus 40-44 8986461-6 1996 In contrast to the effects of FK-506 on IL-2 and IFN-gamma productions in MLN, IL-1 and tumor necrosis factor-alpha in the intestinal wall, which were enhanced by H. nana infection, were not completely decreased as a result of 10.0 mg/kg FK-506 treatment. Tacrolimus 30-36 interferon gamma Mus musculus 49-58 8986461-7 1996 The reverse transcriptase-PCR revealed complete inhibition of IL-2 and IFN-gamma mRNA expression on mesenteric L3T4+ cells that were induced by H. nana infection, when mice were given 10.0 mg/kg/day FK-506 for 5 days. Tacrolimus 199-205 interleukin 2 Mus musculus 62-66 8986461-7 1996 The reverse transcriptase-PCR revealed complete inhibition of IL-2 and IFN-gamma mRNA expression on mesenteric L3T4+ cells that were induced by H. nana infection, when mice were given 10.0 mg/kg/day FK-506 for 5 days. Tacrolimus 199-205 interferon gamma Mus musculus 71-80 8816436-2 1996 In both cases, induction of TNF-alpha gene transcription can be blocked by the immunosuppressants cyclosporin A and FK506, which suggested a role for the NFAT family of proteins in the regulation of the gene in B cells. Tacrolimus 116-121 tumor necrosis factor Homo sapiens 28-37 9010851-9 1996 The complex of CsA or FK506 with CyP or FKBP, respectively, inhibits the activation of calcineurin. Tacrolimus 22-27 peptidylprolyl isomerase G Homo sapiens 33-36 8824230-8 1996 On the other hand, both PP1 and PP2B activities but not PP2A activity of cell extracts were suppressed by the addition of cyclosporin A or FK506 in the culture medium. Tacrolimus 139-144 protein phosphatase 1 catalytic subunit gamma Mus musculus 24-27 8816436-2 1996 In both cases, induction of TNF-alpha gene transcription can be blocked by the immunosuppressants cyclosporin A and FK506, which suggested a role for the NFAT family of proteins in the regulation of the gene in B cells. Tacrolimus 116-121 nuclear factor of activated T cells 2 Homo sapiens 154-158 8798476-2 1996 As the FK506 motif that competes with TbetaR-I for FKBP12 resembles an invariant Leu-Pro dipeptide in TbetaR-I, we replaced Leu193 and Pro194 with Ala, along with mutations across the Gly/Ser box. Tacrolimus 7-12 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 51-57 8702959-6 1996 FKBP12 dissociates from TbetaR-I in the presence of a high concentration of FK506. Tacrolimus 76-81 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 0-6 8774885-3 1996 To examine whether induced oligomerization can alter Raf kinase activity, sequences encoding the FK506-binding protein FKBP12 were fused to the amino terminus of c-Raf-1, introducing a binding site for FK506. Tacrolimus 97-102 FKBP prolyl isomerase 1A pseudogene 3 Homo sapiens 119-125 8774885-4 1996 Oligomerization of recombinant FKBP-Raf in situ, induced by the addition of the dimeric FK506 derivative FK1012A, activated Raf kinase activity at least half as well as epidermal growth factor (EGF). Tacrolimus 88-93 zinc fingers and homeoboxes 2 Homo sapiens 36-39 8774885-4 1996 Oligomerization of recombinant FKBP-Raf in situ, induced by the addition of the dimeric FK506 derivative FK1012A, activated Raf kinase activity at least half as well as epidermal growth factor (EGF). Tacrolimus 88-93 zinc fingers and homeoboxes 2 Homo sapiens 124-127 8702959-6 1996 FKBP12 dissociates from TbetaR-I in the presence of a high concentration of FK506. Tacrolimus 76-81 transforming growth factor beta receptor 1 Homo sapiens 24-32 8883951-8 1996 Complementary experiments with the selective calcineurin inhibitor, FK506, also showed the reduction of LTP threshold in a dose-dependent manner. Tacrolimus 68-73 calcineurin binding protein 1 Rattus norvegicus 45-66 8787699-7 1996 Stepwise regression analysis including tacrolimus, its metabolites, and liver function parameters suggested a model including serum activities of gamma-glutamyltransferase, alkaline phosphatase, and alanine aminotransferase as predictors for increased concentrations of demethyl tacrolimus, didemethyl tacrolimus, and the parent drug. Tacrolimus 39-49 glutamic--pyruvic transaminase Homo sapiens 199-223 8884530-4 1996 FK506 and CsA inhibit keratinocyte proliferation induced by EGF, TGF-alpha or IL-6. Tacrolimus 0-5 epidermal growth factor Homo sapiens 60-63 8884530-4 1996 FK506 and CsA inhibit keratinocyte proliferation induced by EGF, TGF-alpha or IL-6. Tacrolimus 0-5 transforming growth factor alpha Homo sapiens 65-74 8884530-4 1996 FK506 and CsA inhibit keratinocyte proliferation induced by EGF, TGF-alpha or IL-6. Tacrolimus 0-5 interleukin 6 Homo sapiens 78-82 8884530-6 1996 These findings might indicate that the effects of FK506 and CsA on proliferation of cultured normal human keratinocytes are probably related to direct effects on growth regulation of keratinocytes via EGF, TGF-alpha or IL-6 stimulation. Tacrolimus 50-55 epidermal growth factor Homo sapiens 201-204 8884530-6 1996 These findings might indicate that the effects of FK506 and CsA on proliferation of cultured normal human keratinocytes are probably related to direct effects on growth regulation of keratinocytes via EGF, TGF-alpha or IL-6 stimulation. Tacrolimus 50-55 transforming growth factor alpha Homo sapiens 206-215 8884530-6 1996 These findings might indicate that the effects of FK506 and CsA on proliferation of cultured normal human keratinocytes are probably related to direct effects on growth regulation of keratinocytes via EGF, TGF-alpha or IL-6 stimulation. Tacrolimus 50-55 interleukin 6 Homo sapiens 219-223 8880916-4 1996 Analysis of 1H-13C HSQC data acquired for the FKBP-12/ 13C-FK506 and FKBP-12/13C-FK506/CnB/BBD complexes indicates that FKBP-12/FK506 and CnB/BBD are in fast exchange in the quaternary complex. Tacrolimus 81-86 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 69-76 8880916-0 1996 Dynamic NMR studies of ligand-receptor interactions: design and analysis of a rapidly exchanging complex of FKBP-12/FK506 with a 24 kDa calcineurin fragment. Tacrolimus 116-121 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 108-115 8880916-4 1996 Analysis of 1H-13C HSQC data acquired for the FKBP-12/ 13C-FK506 and FKBP-12/13C-FK506/CnB/BBD complexes indicates that FKBP-12/FK506 and CnB/BBD are in fast exchange in the quaternary complex. Tacrolimus 81-86 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 69-76 8880916-2 1996 Using a combination of isotope labeling and isotope edited NMR, we have extended these techniques to characterize interactions of a much larger protein/drug complex, FKBP-12/ FK506 with its receptor protein, calcineurin. Tacrolimus 175-180 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 166-173 8880916-4 1996 Analysis of 1H-13C HSQC data acquired for the FKBP-12/ 13C-FK506 and FKBP-12/13C-FK506/CnB/BBD complexes indicates that FKBP-12/FK506 and CnB/BBD are in fast exchange in the quaternary complex. Tacrolimus 59-64 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 46-53 8857552-2 1996 Interpatient differences in liver CYP3A4 activity, as measured by the ERMBT, seem to account, for the most part, for interindividual differences in the kinetics of cyclosporin A and FK506. Tacrolimus 182-187 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-40 8880916-4 1996 Analysis of 1H-13C HSQC data acquired for the FKBP-12/ 13C-FK506 and FKBP-12/13C-FK506/CnB/BBD complexes indicates that FKBP-12/FK506 and CnB/BBD are in fast exchange in the quaternary complex. Tacrolimus 81-86 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 69-76 8880916-4 1996 Analysis of 1H-13C HSQC data acquired for the FKBP-12/ 13C-FK506 and FKBP-12/13C-FK506/CnB/BBD complexes indicates that FKBP-12/FK506 and CnB/BBD are in fast exchange in the quaternary complex. Tacrolimus 81-86 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 69-76 8702500-7 1996 Similarly, murine mdr3 expression confers resistance to the immunosuppressants cyclosporin A (CsA) and FK506 in a CsA-FK506-sensitive vph6 mutant yeast strain. Tacrolimus 103-108 ATP-binding cassette, sub-family B (MDR/TAP), member 1A Mus musculus 18-22 8702500-7 1996 Similarly, murine mdr3 expression confers resistance to the immunosuppressants cyclosporin A (CsA) and FK506 in a CsA-FK506-sensitive vph6 mutant yeast strain. Tacrolimus 118-123 ATP-binding cassette, sub-family B (MDR/TAP), member 1A Mus musculus 18-22 8702500-8 1996 CsA and FK506 are known to partially overcome Pgp-mediated drug resistance, suggesting the targets of these drugs might regulate Pgp function. Tacrolimus 8-13 ATP binding cassette subfamily B member 1 Homo sapiens 46-49 8702500-8 1996 CsA and FK506 are known to partially overcome Pgp-mediated drug resistance, suggesting the targets of these drugs might regulate Pgp function. Tacrolimus 8-13 ATP binding cassette subfamily B member 1 Homo sapiens 129-132 8702500-12 1996 Our results support the model that immunosuppressants reverse multidrug resistance by competing with other Pgp substrates but reveal that inhibition of FKBP12-dependent Pgp function may also contribute to reversal of multidrug resistance by FK506 and rapamycin. Tacrolimus 241-246 ATP binding cassette subfamily B member 1 Homo sapiens 107-110 8702500-12 1996 Our results support the model that immunosuppressants reverse multidrug resistance by competing with other Pgp substrates but reveal that inhibition of FKBP12-dependent Pgp function may also contribute to reversal of multidrug resistance by FK506 and rapamycin. Tacrolimus 241-246 ATP binding cassette subfamily B member 1 Homo sapiens 169-172 8854096-0 1996 Transient immunosuppression by FK506 permits a sustained high-level dystrophin expression after adenovirus-mediated dystrophin minigene transfer to skeletal muscles of adult dystrophic (mdx) mice. Tacrolimus 31-36 dystrophin, muscular dystrophy Mus musculus 68-78 8854096-3 1996 In this study we treated adult dystrophic (mdx) mice with daily subcutaneous injections of the immunosuppressive drug FK506 (tacrolimus) over 5, 10, 30 and 60 days after AV-mediated dystrophin gene transfer and compared the transduction level with saline-injected mdx controls. Tacrolimus 118-123 dystrophin, muscular dystrophy Mus musculus 182-192 8854096-4 1996 We show that daily FK506 treatment after AV-mediated dystrophin gene transfer into adult mdx muscle results in the maintenance of the initial transgene expression for at least 2 months, even when FK506 treatment was discontinued after 1 month. Tacrolimus 19-24 dystrophin, muscular dystrophy Mus musculus 53-63 8854096-6 1996 Moreover, we find that FK506 efficiently suppresses the humoral immune response against both the vector proteins and the transgene protein product (dystrophin). Tacrolimus 23-28 dystrophin, muscular dystrophy Mus musculus 148-158 8757216-0 1996 Effects of cyclosporin A and FK-506 on stem cell factor-induced histamine secretion and growth of human mast cells. Tacrolimus 29-35 KIT ligand Homo sapiens 39-55 8757216-2 1996 In this study the effects of cyclosporin A (CSA) and FK-506, two potent immunosuppressive drugs, on SCF-dependent histamine release and growth of human MCs were analyzed. Tacrolimus 53-59 KIT ligand Homo sapiens 100-103 8757216-5 1996 The effects of CSA and FK-506 on SCF-dependent release of histamine were dose-dependent (IC50: CSA, 1 to 10 ng/ml; FK-506, 0.3 to 3 ng/ml). Tacrolimus 23-29 KIT ligand Homo sapiens 33-36 8757216-5 1996 The effects of CSA and FK-506 on SCF-dependent release of histamine were dose-dependent (IC50: CSA, 1 to 10 ng/ml; FK-506, 0.3 to 3 ng/ml). Tacrolimus 23-29 ERCC excision repair 8, CSA ubiquitin ligase complex subunit Homo sapiens 95-98 8757216-5 1996 The effects of CSA and FK-506 on SCF-dependent release of histamine were dose-dependent (IC50: CSA, 1 to 10 ng/ml; FK-506, 0.3 to 3 ng/ml). Tacrolimus 115-121 ERCC excision repair 8, CSA ubiquitin ligase complex subunit Homo sapiens 15-18 8757216-5 1996 The effects of CSA and FK-506 on SCF-dependent release of histamine were dose-dependent (IC50: CSA, 1 to 10 ng/ml; FK-506, 0.3 to 3 ng/ml). Tacrolimus 115-121 KIT ligand Homo sapiens 33-36 8757216-9 1996 Together, CSA and FK-506 inhibit SCF-dependent release of histamine from human MCs and even augment SCF-dependent growth of human MCs in long-term culture. Tacrolimus 18-24 KIT ligand Homo sapiens 33-36 8757216-9 1996 Together, CSA and FK-506 inhibit SCF-dependent release of histamine from human MCs and even augment SCF-dependent growth of human MCs in long-term culture. Tacrolimus 18-24 KIT ligand Homo sapiens 100-103 8794888-2 1996 CsA and FK506 associate with intracellular binding proteins (i.e., CsA with cyclophilin A and FK506 with FKBP12) to form protein/drug complexes that suppress the immune system by preventing activation of T cells in response to antigen presentation. Tacrolimus 8-13 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 105-111 8794888-2 1996 CsA and FK506 associate with intracellular binding proteins (i.e., CsA with cyclophilin A and FK506 with FKBP12) to form protein/drug complexes that suppress the immune system by preventing activation of T cells in response to antigen presentation. Tacrolimus 94-99 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 105-111 8794888-4 1996 In previous studies, we identified calcineurin mutations that block binding by the cyclophilin A/CsA or FKBP12/FK506 complexes and thereby render yeast cells resistant to the antifungal effects of CsA or FK506. Tacrolimus 111-116 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 104-110 8794888-4 1996 In previous studies, we identified calcineurin mutations that block binding by the cyclophilin A/CsA or FKBP12/FK506 complexes and thereby render yeast cells resistant to the antifungal effects of CsA or FK506. Tacrolimus 204-209 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 104-110 8874888-1 1996 The effects of FK506, a Ca2+/calmodulin-dependent phosphatase 2B (calcineurin) inhibitor, on the NMDA receptor-mediated potentials and synaptic plasticity were investigated in the CA1 region of the rat hippocampus. Tacrolimus 15-20 carbonic anhydrase 2 Rattus norvegicus 24-27 8874888-1 1996 The effects of FK506, a Ca2+/calmodulin-dependent phosphatase 2B (calcineurin) inhibitor, on the NMDA receptor-mediated potentials and synaptic plasticity were investigated in the CA1 region of the rat hippocampus. Tacrolimus 15-20 carbonic anhydrase 1 Rattus norvegicus 180-183 8874888-6 1996 The differential effects of FK506 on LTP and depotentiation may attribute to the partial inhibition on the activity of NMDA receptors and the subsequent attenuation of intracellular Ca2+ increase. Tacrolimus 28-33 carbonic anhydrase 2 Rattus norvegicus 182-185 8663352-4 1996 In yeast, the immunosuppressive drug FK506 inhibited Pdr5p, thereby potentiating activation of the glucocorticoid receptor by dexamethasone, a ligand that is exported by Pdr5p. Tacrolimus 37-42 ATP-binding cassette multidrug transporter PDR5 Saccharomyces cerevisiae S288C 53-58 8663352-4 1996 In yeast, the immunosuppressive drug FK506 inhibited Pdr5p, thereby potentiating activation of the glucocorticoid receptor by dexamethasone, a ligand that is exported by Pdr5p. Tacrolimus 37-42 nuclear receptor subfamily 3 group C member 1 Homo sapiens 99-122 8663352-4 1996 In yeast, the immunosuppressive drug FK506 inhibited Pdr5p, thereby potentiating activation of the glucocorticoid receptor by dexamethasone, a ligand that is exported by Pdr5p. Tacrolimus 37-42 ATP-binding cassette multidrug transporter PDR5 Saccharomyces cerevisiae S288C 170-175 8752921-0 1996 Non-T cell-derived IL-4 plays an important role in IgE production induced by antigen resensitization and is resistant to FK506. Tacrolimus 121-126 interleukin 4 Mus musculus 19-23 8752921-4 1996 In contrast to its known potent immunosuppressive effects on T cells, FK506 only partially inhibited IL-4 produced by non-T cells; therefore, FK506 was found to be a useful tool for identifying a cell source of IL-4 production. Tacrolimus 70-75 interleukin 4 Mus musculus 101-105 8752921-4 1996 In contrast to its known potent immunosuppressive effects on T cells, FK506 only partially inhibited IL-4 produced by non-T cells; therefore, FK506 was found to be a useful tool for identifying a cell source of IL-4 production. Tacrolimus 142-147 interleukin 4 Mus musculus 211-215 8692927-11 1996 Like the mammalian and yeast FKBP13, the recombinant VfFKBP15 protein has rotamase activity that is inhibited by both FK506 and rapamycin with a Ki value of 30 nM and 0.9 nM, respectively, illustrating that VfFKBP15 binds rapamycin in preference over FK506. Tacrolimus 118-123 FKBP prolyl isomerase 2 Homo sapiens 29-35 8760046-3 1996 Of interest, FK-506 and RAP, but not CyA, are bound by the steroid receptor-associated FK-506-binding heat shock protein of 56 kDa, HSP56. Tacrolimus 13-19 FKBP prolyl isomerase 4 Homo sapiens 132-137 8757947-1 1996 Differential regulation of Fas (CD95) versus Fas ligand expression by cyclosporin A and FK506. Tacrolimus 88-93 Fas (TNF receptor superfamily member 6) Mus musculus 32-36 8757947-4 1996 We have found that CsA- and FK506-treated cells did not exhibit transcription of FasL mRNA after activation and were lacking functional FasL protein on their surface as determined by staining and the ability to induce apoptosis in Fas+ target cells. Tacrolimus 28-33 Fas ligand (TNF superfamily, member 6) Mus musculus 136-140 8757947-9 1996 We therefore conclude that CsA and FK506 block activation-induced apoptosis in T cell hybridomas predominantly by interfering with activation signals leading to FasL expression and, further, that the regulation of the expression of Fas and FasL on activated T cells is differentially controlled. Tacrolimus 35-40 Fas ligand (TNF superfamily, member 6) Mus musculus 161-165 8757947-9 1996 We therefore conclude that CsA and FK506 block activation-induced apoptosis in T cell hybridomas predominantly by interfering with activation signals leading to FasL expression and, further, that the regulation of the expression of Fas and FasL on activated T cells is differentially controlled. Tacrolimus 35-40 Fas ligand (TNF superfamily, member 6) Mus musculus 240-244 21136324-0 1996 Practical applications of time-averaged restrained molecular dynamics to ligand-receptor systems: FK506 bound to the Q50R,A95H,K98I triple mutant of FKBP-13. Tacrolimus 98-103 FKBP prolyl isomerase 2 Homo sapiens 149-156 21136324-2 1996 Practical suggestions are offered for performing TARMD calculations with ligand-receptor systems, and are illustrated for the complex of the immunosuppressant FK506 bound to Q50R,A95H,K98I triple mutant FKBP-13. Tacrolimus 159-164 FKBP prolyl isomerase 2 Homo sapiens 203-210 21136324-3 1996 The structure of (13)C-labeled FK506 bound to triple-mutant FKBP-13 was determined using a set of 87 NOE distance restraints derived from HSQC-NOESY experiments. Tacrolimus 31-36 FKBP prolyl isomerase 2 Homo sapiens 60-67 21136324-4 1996 TARMD was found to be superior to conventional simulated-annealing methods, and produced structures that were conformationally similar to FK506 bound to wild-type FKBP-12. Tacrolimus 138-143 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 163-170 8965835-0 1996 Increased interferon-gamma mRNA expression following alloincompatible myoblast transplantation is inhibited by FK506. Tacrolimus 111-116 interferon gamma Mus musculus 10-26 8757620-2 1996 Here we show that FK506-suppressible, delayed c-Rel induction is similar in B and T cells and is regulated by mRNA production. Tacrolimus 18-23 REL proto-oncogene, NF-kB subunit Homo sapiens 46-51 8757620-1 1996 c-Rel induction in activated lymphocytes is suppressed by the immunosuppressive drug, FK506. Tacrolimus 86-91 REL proto-oncogene, NF-kB subunit Homo sapiens 0-5 8965835-5 1996 Short-term immunosuppressive treatment with FK506 inhibited the transcription of IFN-gamma mRNA compared with that in untreated mice. Tacrolimus 44-49 interferon gamma Mus musculus 81-90 8762016-6 1996 Tacrolimus significantly increased NAG (N-acetyl-beta-glucosaminidase) excretion and associated histological damage, finally decreasing creatinine clearance. Tacrolimus 0-10 O-GlcNAcase Rattus norvegicus 35-38 8642394-7 1996 When the monkeys were immunosuppressed with FK506, muscle fibers expressing beta-galactosidase (beta-gal) were present 1, 4 and 12 weeks after the transplantation. Tacrolimus 44-49 galactosidase beta 1 Homo sapiens 76-94 8642394-7 1996 When the monkeys were immunosuppressed with FK506, muscle fibers expressing beta-galactosidase (beta-gal) were present 1, 4 and 12 weeks after the transplantation. Tacrolimus 44-49 galactosidase beta 1 Homo sapiens 76-84 8843591-6 1996 The doses of tacrolimus in unmatched cases tended to be larger than those in matched cases for every locus except for DQA1. Tacrolimus 13-23 major histocompatibility complex, class II, DQ alpha 1 Homo sapiens 118-122 8843593-0 1996 Inhibition by CsA and FK506 of the in vitro proliferative response of gamma delta T cells on stimulation with anti-TCR delta monoclonal antibody. Tacrolimus 22-27 T cell receptor delta chain Mus musculus 115-124 8843593-4 1996 Using spleen cells from Tg.Tlaa-3-1 mice, we showed that cyclosporin A (CsA) and FK506 inhibited the in vitro proliferative response of gamma delta T cells on stimulation with anti-TCR delta mAb. Tacrolimus 81-86 T cell receptor delta chain Mus musculus 181-190 8843593-5 1996 The dose-dependent inhibitory effect of CsA and FK506 on proliferation of gamma delta T cells on stimulation with anti-TCR delta mAb was similar to that on proliferation of alpha beta T cells on stimulation with anti-TCF beta mAb. Tacrolimus 48-53 T cell receptor delta chain Mus musculus 119-128 8843593-7 1996 The proliferative response of gamma delta T cells among spleen cells from TCR alpha beta-depleted Tg.Tlaa-3-1 mice was also inhibited by CsA and FK506, suggesting that the inhibition directly affected gamma delta T cells without mediation by alpha beta T cells. Tacrolimus 145-150 T cell receptor alpha chain Mus musculus 74-83 8787547-0 1996 Antioncogene P53 and mitogenic cytokine interleukin-8 aberrantly expressed in psoriatic skin are inversely regulated by the antipsoriatic drug tacrolimus (FK506). Tacrolimus 143-153 tumor protein p53 Homo sapiens 13-16 8787547-0 1996 Antioncogene P53 and mitogenic cytokine interleukin-8 aberrantly expressed in psoriatic skin are inversely regulated by the antipsoriatic drug tacrolimus (FK506). Tacrolimus 143-153 C-X-C motif chemokine ligand 8 Homo sapiens 40-53 8787547-0 1996 Antioncogene P53 and mitogenic cytokine interleukin-8 aberrantly expressed in psoriatic skin are inversely regulated by the antipsoriatic drug tacrolimus (FK506). Tacrolimus 155-160 tumor protein p53 Homo sapiens 13-16 8787547-0 1996 Antioncogene P53 and mitogenic cytokine interleukin-8 aberrantly expressed in psoriatic skin are inversely regulated by the antipsoriatic drug tacrolimus (FK506). Tacrolimus 155-160 C-X-C motif chemokine ligand 8 Homo sapiens 40-53 8787547-6 1996 After 1-3 hr, IL-8 mRNA levels were dose-dependently decreased in tacrolimus (FK506)-treated cells. Tacrolimus 66-76 C-X-C motif chemokine ligand 8 Homo sapiens 14-18 8787547-6 1996 After 1-3 hr, IL-8 mRNA levels were dose-dependently decreased in tacrolimus (FK506)-treated cells. Tacrolimus 78-83 C-X-C motif chemokine ligand 8 Homo sapiens 14-18 8787547-8 1996 Interestingly, p53 transcription was clearly induced by FK506 treatment. Tacrolimus 56-61 tumor protein p53 Homo sapiens 15-18 8665940-7 1996 Low concentrations (2 nM) of okadaic acid, a serine/threonine phosphatase inhibitor, prevented TNF-alpha-induced inhibition of MAPK and restored insulin"s effect on MAPK activity, while orthovanadate (a tyrosine phosphatase inhibitor), inhibitor 2 (phosphatase-1 inhibitor) and FK506 (phosphatase-2B inhibitor) were ineffective. Tacrolimus 278-283 tumor necrosis factor Rattus norvegicus 95-104 8784785-1 1996 BACKGROUND: The immunophilins are proteins that mediate actions of immunosuppressant drugs such as FK506 and cyclosporin A by binding to calcineurin, inhibiting its phosphatase activity, and increasing the phosphorylation level of transcription factors required for interleukin 2 formation. Tacrolimus 99-104 interleukin 2 Rattus norvegicus 266-279 8784785-13 1996 Synapsin I, a synaptic vesicle phosphoprotein, displays enhanced phosphorylation in the presence of FK506. Tacrolimus 100-105 synapsin I Rattus norvegicus 0-10 21232286-5 1996 The immunosuppressant drugs FK506 and rapamycin inhibit the prolyl isomerase activity of FKBP12 and could cause cardiac dysfunction by inducing a Ca(2+) leak from the sarcoplasmic reticulum. Tacrolimus 28-33 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 89-95 8627611-3 1996 Analyses of several X-ray crystal structures of FKBP12-urea complexes demonstrate that the urea-containing inhibitors associate with FKBP12 in a manner that is similar to, but significantly different from, that observed for the natural product FK506. Tacrolimus 244-249 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 48-54 8627611-3 1996 Analyses of several X-ray crystal structures of FKBP12-urea complexes demonstrate that the urea-containing inhibitors associate with FKBP12 in a manner that is similar to, but significantly different from, that observed for the natural product FK506. Tacrolimus 244-249 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 133-139 8623162-1 1996 FK506 blocks T cell activation by preventing the transcription of lymphokine genes through binding to the intracellular protein FKBP12 and formation of complex that inhibits the phosphatase activity of calcineurin. Tacrolimus 0-5 FKBP prolyl isomerase 1A Rattus norvegicus 128-134 8603582-0 1996 Immunosuppressant agent FK506 stimulates growth hormone (GH) secretion and gene expression of hypothalamic GH-releasing hormone in the rat. Tacrolimus 24-29 gonadotropin releasing hormone receptor Rattus norvegicus 41-55 8603582-0 1996 Immunosuppressant agent FK506 stimulates growth hormone (GH) secretion and gene expression of hypothalamic GH-releasing hormone in the rat. Tacrolimus 24-29 gonadotropin releasing hormone receptor Rattus norvegicus 57-59 8603582-0 1996 Immunosuppressant agent FK506 stimulates growth hormone (GH) secretion and gene expression of hypothalamic GH-releasing hormone in the rat. Tacrolimus 24-29 gonadotropin releasing hormone receptor Rattus norvegicus 107-109 8603582-6 1996 The FK506 significantly stimulated GH release from the rat anterior pituitary cells in a dose-dependent manner in vitro. Tacrolimus 4-9 gonadotropin releasing hormone receptor Rattus norvegicus 35-37 8603582-7 1996 In in vivo experiments, the area under the curve of GH surges was significantly increased in FK506-treated rats, although the peak height and the trough level of GH surges were not altered. Tacrolimus 93-98 gonadotropin releasing hormone receptor Rattus norvegicus 52-54 8603582-7 1996 In in vivo experiments, the area under the curve of GH surges was significantly increased in FK506-treated rats, although the peak height and the trough level of GH surges were not altered. Tacrolimus 93-98 gonadotropin releasing hormone receptor Rattus norvegicus 162-164 8603582-8 1996 Pituitary GH messenger RNA (mRNA) levels were significantly increased by the FK506 treatment. Tacrolimus 77-82 gonadotropin releasing hormone receptor Rattus norvegicus 10-12 8603582-10 1996 These findings indicate that FK506 stimulates GH secretion and gene expression of hypothalamic GRH in the rat. Tacrolimus 29-34 gonadotropin releasing hormone receptor Rattus norvegicus 46-48 8669110-7 1996 Noninhibitory doses of CsA (8 nM) or FK506 (0.2 nM) suppressed mitogen-induced IL-2 production by 60-80% when combined with a noninhibitory dose (25 nM) of Ro 31-8220, indicating the potent synergy between these agents. Tacrolimus 37-42 interleukin 2 Homo sapiens 79-83 8647935-0 1996 Immunosuppressant FK506 induces interleukin-6 production through the activation of transcription factor nuclear factor (NF)-kappa(B). Tacrolimus 18-23 interleukin 6 Homo sapiens 32-45 8647935-0 1996 Immunosuppressant FK506 induces interleukin-6 production through the activation of transcription factor nuclear factor (NF)-kappa(B). Tacrolimus 18-23 nuclear factor kappa B subunit 1 Homo sapiens 104-131 8647935-2 1996 FK506 is a powerful immunosuppressive drug currently in use that inhibits the activation of several transcription factors (nuclear factor (NF)-AT and NF-kappaB) critical for T cell activation. Tacrolimus 0-5 nuclear factor kappa B subunit 1 Homo sapiens 150-159 8647935-3 1996 We show here that, contrary to the situation in T cells, FK506 activates transcription factor NF-kappaB in nonlymphoid cells such as fibroblasts and renal mesangial cells. Tacrolimus 57-62 nuclear factor kappa B subunit 1 Homo sapiens 94-103 8647935-4 1996 We further show that FK506 induces NF-kappaB-regulated IL-6 production in vitro and in vivo, in particular in kidney. Tacrolimus 21-26 nuclear factor kappa B subunit 1 Homo sapiens 35-44 8647935-4 1996 We further show that FK506 induces NF-kappaB-regulated IL-6 production in vitro and in vivo, in particular in kidney. Tacrolimus 21-26 interleukin 6 Homo sapiens 55-59 8647935-7 1996 These results thus suggest a causal relationship between FK506-induced NF-kappaB activation/IL-6 production and some of FK506-induced renal abnormalities. Tacrolimus 57-62 nuclear factor kappa B subunit 1 Homo sapiens 71-80 8647935-7 1996 These results thus suggest a causal relationship between FK506-induced NF-kappaB activation/IL-6 production and some of FK506-induced renal abnormalities. Tacrolimus 57-62 interleukin 6 Homo sapiens 92-96 8647935-7 1996 These results thus suggest a causal relationship between FK506-induced NF-kappaB activation/IL-6 production and some of FK506-induced renal abnormalities. Tacrolimus 120-125 nuclear factor kappa B subunit 1 Homo sapiens 71-80 8647935-7 1996 These results thus suggest a causal relationship between FK506-induced NF-kappaB activation/IL-6 production and some of FK506-induced renal abnormalities. Tacrolimus 120-125 interleukin 6 Homo sapiens 92-96 8787547-11 1996 Together with earlier results showing downmodulation for IL-8 receptor type A expression in cultured KC treated with FK506, these results suggest that both the mitogenic IL-8/IL-8R system and the cell cycle inhibitor p53 represent potential targets for the antipsoriatic action of the drug, whereas protooncogenes acting downstream in mitogenic signal transduction cascades are unaffected. Tacrolimus 117-122 C-X-C motif chemokine ligand 8 Homo sapiens 57-61 8787547-11 1996 Together with earlier results showing downmodulation for IL-8 receptor type A expression in cultured KC treated with FK506, these results suggest that both the mitogenic IL-8/IL-8R system and the cell cycle inhibitor p53 represent potential targets for the antipsoriatic action of the drug, whereas protooncogenes acting downstream in mitogenic signal transduction cascades are unaffected. Tacrolimus 117-122 C-X-C motif chemokine ligand 8 Homo sapiens 170-174 8787547-11 1996 Together with earlier results showing downmodulation for IL-8 receptor type A expression in cultured KC treated with FK506, these results suggest that both the mitogenic IL-8/IL-8R system and the cell cycle inhibitor p53 represent potential targets for the antipsoriatic action of the drug, whereas protooncogenes acting downstream in mitogenic signal transduction cascades are unaffected. Tacrolimus 117-122 tumor protein p53 Homo sapiens 217-220 8628289-2 1996 Previous work showed that Ca2+ tolerance can be restored to pmc1 mutants by inactivation of calcineurin, a Ca2+/calmodulin-dependent protein phosphatase sensitive to the immunosuppressive drug FK506. Tacrolimus 193-198 calcium-transporting ATPase PMC1 Saccharomyces cerevisiae S288C 60-64 8894806-9 1996 Both CSA and M17 synergized more strongly with FK 506 than they did between themselves. Tacrolimus 47-53 ERCC excision repair 8, CSA ubiquitin ligase complex subunit Homo sapiens 5-8 8812665-0 1996 Immunophilin Modulation of Calcium Channel Gating The FK506 binding protein (FKBP12) is the cytosolic receptor for the immunosuppressant drugs FK506 and rapamycin. Tacrolimus 54-59 peptidylprolyl isomerase A (cyclophilin A) L homeolog Xenopus laevis 0-12 8812665-0 1996 Immunophilin Modulation of Calcium Channel Gating The FK506 binding protein (FKBP12) is the cytosolic receptor for the immunosuppressant drugs FK506 and rapamycin. Tacrolimus 54-59 FKBP prolyl isomerase 1A L homeolog Xenopus laevis 77-83 8812665-4 1996 These effects were reversed by adding FK506 or rapamycin, both of which inhibit FKBP12 isomerase activity and dissociate the FKBP-RyR complex. Tacrolimus 38-43 FKBP prolyl isomerase 1A L homeolog Xenopus laevis 80-86 8623224-0 1996 The inhibition of T-cell-receptor-induced Fas ligand upregulation by cyclosporine and FK 506. Tacrolimus 86-92 Fas ligand Homo sapiens 42-52 8785272-1 1996 The FK506-binding protein (FKBP12) is important in the immunosuppressant action of FK506 and rapamycin. Tacrolimus 4-9 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 27-33 8785272-5 1996 Results obtained for the FKBP12/rapamycin complex are similar to those found for the FKBP12/FK506 complex. Tacrolimus 92-97 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 85-91 8786538-1 1996 FK-506 blocks T cell activation by preventing lymphokine gene transcription through formation of a complex with FKBP12 that inhibits calcineurin phosphatase activity. Tacrolimus 0-6 interleukin 2 Homo sapiens 46-56 8786538-1 1996 FK-506 blocks T cell activation by preventing lymphokine gene transcription through formation of a complex with FKBP12 that inhibits calcineurin phosphatase activity. Tacrolimus 0-6 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 112-118 8762016-6 1996 Tacrolimus significantly increased NAG (N-acetyl-beta-glucosaminidase) excretion and associated histological damage, finally decreasing creatinine clearance. Tacrolimus 0-10 O-GlcNAcase Rattus norvegicus 40-69 8626756-4 1996 MRP and Mdr3 expression produced pleiotropic effects on drug resistance in this mutant, as corresponding VASY2563 transformants also acquired resistance to the anti-fungal agent FK506 and to the K+/H+ ionophore valinomycin. Tacrolimus 178-183 ATP binding cassette subfamily C member 3 Homo sapiens 0-3 8680047-15 1996 Tacrolimus binds to FK binding protein-12 (FKBP-12) to create a complex that inhibits CN. Tacrolimus 0-10 FKBP prolyl isomerase 1A Homo sapiens 20-41 8680047-15 1996 Tacrolimus binds to FK binding protein-12 (FKBP-12) to create a complex that inhibits CN. Tacrolimus 0-10 FKBP prolyl isomerase 1A Homo sapiens 43-50 8599949-6 1996 The rapamycin-FK506 binding protein complex is the effector of the inhibition of 4E-BP1 phosphorylation as excess of FK506 over rapamycin reversed the rapamycin-mediated inhibition of 4E-BP1 phosphorylation. Tacrolimus 14-19 eukaryotic translation initiation factor 4E binding protein 1 Homo sapiens 81-87 8627154-6 1996 CNA alpha -/- T cells remained sensitive to both cyclosporin A and FK506, suggesting that CNA beta or another CNA-like molecule can mediate the action of these immunosuppressive drugs. Tacrolimus 67-72 protein phosphatase 3, catalytic subunit, alpha isoform Mus musculus 0-3 8627154-7 1996 CNA alpha -/- mice provide an animal model for dissecting the physiologic functions of calcineurin as well as the effects of FK506 and CsA. Tacrolimus 125-130 protein phosphatase 3, catalytic subunit, alpha isoform Mus musculus 0-3 8611359-3 1996 Although insulin requirement with tacrolimus therapy has been occasionally reported in adolescent patients post liver transplant, only a single case in a pediatric kidney transplant recipient has been previously documented. Tacrolimus 34-44 insulin Homo sapiens 9-16 9005438-1 1996 The 12 kDa FK506-binding protein FKBP12 is a cis-trans peptidyl-prolyl isomerase that binds the macrolides FK506 and rapamycin. Tacrolimus 11-16 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 33-39 9005438-3 1996 For each mutant FKBP12, we measured the affinity for FK506 and rapamycin and the catalytic efficiency in the cis-frans peptidyl-prolyl isomerase reaction. Tacrolimus 53-58 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 16-22 9005438-4 1996 The mutation of Trp59 or Phe99 generates an FKBP12 with a significantly lower affinity for FK506 than wild-type protein. Tacrolimus 91-96 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 44-50 8566225-3 1996 Accumulation of Ca2+ within the cls2 cells is synergistically elevated by the addition of immunosuppressant, FK506. Tacrolimus 109-114 mannosylinositol phosphorylceramide synthase regulatory subunit Saccharomyces cerevisiae S288C 32-36 8566225-4 1996 Moreover, in the vma3 background, toxicity caused by the cls2 mutation is greatly enhanced by FK506. Tacrolimus 94-99 H(+)-transporting V0 sector ATPase subunit c Saccharomyces cerevisiae S288C 17-21 8566225-4 1996 Moreover, in the vma3 background, toxicity caused by the cls2 mutation is greatly enhanced by FK506. Tacrolimus 94-99 mannosylinositol phosphorylceramide synthase regulatory subunit Saccharomyces cerevisiae S288C 57-61 8566225-5 1996 Given that FK506 inhibits the calcineurin activity, Cls2p likely functions in releasing Ca2+ flux from the endoplasmic reticulum, somehow cooperating with calcineurin. Tacrolimus 11-16 mannosylinositol phosphorylceramide synthase regulatory subunit Saccharomyces cerevisiae S288C 52-57 8576111-3 1996 Inhibition of calcineurin by the immunosuppressive drugs cyclosporin A and FK506 prevents dephosphorylation of NFATp and its translocation to the nucleus. Tacrolimus 75-80 nuclear factor of activated T cells 2 Homo sapiens 111-116 8576111-9 1996 Furthermore, the binding of both forms of NFATp to calcineurin was inhibited by pretreatment of calcineurin with a complex of FK506 and its ligand FKBP12. Tacrolimus 126-131 nuclear factor of activated T cells 2 Homo sapiens 42-47 8576111-9 1996 Furthermore, the binding of both forms of NFATp to calcineurin was inhibited by pretreatment of calcineurin with a complex of FK506 and its ligand FKBP12. Tacrolimus 126-131 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 147-153 8717522-3 1996 The FKBP12.FK506 complex specifically binds to and inhibits calcineurin, a signaling protein required for transcriptional activation of the interleukin (IL)-2 gene in response to T cell antigen receptor engagement. Tacrolimus 11-16 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 4-10 8717522-3 1996 The FKBP12.FK506 complex specifically binds to and inhibits calcineurin, a signaling protein required for transcriptional activation of the interleukin (IL)-2 gene in response to T cell antigen receptor engagement. Tacrolimus 11-16 interleukin 2 Homo sapiens 140-158 8822088-5 1996 FK506 treatment suppressed the accumulation of ED-1-positive cells, CD4-positive cells, CD8-positive cells, interleukin-2 (IL-2)-receptor-positive cells, leukocyte-function-associated antigen-1 (LFA-1)-positive cells and intercellular adhesion molecule-1 (ICAM-1)-expression in nephritic glomeruli. Tacrolimus 0-5 interleukin 2 Rattus norvegicus 123-127 8822088-5 1996 FK506 treatment suppressed the accumulation of ED-1-positive cells, CD4-positive cells, CD8-positive cells, interleukin-2 (IL-2)-receptor-positive cells, leukocyte-function-associated antigen-1 (LFA-1)-positive cells and intercellular adhesion molecule-1 (ICAM-1)-expression in nephritic glomeruli. Tacrolimus 0-5 Cd4 molecule Rattus norvegicus 68-71 8822088-5 1996 FK506 treatment suppressed the accumulation of ED-1-positive cells, CD4-positive cells, CD8-positive cells, interleukin-2 (IL-2)-receptor-positive cells, leukocyte-function-associated antigen-1 (LFA-1)-positive cells and intercellular adhesion molecule-1 (ICAM-1)-expression in nephritic glomeruli. Tacrolimus 0-5 interleukin 2 Rattus norvegicus 108-121 8822088-5 1996 FK506 treatment suppressed the accumulation of ED-1-positive cells, CD4-positive cells, CD8-positive cells, interleukin-2 (IL-2)-receptor-positive cells, leukocyte-function-associated antigen-1 (LFA-1)-positive cells and intercellular adhesion molecule-1 (ICAM-1)-expression in nephritic glomeruli. Tacrolimus 0-5 integrin subunit alpha L Rattus norvegicus 154-193 8822088-5 1996 FK506 treatment suppressed the accumulation of ED-1-positive cells, CD4-positive cells, CD8-positive cells, interleukin-2 (IL-2)-receptor-positive cells, leukocyte-function-associated antigen-1 (LFA-1)-positive cells and intercellular adhesion molecule-1 (ICAM-1)-expression in nephritic glomeruli. Tacrolimus 0-5 integrin subunit alpha L Rattus norvegicus 195-200 8822088-5 1996 FK506 treatment suppressed the accumulation of ED-1-positive cells, CD4-positive cells, CD8-positive cells, interleukin-2 (IL-2)-receptor-positive cells, leukocyte-function-associated antigen-1 (LFA-1)-positive cells and intercellular adhesion molecule-1 (ICAM-1)-expression in nephritic glomeruli. Tacrolimus 0-5 intercellular adhesion molecule 1 Rattus norvegicus 221-254 8822088-5 1996 FK506 treatment suppressed the accumulation of ED-1-positive cells, CD4-positive cells, CD8-positive cells, interleukin-2 (IL-2)-receptor-positive cells, leukocyte-function-associated antigen-1 (LFA-1)-positive cells and intercellular adhesion molecule-1 (ICAM-1)-expression in nephritic glomeruli. Tacrolimus 0-5 intercellular adhesion molecule 1 Rattus norvegicus 256-262 8822088-7 1996 On the other hand, IL-2 production from the spleen cells isolated from nephritic rats treated with FK506 was lower than that in the nephritic control rats. Tacrolimus 99-104 interleukin 2 Rattus norvegicus 19-23 8822088-8 1996 These results suggest that FK506 is effective against crescentic-type anti-GBM nephritis and that the antinephritic mechanisms of FK506 is due to the inhibition of intraglomerular accumulation and activation of leukocytes through the suppression of ICAM-1 expression and IL-2 production. Tacrolimus 130-135 intercellular adhesion molecule 1 Rattus norvegicus 249-255 8822088-8 1996 These results suggest that FK506 is effective against crescentic-type anti-GBM nephritis and that the antinephritic mechanisms of FK506 is due to the inhibition of intraglomerular accumulation and activation of leukocytes through the suppression of ICAM-1 expression and IL-2 production. Tacrolimus 130-135 interleukin 2 Rattus norvegicus 271-275 8622563-7 1996 Nevertheless, if Dex and TGF-beta 1 were dosed together with one of these immunosuppressants, suppressions of histamine and ischemic edema were 53%, 45% (FK506), 45%, 49% (CsA), 44%, 48% (Rapa) and 39%, 51% (DSP), respectively. Tacrolimus 154-159 transforming growth factor, beta 1 Mus musculus 25-35 8890921-3 1996 It has been shown that glucocorticoids and immunosuppressive agents such as cyclosporin and FK-506 inhibit TNF-alpha generation by T-lymphocytes and monocytes. Tacrolimus 92-98 tumor necrosis factor Mus musculus 107-116 8805102-6 1996 Rapamycin depressed the production of IL-6 and TNF-alpha, and FK506 depressed the production of TNF-alpha. Tacrolimus 62-67 tumor necrosis factor Homo sapiens 96-105 8545894-0 1995 Inhibitory effect of plasma FKBP12 on immunosuppressive activity of FK506. Tacrolimus 68-73 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 28-34 8545894-1 1995 To evaluate the roles of extracellular FKBP12, we examined the effect of extracellular FKBP12 on the immunosuppressive activity of FK506 in vitro and clinically. Tacrolimus 131-136 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 87-93 8545894-2 1995 The ability of FK506 to suppress phytohemagglutinin-induced proliferative response of human peripheral blood mononuclear cells was inhibited in the presence of recombinant FKBP12 dose-dependently. Tacrolimus 15-20 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 172-178 8545894-3 1995 We measured plasma levels of FKBP12 using a newly developed enzyme-linked immunosorbent assay system in 34 patients receiving FK506 after liver transplantation. Tacrolimus 126-131 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 29-35 8545894-9 1995 These results suggest that the rapid increase in plasma levels of FKBP12 may contribute to the occurrence and progress of acute cellular rejection probably by inhibiting the immunosuppressive activity of FK506. Tacrolimus 204-209 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 66-72 8524402-0 1995 Crystal structures of human calcineurin and the human FKBP12-FK506-calcineurin complex. Tacrolimus 61-66 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 54-60 8524402-2 1995 CaN is the target of the immunosuppressive drugs cyclosporin A and FK506, which inhibit CaN after forming complexes with cytoplasmic binding proteins (cyclophilin and FKBP12, respectively). Tacrolimus 67-72 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 167-173 8524402-3 1995 We report here the crystal structures of full-length human CaN at 2.1 A resolution and of the complex of human CaN with FKBP12-FK506 at 3.5 A resolution. Tacrolimus 127-132 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 120-126 8524402-6 1995 In the FKBP12-FK506-CaN complex, the auto-inhibitory element is displaced from the active site. Tacrolimus 14-19 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 7-13 8524402-7 1995 The site of binding of FKBP12-FK506 appears to be shared by other non-competitive inhibitors of calcineurin, including a natural anchoring protein. Tacrolimus 30-35 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 23-29 8599949-6 1996 The rapamycin-FK506 binding protein complex is the effector of the inhibition of 4E-BP1 phosphorylation as excess of FK506 over rapamycin reversed the rapamycin-mediated inhibition of 4E-BP1 phosphorylation. Tacrolimus 14-19 eukaryotic translation initiation factor 4E binding protein 1 Homo sapiens 184-190 8599949-6 1996 The rapamycin-FK506 binding protein complex is the effector of the inhibition of 4E-BP1 phosphorylation as excess of FK506 over rapamycin reversed the rapamycin-mediated inhibition of 4E-BP1 phosphorylation. Tacrolimus 117-122 eukaryotic translation initiation factor 4E binding protein 1 Homo sapiens 81-87 8599949-6 1996 The rapamycin-FK506 binding protein complex is the effector of the inhibition of 4E-BP1 phosphorylation as excess of FK506 over rapamycin reversed the rapamycin-mediated inhibition of 4E-BP1 phosphorylation. Tacrolimus 117-122 eukaryotic translation initiation factor 4E binding protein 1 Homo sapiens 184-190 8617295-7 1996 B7-1 stimulation is not mediated by the enhancement of IL-2 production: B7-1 enhancement of IL-2R alpha expression was FK506 resistant, while the inclusion of FK506 abrogated IL-2 production of the Th1 cells. Tacrolimus 119-124 CD80 antigen Mus musculus 72-76 8617295-7 1996 B7-1 stimulation is not mediated by the enhancement of IL-2 production: B7-1 enhancement of IL-2R alpha expression was FK506 resistant, while the inclusion of FK506 abrogated IL-2 production of the Th1 cells. Tacrolimus 119-124 interleukin 2 receptor, alpha chain Mus musculus 92-103 8617295-7 1996 B7-1 stimulation is not mediated by the enhancement of IL-2 production: B7-1 enhancement of IL-2R alpha expression was FK506 resistant, while the inclusion of FK506 abrogated IL-2 production of the Th1 cells. Tacrolimus 119-124 interleukin 2 Mus musculus 92-96 8617295-7 1996 B7-1 stimulation is not mediated by the enhancement of IL-2 production: B7-1 enhancement of IL-2R alpha expression was FK506 resistant, while the inclusion of FK506 abrogated IL-2 production of the Th1 cells. Tacrolimus 159-164 CD80 antigen Mus musculus 0-4 8617295-7 1996 B7-1 stimulation is not mediated by the enhancement of IL-2 production: B7-1 enhancement of IL-2R alpha expression was FK506 resistant, while the inclusion of FK506 abrogated IL-2 production of the Th1 cells. Tacrolimus 159-164 negative elongation factor complex member C/D, Th1l Mus musculus 198-201 8689938-0 1995 Metabolism of the immunosuppressant tacrolimus in the small intestine: cytochrome P450, drug interactions, and interindividual variability. Tacrolimus 36-46 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 71-86 8689938-5 1995 The cytochrome P450 (CYP) enzymes responsible for tacrolimus metabolism in small intestine were identified using specific CYP antibodies and inhibitors. Tacrolimus 50-60 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 4-19 8689938-5 1995 The cytochrome P450 (CYP) enzymes responsible for tacrolimus metabolism in small intestine were identified using specific CYP antibodies and inhibitors. Tacrolimus 50-60 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 21-24 8689938-5 1995 The cytochrome P450 (CYP) enzymes responsible for tacrolimus metabolism in small intestine were identified using specific CYP antibodies and inhibitors. Tacrolimus 50-60 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 122-125 8689938-9 1995 The metabolism of tacrolimus by human small intestine was inhibited by anti-CYP3A, troleandomycin, and erythromycin, indicating that, as in the liver, CYP3A enzymes are the major enzymes for tacrolimus metabolism in the human small intestine. Tacrolimus 18-28 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 76-81 8689938-9 1995 The metabolism of tacrolimus by human small intestine was inhibited by anti-CYP3A, troleandomycin, and erythromycin, indicating that, as in the liver, CYP3A enzymes are the major enzymes for tacrolimus metabolism in the human small intestine. Tacrolimus 18-28 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 151-156 8689938-9 1995 The metabolism of tacrolimus by human small intestine was inhibited by anti-CYP3A, troleandomycin, and erythromycin, indicating that, as in the liver, CYP3A enzymes are the major enzymes for tacrolimus metabolism in the human small intestine. Tacrolimus 191-201 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 76-81 8689938-9 1995 The metabolism of tacrolimus by human small intestine was inhibited by anti-CYP3A, troleandomycin, and erythromycin, indicating that, as in the liver, CYP3A enzymes are the major enzymes for tacrolimus metabolism in the human small intestine. Tacrolimus 191-201 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 151-156 8689938-13 1995 It is concluded that tacrolimus is metabolized by cytochrome CYP3A enzymes in the small intestine. Tacrolimus 21-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 61-66 8689938-14 1995 The rate of the CYP3A enzymatic activities varies about 5 times from patient to patient, and drugs that interfere with the in vitro metabolism of tacrolimus in the liver also inhibit its small intestinal metabolism. Tacrolimus 146-156 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 16-21 8530625-0 1995 Expression of intercellular adhesion molecule-1 on human thyroid cells from patients with autoimmune thyroid disease: study of thyroid xenografts in nude and severe combined immunodeficient mice and treatment with FK-506. Tacrolimus 214-220 intercellular adhesion molecule 1 Homo sapiens 14-47 8530625-6 1995 When the SCID mice engrafted with AITD tissue were treated with the anti-CD4+ T (helper) cell agent FK-506, the expression of ICAM-1 was reduced significantly compared with that in the original tissue or that in nontreated mice engrafted with the same tissue. Tacrolimus 100-106 intercellular adhesion molecule 1 Mus musculus 126-132 8597171-5 1995 Observations on the FK 506-induced release of endothelin-1 from isolated rat kidney mesangial cells suggest that this cell may be an important target associated with the nephrotoxic potential of the drug, and that this action may be mediated via the FKBP. Tacrolimus 20-26 endothelin 1 Rattus norvegicus 46-58 7592869-1 1995 FK506, an immunosuppressant that prolongs allograft survival, is a co-drug with its intracellular receptor, FKBP12. Tacrolimus 0-5 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 108-114 8626235-2 1996 The antascomicins bind strongly to the FK506-binding protein FKBP12 and antagonize the immunosuppressive activity of FK506 and rapamycin. Tacrolimus 39-44 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 61-67 7592869-2 1995 The FKBP12.FK506 complex inhibits calcineurin, a critical signaling molecule during T-cell activation. Tacrolimus 11-16 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 4-10 7592869-3 1995 FKBP12 was, until recently, the sole FKBP known to mediate calcineurin inhibition at clinically relevant FK506 concentrations. Tacrolimus 105-110 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 0-6 7592869-5 1995 Recently, a novel protein, FKBP12.6, was found to inhibit calcineurin at clinically relevant FK506 concentrations. Tacrolimus 93-98 FKBP prolyl isomerase 1B Homo sapiens 27-35 8521476-1 1995 The immunosuppressant drug FK506 binds to the immunophilin protein FKBP12 and inhibits its prolyl isomerase activity. Tacrolimus 27-32 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 67-73 8521476-4 1995 FKBP12 is physically associated with the RyR and IP3R Ca2+ channels in the absence of FK506, with added FK506 disrupting these complexes. Tacrolimus 104-109 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 0-6 7592869-7 1995 In transfected Jurkat cells, FKBP12.6 is equivalent to FKBP12 at mediating the inhibitory effects of FK506. Tacrolimus 101-106 FKBP prolyl isomerase 1B Homo sapiens 29-37 7592869-7 1995 In transfected Jurkat cells, FKBP12.6 is equivalent to FKBP12 at mediating the inhibitory effects of FK506. Tacrolimus 101-106 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 29-35 8521476-6 1995 We now report that calcineurin is physiologically associated with the IP3R-FKBP12 and RyR-FKBP12 receptor complexes and that this interaction can be disrupted by FK506 or rapamycin. Tacrolimus 162-167 inositol 1,4,5-trisphosphate receptor type 3 Homo sapiens 70-74 7592869-10 1995 Our results suggest that FKBP12.6 has both a unique physiological role in excitation-contraction coupling in cardiac muscle and the potential to contribute to the immunosuppressive and toxic effects of FK506 and rapamycin. Tacrolimus 202-207 FKBP prolyl isomerase 1B Homo sapiens 25-33 8521476-6 1995 We now report that calcineurin is physiologically associated with the IP3R-FKBP12 and RyR-FKBP12 receptor complexes and that this interaction can be disrupted by FK506 or rapamycin. Tacrolimus 162-167 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 75-81 8591053-4 1995 The target of the cyclophilin A-cyclosporine A and FKBP12-FK506 complexes is calcineurin, a protein phosphatase required for signaling via the T-cell receptor. Tacrolimus 58-63 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 51-57 8521476-6 1995 We now report that calcineurin is physiologically associated with the IP3R-FKBP12 and RyR-FKBP12 receptor complexes and that this interaction can be disrupted by FK506 or rapamycin. Tacrolimus 162-167 ryanodine receptor 2 Homo sapiens 86-89 8521476-6 1995 We now report that calcineurin is physiologically associated with the IP3R-FKBP12 and RyR-FKBP12 receptor complexes and that this interaction can be disrupted by FK506 or rapamycin. Tacrolimus 162-167 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 90-96 8750397-3 1995 Cyclosporine and tacrolimus are metabolized by the cytochrome P-450 enzyme system. Tacrolimus 17-27 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 51-67 8576317-0 1995 Inhibitory effect of the immunosuppressant FK506 on apoptotic cell death induced by HIV-1 gp120. Tacrolimus 43-48 Envelope surface glycoprotein gp160, precursor Human immunodeficiency virus 1 90-95 8582630-2 1995 A single nuclear mutation, designated cev1 for calcineurin essential for viability, is responsible for the CsA-FK506-sensitive phenotype. Tacrolimus 111-116 Vma22p Saccharomyces cerevisiae S288C 38-42 8582630-3 1995 The peptidyl-prolyl cis-trans isomerases cyclophilin A and FKBP12, respectively, mediate CsA and FK506 toxicity in the cev1 mutant strain. Tacrolimus 97-102 Vma22p Saccharomyces cerevisiae S288C 119-123 8576317-4 1995 Treatment of gp120-primed cells with an immunosuppressant (FK506) before TCR signaling inhibited apoptotic cell death, and this blocking effect of FK506 was concentration dependent. Tacrolimus 59-64 inter-alpha-trypsin inhibitor heavy chain 4 Homo sapiens 13-18 8576317-4 1995 Treatment of gp120-primed cells with an immunosuppressant (FK506) before TCR signaling inhibited apoptotic cell death, and this blocking effect of FK506 was concentration dependent. Tacrolimus 147-152 inter-alpha-trypsin inhibitor heavy chain 4 Homo sapiens 13-18 8584032-0 1995 Evidence that the FK506-binding immunophilin heat shock protein 56 is required for trafficking of the glucocorticoid receptor from the cytoplasm to the nucleus. Tacrolimus 18-23 FKBP prolyl isomerase 4 Homo sapiens 45-66 8584032-0 1995 Evidence that the FK506-binding immunophilin heat shock protein 56 is required for trafficking of the glucocorticoid receptor from the cytoplasm to the nucleus. Tacrolimus 18-23 nuclear receptor subfamily 3 group C member 1 Homo sapiens 102-125 8584032-1 1995 The FK506-binding immunophilin hsp56 (FKBP52) is one of several chaperone proteins associated with untrasformed steroid receptors in a multiprotein heterocomplex. Tacrolimus 4-9 FKBP prolyl isomerase 4 Homo sapiens 31-36 8584032-1 1995 The FK506-binding immunophilin hsp56 (FKBP52) is one of several chaperone proteins associated with untrasformed steroid receptors in a multiprotein heterocomplex. Tacrolimus 4-9 FKBP prolyl isomerase 4 Homo sapiens 38-44 8563622-0 1995 Structure comparison of native and mutant human recombinant FKBP12 complexes with the immunosuppressant drug FK506 (tacrolimus). Tacrolimus 109-114 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 60-66 9346613-5 1995 FK506 (0.5 ng/ mL) reduced both the percentage of interleukin-2 receptor expressing T cells and the cell surface density of this receptor by 7.1% and 8.7% (P < .01), whereas it only reduced the proportion of HLA-DR expressing T cells by 6.8%. Tacrolimus 0-5 interleukin 2 Homo sapiens 50-63 8563622-0 1995 Structure comparison of native and mutant human recombinant FKBP12 complexes with the immunosuppressant drug FK506 (tacrolimus). Tacrolimus 116-126 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 60-66 8563622-2 1995 Here, we examine the effects of "conservative" and "nonconservative" substitutions on the X-ray crystal structures of human recombinant FKBP12 mutants in complex with the immunosuppressant drug FK506 (tacrolimus). Tacrolimus 194-199 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 136-142 8563622-2 1995 Here, we examine the effects of "conservative" and "nonconservative" substitutions on the X-ray crystal structures of human recombinant FKBP12 mutants in complex with the immunosuppressant drug FK506 (tacrolimus). Tacrolimus 201-211 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 136-142 7559604-7 1995 In vitro, both wild-type and CNB1-G2A mutant proteins formed complexes with both cyclophilin A-cyclosporin A (CsA) and FKBP12-FK506 that contained calcineurin A. Interestingly, expression of the nonmyristoylated CNB1-G2A mutant protein rendered yeast cells partially resistant to the immunosuppressant CsA, but not to FK506. Tacrolimus 126-131 calcineurin regulatory subunit B Saccharomyces cerevisiae S288C 29-33 7559604-7 1995 In vitro, both wild-type and CNB1-G2A mutant proteins formed complexes with both cyclophilin A-cyclosporin A (CsA) and FKBP12-FK506 that contained calcineurin A. Interestingly, expression of the nonmyristoylated CNB1-G2A mutant protein rendered yeast cells partially resistant to the immunosuppressant CsA, but not to FK506. Tacrolimus 318-323 calcineurin regulatory subunit B Saccharomyces cerevisiae S288C 29-33 7488022-5 1995 Both CsA and FK506 cause disruption of the CnA1 delta-AID interaction, whereas their presence permits CnA1 delta to bind more strongly to CnB. Tacrolimus 13-18 calcineurin catalytic subunit A Saccharomyces cerevisiae S288C 43-47 7559654-5 1995 p70 was purified to homogeneity; analysis of four tryptic peptides revealed that p70 is identical to the recently described FPR3 gene product, a nucleolarly localized proline rotamase of the FK506- and rapamycin-binding family. Tacrolimus 191-196 peptidylprolyl isomerase FPR3 Saccharomyces cerevisiae S288C 124-128 7565718-9 1995 We have previously shown that growth of fks1 null mutants is highly sensitive to the calcineurin inhibitors FK506 and cyclosporin A. Tacrolimus 108-113 1,3-beta-D-glucan synthase Saccharomyces cerevisiae S288C 40-44 16535142-0 1995 Microbial Demethylation of Immunosuppressant FK-506: Isolation of 31-O-FK-506-Specific Demethylase Showing Cytochrome P-450 Characteristics from Streptomyces rimosus MA187. Tacrolimus 45-51 DF17_RS20860 Streptomyces rimosus 107-123 16535142-2 1995 Treatment of the biotransforming culture with FK-506 increased demethylase activity 2.4-fold and stabilized the cytochrome P-450 protein. Tacrolimus 46-52 DF17_RS20860 Streptomyces rimosus 112-128 16535142-6 1995 The isolated demethylase is therefore a cytochrome P-450 protein that can be used as a catalyst for the synthesis of 31-O-desmethylFK-506, an important immunosuppressant and a known metabolite of FK-506 metabolism by human liver microsomes. Tacrolimus 131-137 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 40-56 7549508-6 1995 Moreover, FK-506, mizoribine and cyclophosphamide clearly inhibited the antigen-induced IL-5 production and cyclosporin A showed the tendency to inhibit IL-5 production. Tacrolimus 10-16 interleukin 5 Mus musculus 88-92 7565718-10 1995 Expression of FKS2 from the heterologous ADH1 promoter results in FK506-resistant growth. Tacrolimus 66-71 1,3-beta-glucan synthase GSC2 Saccharomyces cerevisiae S288C 14-18 7565718-10 1995 Expression of FKS2 from the heterologous ADH1 promoter results in FK506-resistant growth. Tacrolimus 66-71 alcohol dehydrogenase ADH1 Saccharomyces cerevisiae S288C 41-45 7575502-1 1995 The molecular complex formed by the immunosuppressant FK506 and the immunophilin protein FKBP12 potently inhibits the Ca2+/calmodulin-activated protein phosphatase calcineurin. Tacrolimus 54-59 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 89-95 7545671-4 1995 The inhibitory effect of rapamycin on serum-induced p70s6k activation and the phosphorylation of Thr229, Thr389, Ser404, and Ser411 is rescued by FK506, providing further evidence that the inhibitory effect is exerted through a complex of rapamycin-FKBP12. Tacrolimus 146-151 ribosomal protein S6 kinase, polypeptide 1 Mus musculus 52-58 7545680-8 1995 Both of these events were blocked by preincubation of the cells with FK506, a calcineurin inhibitor, consistent with the hypothesis that NFATp is a calcineurin substrate in cells. Tacrolimus 69-74 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 2 Mus musculus 137-142 7545671-4 1995 The inhibitory effect of rapamycin on serum-induced p70s6k activation and the phosphorylation of Thr229, Thr389, Ser404, and Ser411 is rescued by FK506, providing further evidence that the inhibitory effect is exerted through a complex of rapamycin-FKBP12. Tacrolimus 146-151 FK506 binding protein 1a Mus musculus 249-255 8575571-0 1995 FK506 and cyclosporin A inhibit granulocyte/macrophage colony-stimulating factor production by mononuclear cells in asthma. Tacrolimus 0-5 colony stimulating factor 2 Homo sapiens 32-80 8575571-3 1995 To assess this, we compared the inhibitory effects of FK506 and cyclosporin A on production of granulocyte/macrophage colony-stimulating factor and interleukin-5 by interleukin-2- or Dermatophagoides farinae-stimulated mononuclear cells from patients with asthma, and their contribution to proliferation and survival of eosinophils in vitro. Tacrolimus 54-59 colony stimulating factor 2 Homo sapiens 95-143 8575571-3 1995 To assess this, we compared the inhibitory effects of FK506 and cyclosporin A on production of granulocyte/macrophage colony-stimulating factor and interleukin-5 by interleukin-2- or Dermatophagoides farinae-stimulated mononuclear cells from patients with asthma, and their contribution to proliferation and survival of eosinophils in vitro. Tacrolimus 54-59 interleukin 5 Homo sapiens 148-161 8575571-4 1995 FK506 inhibited granulocyte/macrophage colony-stimulating factor production by stimulated mononuclear cells from asthma patients at lower concentrations than cyclosporin A. Tacrolimus 0-5 colony stimulating factor 2 Homo sapiens 16-64 7495746-0 1995 Cross-linking of the TCR-CD3 complex with CD4, CD8 or LFA-1 induces an anti-apoptotic signal in thymocytes: the signal is canceled by FK506. Tacrolimus 134-139 CD4 molecule Homo sapiens 42-45 7495746-0 1995 Cross-linking of the TCR-CD3 complex with CD4, CD8 or LFA-1 induces an anti-apoptotic signal in thymocytes: the signal is canceled by FK506. Tacrolimus 134-139 CD8a molecule Homo sapiens 47-50 7495746-0 1995 Cross-linking of the TCR-CD3 complex with CD4, CD8 or LFA-1 induces an anti-apoptotic signal in thymocytes: the signal is canceled by FK506. Tacrolimus 134-139 integrin subunit alpha L Homo sapiens 54-59 7495746-3 1995 As positive selection depends on the inhibition of thymocyte apoptosis at its DP stage by signaling through the TCR-CD3 complex and some of the accessory molecules, including CD4, CD8 and LFA-1, we studied the possibility that FK506 enhanced apoptosis by itself or canceled the inhibition of apoptosis. Tacrolimus 227-232 CD4 molecule Homo sapiens 175-178 7495746-3 1995 As positive selection depends on the inhibition of thymocyte apoptosis at its DP stage by signaling through the TCR-CD3 complex and some of the accessory molecules, including CD4, CD8 and LFA-1, we studied the possibility that FK506 enhanced apoptosis by itself or canceled the inhibition of apoptosis. Tacrolimus 227-232 integrin subunit alpha L Homo sapiens 188-193 7495746-5 1995 On the other hand, upon cross-linking TCR-CD3 together with CD4, CD8 or LFA-1, FK506 markedly enhanced DNA fragmentation and cytolysis. Tacrolimus 79-84 CD4 molecule Homo sapiens 60-63 7495746-5 1995 On the other hand, upon cross-linking TCR-CD3 together with CD4, CD8 or LFA-1, FK506 markedly enhanced DNA fragmentation and cytolysis. Tacrolimus 79-84 CD8a molecule Homo sapiens 65-68 7495746-5 1995 On the other hand, upon cross-linking TCR-CD3 together with CD4, CD8 or LFA-1, FK506 markedly enhanced DNA fragmentation and cytolysis. Tacrolimus 79-84 integrin subunit alpha L Homo sapiens 72-77 7495746-7 1995 Cross-linking of TCR-CD3 together with CD4, CD8 or LFA-1 markedly inhibited glucocorticoid-induced death and the inhibition was canceled by FK506. Tacrolimus 140-145 CD4 molecule Homo sapiens 39-42 7495746-7 1995 Cross-linking of TCR-CD3 together with CD4, CD8 or LFA-1 markedly inhibited glucocorticoid-induced death and the inhibition was canceled by FK506. Tacrolimus 140-145 CD8a molecule Homo sapiens 44-47 7495746-7 1995 Cross-linking of TCR-CD3 together with CD4, CD8 or LFA-1 markedly inhibited glucocorticoid-induced death and the inhibition was canceled by FK506. Tacrolimus 140-145 integrin subunit alpha L Homo sapiens 51-56 7495746-8 1995 Furthermore, cross-linking of TCR-CD3 together with LFA-1 potentially induces both an apoptosis-inducing signal and an FK506-sensitive anti-apoptotic signal, and that the latter signal may be related to an essential signal for positive selection. Tacrolimus 119-124 integrin subunit alpha L Homo sapiens 52-57 8557519-1 1995 We investigated the transcription and expression of the interleukin-2 receptor (IL-2R, CD25) in human T-lymphocytes after different modes of T-lymphocyte stimulation in the presence of the immunosuppressants cyclosporin (CsA) and tacrolimus (FK506) as well as the structurally related macrolide rapamycin. Tacrolimus 230-240 interleukin 2 receptor subunit alpha Homo sapiens 56-78 8557519-1 1995 We investigated the transcription and expression of the interleukin-2 receptor (IL-2R, CD25) in human T-lymphocytes after different modes of T-lymphocyte stimulation in the presence of the immunosuppressants cyclosporin (CsA) and tacrolimus (FK506) as well as the structurally related macrolide rapamycin. Tacrolimus 242-247 interleukin 2 receptor subunit alpha Homo sapiens 56-78 8557519-2 1995 We demonstrate that CsA and FK506 inhibited IL-2R (CD25) gene transcription and protein expression after stimulation by anti-CD3 or ionomycin, but not by phorbol ester or IL-2. Tacrolimus 28-33 interleukin 2 receptor subunit alpha Homo sapiens 44-49 8557519-2 1995 We demonstrate that CsA and FK506 inhibited IL-2R (CD25) gene transcription and protein expression after stimulation by anti-CD3 or ionomycin, but not by phorbol ester or IL-2. Tacrolimus 28-33 interleukin 2 receptor subunit alpha Homo sapiens 51-55 8557519-2 1995 We demonstrate that CsA and FK506 inhibited IL-2R (CD25) gene transcription and protein expression after stimulation by anti-CD3 or ionomycin, but not by phorbol ester or IL-2. Tacrolimus 28-33 interleukin 2 Homo sapiens 44-48 8846199-6 1995 FK506 strongly suppressed the production of IL-2 (IC50 = 0.01 microM) and GM-CSF (IC50 = 0.03 microM), but was inactive (< 30% inhibition at 1 microM) against IL-5 and IFN-gamma. Tacrolimus 0-5 interleukin 2 Homo sapiens 44-48 8846199-6 1995 FK506 strongly suppressed the production of IL-2 (IC50 = 0.01 microM) and GM-CSF (IC50 = 0.03 microM), but was inactive (< 30% inhibition at 1 microM) against IL-5 and IFN-gamma. Tacrolimus 0-5 colony stimulating factor 2 Homo sapiens 74-80 8846199-6 1995 FK506 strongly suppressed the production of IL-2 (IC50 = 0.01 microM) and GM-CSF (IC50 = 0.03 microM), but was inactive (< 30% inhibition at 1 microM) against IL-5 and IFN-gamma. Tacrolimus 0-5 interferon gamma Homo sapiens 171-180 7657624-0 1995 The cyclosporin A-binding immunophilin CyP-40 and the FK506-binding immunophilin hsp56 bind to a common site on hsp90 and exist in independent cytosolic heterocomplexes with the untransformed glucocorticoid receptor. Tacrolimus 54-59 glucocorticoid receptor Oryctolagus cuniculus 192-215 8748119-6 1995 Despite the fact these drugs did not modulate the actions of glucocorticoids on corticotrope cells, both FK506 and CsA were potent stimulators of basal beta-endorphin secretion (4-6 fold) from rat anterior pituitary cultures and AtT20 cells. Tacrolimus 105-110 pro-opiomelanocortin-alpha Mus musculus 152-166 8748119-7 1995 In addition, FK506 and CsA potentiated beta-endorphin secretion induced by corticotropin releasing factor (CRF) and phorbol ester, but had no apparent acute (60 min) effect on POMC hnRNA levels. Tacrolimus 13-18 pro-opiomelanocortin-alpha Mus musculus 39-53 8748119-7 1995 In addition, FK506 and CsA potentiated beta-endorphin secretion induced by corticotropin releasing factor (CRF) and phorbol ester, but had no apparent acute (60 min) effect on POMC hnRNA levels. Tacrolimus 13-18 corticotropin releasing hormone Mus musculus 75-105 8748119-9 1995 Taken together these data suggest that FK506 and CsA do not alter GR activation or function in corticotrope cells, however, they are potent but short lived stimulators of POMC-derived peptide secretion. Tacrolimus 39-44 pro-opiomelanocortin-alpha Mus musculus 171-175 8748119-10 1995 The observation that CsA and FK506 stimulate POMC-derived peptide secretion, and potentiate both phorbol ester and CRF induced secretion, suggests that these immunosuppressant drugs are acting upon a common point within these intracellular pathways. Tacrolimus 29-34 pro-opiomelanocortin-alpha Mus musculus 45-49 7583777-1 1995 The effects of cyclosporin A (CsA), FK506 and rapamycin (Rapa) on the intracellular localization of a mutated rabbit progesterone receptor (PR) which lacks the main constitutive nuclear localization signal (NLS) (delta 638-642) and is cytoplasmic in the absence of progesterone (Prog), were assayed by indirect immunofluorescence in Lcl3 cells, a mouse L-cell line stably expressing this mutant. Tacrolimus 36-41 progesterone receptor Oryctolagus cuniculus 117-138 7643878-7 1995 When such transplantations were done in mice immunosuppressed with cyclosporine or FK-506, normal dystrophin mRNA accounted for 31% and 36% of the total dystrophin mRNA, respectively. Tacrolimus 83-89 dystrophin, muscular dystrophy Mus musculus 98-108 7643878-8 1995 In fact, one animal immunosuppressed with FK-506 expressed as much as 57% of normal dystrophin mRNA. Tacrolimus 42-48 dystrophin, muscular dystrophy Mus musculus 84-94 7643878-9 1995 These results thus show that FK-506 makes it possible to restore dystrophin expression to a level comparable to that observed in DMD carriers that are usually asymptomatic. Tacrolimus 29-35 dystrophin, muscular dystrophy Mus musculus 65-75 7650004-7 1995 Additionally, thymic NFATc3 undergoes modifications in response to agents that mimic T cell receptor signaling, including a decrease in apparent molecular mass upon elevation of intracellular calcium that is inhibited by the immunosuppressant FK506. Tacrolimus 243-248 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 3 Mus musculus 21-27 7543369-0 1995 X-ray structure of calcineurin inhibited by the immunophilin-immunosuppressant FKBP12-FK506 complex. Tacrolimus 86-91 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 79-85 7543369-1 1995 The X-ray structure of the ternary complex of a calcineurin A fragment, calcineurin B, FKBP12, and the immunosuppressant drug FK506 (also known as tacrolimus) has been determined at 2.5 A resolution, providing a description of how FK506 functions at the atomic level. Tacrolimus 126-131 protein phosphatase 3 regulatory subunit B, alpha Homo sapiens 72-85 7543369-1 1995 The X-ray structure of the ternary complex of a calcineurin A fragment, calcineurin B, FKBP12, and the immunosuppressant drug FK506 (also known as tacrolimus) has been determined at 2.5 A resolution, providing a description of how FK506 functions at the atomic level. Tacrolimus 126-131 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 87-93 7543369-1 1995 The X-ray structure of the ternary complex of a calcineurin A fragment, calcineurin B, FKBP12, and the immunosuppressant drug FK506 (also known as tacrolimus) has been determined at 2.5 A resolution, providing a description of how FK506 functions at the atomic level. Tacrolimus 147-157 protein phosphatase 3 regulatory subunit B, alpha Homo sapiens 72-85 7543369-1 1995 The X-ray structure of the ternary complex of a calcineurin A fragment, calcineurin B, FKBP12, and the immunosuppressant drug FK506 (also known as tacrolimus) has been determined at 2.5 A resolution, providing a description of how FK506 functions at the atomic level. Tacrolimus 147-157 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 87-93 7543369-1 1995 The X-ray structure of the ternary complex of a calcineurin A fragment, calcineurin B, FKBP12, and the immunosuppressant drug FK506 (also known as tacrolimus) has been determined at 2.5 A resolution, providing a description of how FK506 functions at the atomic level. Tacrolimus 231-236 protein phosphatase 3 regulatory subunit B, alpha Homo sapiens 72-85 7543369-2 1995 In the structure, the FKBP12-FK506 binary complex does not contact the phosphatase active site on calcineurin A that is more than 10 A removed. Tacrolimus 29-34 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 22-28 7543369-3 1995 Instead, FKBP12-FK506 is so positioned that it can inhibit the dephosphorylation of its macromolecular substrates by physically hindering their approach to the active site. Tacrolimus 16-21 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 9-15 7543369-4 1995 The ternary complex described here represents the three-dimensional structure of a Ser/Thr protein phosphatase and provides a structural basis for understanding calcineurin inhibition by FKBP12-FK506. Tacrolimus 194-199 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 187-193 7642551-2 1995 The 12- and 13-kDa FK506 binding proteins (FKBP12 and FKBP13) are cis-trans peptidyl-prolyl isomerases that bind the macrolides FK506 (Tacrolimus) and rapamycin (Sirolimus). Tacrolimus 19-24 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 43-49 7642551-2 1995 The 12- and 13-kDa FK506 binding proteins (FKBP12 and FKBP13) are cis-trans peptidyl-prolyl isomerases that bind the macrolides FK506 (Tacrolimus) and rapamycin (Sirolimus). Tacrolimus 19-24 FKBP prolyl isomerase 2 Homo sapiens 54-60 7642551-2 1995 The 12- and 13-kDa FK506 binding proteins (FKBP12 and FKBP13) are cis-trans peptidyl-prolyl isomerases that bind the macrolides FK506 (Tacrolimus) and rapamycin (Sirolimus). Tacrolimus 128-133 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 43-49 7642551-2 1995 The 12- and 13-kDa FK506 binding proteins (FKBP12 and FKBP13) are cis-trans peptidyl-prolyl isomerases that bind the macrolides FK506 (Tacrolimus) and rapamycin (Sirolimus). Tacrolimus 128-133 FKBP prolyl isomerase 2 Homo sapiens 54-60 7642551-2 1995 The 12- and 13-kDa FK506 binding proteins (FKBP12 and FKBP13) are cis-trans peptidyl-prolyl isomerases that bind the macrolides FK506 (Tacrolimus) and rapamycin (Sirolimus). Tacrolimus 135-145 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 43-49 7642551-2 1995 The 12- and 13-kDa FK506 binding proteins (FKBP12 and FKBP13) are cis-trans peptidyl-prolyl isomerases that bind the macrolides FK506 (Tacrolimus) and rapamycin (Sirolimus). Tacrolimus 135-145 FKBP prolyl isomerase 2 Homo sapiens 54-60 7642551-3 1995 The FKBP12.FK506 complex is immunosuppressive, acting as an inhibitor of the protein phosphatase calcineurin. Tacrolimus 11-16 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 4-10 7642551-6 1995 Mutations at FKBP12 residues Asp-37, Arg-42, His-87, and Ile-90 decrease calcineurin affinity of the mutant FKBP12.FK506 complex by as much as 2600-fold in the case of I90K. Tacrolimus 115-120 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 13-19 7642551-6 1995 Mutations at FKBP12 residues Asp-37, Arg-42, His-87, and Ile-90 decrease calcineurin affinity of the mutant FKBP12.FK506 complex by as much as 2600-fold in the case of I90K. Tacrolimus 115-120 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 108-114 7642551-7 1995 Replacement of three FKBP13 surface residues (Gln-50, Ala-95, and Lys-98) with the corresponding homologous FKBP12 residues (Arg-42, His-87, and Ile-90) generates an FKBP13 variant that is equivalent to FKBP12 in its affinity for FK506, rapamycin, and calcineurin. Tacrolimus 230-235 FKBP prolyl isomerase 2 Homo sapiens 21-27 7642551-7 1995 Replacement of three FKBP13 surface residues (Gln-50, Ala-95, and Lys-98) with the corresponding homologous FKBP12 residues (Arg-42, His-87, and Ile-90) generates an FKBP13 variant that is equivalent to FKBP12 in its affinity for FK506, rapamycin, and calcineurin. Tacrolimus 230-235 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 108-114 7642551-7 1995 Replacement of three FKBP13 surface residues (Gln-50, Ala-95, and Lys-98) with the corresponding homologous FKBP12 residues (Arg-42, His-87, and Ile-90) generates an FKBP13 variant that is equivalent to FKBP12 in its affinity for FK506, rapamycin, and calcineurin. Tacrolimus 230-235 FKBP prolyl isomerase 2 Homo sapiens 166-172 7476967-0 1995 Interaction of the progesterone receptor with binding proteins for FK506 and cyclosporin A. Tacrolimus 67-72 progesterone receptor Homo sapiens 19-40 7639278-1 1995 P-glycoprotein 170 (P-gp), the multidrug transport pump, excludes drugs from the interior of cells and is inhibited by agents such as cyclosporin A (CsA), verapamil, and FK-506, which are also substrates for the P-gp pump. Tacrolimus 170-176 phosphoglycolate phosphatase Homo sapiens 0-18 7639278-1 1995 P-glycoprotein 170 (P-gp), the multidrug transport pump, excludes drugs from the interior of cells and is inhibited by agents such as cyclosporin A (CsA), verapamil, and FK-506, which are also substrates for the P-gp pump. Tacrolimus 170-176 phosphoglycolate phosphatase Homo sapiens 20-24 7639278-1 1995 P-glycoprotein 170 (P-gp), the multidrug transport pump, excludes drugs from the interior of cells and is inhibited by agents such as cyclosporin A (CsA), verapamil, and FK-506, which are also substrates for the P-gp pump. Tacrolimus 170-176 phosphoglycolate phosphatase Homo sapiens 212-216 7544285-3 1995 FKBP59 binds immunosuppressant FK506 and has peptidylprolyl cis-trans-isomerase activity, both properties being localized in the N-terminal domain (FKBP59-I). Tacrolimus 31-36 FKBP prolyl isomerase 4 Homo sapiens 0-6 7543492-5 1995 FK506 treatment significantly augmented thymic apoptosis induced by in vivo anti-CD3 Ab administration. Tacrolimus 0-5 CD3 antigen, epsilon polypeptide Mus musculus 81-84 7543492-6 1995 Increased thymic apoptosis resulted in the disappearance of CD4+ CD8+ thymocytes after anti-CD3 Ab/FK506 treatment. Tacrolimus 99-104 CD4 antigen Mus musculus 60-63 7543492-6 1995 Increased thymic apoptosis resulted in the disappearance of CD4+ CD8+ thymocytes after anti-CD3 Ab/FK506 treatment. Tacrolimus 99-104 CD3 antigen, epsilon polypeptide Mus musculus 92-95 7542741-6 1995 CND1 is identical to the gene identified previously as FKS1, ETG1, and CWH53, cnd1 mutants are sensitive to FK506 and cyclosporin A and exhibit slow growth that is improved by the addition of osmotic stabilizing agents. Tacrolimus 108-113 1,3-beta-D-glucan synthase Saccharomyces cerevisiae S288C 0-4 7542741-6 1995 CND1 is identical to the gene identified previously as FKS1, ETG1, and CWH53, cnd1 mutants are sensitive to FK506 and cyclosporin A and exhibit slow growth that is improved by the addition of osmotic stabilizing agents. Tacrolimus 108-113 1,3-beta-D-glucan synthase Saccharomyces cerevisiae S288C 55-59 7542741-6 1995 CND1 is identical to the gene identified previously as FKS1, ETG1, and CWH53, cnd1 mutants are sensitive to FK506 and cyclosporin A and exhibit slow growth that is improved by the addition of osmotic stabilizing agents. Tacrolimus 108-113 1,3-beta-D-glucan synthase Saccharomyces cerevisiae S288C 61-65 7542741-6 1995 CND1 is identical to the gene identified previously as FKS1, ETG1, and CWH53, cnd1 mutants are sensitive to FK506 and cyclosporin A and exhibit slow growth that is improved by the addition of osmotic stabilizing agents. Tacrolimus 108-113 1,3-beta-D-glucan synthase Saccharomyces cerevisiae S288C 71-76 7542741-6 1995 CND1 is identical to the gene identified previously as FKS1, ETG1, and CWH53, cnd1 mutants are sensitive to FK506 and cyclosporin A and exhibit slow growth that is improved by the addition of osmotic stabilizing agents. Tacrolimus 108-113 1,3-beta-D-glucan synthase Saccharomyces cerevisiae S288C 78-82 7542743-7 1995 As judged from peptidyl prolyl isomerase activity, FKBP51 had a slightly higher affinity for rapamycin than for FK520, an FK506 analog. Tacrolimus 122-127 FK506 binding protein 5 Mus musculus 51-57 7623828-10 1995 Furthermore, the activating function of p95vav is blocked by FK506, suggesting that its activity also depends on calcineurin. Tacrolimus 61-66 vav 1 oncogene Mus musculus 40-46 8575571-6 1995 Interleukin-5 production by stimulated mononuclear cells was also inhibited both by FK506 and cyclosporin A. Tacrolimus 84-89 interleukin 5 Homo sapiens 0-13 7542815-11 1995 FK506 decreased steady-state insulin secretion during the last 60 min of the clamp, regardless of initial glucose tolerance. Tacrolimus 0-5 insulin Homo sapiens 29-36 15299838-2 1995 FK506, in complex with its 12 kDa cytosolic receptor (FKBP12), is a potent agonist of immunosuppression through the inhibition of the phosphatase activity of calcineurin. Tacrolimus 0-5 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 54-60 15299838-3 1995 Rapamycin (sirolimus), which is itself an immunosuppressant by a different mechanism, completes with FK506 for binding to FKBP12 and thereby acts as an antagonist of calcineurin inhibition. Tacrolimus 101-106 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 122-128 15299838-4 1995 We have solved the X-ray structure of unliganded FKBP12 and of FKBP12 in complex with FK506 and with rapamycin; these structures show localized differences in conformation and mobility in those regions of the protein that are known, by site-directed mutagenesis, to be involved in calcineurin inhibition. Tacrolimus 86-91 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 49-55 15299838-4 1995 We have solved the X-ray structure of unliganded FKBP12 and of FKBP12 in complex with FK506 and with rapamycin; these structures show localized differences in conformation and mobility in those regions of the protein that are known, by site-directed mutagenesis, to be involved in calcineurin inhibition. Tacrolimus 86-91 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 63-69 15299839-0 1995 Design, synthesis and structure of non-macrocyclic inhibitors of FKBP12, the major binding protein for the immunosuppressant FK506. Tacrolimus 125-130 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 65-71 15299839-1 1995 We have synthesized a series of non-macrocyclic ligands to FKBP12 that are comparable in binding potency and peptidyl prolyl isomerase (PPIase) inhibition to FK506 itself. Tacrolimus 158-163 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 59-65 15299839-5 1995 In the FKBP12-FK506 complex, a significant portion of the FK506 ligand, its "effector domain", projects beyond the envelope of the binding protein in a manner that is suggestive of a potential interaction with a second protein, the calcium-dependent phosphatase, calcineurin, whose inhibition by the FKBP 12-FK506 complex interrupts the T-cell activation events leading to immunosuppression. Tacrolimus 14-19 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 7-13 15299839-5 1995 In the FKBP12-FK506 complex, a significant portion of the FK506 ligand, its "effector domain", projects beyond the envelope of the binding protein in a manner that is suggestive of a potential interaction with a second protein, the calcium-dependent phosphatase, calcineurin, whose inhibition by the FKBP 12-FK506 complex interrupts the T-cell activation events leading to immunosuppression. Tacrolimus 14-19 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 300-307 15299839-5 1995 In the FKBP12-FK506 complex, a significant portion of the FK506 ligand, its "effector domain", projects beyond the envelope of the binding protein in a manner that is suggestive of a potential interaction with a second protein, the calcium-dependent phosphatase, calcineurin, whose inhibition by the FKBP 12-FK506 complex interrupts the T-cell activation events leading to immunosuppression. Tacrolimus 58-63 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 7-13 15299839-5 1995 In the FKBP12-FK506 complex, a significant portion of the FK506 ligand, its "effector domain", projects beyond the envelope of the binding protein in a manner that is suggestive of a potential interaction with a second protein, the calcium-dependent phosphatase, calcineurin, whose inhibition by the FKBP 12-FK506 complex interrupts the T-cell activation events leading to immunosuppression. Tacrolimus 58-63 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 300-307 15299839-5 1995 In the FKBP12-FK506 complex, a significant portion of the FK506 ligand, its "effector domain", projects beyond the envelope of the binding protein in a manner that is suggestive of a potential interaction with a second protein, the calcium-dependent phosphatase, calcineurin, whose inhibition by the FKBP 12-FK506 complex interrupts the T-cell activation events leading to immunosuppression. Tacrolimus 58-63 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 7-13 15299839-5 1995 In the FKBP12-FK506 complex, a significant portion of the FK506 ligand, its "effector domain", projects beyond the envelope of the binding protein in a manner that is suggestive of a potential interaction with a second protein, the calcium-dependent phosphatase, calcineurin, whose inhibition by the FKBP 12-FK506 complex interrupts the T-cell activation events leading to immunosuppression. Tacrolimus 58-63 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 300-307 7476967-5 1995 A third 59-kilodalton (kDa) protein observed previously was confirmed to be p59 (also called hsp56 or FKBP52), which has been shown to bind the immunosuppressant drug FK506. Tacrolimus 167-172 HLA complex P5B Homo sapiens 76-79 7476967-5 1995 A third 59-kilodalton (kDa) protein observed previously was confirmed to be p59 (also called hsp56 or FKBP52), which has been shown to bind the immunosuppressant drug FK506. Tacrolimus 167-172 FKBP prolyl isomerase 4 Homo sapiens 93-98 7476967-5 1995 A third 59-kilodalton (kDa) protein observed previously was confirmed to be p59 (also called hsp56 or FKBP52), which has been shown to bind the immunosuppressant drug FK506. Tacrolimus 167-172 FKBP prolyl isomerase 4 Homo sapiens 102-108 7541044-0 1995 Interaction of FKBP12-FK506 with calcineurin A at the B subunit-binding domain. Tacrolimus 22-27 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 15-21 7541044-6 1995 Furthermore, calcineurin A subunit mutants of residues Thr351, Leu354, and Lys360 showed NF kappa B transactivation activity and phosphatase activity with increased resistance to FKBP12-FK506 but displayed no or minimal increase in resistance for cyclosporin A inhibition. Tacrolimus 186-191 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 179-185 7541044-7 1995 Together, these results strongly suggest that the B subunit-binding domain is required for calcineurin activity intracellulary and interacts with the FKBP12-FK506 complex. Tacrolimus 157-162 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 150-156 7539960-10 1995 Thus, as in the case with NF-AT in T cells, these findings point to the reduction of unidentified nuclear factors for insulin mRNA transcription caused by the binding of FK506 to FKBP-12 and a subsequent inhibition of calcineurin in the beta-cells. Tacrolimus 170-175 FKBP prolyl isomerase 1A Rattus norvegicus 179-186 7541038-4 1995 Cyclosporin A and FK506 efficiently disrupt the YY1-CyPA and YY1-FKBP12 interactions. Tacrolimus 18-23 YY1 transcription factor Homo sapiens 48-51 7541038-4 1995 Cyclosporin A and FK506 efficiently disrupt the YY1-CyPA and YY1-FKBP12 interactions. Tacrolimus 18-23 peptidylprolyl isomerase A Homo sapiens 52-56 7541038-4 1995 Cyclosporin A and FK506 efficiently disrupt the YY1-CyPA and YY1-FKBP12 interactions. Tacrolimus 18-23 YY1 transcription factor Homo sapiens 61-64 7541038-4 1995 Cyclosporin A and FK506 efficiently disrupt the YY1-CyPA and YY1-FKBP12 interactions. Tacrolimus 18-23 FKBP prolyl isomerase 1A Homo sapiens 65-71 7540976-4 1995 One mutation that confers dominant FK506 resistance alters a single residue (W430C) in the calcineurin A catalytic subunit CMP2. Tacrolimus 35-40 calcineurin catalytic subunit A Saccharomyces cerevisiae S288C 123-127 7759865-7 1995 p40cdk6 also increased in amount in cells activated in the presence of cyclosporin A or FK506, drugs that inhibit production of IL-2 and cell proliferation, suggesting that initial induction occurred independently of IL-2-mediated cell cycle progression. Tacrolimus 88-93 interleukin 2 Homo sapiens 128-132 7759865-7 1995 p40cdk6 also increased in amount in cells activated in the presence of cyclosporin A or FK506, drugs that inhibit production of IL-2 and cell proliferation, suggesting that initial induction occurred independently of IL-2-mediated cell cycle progression. Tacrolimus 88-93 interleukin 2 Homo sapiens 217-221 7544633-8 1995 Activities of myeloperoxidase and concentrations of 6-keto-prostaglandin F1 alpha (6-keto-PGF1 alpha), PGF2 alpha and PGE2 in colonic tissue increased significantly following induction of experimental colitis, however, FK506 did not affect these changes. Tacrolimus 219-224 myeloperoxidase Rattus norvegicus 14-29 7552894-2 1995 Tacrolimus prevents rejection of the transplanted organ by inhibiting the expression of interleukin-2 in T cells and inhibiting T-cell growth and proliferation. Tacrolimus 0-10 interleukin 2 Homo sapiens 88-101 7552894-4 1995 Tacrolimus is extensively metabolized by cytochrome P-450 3A4 isoenzyme, resulting in several known drug interactions. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 41-61 7540976-6 1995 When introduced into the CMP1 subunit, the FK506 resistance mutation (W388C) blocks binding by FKBP12-FK506, but not by cyclophilin A-CsA. Tacrolimus 43-48 calcineurin catalytic subunit A Saccharomyces cerevisiae S288C 25-29 7540976-6 1995 When introduced into the CMP1 subunit, the FK506 resistance mutation (W388C) blocks binding by FKBP12-FK506, but not by cyclophilin A-CsA. Tacrolimus 102-107 calcineurin catalytic subunit A Saccharomyces cerevisiae S288C 25-29 7540976-8 1995 Double mutant calcineurin A subunits (Y377F, W388C CMP1 and Y419F, W430C CMP2) confer resistance to CsA, to FK506 and to CsA plus FK506. Tacrolimus 108-113 calcineurin catalytic subunit A Saccharomyces cerevisiae S288C 73-77 7540976-8 1995 Double mutant calcineurin A subunits (Y377F, W388C CMP1 and Y419F, W430C CMP2) confer resistance to CsA, to FK506 and to CsA plus FK506. Tacrolimus 130-135 calcineurin catalytic subunit A Saccharomyces cerevisiae S288C 73-77 7538911-5 1995 These mutants were still fully sensitive to FK-506, an immunosuppressant structurally related to RAP whose mode of action also involves an interaction with FKBPs. Tacrolimus 44-50 regulatory associated protein of MTOR, complex 1 Mus musculus 97-100 7577807-0 1995 Suppression of adult T cell leukemia-derived factor/human thioredoxin induction by FK506 and cyclosporin A: a new mechanism of immune modulation via redox control. Tacrolimus 83-88 thioredoxin Homo sapiens 58-69 7544064-7 1995 With decrease in the dose of FK506, the TL was normalized, and the dose of IS could be decreased. Tacrolimus 29-34 insulin Homo sapiens 75-77 7544064-8 1995 FK506 has been reported to inhibit IS secretion. Tacrolimus 0-5 insulin Homo sapiens 35-37 7577807-9 1995 These results suggest that ADF/TRX produced and released from PBMC may be a crucial event in lymphocyte activation, and that FK506 and CsA may exert the immune suppression partly through inhibiting the induction of the endogenous reducing factor ADF/TRX. Tacrolimus 125-130 thioredoxin Homo sapiens 246-249 7577807-4 1995 ADF/TRX induction in PBMC by PHA, Con A or OKT3 mAb was almost completely suppressed by FK506. Tacrolimus 88-93 thioredoxin Homo sapiens 0-3 7577807-9 1995 These results suggest that ADF/TRX produced and released from PBMC may be a crucial event in lymphocyte activation, and that FK506 and CsA may exert the immune suppression partly through inhibiting the induction of the endogenous reducing factor ADF/TRX. Tacrolimus 125-130 thioredoxin Homo sapiens 250-253 7577807-4 1995 ADF/TRX induction in PBMC by PHA, Con A or OKT3 mAb was almost completely suppressed by FK506. Tacrolimus 88-93 thioredoxin Homo sapiens 4-7 7577807-8 1995 Furthermore, when recombinant ADF (rADF) was added to a culture of PBMC 1 h before the addition of PHA and FK506, the action of FK506 was partially reversed as determined by [3H]thymidine incorporation and viable cell counts. Tacrolimus 107-112 thioredoxin Homo sapiens 30-33 7577807-8 1995 Furthermore, when recombinant ADF (rADF) was added to a culture of PBMC 1 h before the addition of PHA and FK506, the action of FK506 was partially reversed as determined by [3H]thymidine incorporation and viable cell counts. Tacrolimus 128-133 thioredoxin Homo sapiens 30-33 7538541-13 1995 Finally, immunosuppressant cyclosporin A (100 nM) and FK-506 (10 nM) significantly inhibited mast cell adhesion to both fibronectin and laminin (p < 0.05). Tacrolimus 54-60 fibronectin 1 Homo sapiens 120-131 7545487-2 1995 FK506 which has a similar immunosuppressive mechanism to that of CsA also showed the same inhibitory effects except for decreased IL-5 and IL-6 mRNA expression. Tacrolimus 0-5 interleukin 5 Homo sapiens 130-134 7539555-9 1995 Cellular expression of IL-1 alpha, IL-2, IL-6, gamma-INF, FGF, and TGF-beta mRNA was suppressed with FK506 to below isograft levels, and clinical rejection was not observed with the doses, routes, and schedules used. Tacrolimus 101-106 interleukin 1 alpha Rattus norvegicus 23-33 7539555-9 1995 Cellular expression of IL-1 alpha, IL-2, IL-6, gamma-INF, FGF, and TGF-beta mRNA was suppressed with FK506 to below isograft levels, and clinical rejection was not observed with the doses, routes, and schedules used. Tacrolimus 101-106 interleukin 2 Rattus norvegicus 35-39 7539555-9 1995 Cellular expression of IL-1 alpha, IL-2, IL-6, gamma-INF, FGF, and TGF-beta mRNA was suppressed with FK506 to below isograft levels, and clinical rejection was not observed with the doses, routes, and schedules used. Tacrolimus 101-106 interleukin 6 Rattus norvegicus 41-45 7539555-9 1995 Cellular expression of IL-1 alpha, IL-2, IL-6, gamma-INF, FGF, and TGF-beta mRNA was suppressed with FK506 to below isograft levels, and clinical rejection was not observed with the doses, routes, and schedules used. Tacrolimus 101-106 transforming growth factor, beta 1 Rattus norvegicus 67-75 7538591-0 1995 Determination of the differential effects of hydrogen bonding and water release on the binding of FK506 to native and Tyr82-->Phe82 FKBP-12 proteins using free energy simulations. Tacrolimus 98-103 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 135-142 7538591-1 1995 We use the thermodynamic integration technique to calculate the free energy associated with the Tyr82-->Phe82 mutation (Y82F) in the protein FKBP-12, both free and bound to known inhibitor FK506 (tacrolimis). Tacrolimus 192-197 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 144-151 7545487-2 1995 FK506 which has a similar immunosuppressive mechanism to that of CsA also showed the same inhibitory effects except for decreased IL-5 and IL-6 mRNA expression. Tacrolimus 0-5 interleukin 6 Homo sapiens 139-143 7545487-3 1995 In contrast, both CsA and FK506 enhanced transforming growth factor beta (TGF beta) and IL-1 beta mRNA expression. Tacrolimus 26-31 transforming growth factor beta 1 Homo sapiens 41-72 7537219-5 1995 The amino acids in human FKBP12 which are proposed to be important for FK506 interaction are conserved in the schistosome protein. Tacrolimus 71-76 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 25-31 7613145-3 1995 The immunosuppressive agents CsA and FK506 enhanced the release of leukotriene B4 (LTB4) from human neutrophil granulocytes dependent on the priming with G-CSF and IL-3. Tacrolimus 37-42 colony stimulating factor 3 Homo sapiens 154-159 7613145-3 1995 The immunosuppressive agents CsA and FK506 enhanced the release of leukotriene B4 (LTB4) from human neutrophil granulocytes dependent on the priming with G-CSF and IL-3. Tacrolimus 37-42 interleukin 3 Homo sapiens 164-168 7613145-4 1995 IL-3-primed neutrophils released up to threefold higher amounts of LTB4 after subsequent stimulation with FK506 and fMLP. Tacrolimus 106-111 interleukin 3 Homo sapiens 0-4 7542077-6 1995 FK506 suppressed IL-5 production and gene expression in vitro in a dose-dependent manner. Tacrolimus 0-5 interleukin 5 Homo sapiens 17-21 7543725-8 1995 CsA- and FK506-treated rats, but not those treated with rapamycin, demonstrated high turnover osteoporosis with raised serum 1,25(OH)2D (p < 0.05) and elevated serum osteocalcin (p < 0.05). Tacrolimus 9-14 bone gamma-carboxyglutamate protein Rattus norvegicus 169-180 7545487-3 1995 In contrast, both CsA and FK506 enhanced transforming growth factor beta (TGF beta) and IL-1 beta mRNA expression. Tacrolimus 26-31 transforming growth factor beta 1 Homo sapiens 74-82 7545487-3 1995 In contrast, both CsA and FK506 enhanced transforming growth factor beta (TGF beta) and IL-1 beta mRNA expression. Tacrolimus 26-31 interleukin 1 beta Homo sapiens 88-97 7538962-0 1995 FKBP39, a Drosophila member of a family of proteins that bind the immunosuppressive drug FK506. Tacrolimus 89-94 FK506-binding protein 39kD Drosophila melanogaster 0-6 7709436-4 1995 Cox"s proportional hazards univariate and multivariate analyses showed that significant first-episode risk factors were: CMV seropositive donors for negative recipients (relative risk [RR], 3.86; P = 0.02), the average daily plasma trough level of tacrolimus (RR, 2.15; P = 0.04), and total amount of steroid boluses (RR, 2.90; P = 0.02). Tacrolimus 248-258 cytochrome c oxidase subunit 8A Homo sapiens 0-3 7536932-7 1995 Neutrophil activation by mast cell-derived FKBP12 is prevented by complexing FKBP12 with FK506 or rapamycin. Tacrolimus 89-94 FKBP prolyl isomerase 1A Homo sapiens 43-49 7537264-2 1995 We report here that the immunosuppressants FK506 and cyclosporin A cause general growth inhibition of the vma3 mutant. Tacrolimus 43-48 H(+)-transporting V0 sector ATPase subunit c Saccharomyces cerevisiae S288C 106-110 7537264-5 1995 The addition of FK506 decreases the cytosolic free concentration of Ca2+ in the vma3 mutant cells. Tacrolimus 16-21 H(+)-transporting V0 sector ATPase subunit c Saccharomyces cerevisiae S288C 80-84 7535208-9 1995 IL-10 and interferon-gamma (IFN-gamma) mRNAs were induced by FK506, CY and by the drug combination. Tacrolimus 61-66 interleukin 10 Mus musculus 0-5 7536932-7 1995 Neutrophil activation by mast cell-derived FKBP12 is prevented by complexing FKBP12 with FK506 or rapamycin. Tacrolimus 89-94 FKBP prolyl isomerase 1A Homo sapiens 77-83 7535208-9 1995 IL-10 and interferon-gamma (IFN-gamma) mRNAs were induced by FK506, CY and by the drug combination. Tacrolimus 61-66 interferon gamma Mus musculus 10-26 7536932-9 1995 They further suggest a pathophysiological role for FKBP12 as a mediator in immediate or type I hypersensitivity and may have implications for novel therapeutic strategies in the treatment of allergic disorders with FK506 and rapamycin. Tacrolimus 215-220 FKBP prolyl isomerase 1A Homo sapiens 51-57 7535208-9 1995 IL-10 and interferon-gamma (IFN-gamma) mRNAs were induced by FK506, CY and by the drug combination. Tacrolimus 61-66 interferon gamma Mus musculus 28-37 7534792-6 1995 Expression of p68 c-rel protein, but not p50 or p65, was suppressed by the immunosuppressive drug FK506. Tacrolimus 98-103 DNA polymerase delta 3, accessory subunit Homo sapiens 14-17 7543780-5 1995 Simultaneous addition of Rap and CsA or Rap and FK506 inhibit the IL-2-mediated proliferation of TS1 beta and TS1 alpha beta cells and therefore FK506 does not revert the inhibition mediated by Rap in TS1 alpha beta cells. Tacrolimus 48-53 interleukin 2 Homo sapiens 66-70 7547679-6 1995 The effect of CsA on Bcl-2 expression is controlled by calcineurin since we have shown that FK506 but not rapamycin had the same effect on Bcl-2 expression, whereas okadaic acid, an inhibitor of phosphatases 1, 2A and 2C, was ineffective. Tacrolimus 92-97 BCL2 apoptosis regulator Homo sapiens 21-26 7547679-6 1995 The effect of CsA on Bcl-2 expression is controlled by calcineurin since we have shown that FK506 but not rapamycin had the same effect on Bcl-2 expression, whereas okadaic acid, an inhibitor of phosphatases 1, 2A and 2C, was ineffective. Tacrolimus 92-97 BCL2 apoptosis regulator Homo sapiens 139-144 7534792-6 1995 Expression of p68 c-rel protein, but not p50 or p65, was suppressed by the immunosuppressive drug FK506. Tacrolimus 98-103 REL proto-oncogene, NF-kB subunit Homo sapiens 18-23 7534792-7 1995 Because FK506 specifically inhibits the appearance of mature single-positive thymocytes, gene expression regulated by p68 c-rel may play a role in selection and maturational signals involved in the double-positive to single-positive transition. Tacrolimus 8-13 DNA polymerase delta 3, accessory subunit Homo sapiens 118-121 7535208-0 1995 Combined effects of FK506 (tacrolimus) and cyclophosphamide on atypical B220+ T cells, cytokine gene expression and disease activity in MRL/MpJ-lpr/lpr mice. Tacrolimus 20-25 Fas (TNF receptor superfamily member 6) Mus musculus 144-147 7536825-3 1995 The complex of FK506 and FKBP-12 inhibits the calcium activated phosphatase, calcineurin, increasing phosphorylated levels of calcineurin substrates with growth associated protein-43 (GAP-43), being most prominent in the brain. Tacrolimus 15-20 FKBP prolyl isomerase 1A Homo sapiens 25-32 7536825-3 1995 The complex of FK506 and FKBP-12 inhibits the calcium activated phosphatase, calcineurin, increasing phosphorylated levels of calcineurin substrates with growth associated protein-43 (GAP-43), being most prominent in the brain. Tacrolimus 15-20 growth associated protein 43 Homo sapiens 154-182 7536825-3 1995 The complex of FK506 and FKBP-12 inhibits the calcium activated phosphatase, calcineurin, increasing phosphorylated levels of calcineurin substrates with growth associated protein-43 (GAP-43), being most prominent in the brain. Tacrolimus 15-20 growth associated protein 43 Homo sapiens 184-190 7532912-9 1995 These data demonstrate that: 1) FK 506 can be used to treat PSC; 2) the response to FK 506 by patients with PSC is rapid; and, 3) no adverse effect on the serum BUN and creatinine levels was observed. Tacrolimus 32-38 proteasome 20S subunit alpha 2 Homo sapiens 60-66 7534792-7 1995 Because FK506 specifically inhibits the appearance of mature single-positive thymocytes, gene expression regulated by p68 c-rel may play a role in selection and maturational signals involved in the double-positive to single-positive transition. Tacrolimus 8-13 REL proto-oncogene, NF-kB subunit Homo sapiens 122-127 7628296-9 1995 Therefore, compounds interacting with CYP3A proteins are expected to cause drug-drug interactions (i.e. the antimycotics ketoconazole and clotrimazole, the steroids ethinylestradiol and testosterone, the ergots, the calcium channel blocker nifedipine, and the immunosuppressants FK-506 and rapamycin). Tacrolimus 279-285 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-43 7538492-6 1995 The presence of IFN-gamma and LPS in the culture increased NO2- production by casein-elicited macrophages and partially eliminated the inhibition exerted by CsA and FK506. Tacrolimus 165-170 interferon gamma Mus musculus 16-25 7538492-7 1995 Both drugs acted directly on the nitric oxide synthase (NOS), since CsA and FK506 reduced by 35% and by 17%, respectively, NOS activity in the crude cytosolic fraction. Tacrolimus 76-81 nitric oxide synthase 1, neuronal Mus musculus 33-54 7540862-0 1995 IL-5 production by CD4+ T cells of asthmatic patients is suppressed by glucocorticoids and the immunosuppressants FK506 and cyclosporin A. Tacrolimus 114-119 interleukin 5 Homo sapiens 0-4 7540862-0 1995 IL-5 production by CD4+ T cells of asthmatic patients is suppressed by glucocorticoids and the immunosuppressants FK506 and cyclosporin A. Tacrolimus 114-119 CD4 molecule Homo sapiens 19-22 7540862-6 1995 Dexamethasone, FK506 and cyclosporin A suppressed IL-5 production in vitro in a dose-dependent manner. Tacrolimus 15-20 interleukin 5 Homo sapiens 50-54 7540862-7 1995 Clear dose-dependent suppression of IL-5 gene expression by FK506 was also observed. Tacrolimus 60-65 interleukin 5 Homo sapiens 36-40 7532665-3 1995 In this report, we investigated the effects of dexamethasone, cyclosporin A, FK506, and pyrrolidine dithiocarbamate (PDTC) on the induction of the ICAM-1 gene by cytokines in fibroblasts. Tacrolimus 77-82 intercellular adhesion molecule 1 Homo sapiens 147-153 7532676-0 1995 FK506 inhibits antigen receptor-mediated induction of c-rel in B and T lymphoid cells. Tacrolimus 0-5 REL proto-oncogene, NF-kB subunit Homo sapiens 54-59 7532676-4 1995 Furthermore, c-rel induction is blocked by the immunosuppressive drug FK506 that is known to inhibit B and T cell activation. Tacrolimus 70-75 REL proto-oncogene, NF-kB subunit Homo sapiens 13-18 7532685-3 1995 The effect of FK506, an inhibitor of calcineurin activation, on positive and negative selection in CD4+CD8+ double positive (DP) thymocytes was examined in normal mice and in a TCR transgenic mouse model. Tacrolimus 14-19 CD4 antigen Mus musculus 99-102 7532685-4 1995 In vivo FK506 treatment blocked the generation of mature TCRhighCD4+CD8- and TCRhighCD4-CD8+ thymocytes, and the induction of CD69 expression on DP thymocytes. Tacrolimus 8-13 CD69 antigen Mus musculus 126-130 7532685-5 1995 In addition, the shutdown of recombination activating gene 1 (RAG-1) transcription and the downregulation of CD4 and CD8 expression were inhibited by FK506 treatment suggesting that the activation of calcineurin is required for the first step (or the very early intracellular signaling events) of TCR-mediated positive selection of DP thymocytes. Tacrolimus 150-155 recombination activating 1 Mus musculus 29-60 7532685-5 1995 In addition, the shutdown of recombination activating gene 1 (RAG-1) transcription and the downregulation of CD4 and CD8 expression were inhibited by FK506 treatment suggesting that the activation of calcineurin is required for the first step (or the very early intracellular signaling events) of TCR-mediated positive selection of DP thymocytes. Tacrolimus 150-155 recombination activating 1 Mus musculus 62-67 7532685-5 1995 In addition, the shutdown of recombination activating gene 1 (RAG-1) transcription and the downregulation of CD4 and CD8 expression were inhibited by FK506 treatment suggesting that the activation of calcineurin is required for the first step (or the very early intracellular signaling events) of TCR-mediated positive selection of DP thymocytes. Tacrolimus 150-155 CD4 antigen Mus musculus 109-112 7538218-1 1995 We investigated the inhibitory action of FK506 (0.0005-5 micrograms/ml) on the metabolism of arachidonate 5-lipoxygenase in rat basophilic leukemia-1 cells. Tacrolimus 41-46 arachidonate 5-lipoxygenase Rattus norvegicus 93-120 9383417-3 1995 Rapamycin, ascomycin and FK506 have a common domain responsible for binding to FKBP12, their cellular receptor, and different effector domains that determine the target of the complex. Tacrolimus 25-30 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 79-85 9383417-7 1995 CONCLUSIONS: The designed rapamycin-based FKBP12 ligand exhibits powerful binding properties but, unlike rapamycin, shows no activity in IL-6 dependent B-cell proliferation and, in contrast to FK506, shows no activity in the IL-2 reporter assay. Tacrolimus 193-198 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 42-48 7551978-1 1995 This study evaluates the ability of the immunosuppressive drugs dexamethasone, cyclosporine, FK506 and rapamycin, alone and in combination to suppress interleukin-1 beta (IL-1 beta) secretion in vitro by THP-1 cells when stimulated by lipopolysaccharide. Tacrolimus 93-98 interleukin 1 beta Homo sapiens 151-169 7551978-1 1995 This study evaluates the ability of the immunosuppressive drugs dexamethasone, cyclosporine, FK506 and rapamycin, alone and in combination to suppress interleukin-1 beta (IL-1 beta) secretion in vitro by THP-1 cells when stimulated by lipopolysaccharide. Tacrolimus 93-98 interleukin 1 beta Homo sapiens 171-180 7551978-4 1995 Cyclosporine, FK506 and rapamycin only partially suppress secretion of IL-1 beta at concentrations within their therapeutic ranges and increasing concentrations of the drugs do not result in further suppression of secretion. Tacrolimus 14-19 interleukin 1 beta Homo sapiens 71-80 7551978-7 1995 These data suggest that cyclosporine, FK506 and rapamycin all share a common effect on the production of IL-1 beta, different from that of dexamethasone. Tacrolimus 38-43 interleukin 1 beta Homo sapiens 105-114 7878764-11 1995 Tacrolimus immunosuppression of transplant rejection prevented the appearance of hsp-reactive lymphocytes in allografts. Tacrolimus 0-10 selenoprotein K Rattus norvegicus 81-84 7530743-1 1995 FK506 and cyclosporin A (CsA) are immunosuppressive agents that inhibit IL-2 production by activated T cells, but only CsA inhibits IgE activation-induced cytokine transcripts in mouse IL-3-dependent, bone marrow-derived mast cells (BMMC). Tacrolimus 0-5 interleukin 2 Mus musculus 72-76 7530743-1 1995 FK506 and cyclosporin A (CsA) are immunosuppressive agents that inhibit IL-2 production by activated T cells, but only CsA inhibits IgE activation-induced cytokine transcripts in mouse IL-3-dependent, bone marrow-derived mast cells (BMMC). Tacrolimus 0-5 interleukin 3 Mus musculus 185-189 7530743-2 1995 We previously associated the resistance of BMMC to FK506 with a deficiency in the expression of FK506 binding protein (FKBP) 12, a molecule that forms a complex with FK506 capable of inhibiting calcineurin phosphatase activity in vitro. Tacrolimus 51-56 FK506 binding protein 1a Mus musculus 96-117 7530743-2 1995 We previously associated the resistance of BMMC to FK506 with a deficiency in the expression of FK506 binding protein (FKBP) 12, a molecule that forms a complex with FK506 capable of inhibiting calcineurin phosphatase activity in vitro. Tacrolimus 51-56 FK506 binding protein 1a Mus musculus 119-123 7530743-2 1995 We previously associated the resistance of BMMC to FK506 with a deficiency in the expression of FK506 binding protein (FKBP) 12, a molecule that forms a complex with FK506 capable of inhibiting calcineurin phosphatase activity in vitro. Tacrolimus 96-101 FK506 binding protein 1a Mus musculus 119-123 7530743-3 1995 In this report, we establish that FKBP12 mediates FK506 inhibition of both calcineurin phosphatase activity and IgE activation-induced cytokine transcripts in a Kirsten murine sarcoma virus-immortalized mast cell line that is FKBP12 deficient. Tacrolimus 50-55 FK506 binding protein 1a Mus musculus 34-40 7530743-3 1995 In this report, we establish that FKBP12 mediates FK506 inhibition of both calcineurin phosphatase activity and IgE activation-induced cytokine transcripts in a Kirsten murine sarcoma virus-immortalized mast cell line that is FKBP12 deficient. Tacrolimus 50-55 FK506 binding protein 1a Mus musculus 226-232 7530743-4 1995 Overexpression of FKBP12 by transfection enhanced the ability of FK506 to inhibit calcineurin phosphatase activity (IC50 = 2 nM), compared with cells transfected with the expression vector alone (IC50 > 30 nM). Tacrolimus 65-70 FK506 binding protein 1a Mus musculus 18-24 7530743-5 1995 The IC50 value for FK506 inhibition of IgE activation-induced transcripts for TNF-alpha decreased from 40 nM in vector control cells to 10 nM in FKBP12 transfectants. Tacrolimus 19-24 tumor necrosis factor Mus musculus 78-87 7530743-5 1995 The IC50 value for FK506 inhibition of IgE activation-induced transcripts for TNF-alpha decreased from 40 nM in vector control cells to 10 nM in FKBP12 transfectants. Tacrolimus 19-24 FK506 binding protein 1a Mus musculus 145-151 7530743-7 1995 In contrast, activation-elicited release of the secretory granule mediator beta-hexosaminidase was only partially inhibited by FK506 at 1000 nM, regardless of the levels of FKBP12 expressed by the cells. Tacrolimus 127-132 O-GlcNAcase Mus musculus 75-94 7530743-8 1995 Thus, FKBP12 is the dominant cytosolic protein that mediates FK506 inhibition of TNF-alpha and IL-6 transcripts. Tacrolimus 61-66 FK506 binding protein 1a Mus musculus 6-12 7530743-8 1995 Thus, FKBP12 is the dominant cytosolic protein that mediates FK506 inhibition of TNF-alpha and IL-6 transcripts. Tacrolimus 61-66 tumor necrosis factor Mus musculus 81-90 7530743-8 1995 Thus, FKBP12 is the dominant cytosolic protein that mediates FK506 inhibition of TNF-alpha and IL-6 transcripts. Tacrolimus 61-66 interleukin 6 Mus musculus 95-99 7532879-5 1995 In contrast, only the highest concentrations of FK506 and CsA significantly altered PDGF- or bFGF-induced VSMC DNA synthesis. Tacrolimus 48-53 fibroblast growth factor 2 Rattus norvegicus 93-97 7532879-7 1995 The extent of the antagonism of RPM"s inhibition of bFGF-induced VSMC DNA synthesis by FK506 was inversely proportional to RPM concentration and directly proportional to FK506 concentration. Tacrolimus 87-92 fibroblast growth factor 2 Rattus norvegicus 52-56 7532879-7 1995 The extent of the antagonism of RPM"s inhibition of bFGF-induced VSMC DNA synthesis by FK506 was inversely proportional to RPM concentration and directly proportional to FK506 concentration. Tacrolimus 170-175 fibroblast growth factor 2 Rattus norvegicus 52-56 7531689-2 1995 FKBP-12 (FKBP), the soluble receptor for the immunosuppresant drug FK-506, is tightly bound to the calcium release channel (CRC)/ryanodine receptor (RyR) of skeletal muscle terminal cisternae (TC) of sarcoplasmic reticulum with a stoichiometry of 4 mol of FKBP per tetrameric RyR complex. Tacrolimus 67-73 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 0-7 7531689-2 1995 FKBP-12 (FKBP), the soluble receptor for the immunosuppresant drug FK-506, is tightly bound to the calcium release channel (CRC)/ryanodine receptor (RyR) of skeletal muscle terminal cisternae (TC) of sarcoplasmic reticulum with a stoichiometry of 4 mol of FKBP per tetrameric RyR complex. Tacrolimus 67-73 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 0-4 7531689-2 1995 FKBP-12 (FKBP), the soluble receptor for the immunosuppresant drug FK-506, is tightly bound to the calcium release channel (CRC)/ryanodine receptor (RyR) of skeletal muscle terminal cisternae (TC) of sarcoplasmic reticulum with a stoichiometry of 4 mol of FKBP per tetrameric RyR complex. Tacrolimus 67-73 ryanodine receptor 1 Homo sapiens 149-152 7531689-2 1995 FKBP-12 (FKBP), the soluble receptor for the immunosuppresant drug FK-506, is tightly bound to the calcium release channel (CRC)/ryanodine receptor (RyR) of skeletal muscle terminal cisternae (TC) of sarcoplasmic reticulum with a stoichiometry of 4 mol of FKBP per tetrameric RyR complex. Tacrolimus 67-73 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 9-13 7531627-0 1995 IL-8/IL-8 receptor expression in psoriasis and the response to systemic tacrolimus (FK506) therapy. Tacrolimus 72-82 C-X-C motif chemokine ligand 8 Homo sapiens 0-4 7531627-0 1995 IL-8/IL-8 receptor expression in psoriasis and the response to systemic tacrolimus (FK506) therapy. Tacrolimus 72-82 C-X-C motif chemokine ligand 8 Homo sapiens 5-9 7531627-0 1995 IL-8/IL-8 receptor expression in psoriasis and the response to systemic tacrolimus (FK506) therapy. Tacrolimus 84-89 C-X-C motif chemokine ligand 8 Homo sapiens 0-4 7531627-0 1995 IL-8/IL-8 receptor expression in psoriasis and the response to systemic tacrolimus (FK506) therapy. Tacrolimus 84-89 C-X-C motif chemokine ligand 8 Homo sapiens 5-9 7531627-5 1995 IL-8 mRNA was not detected in the skin of any patient after the start of systemic tacrolimus therapy; IL-1 beta, IL-6 and IFN-gamma transcripts were also reduced. Tacrolimus 82-92 C-X-C motif chemokine ligand 8 Homo sapiens 0-4 7531627-8 1995 Estimation of circulating IL-8 levels by enzyme immunoassay showed that all patients with detectable IL-8 before treatment had decreased levels in response to treatment with tacrolimus; reductions in PASI scores were accompanied by decreases in IL-8 levels, that varied both in rate and extent. Tacrolimus 174-184 C-X-C motif chemokine ligand 8 Homo sapiens 26-30 7531627-8 1995 Estimation of circulating IL-8 levels by enzyme immunoassay showed that all patients with detectable IL-8 before treatment had decreased levels in response to treatment with tacrolimus; reductions in PASI scores were accompanied by decreases in IL-8 levels, that varied both in rate and extent. Tacrolimus 174-184 C-X-C motif chemokine ligand 8 Homo sapiens 101-105 7531627-8 1995 Estimation of circulating IL-8 levels by enzyme immunoassay showed that all patients with detectable IL-8 before treatment had decreased levels in response to treatment with tacrolimus; reductions in PASI scores were accompanied by decreases in IL-8 levels, that varied both in rate and extent. Tacrolimus 174-184 C-X-C motif chemokine ligand 8 Homo sapiens 101-105 7531627-11 1995 They further suggest that interference with IL-8 production and/or that of other key chemokines may be an important mechanism underlying the therapeutic efficacy of tacrolimus, and other agents such as cyclosporin A, with similar molecular actions. Tacrolimus 165-175 C-X-C motif chemokine ligand 8 Homo sapiens 44-48 7538218-8 1995 These results indicate that FK506 inhibits the production of peptide LTs, LTB4 and 5-HETE by inhibiting 5-lipoxygenase activity in intact cells. Tacrolimus 28-33 arachidonate 5-lipoxygenase Rattus norvegicus 104-118 7875200-7 1995 The immunosuppressant FK506 as well as dominant negative alleles of Ras and Raf inhibited HamT-induced IL-2 transcription. Tacrolimus 22-27 interleukin 2 Mus musculus 103-107 7544748-4 1995 Using a cytotoxicity assay and a radioimmunoassay, we observed significant increases in levels of tumor necrosis factor-alpha (TNF-alpha) in the colitis mucosa and detected interleukin-1 alpha in the mucosa of 3 of 5 DSS rats and an increase in TNF-alpha had a tendency to be inhibited by treatment with FK506. Tacrolimus 304-309 tumor necrosis factor Rattus norvegicus 98-125 7532989-2 1995 Based on functional and sequence homology studies, it was recently discovered that hsp56 also belongs to the FKBP class of immunophilin proteins, which are thought to mediate the actions of the immunosuppressive drugs FK506 and rapamycin. Tacrolimus 218-223 FKBP prolyl isomerase 4 Homo sapiens 83-88 7532989-6 1995 It was also found that the untransformed but not the transformed GR was retained following affinity chromatography with FK506-affigel resin, reinforcing the possibility that hsp56 within the untransformed GR complex could be a target for the actions of FK506. Tacrolimus 253-258 FKBP prolyl isomerase 4 Homo sapiens 174-179 7532989-8 1995 This inhibition of GR transformation by FK506 was shown to correlate with an inhibition of Dex-induced GR/hsp90 dissociation, with 10 microM FK506 preventing 48% of the GR/hsp90 complexes from dissociating. Tacrolimus 40-45 heat shock protein 86, pseudogene 1 Mus musculus 106-111 7532989-8 1995 This inhibition of GR transformation by FK506 was shown to correlate with an inhibition of Dex-induced GR/hsp90 dissociation, with 10 microM FK506 preventing 48% of the GR/hsp90 complexes from dissociating. Tacrolimus 141-146 heat shock protein 86, pseudogene 1 Mus musculus 106-111 7532989-8 1995 This inhibition of GR transformation by FK506 was shown to correlate with an inhibition of Dex-induced GR/hsp90 dissociation, with 10 microM FK506 preventing 48% of the GR/hsp90 complexes from dissociating. Tacrolimus 141-146 heat shock protein 86, pseudogene 1 Mus musculus 172-177 7532989-11 1995 Although we speculate that these actions of FK506 on the GR complex are mediated by the associated hsp56 component, other possible mechanisms are also discussed. Tacrolimus 44-49 FKBP prolyl isomerase 4 Homo sapiens 99-104 7533409-0 1995 Inhibition of insulin production by FK 506 is caused at the transcriptional level in pancreatic beta cell when FK BP-12 content is relatively high. Tacrolimus 36-42 FKBP prolyl isomerase 1A Homo sapiens 111-119 7531976-1 1995 The ability of the immunosuppressive agent FK506 to affect growth of the epidermal growth factor-receptor (EGF-R) overexpressing cell line, A431, was compared with that of the structurally unrelated immunosuppressive compound, cyclosporin A (CyA). Tacrolimus 43-48 epidermal growth factor receptor Homo sapiens 73-105 7531976-1 1995 The ability of the immunosuppressive agent FK506 to affect growth of the epidermal growth factor-receptor (EGF-R) overexpressing cell line, A431, was compared with that of the structurally unrelated immunosuppressive compound, cyclosporin A (CyA). Tacrolimus 43-48 epidermal growth factor receptor Homo sapiens 107-112 7530217-0 1995 Rapamycin, FK506 and cyclosporin A inhibit human prolactin gene expression. Tacrolimus 11-16 prolactin Homo sapiens 49-58 7530217-1 1995 In this work we demonstrate that transcription of the human prolactin gene is inhibited by the immunosuppressants FK506 (IC50 = 25 nM), cyclosporin A (IC50 = 190 nM) and rapamycin (IC50 = 25 nM). Tacrolimus 114-119 prolactin Homo sapiens 60-69 7530217-2 1995 Whereas the effect of FK506 and cyclosporin A is specific for prolactin gene transcription, rapamycin has a more general effect on transcription and/or translation in pituitary cells. Tacrolimus 22-27 prolactin Homo sapiens 62-71 7529414-4 1995 They interrupt the cytoplasmic portion of T-cell signaling by forming a complex with a binding protein--FKBP12 in the case of FK506 and rapamycin and cyclophilin A (CyPA) in the case of cyclosporin A (CsA). Tacrolimus 126-131 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 104-110 7529414-7 1995 The existence of strong FK506-FKBP12 binding suggests that FK506 is mimicking some natural ligand for FKBP12. Tacrolimus 24-29 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 30-36 7529414-7 1995 The existence of strong FK506-FKBP12 binding suggests that FK506 is mimicking some natural ligand for FKBP12. Tacrolimus 24-29 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 102-108 7487142-0 1995 FK506: therapeutic effects on lupus dermatoses in autoimmune-prone MRL/Mp-lpr/lpr mice. Tacrolimus 0-5 Fas (TNF receptor superfamily member 6) Mus musculus 67-81 8744655-2 1995 The present study examines the in vitro interactions of classical immunosuppressive agents--FK 506 and Cyclosporine A (CsA) with 2-CdA at the level of T and B cells proliferation, expression receptor for interleukin 2 (R-IL-2) and Ig synthesis. Tacrolimus 92-98 interleukin 2 Homo sapiens 204-217 7529995-3 1995 The existence of a slow cis-trans interconversion of an imidic bond in the inhibitor molecule during the course of the formation of the CsA-CyP18cy complex (where CyP18cy is human 18 kDa cytosolic CyP) prompted us to investigate the reaction of the peptidomacrolides FK506, ascomycin and rapamycin with two specific binding-proteins in more detail. Tacrolimus 267-272 peptidylprolyl isomerase G Homo sapiens 140-143 7529995-5 1995 For FK506, the kinetics of inhibition of human 12 kDa cytosolic FKBP (FKBP12cy) were clearly dependent on time. Tacrolimus 4-9 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 70-76 7529995-9 1995 On the other hand, the kinetics and amplitudes of the inhibition of FKBP12cy varied significantly if rapamycin was used as an inhibitor instead of FK 506. Tacrolimus 147-153 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 68-74 7544748-4 1995 Using a cytotoxicity assay and a radioimmunoassay, we observed significant increases in levels of tumor necrosis factor-alpha (TNF-alpha) in the colitis mucosa and detected interleukin-1 alpha in the mucosa of 3 of 5 DSS rats and an increase in TNF-alpha had a tendency to be inhibited by treatment with FK506. Tacrolimus 304-309 tumor necrosis factor Rattus norvegicus 127-136 22827272-6 1995 IL-8 production by TCC from the ocular fluid was further up-regulated upon stimulatation with PHA, but was suppressed by FK506 and hydrocortisone, though not by diclofenac sodium. Tacrolimus 121-126 C-X-C motif chemokine ligand 8 Homo sapiens 0-4 7530227-0 1994 The yeast FKS1 gene encodes a novel membrane protein, mutations in which confer FK506 and cyclosporin A hypersensitivity and calcineurin-dependent growth. Tacrolimus 80-85 1,3-beta-D-glucan synthase Saccharomyces cerevisiae S288C 10-14 7530227-4 1994 We and others have defined the Saccharomyces cerevisiae FKS1 gene by recessive mutations resulting in 100-1000-fold hypersensitivity to FK506 and CsA (as compared to wild type), but which do not affect sensitivity to a variety of other antifungal drugs. Tacrolimus 136-141 1,3-beta-D-glucan synthase Saccharomyces cerevisiae S288C 56-60 7530227-12 1994 These data suggest that FKS1 provides a unique cellular function which, when absent, increases FK506 and CsA sensitivity by making the CNs (or a CN-dependent function) essential. Tacrolimus 95-100 1,3-beta-D-glucan synthase Saccharomyces cerevisiae S288C 24-28 7527548-1 1994 A soluble 12-kDa FK506 binding protein (FKBP12), the cellular receptor of the immunosuppressive drug FK506, is tightly associated with the Ca2+ release channel of rabbit skeletal muscle sarcoplasmic reticulum [Jayaraman, T., Brillantes, A. M., Timerman, A. P., Fleischer, S., Erdjument-Bromage, H., Tempst, P. & Marks, A. Tacrolimus 17-22 peptidyl-prolyl cis-trans isomerase FKBP1A Oryctolagus cuniculus 40-46 7806527-3 1994 This up-regulation of Cdk4 mRNA and protein was resistant to the immunosuppressant drugs cyclosporin A (CsA) and FK506. Tacrolimus 113-118 cyclin dependent kinase 4 Homo sapiens 22-26 7529023-8 1994 The interaction between FKBP-12 (FK506 binding protein) and the ryanodine-binding Ca2+ channel may be an essential link in the chain of events by which FK506 alters Ca(2+)-dependent cellular processes. Tacrolimus 33-38 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 24-31 7529175-1 1994 The peptidyl-prolyl isomerases FKBP12 and cyclophilin A (immunophilins) form complexes with the immunosuppressants FK506 and cyclosporin A that inhibit the phosphatase calcineurin. Tacrolimus 115-120 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 31-37 7529175-2 1994 With the yeast two hybrid system, we detect complexes between FKBP12 and the calcineurin A catalytic subunit in both the presence and absence of FK506. Tacrolimus 145-150 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 62-68 7529175-3 1994 Mutations in FKBP12 surface residues or the absence of the calcineurin B regulatory subunit perturb the FK506-dependent, but not the ligand-independent, FKBP12-calcineurin complex. Tacrolimus 104-109 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 13-19 7529175-3 1994 Mutations in FKBP12 surface residues or the absence of the calcineurin B regulatory subunit perturb the FK506-dependent, but not the ligand-independent, FKBP12-calcineurin complex. Tacrolimus 104-109 protein phosphatase 3 regulatory subunit B, alpha Homo sapiens 59-72 7529739-1 1994 FKBP12 is an 11.8-kDa protein that binds the potent immunosuppressants FK506 and rapamycin. Tacrolimus 71-76 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 0-6 7529739-2 1994 When bound to FK506, FKBP12 forms an inhibitory complex with calcineurin and interferes with signal transduction in activated T lymphocytes. Tacrolimus 14-19 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 21-27 7528676-1 1994 Ligation of CD40 activates B cells via a Ca(++)-dependent, FK506-sensitive pathway. Tacrolimus 59-64 CD40 antigen Mus musculus 12-16 7528676-5 1994 However, the effects of the drug on proliferative responses elicited by anti-Ig or anti-CD40 differ significantly: firstly, the response to anti-CD40 + IL-4 becomes completely FK506-resistant within 24 h, whilst that to anti-Ig remains sensitive significantly longer. Tacrolimus 176-181 CD40 antigen Mus musculus 88-92 7528676-5 1994 However, the effects of the drug on proliferative responses elicited by anti-Ig or anti-CD40 differ significantly: firstly, the response to anti-CD40 + IL-4 becomes completely FK506-resistant within 24 h, whilst that to anti-Ig remains sensitive significantly longer. Tacrolimus 176-181 CD40 antigen Mus musculus 145-149 7528676-5 1994 However, the effects of the drug on proliferative responses elicited by anti-Ig or anti-CD40 differ significantly: firstly, the response to anti-CD40 + IL-4 becomes completely FK506-resistant within 24 h, whilst that to anti-Ig remains sensitive significantly longer. Tacrolimus 176-181 interleukin 4 Mus musculus 152-156 7528676-6 1994 Secondly, stimulating B cells concurrently via CD40, surface Ig (sIg) and IL-4 receptors invokes an FK506-resistant activation pathway. Tacrolimus 100-105 CD40 antigen Mus musculus 47-51 7528676-6 1994 Secondly, stimulating B cells concurrently via CD40, surface Ig (sIg) and IL-4 receptors invokes an FK506-resistant activation pathway. Tacrolimus 100-105 interleukin 4 Mus musculus 74-78 7528676-7 1994 We previously reported that ligation of either sIg or CD40 receptors, in conjunction with IL-4, induces the transcription factor, nuclear factor of activated T cells (NF-AT) in B cells, via a CsA/FK506-sensitive pathway. Tacrolimus 196-201 CD40 antigen Mus musculus 54-58 7528676-7 1994 We previously reported that ligation of either sIg or CD40 receptors, in conjunction with IL-4, induces the transcription factor, nuclear factor of activated T cells (NF-AT) in B cells, via a CsA/FK506-sensitive pathway. Tacrolimus 196-201 interleukin 4 Mus musculus 90-94 7528676-8 1994 However, NF-AT induction elicited by anti-Ig/anti-CD40/IL-4 is still FK506 sensitive, implying that the drug resistance of the response to these three stimuli involves additional components than NF-AT. Tacrolimus 69-74 CD40 antigen Mus musculus 50-54 7530693-2 1994 The effect of the immunosuppressant FK506 on the expression of TCR alpha beta in rat CD4- CD8- thymocytes was also examined. Tacrolimus 36-41 Cd4 molecule Rattus norvegicus 85-88 7530693-6 1994 In contrast, continuous treatment with FK506 for 7 days markedly decreased not only the percentages of CD4+ CD8- TCR alpha beta high and CD4- CD8+ TCR alpha beta high thymocytes, but also that of CD4- CD8- TCR alpha beta high thymocytes. Tacrolimus 39-44 Cd4 molecule Rattus norvegicus 103-106 7530693-6 1994 In contrast, continuous treatment with FK506 for 7 days markedly decreased not only the percentages of CD4+ CD8- TCR alpha beta high and CD4- CD8+ TCR alpha beta high thymocytes, but also that of CD4- CD8- TCR alpha beta high thymocytes. Tacrolimus 39-44 Cd4 molecule Rattus norvegicus 137-140 7530693-6 1994 In contrast, continuous treatment with FK506 for 7 days markedly decreased not only the percentages of CD4+ CD8- TCR alpha beta high and CD4- CD8+ TCR alpha beta high thymocytes, but also that of CD4- CD8- TCR alpha beta high thymocytes. Tacrolimus 39-44 Cd4 molecule Rattus norvegicus 137-140 7525815-4 1994 On the other hand, an immunosuppressant, FK506, and a glucocorticoid inhibit the gene transcription as well as the production of IL-8. Tacrolimus 41-46 C-X-C motif chemokine ligand 8 Homo sapiens 129-133 7530727-0 1994 A soluble binding assay for measuring 3H-FK506 binding to the hsp56 immunophilin. Tacrolimus 41-46 FKBP prolyl isomerase 4 Homo sapiens 62-67 7530727-1 1994 Heat shock protein 56 (hsp56) was previously identified as an immunophilin based on its ability to specifically bind to FK506-Affi-Gel 10. Tacrolimus 120-125 FKBP prolyl isomerase 4 Homo sapiens 0-21 7530727-1 1994 Heat shock protein 56 (hsp56) was previously identified as an immunophilin based on its ability to specifically bind to FK506-Affi-Gel 10. Tacrolimus 120-125 FKBP prolyl isomerase 4 Homo sapiens 23-28 7530727-6 1994 These results demonstrate that hsp56 binds FK506 and rapamycin with similar affinities, and suggest that hsp56 may play a role in mediating the cellular function of both of these drugs. Tacrolimus 43-48 FKBP prolyl isomerase 4 Homo sapiens 31-36 7530727-6 1994 These results demonstrate that hsp56 binds FK506 and rapamycin with similar affinities, and suggest that hsp56 may play a role in mediating the cellular function of both of these drugs. Tacrolimus 43-48 FKBP prolyl isomerase 4 Homo sapiens 105-110 7523855-2 1994 We reported previously that an FK506-sensitive target in S. cerevisiae is required for amino acid import and that overexpression of two new genes, TAT1 and TAT2 (formerly called TAP1 and TAP2), confers resistance to the drug. Tacrolimus 31-36 amino acid transporter TAT1 Saccharomyces cerevisiae S288C 147-151 7523855-2 1994 We reported previously that an FK506-sensitive target in S. cerevisiae is required for amino acid import and that overexpression of two new genes, TAT1 and TAT2 (formerly called TAP1 and TAP2), confers resistance to the drug. Tacrolimus 31-36 aromatic amino acid transmembrane transporter TAT2 Saccharomyces cerevisiae S288C 156-160 7533090-7 1995 Increased expression of FKBP12 resulted in increased sensitivity to FK506 and rapamycin, as measured by inhibition of calcineurin activity and p70 S6 kinase activity, respectively. Tacrolimus 68-73 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 24-30 7533090-9 1995 Two distinct point mutations in FKBP12, one altering a hydrophobic residue within the drug-binding pocket and the other changing a charged surface residue of FKBP12, abrogated its ability to mediate sensitivity to FK506 and rapamycin. Tacrolimus 214-219 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 32-38 7533090-9 1995 Two distinct point mutations in FKBP12, one altering a hydrophobic residue within the drug-binding pocket and the other changing a charged surface residue of FKBP12, abrogated its ability to mediate sensitivity to FK506 and rapamycin. Tacrolimus 214-219 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 158-164 7533090-10 1995 These results establish that FKBP12 can mediate sensitivity to both FK506 and rapamycin in mammalian cells. Tacrolimus 68-73 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 29-35 7536706-1 1994 The immunosuppressant FK506 inhibits N-alpha-benzyloxylcarbonyl-L-lysine thiobenzyl ester (BLT) esterase release from cytotoxic T lymphocytes (CTL). Tacrolimus 22-27 granzyme A Mus musculus 37-104 7708060-2 1994 These untransformed nuclear receptors exist in a heterocomplex containing three heat shock proteins, hsp90, hsp70, and hsp56, the latter being an immunophilin of the FK506 binding type whose cellular function is unknown. Tacrolimus 166-171 heat shock protein 90 alpha family class A member 1 Rattus norvegicus 101-106 7524662-0 1994 Solution structure of FK506 bound to the R42K, H87V double mutant of FKBP-12. Tacrolimus 22-27 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 69-76 7524662-1 1994 The binding of the FK506/FKBP-12 complex to calcineurin (CN), its putative target for immunosuppression, involves recognition of solvent-exposed regions of the ligand as well as FKBP-12 residues near the active site. Tacrolimus 19-24 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 25-32 7524662-1 1994 The binding of the FK506/FKBP-12 complex to calcineurin (CN), its putative target for immunosuppression, involves recognition of solvent-exposed regions of the ligand as well as FKBP-12 residues near the active site. Tacrolimus 19-24 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 178-185 7524662-6 1994 This work reports the solution structure of 13C-labeled FK506 bound to R42K, H87V FKBP-12. Tacrolimus 56-61 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 82-89 7524662-10 1994 Comparison with the NMR structure of FK506 bound to wild-type FKBP-12 reveals that the R42K, H87V mutation causes the ligand backbone near C16 to move by 2.5 to 4.5 A, reorients 15-MeO by 90 degrees, and shifts 13-MeO by approximately 1.5 A. Tacrolimus 37-42 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 62-69 7526495-1 1994 The microbial products FK506 and CsA are potent immunosuppressive agents that prevent early transcriptional events in TcR-mediated activation. Tacrolimus 23-28 T cell receptor alpha variable 6-3 Mus musculus 118-121 7531458-0 1994 FK506 can inhibit apoptotic cell death induced by the HIV-1 envelope glycoprotein gp120. Tacrolimus 0-5 Envelope surface glycoprotein gp160, precursor Human immunodeficiency virus 1 82-87 7525596-0 1994 A novel FK506- and rapamycin-binding protein (FPR3 gene product) in the yeast Saccharomyces cerevisiae is a proline rotamase localized to the nucleolus. Tacrolimus 8-13 peptidylprolyl isomerase FPR3 Saccharomyces cerevisiae S288C 46-50 7522636-7 1994 Cyclosporin A and FK506 act on two distinct levels of the IL-2 control mechanism. Tacrolimus 18-23 interleukin 2 Homo sapiens 58-62 7522130-2 1994 Although no change in cytoplasmic calcium level ([Ca2+]i) was detectable during antigen-specific signal transduction of 171-CD4+ cells, IL2 induction was inhibited by FK506 and CsA. Tacrolimus 167-172 interleukin 2 Homo sapiens 136-139 7522130-5 1994 We suggest that IL2 secretion induced by antigen presentation to TCR/CD4/p56lck requires an FK506 and cyclosporin A-sensitive step which may be independent of calcium signaling. Tacrolimus 92-97 interleukin 2 Homo sapiens 16-19 7522130-5 1994 We suggest that IL2 secretion induced by antigen presentation to TCR/CD4/p56lck requires an FK506 and cyclosporin A-sensitive step which may be independent of calcium signaling. Tacrolimus 92-97 CD4 molecule Homo sapiens 69-72 7522130-5 1994 We suggest that IL2 secretion induced by antigen presentation to TCR/CD4/p56lck requires an FK506 and cyclosporin A-sensitive step which may be independent of calcium signaling. Tacrolimus 92-97 LCK proto-oncogene, Src family tyrosine kinase Homo sapiens 73-79 7528255-7 1994 After the induction of FK506, the number of CD8 positive cells decreased and cardiac rejection was successfully resolved. Tacrolimus 23-28 CD8a molecule Homo sapiens 44-47 7522303-1 1994 The immunosuppressive action of the drug FK506 involves inhibition of calcineurin in T-lymphocytes by a complex of FK506 and an FK506 binding protein, FKBP12, a member of the immunophilin protein family. Tacrolimus 41-46 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 151-157 7522303-1 1994 The immunosuppressive action of the drug FK506 involves inhibition of calcineurin in T-lymphocytes by a complex of FK506 and an FK506 binding protein, FKBP12, a member of the immunophilin protein family. Tacrolimus 115-120 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 151-157 7522447-2 1994 Contrarily to the inhibition observed with the immunosuppressant complex FKBP-12-FK506, no significant inhibition was observed with FKBP-59/HBI or FKBP-59/HBI-I in the presence of FK506, even though FKBP-59/HBI-1 is nearly 55% homologous to the immunophilin FKBP-12. Tacrolimus 81-86 peptidyl-prolyl cis-trans isomerase FKBP1A Oryctolagus cuniculus 73-80 7521210-0 1994 Potentiation of progesterone receptor-mediated transcription by the immunosuppressant FK506. Tacrolimus 86-91 progesterone receptor Homo sapiens 16-37 7521210-7 1994 To gain insight into the mechanism of FK506"s regulation of PR action, we questioned whether calcineurin is involved, because it has been shown that FK506 is a specific inhibitor of calcineurin, a Ca(2+)- and calmodulin-regulated phosphatase, through the formation of an FKBP12-FK506-calcineurin-calmodulin complex. Tacrolimus 149-154 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 271-277 7521210-7 1994 To gain insight into the mechanism of FK506"s regulation of PR action, we questioned whether calcineurin is involved, because it has been shown that FK506 is a specific inhibitor of calcineurin, a Ca(2+)- and calmodulin-regulated phosphatase, through the formation of an FKBP12-FK506-calcineurin-calmodulin complex. Tacrolimus 149-154 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 271-277 7521210-10 1994 Furthermore, immunoblot analysis showed that both FK506 and calmidazolium potentiated the effect of progesterone in decreasing the mobility of hPR-B upon sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE). Tacrolimus 50-55 RB transcriptional corepressor 1 Homo sapiens 143-148 7521210-11 1994 This suggests that FK506 and calmidazolium may cooperate with progesterone in increasing the level of hPR-B phosphorylation. Tacrolimus 19-24 RB transcriptional corepressor 1 Homo sapiens 102-107 7520912-0 1994 The native v-Raf.hsp90.p50 heterocomplex contains a novel immunophilin of the FK506 binding class. Tacrolimus 78-83 heat shock protein 90 alpha family class A member 1 Rattus norvegicus 17-22 7520912-10 1994 We have immunoadsorbed v-Raf from stably transfected rat 3Y1 fibroblasts and show that the immunoadsorbed v-Raf.hsp90.p50 heterocomplex binds the immunosuppressant drug [3H]FK506. Tacrolimus 173-178 heat shock protein 90 alpha family class A member 1 Rattus norvegicus 112-117 7528280-0 1994 FK506, an immunosuppressant, partially inhibits interleukin 6 production by adherent rheumatoid synovial cells. Tacrolimus 0-5 interleukin 6 Homo sapiens 48-61 7528280-1 1994 OBJECTIVE: To investigate the effect of a new immunosuppressant, FK506, on interleukin 6 (IL-6) production by freshly prepared rheumatoid synovial cells. Tacrolimus 65-70 interleukin 6 Homo sapiens 75-88 7528280-1 1994 OBJECTIVE: To investigate the effect of a new immunosuppressant, FK506, on interleukin 6 (IL-6) production by freshly prepared rheumatoid synovial cells. Tacrolimus 65-70 interleukin 6 Homo sapiens 90-94 7528280-7 1994 This spontaneous production of IL-6 was significantly inhibited by FK506 at the concentration of 10(-8) to 10(-6) M in a dose dependent manner. Tacrolimus 67-72 interleukin 6 Homo sapiens 31-35 7528280-8 1994 In the preincubation study, FK506 required more than 12 h to inhibit IL-6 production by synovial cells. Tacrolimus 28-33 interleukin 6 Homo sapiens 69-73 7528280-9 1994 CONCLUSION: These results suggest that FK506 may be beneficial for patients with RA via inhibiting IL-6 production in inflammatory joints. Tacrolimus 39-44 interleukin 6 Homo sapiens 99-103 7974924-2 1994 Several new drugs have been found to be effective immunosuppressive agents: FK 506, a macrolid antibiotic inhibiting lymphokine gene transcription, lymphokine production and secretion, rapamycin, which blocks effects of lymphokine-induced signal transduction, and RS 61443, brequinar and mizoribine, which inhibit DNA/RNA synthesis and lymphocyte proliferation. Tacrolimus 76-82 interleukin 2 Homo sapiens 117-127 7523855-0 1994 Two FK506 resistance-conferring genes in Saccharomyces cerevisiae, TAT1 and TAT2, encode amino acid permeases mediating tyrosine and tryptophan uptake. Tacrolimus 4-9 amino acid transporter TAT1 Saccharomyces cerevisiae S288C 67-71 7523855-0 1994 Two FK506 resistance-conferring genes in Saccharomyces cerevisiae, TAT1 and TAT2, encode amino acid permeases mediating tyrosine and tryptophan uptake. Tacrolimus 4-9 aromatic amino acid transmembrane transporter TAT2 Saccharomyces cerevisiae S288C 76-80 7520433-5 1994 Preincubation with the calcineurin inhibitors FK-506 or cyclosporin A strongly enhanced expression of NGFI-A and blocked transcription of NGFI-B, but it had no significant effect on Ca(2+)-stimulated transcription of c-fos. Tacrolimus 46-52 early growth response 1 Rattus norvegicus 102-108 7520433-5 1994 Preincubation with the calcineurin inhibitors FK-506 or cyclosporin A strongly enhanced expression of NGFI-A and blocked transcription of NGFI-B, but it had no significant effect on Ca(2+)-stimulated transcription of c-fos. Tacrolimus 46-52 nuclear receptor subfamily 4, group A, member 1 Rattus norvegicus 138-144 7520433-5 1994 Preincubation with the calcineurin inhibitors FK-506 or cyclosporin A strongly enhanced expression of NGFI-A and blocked transcription of NGFI-B, but it had no significant effect on Ca(2+)-stimulated transcription of c-fos. Tacrolimus 46-52 Fos proto-oncogene, AP-1 transcription factor subunit Rattus norvegicus 217-222 7520438-3 1994 The FKBP12.FK-506 complex inhibits calcineurin, a calcium-dependent phosphatase that is a component of the signal transduction pathway leading to early lymphokine gene transcription. Tacrolimus 11-17 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 4-10 7520438-8 1994 When complexed with FK-506, FKBP12.6 binds to and inhibits calcineurin, making it only the second FKBP discovered thus far to do so. Tacrolimus 20-26 FKBP prolyl isomerase 1B Homo sapiens 28-36 7520438-9 1994 The ability to inhibit calcineurin establishes the potential relevance of FKBP12.6 to the immunosuppressive or toxic side effects of FK-506. Tacrolimus 133-139 FKBP prolyl isomerase 1B Homo sapiens 74-82 7520353-0 1994 Inhibition of anthralin-caused skin tumor promotion and interleukin-1 alpha production by potent immunosuppressant FK506. Tacrolimus 115-120 interleukin 1 alpha Mus musculus 56-75 7520353-5 1994 Both production and release of Il-1 alpha were markedly inhibited by FK506 (0.1 or 1 microM). Tacrolimus 69-74 interleukin 1 alpha Mus musculus 31-41 7520353-7 1994 It may be possible that the inhibition of IL-1 alpha production by FK506 is related to its anti-tumor-promoting action. Tacrolimus 67-72 interleukin 1 alpha Mus musculus 42-52 7518783-10 1994 Increased hepatic collagen and higher messenger RNA levels of transforming growth factor beta 1 and collagens I, III, and IV were found in the FK506-treated group. Tacrolimus 143-148 transforming growth factor, beta 1 Rattus norvegicus 62-95 7518783-11 1994 Rat fibroblasts treated with FK506 expressed higher levels of collagens I and III, fibronectin, macrophage-colony stimulating factor, tissue inhibitor of metalloprotease, and transforming growth factor beta 1 messenger RNAs. Tacrolimus 29-34 fibronectin 1 Rattus norvegicus 83-94 8046352-1 1994 The tumor necrosis factor alpha (TNF-alpha) gene is rapidly transcribed in activated T cells via a calcium-dependent pathway that does not require de novo protein synthesis, but is completely blocked by the immunosuppressive drugs cyclosporin A (CsA) and FK506. Tacrolimus 255-260 tumor necrosis factor Homo sapiens 4-31 8046352-1 1994 The tumor necrosis factor alpha (TNF-alpha) gene is rapidly transcribed in activated T cells via a calcium-dependent pathway that does not require de novo protein synthesis, but is completely blocked by the immunosuppressive drugs cyclosporin A (CsA) and FK506. Tacrolimus 255-260 tumor necrosis factor Homo sapiens 33-42 8046352-3 1994 The ability of analogues of CsA and FK506 to block calcineurin phosphatase activity correlates completely with their ability to inhibit induction of TNF-alpha mRNA, induction of a TNF-alpha promoter reporter plasmid in transiently transfected T cells, and induction of the kappa 3 binding factor in an electrophoretic mobility shift assay. Tacrolimus 36-41 tumor necrosis factor Homo sapiens 149-158 8046352-3 1994 The ability of analogues of CsA and FK506 to block calcineurin phosphatase activity correlates completely with their ability to inhibit induction of TNF-alpha mRNA, induction of a TNF-alpha promoter reporter plasmid in transiently transfected T cells, and induction of the kappa 3 binding factor in an electrophoretic mobility shift assay. Tacrolimus 36-41 tumor necrosis factor Homo sapiens 180-189 8046352-6 1994 Using the panel of CsA and FK506 analogues, we show that calcineurin participates in the induction of TNF-alpha transcription in activated B cells. Tacrolimus 27-32 tumor necrosis factor Homo sapiens 102-111 7518925-2 1994 Antibody directed at surface immunoglobulin (anti-Ig) on B cells has previously been shown to induce a rapid burst of TNF-alpha gene transcription, which can be blocked by the immunosuppressants cyclosporin A (CsA) and FK506. Tacrolimus 219-224 tumor necrosis factor Homo sapiens 118-127 7518356-1 1994 The immunosuppressants rapamycin and FK506 bind to the same intracellular protein, the immunophilin FKBP12. Tacrolimus 37-42 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 100-106 7813402-6 1994 For each isoform of the enzyme the peptidyl-prolyl cis/trans isomerase activity of the separated proteins was inhibited by cyclosporin A but was resistant toward FK 506. Tacrolimus 162-168 FKBP prolyl isomerase like Homo sapiens 35-70 8008069-1 1994 The structurally related natural products rapamycin and FK506 bind to the same intracellular receptor, FKBP12, yet the resulting complexes interfere with distinct signalling pathways. Tacrolimus 56-61 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 103-109 7517078-0 1994 The direct effect of FK506 and rapamycin on interleukin 1(beta) and immunoglobulin production in vitro. Tacrolimus 21-26 interleukin 1 beta Homo sapiens 44-63 7584489-7 1994 These results suggest that combined treatment with FK506 and GC acts complexly to decrease rat CD4+8+ thymocytes and prevents thymocyte differentiation and maturation. Tacrolimus 51-56 Cd4 molecule Rattus norvegicus 95-98 7514602-3 1994 Chemical cross-linking studies with disuccinimidyl suberate in the presence of either cyclophilin A, B, or C in complex with cyclosporin A or FK506 binding protein-FK506 result on the other hand in the apparently exclusive and strictly immunosuppressant-dependent formation of covalent immunophilin-calcineurin B subunit products. Tacrolimus 142-147 peptidyl-prolyl cis-trans isomerase A Bos taurus 86-99 7514602-3 1994 Chemical cross-linking studies with disuccinimidyl suberate in the presence of either cyclophilin A, B, or C in complex with cyclosporin A or FK506 binding protein-FK506 result on the other hand in the apparently exclusive and strictly immunosuppressant-dependent formation of covalent immunophilin-calcineurin B subunit products. Tacrolimus 164-169 peptidyl-prolyl cis-trans isomerase A Bos taurus 86-99 7514602-3 1994 Chemical cross-linking studies with disuccinimidyl suberate in the presence of either cyclophilin A, B, or C in complex with cyclosporin A or FK506 binding protein-FK506 result on the other hand in the apparently exclusive and strictly immunosuppressant-dependent formation of covalent immunophilin-calcineurin B subunit products. Tacrolimus 164-169 protein phosphatase 3 regulatory subunit B, alpha Bos taurus 299-312 7512379-1 1994 Backbone dynamics of the ligand- (FK506-) bound protein FKBP-12 (107 amino acids) have been examined using 15N relaxation data derived from inverse-detected two-dimensional 1H-15N NMR spectra. Tacrolimus 34-39 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 56-63 7523855-2 1994 We reported previously that an FK506-sensitive target in S. cerevisiae is required for amino acid import and that overexpression of two new genes, TAT1 and TAT2 (formerly called TAP1 and TAP2), confers resistance to the drug. Tacrolimus 31-36 amino acid transporter TAT1 Saccharomyces cerevisiae S288C 178-182 7523855-2 1994 We reported previously that an FK506-sensitive target in S. cerevisiae is required for amino acid import and that overexpression of two new genes, TAT1 and TAT2 (formerly called TAP1 and TAP2), confers resistance to the drug. Tacrolimus 31-36 aromatic amino acid transmembrane transporter TAT2 Saccharomyces cerevisiae S288C 187-191 7519613-0 1994 Cloning and expression of cyclosporin A- and FK506-sensitive nuclear factor of activated T-cells: NF45 and NF90. Tacrolimus 45-50 interleukin enhancer binding factor 2 Homo sapiens 98-102 7519613-0 1994 Cloning and expression of cyclosporin A- and FK506-sensitive nuclear factor of activated T-cells: NF45 and NF90. Tacrolimus 45-50 interleukin enhancer binding factor 3 Homo sapiens 107-111 7519613-11 1994 Histidine-tagged NF45 and NF90 proteins, affinity-purified on nickel chelate columns, encode a NF-AT DNA-binding activity that is enhanced following T-cell stimulation, and this enhancement is blocked when T-cells are stimulated in the presence of cyclosporin A or FK506. Tacrolimus 265-270 interleukin enhancer binding factor 2 Homo sapiens 17-21 7519613-11 1994 Histidine-tagged NF45 and NF90 proteins, affinity-purified on nickel chelate columns, encode a NF-AT DNA-binding activity that is enhanced following T-cell stimulation, and this enhancement is blocked when T-cells are stimulated in the presence of cyclosporin A or FK506. Tacrolimus 265-270 interleukin enhancer binding factor 3 Homo sapiens 26-30 7798592-2 1994 Both methods were used to measure inhibition of proliferative responses of phytohaemagglutinin (PHA1)-stimulated human peripheral blood lymphocytes by tacrolimus (FK 506(1)), cyclosporine A (CsA1), rapamycin (RA1), dexamethasone (DEX1), prednisolone (PR1), and methylprednisolone (MP1). Tacrolimus 151-161 sodium channel epithelial 1 subunit gamma Homo sapiens 96-100 7798592-2 1994 Both methods were used to measure inhibition of proliferative responses of phytohaemagglutinin (PHA1)-stimulated human peripheral blood lymphocytes by tacrolimus (FK 506(1)), cyclosporine A (CsA1), rapamycin (RA1), dexamethasone (DEX1), prednisolone (PR1), and methylprednisolone (MP1). Tacrolimus 163-169 sodium channel epithelial 1 subunit gamma Homo sapiens 96-100 7518461-1 1994 The immunosuppressant FK-506 (tacrolimus) forms a complex with a ubiquitous intracellular receptor, FK-506 binding protein (FKBP12), and this complex inhibits the heterodimeric Ca2+/calmodulin-dependent phosphatase, calcineurin, an essential component of the T-cell receptor signal transduction pathway. Tacrolimus 22-28 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 124-130 7518461-1 1994 The immunosuppressant FK-506 (tacrolimus) forms a complex with a ubiquitous intracellular receptor, FK-506 binding protein (FKBP12), and this complex inhibits the heterodimeric Ca2+/calmodulin-dependent phosphatase, calcineurin, an essential component of the T-cell receptor signal transduction pathway. Tacrolimus 30-40 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 124-130 7518461-6 1994 To assess the role of the autoinhibitory domain in regulating the interaction of CaN with the FK-506.FKBP12 complex, we reconstituted wild type and mutant phosphatase heterodimers using in vitro transcribed and translated subunits. Tacrolimus 94-100 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 101-107 7518461-7 1994 Association of the reconstituted calcineurin heterodimers with FKBP12 was dependent on FK-506. Tacrolimus 87-93 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 63-69 7518461-8 1994 In the case of the wild type heterodimer, association with the FK-506.FKBP12 complex was also dependent upon Ca2+; however, mutant catalytic subunits, in which the autoinhibitory domains were deleted, associated with the drug-binding protein complex in the presence of 10 mM EGTA. Tacrolimus 63-69 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 70-76 7518461-9 1994 These results indicate that the conserved autoinhibitory domain regulates both Ca(2+)-dependent phosphatase activity and association with the FK-506.FKBP12 complex. Tacrolimus 142-148 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 149-155 7518925-3 1994 Here, TNF-alpha gene transcription is shown also to be highly and rapidly induced in human B cells after stimulation via the CD40 and interleukin 4 pathways, which similarly is inhibited by CsA and a panel of CsA or FK506 analogues that block calcineurin phosphatase activity. Tacrolimus 216-221 tumor necrosis factor Homo sapiens 6-15 7518925-3 1994 Here, TNF-alpha gene transcription is shown also to be highly and rapidly induced in human B cells after stimulation via the CD40 and interleukin 4 pathways, which similarly is inhibited by CsA and a panel of CsA or FK506 analogues that block calcineurin phosphatase activity. Tacrolimus 216-221 CD40 molecule Homo sapiens 125-129 7518925-3 1994 Here, TNF-alpha gene transcription is shown also to be highly and rapidly induced in human B cells after stimulation via the CD40 and interleukin 4 pathways, which similarly is inhibited by CsA and a panel of CsA or FK506 analogues that block calcineurin phosphatase activity. Tacrolimus 216-221 interleukin 4 Homo sapiens 134-147 7518678-1 1994 Tacrolimus(FK506) is a strong immuno-suppressant and shows its activity through inhibiting IL-2 mRNA transcription by forming pentameric complex with intracellular receptor(FK506 binding protein 12 kDa or FKBP12), Ca2+, calmodulin, and calcineurin. Tacrolimus 0-10 interleukin 2 Homo sapiens 91-95 7518678-1 1994 Tacrolimus(FK506) is a strong immuno-suppressant and shows its activity through inhibiting IL-2 mRNA transcription by forming pentameric complex with intracellular receptor(FK506 binding protein 12 kDa or FKBP12), Ca2+, calmodulin, and calcineurin. Tacrolimus 0-10 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 205-211 7518678-1 1994 Tacrolimus(FK506) is a strong immuno-suppressant and shows its activity through inhibiting IL-2 mRNA transcription by forming pentameric complex with intracellular receptor(FK506 binding protein 12 kDa or FKBP12), Ca2+, calmodulin, and calcineurin. Tacrolimus 11-16 interleukin 2 Homo sapiens 91-95 7518678-1 1994 Tacrolimus(FK506) is a strong immuno-suppressant and shows its activity through inhibiting IL-2 mRNA transcription by forming pentameric complex with intracellular receptor(FK506 binding protein 12 kDa or FKBP12), Ca2+, calmodulin, and calcineurin. Tacrolimus 11-16 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 205-211 7519528-11 1994 RESULTS: After 4-6 weeks of FK-506 therapy, human IgG, all thyroid antibodies and IFN-gamma were suppressed, while the levels remained elevated in the control group. Tacrolimus 28-34 immunoglobulin heavy variable V1-62 Mus musculus 50-53 7519528-11 1994 RESULTS: After 4-6 weeks of FK-506 therapy, human IgG, all thyroid antibodies and IFN-gamma were suppressed, while the levels remained elevated in the control group. Tacrolimus 28-34 interferon gamma Homo sapiens 82-91 7923750-4 1994 Cyclosporine and related agents such as FK-506 and rapamycin selectively inhibit adaptive immune responses by blocking T cell-dependent biosynthesis of lymphokines, particularly interleukin 2 at the level of messenger ribonucleic acid (mRNA) transcription. Tacrolimus 40-46 interleukin 2 Homo sapiens 178-191 7517981-5 1994 In regard to FK-506, we found that 1) FK-506 completely blocked the production of IL-2; 2) exogeneous IL-2 consistently restored the FK-506-induced inhibition; 3) FK-506 affected the phorbol myristate acetate-induced IL-2 responsiveness very little, if any; and 4) the significant suppression was observed only when FK-506 was added within 24 h after the initiation of culture. Tacrolimus 38-44 interleukin 2 Homo sapiens 82-86 7517981-5 1994 In regard to FK-506, we found that 1) FK-506 completely blocked the production of IL-2; 2) exogeneous IL-2 consistently restored the FK-506-induced inhibition; 3) FK-506 affected the phorbol myristate acetate-induced IL-2 responsiveness very little, if any; and 4) the significant suppression was observed only when FK-506 was added within 24 h after the initiation of culture. Tacrolimus 38-44 interleukin 2 Homo sapiens 82-86 7517981-5 1994 In regard to FK-506, we found that 1) FK-506 completely blocked the production of IL-2; 2) exogeneous IL-2 consistently restored the FK-506-induced inhibition; 3) FK-506 affected the phorbol myristate acetate-induced IL-2 responsiveness very little, if any; and 4) the significant suppression was observed only when FK-506 was added within 24 h after the initiation of culture. Tacrolimus 38-44 interleukin 2 Homo sapiens 82-86 7517981-5 1994 In regard to FK-506, we found that 1) FK-506 completely blocked the production of IL-2; 2) exogeneous IL-2 consistently restored the FK-506-induced inhibition; 3) FK-506 affected the phorbol myristate acetate-induced IL-2 responsiveness very little, if any; and 4) the significant suppression was observed only when FK-506 was added within 24 h after the initiation of culture. Tacrolimus 38-44 interleukin 2 Homo sapiens 82-86 7517981-7 1994 Conversely, FK-506 acts as a strong inhibitor of IL-2 production without a prominent effect on IL-2 responsiveness. Tacrolimus 12-18 interleukin 2 Homo sapiens 49-53 8068174-1 1994 The transcription factor NF-ATp is a target in activated T cells for the calcium-regulated phosphatase calcineurin, and is therefore a secondary target for the immunosuppressive drugs cyclosporin A and FK506. Tacrolimus 202-207 nuclear factor of activated T cells 2 Homo sapiens 25-31 7524055-6 1994 Correlation of the 6 beta-testosterone hydroxylase activity with the FK 506 metabolite (M1) initial formation rate is consistent with the belief that CYP 3A isozymes are involved in FK 506 metabolism in male rats. Tacrolimus 69-75 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 150-156 7524055-6 1994 Correlation of the 6 beta-testosterone hydroxylase activity with the FK 506 metabolite (M1) initial formation rate is consistent with the belief that CYP 3A isozymes are involved in FK 506 metabolism in male rats. Tacrolimus 182-188 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 150-156 7514503-1 1994 FK506-binding protein (FKBP12) was originally identified as the cytosolic receptor for the immunosuppressant drugs FK506 and rapamycin. Tacrolimus 0-5 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 23-29 7514503-5 1994 FK506 or rapamycin, inhibitors of FKBP12 isomerase activity, reverse these stabilizing effects. Tacrolimus 0-5 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 34-40 7514263-2 1994 The macrolides FK506 and FK520 stimulate the Pgp-ATPase activity with affinities in the 100 nM range, nearly 10 times higher than that of verapamil, a well known Pgp substrate. Tacrolimus 15-20 ATP binding cassette subfamily B member 1 Homo sapiens 45-48 7514263-2 1994 The macrolides FK506 and FK520 stimulate the Pgp-ATPase activity with affinities in the 100 nM range, nearly 10 times higher than that of verapamil, a well known Pgp substrate. Tacrolimus 15-20 dynein axonemal heavy chain 8 Homo sapiens 49-55 7514263-2 1994 The macrolides FK506 and FK520 stimulate the Pgp-ATPase activity with affinities in the 100 nM range, nearly 10 times higher than that of verapamil, a well known Pgp substrate. Tacrolimus 15-20 ATP binding cassette subfamily B member 1 Homo sapiens 162-165 7518966-2 1994 Nonspecific inhibitors of cytochrome P-450, such as ketoconazole, itraconazole, fluconazole and SKF 525 A, and most of the cytochrome P-450 IIIA specific substrates used in this study significantly inhibited FK 506 metabolism. Tacrolimus 208-214 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 26-42 7518966-2 1994 Nonspecific inhibitors of cytochrome P-450, such as ketoconazole, itraconazole, fluconazole and SKF 525 A, and most of the cytochrome P-450 IIIA specific substrates used in this study significantly inhibited FK 506 metabolism. Tacrolimus 208-214 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 123-139 7518966-4 1994 Cytochrome P-450 II substrates had minimal but significant effect on FK 506 metabolism. Tacrolimus 69-75 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 0-16 7518966-5 1994 This data supports our earlier observations that FK 506 metabolism is mediated predominantly by the steroid inducible cytochrome P-450 IIIA enzyme subfamily. Tacrolimus 49-55 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 118-134 7518966-6 1994 The results of this study indicate that in transplant patients there is a potential for an interaction of FK 506 with other drugs that are metabolized by the cytochrome P-450 IIIA subfamily or those that alter the activity of cytochrome P-450 IIIA subfamily. Tacrolimus 106-112 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 158-174 7518966-6 1994 The results of this study indicate that in transplant patients there is a potential for an interaction of FK 506 with other drugs that are metabolized by the cytochrome P-450 IIIA subfamily or those that alter the activity of cytochrome P-450 IIIA subfamily. Tacrolimus 106-112 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 226-242 7510691-0 1994 The interleukin-8 AP-1 and kappa B-like sites are genetic end targets of FK506-sensitive pathway accompanied by calcium mobilization. Tacrolimus 73-78 C-X-C motif chemokine ligand 8 Homo sapiens 4-17 7510691-2 1994 We observed that FK506 suppressed the transcription of a chemotactic cytokine, interleukin-8 (IL-8) in a human T cell line, Jurkat cells, activated by phorbol 12-myristate 13-acetate (PMA) and calcium (Ca2+) ionophore (ionomycin). Tacrolimus 17-22 C-X-C motif chemokine ligand 8 Homo sapiens 79-92 7510691-2 1994 We observed that FK506 suppressed the transcription of a chemotactic cytokine, interleukin-8 (IL-8) in a human T cell line, Jurkat cells, activated by phorbol 12-myristate 13-acetate (PMA) and calcium (Ca2+) ionophore (ionomycin). Tacrolimus 17-22 C-X-C motif chemokine ligand 8 Homo sapiens 94-98 7510691-6 1994 In contrast, FK506 or EGTA (Ca2+ chelator) similarly affected the formation of kappa B-like site binding complexes, which were not recognized by any antibodies against the human Rel family proteins (c-Rel, p65, p50, and p49). Tacrolimus 13-18 REL proto-oncogene, NF-kB subunit Homo sapiens 199-204 7510691-6 1994 In contrast, FK506 or EGTA (Ca2+ chelator) similarly affected the formation of kappa B-like site binding complexes, which were not recognized by any antibodies against the human Rel family proteins (c-Rel, p65, p50, and p49). Tacrolimus 13-18 RELA proto-oncogene, NF-kB subunit Homo sapiens 206-209 7510691-6 1994 In contrast, FK506 or EGTA (Ca2+ chelator) similarly affected the formation of kappa B-like site binding complexes, which were not recognized by any antibodies against the human Rel family proteins (c-Rel, p65, p50, and p49). Tacrolimus 13-18 nuclear factor kappa B subunit 1 Homo sapiens 211-214 7510691-6 1994 In contrast, FK506 or EGTA (Ca2+ chelator) similarly affected the formation of kappa B-like site binding complexes, which were not recognized by any antibodies against the human Rel family proteins (c-Rel, p65, p50, and p49). Tacrolimus 13-18 DNA primase subunit 1 Homo sapiens 220-223 7510691-7 1994 Furthermore, we confirmed the previous report that FK506 suppressed the PMA/ionomycin-induced activation through authentic kappa B site of immunoglobulin (Ig) gene, to which NF-kappa B binding was also decreased by FK506, indicating that both IL-8 kappa B-like site and Ig kappa B site are FK506-sensitive in spite of the difference of binding factors. Tacrolimus 51-56 nuclear factor kappa B subunit 1 Homo sapiens 174-184 7510691-7 1994 Furthermore, we confirmed the previous report that FK506 suppressed the PMA/ionomycin-induced activation through authentic kappa B site of immunoglobulin (Ig) gene, to which NF-kappa B binding was also decreased by FK506, indicating that both IL-8 kappa B-like site and Ig kappa B site are FK506-sensitive in spite of the difference of binding factors. Tacrolimus 51-56 C-X-C motif chemokine ligand 8 Homo sapiens 243-247 7510691-7 1994 Furthermore, we confirmed the previous report that FK506 suppressed the PMA/ionomycin-induced activation through authentic kappa B site of immunoglobulin (Ig) gene, to which NF-kappa B binding was also decreased by FK506, indicating that both IL-8 kappa B-like site and Ig kappa B site are FK506-sensitive in spite of the difference of binding factors. Tacrolimus 215-220 nuclear factor kappa B subunit 1 Homo sapiens 174-184 7510691-7 1994 Furthermore, we confirmed the previous report that FK506 suppressed the PMA/ionomycin-induced activation through authentic kappa B site of immunoglobulin (Ig) gene, to which NF-kappa B binding was also decreased by FK506, indicating that both IL-8 kappa B-like site and Ig kappa B site are FK506-sensitive in spite of the difference of binding factors. Tacrolimus 215-220 C-X-C motif chemokine ligand 8 Homo sapiens 243-247 7510691-7 1994 Furthermore, we confirmed the previous report that FK506 suppressed the PMA/ionomycin-induced activation through authentic kappa B site of immunoglobulin (Ig) gene, to which NF-kappa B binding was also decreased by FK506, indicating that both IL-8 kappa B-like site and Ig kappa B site are FK506-sensitive in spite of the difference of binding factors. Tacrolimus 215-220 nuclear factor kappa B subunit 1 Homo sapiens 174-184 7510691-7 1994 Furthermore, we confirmed the previous report that FK506 suppressed the PMA/ionomycin-induced activation through authentic kappa B site of immunoglobulin (Ig) gene, to which NF-kappa B binding was also decreased by FK506, indicating that both IL-8 kappa B-like site and Ig kappa B site are FK506-sensitive in spite of the difference of binding factors. Tacrolimus 215-220 C-X-C motif chemokine ligand 8 Homo sapiens 243-247 7510691-8 1994 Our results indicate that not only the reported IL-2 NF-AT and NFIL-2A sites and Ig kappa B site, but also the IL-8 AP-1 and kappa B-like sites are terminals of FK506-sensitive pathway involving Ca2+ mobilization. Tacrolimus 161-166 C-X-C motif chemokine ligand 8 Homo sapiens 111-115 7511258-0 1994 Anti-CD2 monoclonal antibodies synergize with FK506 but not with cyclosporine or rapamycin to induce tolerance. Tacrolimus 46-51 CD2 molecule Homo sapiens 5-8 7511258-15 1994 This suggests that FK506 acts at a different locus in allograft immunity compared with the other immunosuppressants and this may be related to the alternative CD2 T cell activation pathway. Tacrolimus 19-24 CD2 molecule Homo sapiens 159-162 8137548-10 1994 Treatment with low-dose cyclosporin A (CsA) or FK506 in combination with BRC has proved more effective than either drug alone in suppression of T cell proliferation and CD25 antigen expression. Tacrolimus 47-52 interleukin 2 receptor subunit alpha Homo sapiens 169-173 7521274-5 1994 Both CsA and FK506 (at 1 mumol/L) significantly inhibited nitrite production induced by recombinant murine interleukin-1 beta (rIL-1 beta). Tacrolimus 13-18 interleukin 1 beta Mus musculus 107-125 7521274-5 1994 Both CsA and FK506 (at 1 mumol/L) significantly inhibited nitrite production induced by recombinant murine interleukin-1 beta (rIL-1 beta). Tacrolimus 13-18 interleukin 1 beta Rattus norvegicus 127-137 7510408-2 1994 Changing tyrosine-82 to phenylalanine in FKBP-12 abolishes protein-ligand hydrogen bond interactions in the FKBP-12 complexes with tacrolimus or rapamycin and leads to a large apparent enthalpic stabilization of binding in both H2O and D2O. Tacrolimus 131-141 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 41-48 7510408-2 1994 Changing tyrosine-82 to phenylalanine in FKBP-12 abolishes protein-ligand hydrogen bond interactions in the FKBP-12 complexes with tacrolimus or rapamycin and leads to a large apparent enthalpic stabilization of binding in both H2O and D2O. Tacrolimus 131-141 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 108-115 8112299-3 1994 Calcineurin, a Ca2+/calmodulin-dependent protein phosphatase, is the FK-506- and CsA-sensitive enzyme required for TcR mediated activation of the IL-2 promoter. Tacrolimus 69-75 T cell receptor beta variable 20/OR9-2 (non-functional) Homo sapiens 115-118 8112299-3 1994 Calcineurin, a Ca2+/calmodulin-dependent protein phosphatase, is the FK-506- and CsA-sensitive enzyme required for TcR mediated activation of the IL-2 promoter. Tacrolimus 69-75 interleukin 2 Homo sapiens 146-150 7511990-2 1994 The immunosuppressant drug FK-506 effectively dissociates FKBP-12 from the calcium release channel of terminal cisternae (TC) vesicles. Tacrolimus 27-33 peptidyl-prolyl cis-trans isomerase FKBP1A Oryctolagus cuniculus 58-65 7516291-0 1994 Evidence that FK506 alleviates ischemia/reperfusion injury to the rat liver: in vivo demonstration for suppression of TNF-a production in response to endotoxemia. Tacrolimus 14-19 tumor necrosis factor Rattus norvegicus 118-123 7507493-6 1994 Mutations in calcineurin A or B subunits or the inhibitory compounds FK506 and cyclosporin A restore growth of pmc1 mutants in high Ca2+ media. Tacrolimus 69-74 calcium-transporting ATPase PMC1 Saccharomyces cerevisiae S288C 111-115 7507662-0 1994 Catalytic and ligand binding properties of the FK506 binding protein FKBP12: effects of the single amino acid substitution of Tyr82 to Leu. Tacrolimus 47-52 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 69-75 7507662-1 1994 The binding of FK506 and rapamycin to their cytosolic receptor FKBP12 is an intermediate step in the paths leading to their potent immunosuppressive properties. Tacrolimus 15-20 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 63-69 7887301-4 1994 The activation of calcineurin and the nuclear import of NF-ATc can both be blocked by cyclosporin A or FK506 in complex with their respective immunophilins. Tacrolimus 103-108 nuclear factor of activated T cells 1 Homo sapiens 56-62 7512020-3 1994 CYP3A enzymes are thought to be responsible for metabolizing FK 506 in male rats. Tacrolimus 61-67 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 0-5 7512393-0 1994 Regulation of interleukin-5 production by peripheral blood mononuclear cells from atopic patients with FK506, cyclosporin A and glucocorticoid. Tacrolimus 103-108 interleukin 5 Homo sapiens 14-27 7512393-3 1994 IL-5 induction in vitro was completely inhibited by immunosuppressant FK506, cyclosporin A and dexamethasone. Tacrolimus 70-75 interleukin 5 Homo sapiens 0-4 7512393-4 1994 FK506 applied in vivo effectively suppressed clinical symptoms of atopic dermatitis and IL-5 production of PBMC. Tacrolimus 0-5 interleukin 5 Homo sapiens 88-92 7510997-3 1994 A recombinant p59/HBI-glutathione-S-transferase fusion protein, purified by Sephadex LH-20 filtration of tritiated drug-p59/HBI complexes, binds FK506 and RAP with apparent Kd values of 75 +/- 40 and 40 +/- 15 nM, respectively. Tacrolimus 145-150 FKBP prolyl isomerase 4 Homo sapiens 124-127 7507994-1 1994 The structurally related immunosuppressive macrolides FK-506 and rapamycin (RAP) exert distinct biological effects: inhibition of interleukin-2 production and inhibition of interleukin-2-induced proliferation, respectively, through binding to intracellular receptors, termed FKBPs. Tacrolimus 54-60 interleukin 2 Homo sapiens 130-143 7507994-1 1994 The structurally related immunosuppressive macrolides FK-506 and rapamycin (RAP) exert distinct biological effects: inhibition of interleukin-2 production and inhibition of interleukin-2-induced proliferation, respectively, through binding to intracellular receptors, termed FKBPs. Tacrolimus 54-60 interleukin 2 Homo sapiens 173-186 7510997-9 1994 Purification of cytosol PR on immobilized FK506 yields a 9S form still containing hsp90, hsp70 and p59/HBI associated to PR units. Tacrolimus 42-47 progesterone receptor Homo sapiens 24-26 7510997-9 1994 Purification of cytosol PR on immobilized FK506 yields a 9S form still containing hsp90, hsp70 and p59/HBI associated to PR units. Tacrolimus 42-47 heat shock protein 90 alpha family class A member 1 Homo sapiens 82-87 7510997-9 1994 Purification of cytosol PR on immobilized FK506 yields a 9S form still containing hsp90, hsp70 and p59/HBI associated to PR units. Tacrolimus 42-47 heat shock protein family A (Hsp70) member 4 Homo sapiens 89-94 7510997-9 1994 Purification of cytosol PR on immobilized FK506 yields a 9S form still containing hsp90, hsp70 and p59/HBI associated to PR units. Tacrolimus 42-47 HLA complex P5B Homo sapiens 99-102 7510997-9 1994 Purification of cytosol PR on immobilized FK506 yields a 9S form still containing hsp90, hsp70 and p59/HBI associated to PR units. Tacrolimus 42-47 FKBP prolyl isomerase 4 Homo sapiens 103-106 7510997-9 1994 Purification of cytosol PR on immobilized FK506 yields a 9S form still containing hsp90, hsp70 and p59/HBI associated to PR units. Tacrolimus 42-47 progesterone receptor Homo sapiens 121-123 7538609-3 1994 P-glycoprotein also transports MDR modulators such as cyclosporin A, FK506, and calcium channel blockers. Tacrolimus 69-74 ATP binding cassette subfamily B member 1 Homo sapiens 0-14 7510997-0 1994 Effects of immunosuppressants FK506 and rapamycin on the heterooligomeric form of the progesterone receptor. Tacrolimus 30-35 progesterone receptor Homo sapiens 86-107 7526029-0 1994 Inhibitory effect of FK506 on intercellular adhesion molecule-1 (ICAM-1) expression on cultured thyroid cells. Tacrolimus 21-26 intercellular adhesion molecule 1 Homo sapiens 30-63 7526029-0 1994 Inhibitory effect of FK506 on intercellular adhesion molecule-1 (ICAM-1) expression on cultured thyroid cells. Tacrolimus 21-26 intercellular adhesion molecule 1 Homo sapiens 65-71 7526029-1 1994 The effect of FK506, an immunosuppressive agent, on phytohemagglutinin (PHA) or interferon gamma (IFN gamma)-induced intercellular adhesion molecule-1 (ICAM-1) expression on cultured human thyroid cells from patients with Graves" disease was investigated. Tacrolimus 14-19 intercellular adhesion molecule 1 Homo sapiens 117-150 7526029-1 1994 The effect of FK506, an immunosuppressive agent, on phytohemagglutinin (PHA) or interferon gamma (IFN gamma)-induced intercellular adhesion molecule-1 (ICAM-1) expression on cultured human thyroid cells from patients with Graves" disease was investigated. Tacrolimus 14-19 intercellular adhesion molecule 1 Homo sapiens 152-158 7526029-2 1994 Primary cultured thyroid cells were incubated for three days with IFN gamma (10 to 800 U/ml) or PHA (1 to 50 micrograms/ml) in the presence of FK506. Tacrolimus 143-148 interferon gamma Homo sapiens 66-75 7526029-5 1994 FK506 inhibited the PHA-induced ICAM-1 expression in thyroid cells, but not the induction by IFN gamma. Tacrolimus 0-5 intercellular adhesion molecule 1 Homo sapiens 32-38 7526029-8 1994 This data indicates that the inhibitory effect of FK506 on ICAM-1 expression in primary cultured thyroid cells may be due to actions on infiltrating lymphocytes in the thyroid gland. Tacrolimus 50-55 intercellular adhesion molecule 1 Homo sapiens 59-65 7526029-9 1994 Further studies are necessary to elucidate whether the inhibition of ICAM-1 by FK506 results in the suppression of autoimmune reactions in the thyroid gland. Tacrolimus 79-84 intercellular adhesion molecule 1 Homo sapiens 69-75 7520521-1 1994 An immunosuppressant FK506 binds with a component (hsp 56) of glucocorticoid receptor (GR) complex. Tacrolimus 21-26 nuclear receptor subfamily 3, group C, member 1 Mus musculus 62-85 7520521-1 1994 An immunosuppressant FK506 binds with a component (hsp 56) of glucocorticoid receptor (GR) complex. Tacrolimus 21-26 nuclear receptor subfamily 3, group C, member 1 Mus musculus 87-89 7520521-6 1994 FK506, not cyclosporin A, was demonstrated for the first time in vivo to enhance GR and a hypothesis is proposed that FK506 might enhance GR and AP-1 signalings in a system reciprocally controlled by NO and H2O2. Tacrolimus 0-5 nuclear receptor subfamily 3, group C, member 1 Mus musculus 81-83 7520521-6 1994 FK506, not cyclosporin A, was demonstrated for the first time in vivo to enhance GR and a hypothesis is proposed that FK506 might enhance GR and AP-1 signalings in a system reciprocally controlled by NO and H2O2. Tacrolimus 118-123 nuclear receptor subfamily 3, group C, member 1 Mus musculus 138-140 18475583-1 1994 The effect of FK506 and cyclosporin A (CsA) on the production of interleukin 6 (IL-6) in adherent monocytes was studied at a single-cell level by the avidinbiotin- peroxidase complex methods. Tacrolimus 14-19 interleukin 6 Homo sapiens 65-78 18475583-1 1994 The effect of FK506 and cyclosporin A (CsA) on the production of interleukin 6 (IL-6) in adherent monocytes was studied at a single-cell level by the avidinbiotin- peroxidase complex methods. Tacrolimus 14-19 interleukin 6 Homo sapiens 80-84 18475583-3 1994 Both FK506 and CsA enhanced the percentage of IL-6- producing monocytes stimulated with 100 pg/ml-1 mug/ml of LPS up to values near those obtained with 10 mug/ml of LPS. Tacrolimus 5-10 interleukin 6 Homo sapiens 46-50 18475583-8 1994 Moreover, pretreatment of monocytes with FK506 and CsA had a significant enhancing effect on LPS-induced IL-6 production, while treatment with FK506 or CsA after LPS stimulation had no effects on IL-6 production, suggesting that the enhancing effect of each drug is exerted before LPS stimulation or at an early stage of the post-receptor pathway after LPS stimulation. Tacrolimus 41-46 interleukin 6 Homo sapiens 105-109 18475583-9 1994 These experiments demonstrate that FK506 and CsA can selectively enhance IL-6 production in monocytes under certain conditions in vitro and, possibly, also in vivo. Tacrolimus 35-40 interleukin 6 Homo sapiens 73-77 8186461-2 1994 The expression of GM-CSF and IL-2 is inhibited by immunosuppressive drugs such as cyclosporin A (CsA) and FK506. Tacrolimus 106-111 colony stimulating factor 2 Homo sapiens 18-24 8186461-2 1994 The expression of GM-CSF and IL-2 is inhibited by immunosuppressive drugs such as cyclosporin A (CsA) and FK506. Tacrolimus 106-111 interleukin 2 Homo sapiens 29-33 8302298-11 1994 The immunosuppressive drugs Cyclosporin A and FK506 completely blocked CD28 and CD3 mediated IL-2 production in these transfectants whereas rapamycin had only a partial inhibitory effect. Tacrolimus 46-51 CD28 molecule Homo sapiens 71-75 8302298-11 1994 The immunosuppressive drugs Cyclosporin A and FK506 completely blocked CD28 and CD3 mediated IL-2 production in these transfectants whereas rapamycin had only a partial inhibitory effect. Tacrolimus 46-51 interleukin 2 Homo sapiens 93-97 7529381-0 1994 In-vitro effects of cyclosporin A, FK506, 6-mercaptopurine, and prednisolone on lymphokine-activated killer cells. Tacrolimus 35-40 interleukin 2 Homo sapiens 80-90 7517020-0 1994 FK 506 for vascular permeability factor production in minimal change nephrotic syndrome. Tacrolimus 0-6 vascular endothelial growth factor A Homo sapiens 11-39 7539646-7 1994 In the histological examination, the congestion observed in the periportal region of the control group was mild, while there was less induction of ICAM-1 in the endothelial cells of the portal veins and hepatic veins in the FK506 group. Tacrolimus 224-229 intercellular adhesion molecule 1 Rattus norvegicus 147-153 7521743-3 1994 Continuous daily treatment of syngeneically reconstituted B10 mice with FK506 delayed the development of thymocytes from the CD4+CD8+ to CD4+CD8- stage, while no effect was observed at the earlier CD4-CD8- to CD4+CD8+ stage. Tacrolimus 72-77 granzyme C Mus musculus 58-61 7521743-3 1994 Continuous daily treatment of syngeneically reconstituted B10 mice with FK506 delayed the development of thymocytes from the CD4+CD8+ to CD4+CD8- stage, while no effect was observed at the earlier CD4-CD8- to CD4+CD8+ stage. Tacrolimus 72-77 CD4 antigen Mus musculus 125-128 7521743-3 1994 Continuous daily treatment of syngeneically reconstituted B10 mice with FK506 delayed the development of thymocytes from the CD4+CD8+ to CD4+CD8- stage, while no effect was observed at the earlier CD4-CD8- to CD4+CD8+ stage. Tacrolimus 72-77 CD4 antigen Mus musculus 137-140 7521743-3 1994 Continuous daily treatment of syngeneically reconstituted B10 mice with FK506 delayed the development of thymocytes from the CD4+CD8+ to CD4+CD8- stage, while no effect was observed at the earlier CD4-CD8- to CD4+CD8+ stage. Tacrolimus 72-77 CD4 antigen Mus musculus 137-140 7521743-3 1994 Continuous daily treatment of syngeneically reconstituted B10 mice with FK506 delayed the development of thymocytes from the CD4+CD8+ to CD4+CD8- stage, while no effect was observed at the earlier CD4-CD8- to CD4+CD8+ stage. Tacrolimus 72-77 CD4 antigen Mus musculus 137-140 7521743-7 1994 Levels of expression of V beta 5+ and V beta 11+ T cells in FK506-treated B10.BR-->B10.BR recipients were similar to those observed in unmanipulated, syngeneically reconstituted B10.BR-->B10.BR controls. Tacrolimus 60-65 granzyme C Mus musculus 74-77 7521743-7 1994 Levels of expression of V beta 5+ and V beta 11+ T cells in FK506-treated B10.BR-->B10.BR recipients were similar to those observed in unmanipulated, syngeneically reconstituted B10.BR-->B10.BR controls. Tacrolimus 60-65 granzyme C Mus musculus 86-89 7521743-7 1994 Levels of expression of V beta 5+ and V beta 11+ T cells in FK506-treated B10.BR-->B10.BR recipients were similar to those observed in unmanipulated, syngeneically reconstituted B10.BR-->B10.BR controls. Tacrolimus 60-65 granzyme C Mus musculus 86-89 7521743-7 1994 Levels of expression of V beta 5+ and V beta 11+ T cells in FK506-treated B10.BR-->B10.BR recipients were similar to those observed in unmanipulated, syngeneically reconstituted B10.BR-->B10.BR controls. Tacrolimus 60-65 granzyme C Mus musculus 86-89 7532330-3 1994 However, defects in the maturation of CD4+8+ cells to CD4+8- cells and of TCR alpha beta low MHC class I+ cells to TCR alpha beta high MHC class I+ cells were observed after FK506 administration. Tacrolimus 174-179 Cd4 molecule Rattus norvegicus 38-41 7532330-6 1994 These results suggest that the maturation of CD4-8- TCR alpha beta- MHC class I- cells to CD4+8+ TCR alpha beta low MHC class I+ cells may be FK506 resistant, whereas FK506 may interfere with the maturation of CD4+8+ TCR alpha beta low MHC class I+ thymocytes not only to CD4+8- TCR alpha beta high MHC class I+ cells but also to CD4-8+ TCR alpha beta high MHC class I+ cells. Tacrolimus 142-147 Cd4 molecule Rattus norvegicus 45-48 7532330-6 1994 These results suggest that the maturation of CD4-8- TCR alpha beta- MHC class I- cells to CD4+8+ TCR alpha beta low MHC class I+ cells may be FK506 resistant, whereas FK506 may interfere with the maturation of CD4+8+ TCR alpha beta low MHC class I+ thymocytes not only to CD4+8- TCR alpha beta high MHC class I+ cells but also to CD4-8+ TCR alpha beta high MHC class I+ cells. Tacrolimus 142-147 Cd4 molecule Rattus norvegicus 90-93 7532330-6 1994 These results suggest that the maturation of CD4-8- TCR alpha beta- MHC class I- cells to CD4+8+ TCR alpha beta low MHC class I+ cells may be FK506 resistant, whereas FK506 may interfere with the maturation of CD4+8+ TCR alpha beta low MHC class I+ thymocytes not only to CD4+8- TCR alpha beta high MHC class I+ cells but also to CD4-8+ TCR alpha beta high MHC class I+ cells. Tacrolimus 142-147 Cd4 molecule Rattus norvegicus 90-93 7532330-6 1994 These results suggest that the maturation of CD4-8- TCR alpha beta- MHC class I- cells to CD4+8+ TCR alpha beta low MHC class I+ cells may be FK506 resistant, whereas FK506 may interfere with the maturation of CD4+8+ TCR alpha beta low MHC class I+ thymocytes not only to CD4+8- TCR alpha beta high MHC class I+ cells but also to CD4-8+ TCR alpha beta high MHC class I+ cells. Tacrolimus 142-147 Cd4 molecule Rattus norvegicus 90-93 7532330-6 1994 These results suggest that the maturation of CD4-8- TCR alpha beta- MHC class I- cells to CD4+8+ TCR alpha beta low MHC class I+ cells may be FK506 resistant, whereas FK506 may interfere with the maturation of CD4+8+ TCR alpha beta low MHC class I+ thymocytes not only to CD4+8- TCR alpha beta high MHC class I+ cells but also to CD4-8+ TCR alpha beta high MHC class I+ cells. Tacrolimus 142-147 Cd48 molecule Rattus norvegicus 45-50 7532330-6 1994 These results suggest that the maturation of CD4-8- TCR alpha beta- MHC class I- cells to CD4+8+ TCR alpha beta low MHC class I+ cells may be FK506 resistant, whereas FK506 may interfere with the maturation of CD4+8+ TCR alpha beta low MHC class I+ thymocytes not only to CD4+8- TCR alpha beta high MHC class I+ cells but also to CD4-8+ TCR alpha beta high MHC class I+ cells. Tacrolimus 167-172 Cd4 molecule Rattus norvegicus 45-48 7532330-6 1994 These results suggest that the maturation of CD4-8- TCR alpha beta- MHC class I- cells to CD4+8+ TCR alpha beta low MHC class I+ cells may be FK506 resistant, whereas FK506 may interfere with the maturation of CD4+8+ TCR alpha beta low MHC class I+ thymocytes not only to CD4+8- TCR alpha beta high MHC class I+ cells but also to CD4-8+ TCR alpha beta high MHC class I+ cells. Tacrolimus 167-172 Cd4 molecule Rattus norvegicus 90-93 7532330-6 1994 These results suggest that the maturation of CD4-8- TCR alpha beta- MHC class I- cells to CD4+8+ TCR alpha beta low MHC class I+ cells may be FK506 resistant, whereas FK506 may interfere with the maturation of CD4+8+ TCR alpha beta low MHC class I+ thymocytes not only to CD4+8- TCR alpha beta high MHC class I+ cells but also to CD4-8+ TCR alpha beta high MHC class I+ cells. Tacrolimus 167-172 Cd4 molecule Rattus norvegicus 90-93 7532330-6 1994 These results suggest that the maturation of CD4-8- TCR alpha beta- MHC class I- cells to CD4+8+ TCR alpha beta low MHC class I+ cells may be FK506 resistant, whereas FK506 may interfere with the maturation of CD4+8+ TCR alpha beta low MHC class I+ thymocytes not only to CD4+8- TCR alpha beta high MHC class I+ cells but also to CD4-8+ TCR alpha beta high MHC class I+ cells. Tacrolimus 167-172 Cd4 molecule Rattus norvegicus 90-93 7532330-6 1994 These results suggest that the maturation of CD4-8- TCR alpha beta- MHC class I- cells to CD4+8+ TCR alpha beta low MHC class I+ cells may be FK506 resistant, whereas FK506 may interfere with the maturation of CD4+8+ TCR alpha beta low MHC class I+ thymocytes not only to CD4+8- TCR alpha beta high MHC class I+ cells but also to CD4-8+ TCR alpha beta high MHC class I+ cells. Tacrolimus 167-172 Cd48 molecule Rattus norvegicus 45-50 11271304-0 1994 FK 506 and cyclosporin each block antigen-induced T cell receptor signalling that is dependent on CD4 co-receptor and operates in the absence of detectable cytoplasmic calcium fluxes. Tacrolimus 0-6 CD4 molecule Homo sapiens 98-101 11271304-3 1994 Using 171, 171-CD4 (wild-type) and 171-CD4 (mutant), we found that IL-2 secretion was inhibited by FK 506 and cyclosporin but not by rapamycin. Tacrolimus 99-105 CD4 molecule Homo sapiens 15-18 11271304-3 1994 Using 171, 171-CD4 (wild-type) and 171-CD4 (mutant), we found that IL-2 secretion was inhibited by FK 506 and cyclosporin but not by rapamycin. Tacrolimus 99-105 CD4 molecule Homo sapiens 39-42 11271304-3 1994 Using 171, 171-CD4 (wild-type) and 171-CD4 (mutant), we found that IL-2 secretion was inhibited by FK 506 and cyclosporin but not by rapamycin. Tacrolimus 99-105 interleukin 2 Homo sapiens 67-71 11271304-5 1994 Thus, although FK 506 and cyclosporin inhibited calcium-dependent signalling to the IL-2 promoter via inhibition of the protein phosphatase calcineurin, it is possible that IL-2 induction via TCR/CD4 requires an FK 506 (and cyclosporin) sensitive step which is independent of cytoplasmic calcium changes. Tacrolimus 15-21 interleukin 2 Homo sapiens 84-88 11271305-0 1994 Effect of immunosuppressive agents FK 506 and cyclosporin and steroids on the expression of IL-6 and its receptor by stimulated lymphocytes and monocytes. Tacrolimus 35-41 interleukin 6 Homo sapiens 92-96 11271305-5 1994 Dexamethazone, cyclosporin (CyA), and FK 506 at immunosuppressive concentrations induced a dose-dependent inhibition of IL-6 secretion from adherent monocytes (MO) stimulated with phytohemagglutinin (PHA). Tacrolimus 38-44 interleukin 6 Homo sapiens 120-124 11271305-9 1994 Treatment of PHA-stimulated adherent MO with different concentrations of CyA and FK 506 induced a restoration of IL-6R expression. Tacrolimus 81-87 interleukin 6 receptor Homo sapiens 113-118 11271305-10 1994 FK 506 was 100 time more effective in restoring IL-6R than CyA. Tacrolimus 0-6 interleukin 6 receptor Homo sapiens 48-53 11271305-12 1994 FK 506, CyA, and steroids may exert their immunosuppressive effect by inhibiting IL-6 secretion and partially restoring MO IL-6R, which may be important in protecting the cell target against IL-6 autocrine stimulation. Tacrolimus 0-6 interleukin 6 Homo sapiens 81-85 11271305-12 1994 FK 506, CyA, and steroids may exert their immunosuppressive effect by inhibiting IL-6 secretion and partially restoring MO IL-6R, which may be important in protecting the cell target against IL-6 autocrine stimulation. Tacrolimus 0-6 interleukin 6 receptor Homo sapiens 123-128 11271305-12 1994 FK 506, CyA, and steroids may exert their immunosuppressive effect by inhibiting IL-6 secretion and partially restoring MO IL-6R, which may be important in protecting the cell target against IL-6 autocrine stimulation. Tacrolimus 0-6 interleukin 6 Homo sapiens 123-127 7505578-6 1993 This protochordate protein is substantially similar to 12-13 kDa FKBPs, most remarkably to one of the receptors that had been proposed to mediate the immunosuppressive actions of FK506, the human FKBP-13 (62% amino acid identity and 74% similarity). Tacrolimus 179-184 FKBP prolyl isomerase 2 Homo sapiens 196-203 7509103-1 1993 We investigated the effects of FK506, a novel immunosuppressive agent, on the phytohemagglutinin (PHA) or interferon-gamma (IFN-gamma)-induced expression of HLA-DR antigen, accessory cell function and proliferation of primary cultured human thyroid cells. Tacrolimus 31-36 interferon gamma Homo sapiens 106-133 7522118-0 1993 Immunological identification of a 50 kDa Mr FK506-binding immunophilin as a component of the non-DNA binding, hsp90 and hsp70 containing, heterooligomeric form of the chick oviduct progesterone receptor. Tacrolimus 44-49 heat shock protein family A (Hsp70) member 2 Gallus gallus 120-125 7522118-2 1993 P59/HBI belongs to the FKBP family since it binds the immunosuppressants FK506 and Rapamycin. Tacrolimus 73-78 peptidyl-prolyl cis-trans isomerase FKBP4 Oryctolagus cuniculus 0-3 7522118-2 1993 P59/HBI belongs to the FKBP family since it binds the immunosuppressants FK506 and Rapamycin. Tacrolimus 73-78 peptidyl-prolyl cis-trans isomerase FKBP4 Oryctolagus cuniculus 4-7 7522118-5 1993 Following incubation of this FK506-affinity purified 9S-PR with BF4, a specific anti-chick hsp90 monoclonal antibody, a shift of the [3H]Org 2058-PR complexes from 9S to 11S has been observed, indicating the presence of hsp90, hsp70 also is included in the 9S-PR complexes as demonstrated by Western blotting and density gradient experiments. Tacrolimus 29-34 heat shock protein family A (Hsp70) member 2 Gallus gallus 227-232 7510323-1 1993 The immunosuppressants FK506 and cyclosporin A (CsA) bound to their receptors, FKBP12 or cyclophilin, inhibit the Ca2+/calmodulin-dependent protein phosphatase, calcineurin, preventing T cell activation or, in yeast, recovery from alpha-mating factor arrest. Tacrolimus 23-28 peptidylprolyl isomerase FPR1 Saccharomyces cerevisiae S288C 79-85 7510323-7 1993 Overexpression of CNA1 or CNA2, in conjunction with CNB1, results in a significant decrease in hypersensitivity to FK506 and CsA. Tacrolimus 115-120 calcineurin catalytic subunit A Saccharomyces cerevisiae S288C 18-22 7510323-7 1993 Overexpression of CNA1 or CNA2, in conjunction with CNB1, results in a significant decrease in hypersensitivity to FK506 and CsA. Tacrolimus 115-120 calcineurin catalytic subunit A Saccharomyces cerevisiae S288C 26-30 7510323-7 1993 Overexpression of CNA1 or CNA2, in conjunction with CNB1, results in a significant decrease in hypersensitivity to FK506 and CsA. Tacrolimus 115-120 calcineurin regulatory subunit B Saccharomyces cerevisiae S288C 52-56 7506454-3 1993 In the present study, we have compared the effects of CsA and FK506 on glucose-stimulated insulin release from the isolated dog pancreatic islets, which have been maintained in culture for 3 days after isolation. Tacrolimus 62-67 insulin Homo sapiens 90-97 7510077-1 1993 The major immunophilins that bind cyclosporine (cyclophilin) and FK-506/rapamycin (FK-BP 12) have been well characterized. Tacrolimus 65-71 FKBP prolyl isomerase 1A Homo sapiens 83-91 7510997-3 1994 A recombinant p59/HBI-glutathione-S-transferase fusion protein, purified by Sephadex LH-20 filtration of tritiated drug-p59/HBI complexes, binds FK506 and RAP with apparent Kd values of 75 +/- 40 and 40 +/- 15 nM, respectively. Tacrolimus 145-150 HLA complex P5B Homo sapiens 14-17 7510997-3 1994 A recombinant p59/HBI-glutathione-S-transferase fusion protein, purified by Sephadex LH-20 filtration of tritiated drug-p59/HBI complexes, binds FK506 and RAP with apparent Kd values of 75 +/- 40 and 40 +/- 15 nM, respectively. Tacrolimus 145-150 peptidyl-prolyl cis-trans isomerase FKBP4 Oryctolagus cuniculus 18-21 7510997-3 1994 A recombinant p59/HBI-glutathione-S-transferase fusion protein, purified by Sephadex LH-20 filtration of tritiated drug-p59/HBI complexes, binds FK506 and RAP with apparent Kd values of 75 +/- 40 and 40 +/- 15 nM, respectively. Tacrolimus 145-150 HLA complex P5B Homo sapiens 120-123 7510997-6 1994 In contrast 30 to 50% of the original 9S-PR species containing hsps and p59/HBI, was eluted in the absence of tungstate ions but after exposure of cytosol to 5 microM FK506 or RAP. Tacrolimus 167-172 progesterone receptor Homo sapiens 41-43 7504525-0 1993 An active FK506-binding domain of 17,000 daltons is isolated following limited proteolysis of chicken thymus hsp56. Tacrolimus 10-15 FKBP prolyl isomerase 4 Homo sapiens 109-114 7504525-5 1993 We now report that hsp56 is also found to be a major immunophilin in chicken thymus, by virtue of binding to FK506-Affi-Gel-10 as well as positive cross-reactivity with a polyclonal antiserum directed against human hsp56. Tacrolimus 109-114 FKBP prolyl isomerase 4 Homo sapiens 19-24 7504525-7 1993 Peptide mapping provided additional proof that p17 is a fragment which comprises the entire FK506 binding domain I of chicken hsp56, terminating with an Arg-Lys which might represent a processing site. Tacrolimus 92-97 FKBP prolyl isomerase 4 Homo sapiens 126-131 7504525-11 1993 This work demonstrates the excision of a domain from an hsp56 protein that is active in binding FK506 and functionally distinct from FKBP-12, a protein of similar size and structure. Tacrolimus 96-101 FKBP prolyl isomerase 4 Homo sapiens 56-61 8251509-0 1993 Mechanism for the rotamase activity of FK506 binding protein from molecular dynamics simulations. Tacrolimus 39-44 FKBP prolyl isomerase 10 Homo sapiens 18-26 8397339-2 1993 NFAT, a DNA-binding protein required for interleukin-2 gene transcription, is a potential target for calcineurin, cyclosporin A and FK506. Tacrolimus 132-137 nuclear factor of activated T cells 2 Homo sapiens 0-4 7693698-4 1993 Both p50 and p54 bind an FK506 affinity resin at 0.5 M KCl, but only p50 binds efficiently in low salt conditions. Tacrolimus 25-30 nuclear factor kappa B subunit 1 Homo sapiens 5-8 7693698-4 1993 Both p50 and p54 bind an FK506 affinity resin at 0.5 M KCl, but only p50 binds efficiently in low salt conditions. Tacrolimus 25-30 FKBP prolyl isomerase 5 Homo sapiens 13-16 7693698-6 1993 The poor retention of p54 on FK506 resin at low ionic strength compared with the high retention of p50 suggests that these proteins may largely exist in separate complexes and may interact with other proteins, such as progesterone receptor, in distinctive manners. Tacrolimus 29-34 FKBP prolyl isomerase 5 Homo sapiens 22-25 7693684-3 1993 CsA and FK506 inhibited depolarization-induced glucagon gene transcription, FK506 being more potent than CsA. Tacrolimus 76-81 ERCC excision repair 8, CSA ubiquitin ligase complex subunit Homo sapiens 0-3 7693684-4 1993 CsA/FK506 responsiveness was mediated by the glucagon CRE and also by well characterized CREs of the choriogonadotropin and somatostatin genes. Tacrolimus 4-9 ERCC excision repair 8, CSA ubiquitin ligase complex subunit Homo sapiens 0-3 7693684-5 1993 Rapamycin antagonized the inhibitory effect of FK506 but not CsA, suggesting that FK506 and CsA may act through complex formation with distinct intracellular immunophilins. Tacrolimus 47-52 ERCC excision repair 8, CSA ubiquitin ligase complex subunit Homo sapiens 92-95 7693684-7 1993 These results demonstrate an inhibition by CsA and FK506 of CRE-mediated, calcium-induced transcription and suggest that membrane depolarization relies on calcineurin phosphatase activity for activation of CREB/CRE-mediated gene transcription. Tacrolimus 51-56 cAMP responsive element binding protein 1 Homo sapiens 206-210 7693684-8 1993 The interference with CRE-mediated gene transcription represents a novel mechanism of CsA/FK506 action, which may underlie pharmacological effects and toxic manifestations of these potent immunosuppressive drugs. Tacrolimus 90-95 ERCC excision repair 8, CSA ubiquitin ligase complex subunit Homo sapiens 86-89 7693482-3 1993 Furthermore, other immunosuppressive agents FK506 and dexamethasone inhibit E-selectin expression, indicating that the enhancement observed in the presence of Cys A is not a consequence of general immunosuppression. Tacrolimus 44-49 selectin E Homo sapiens 76-86 7507077-1 1993 We have isolated a unique gene from a mouse JB6 epidermal cell cDNA expression library, termed FKBPRP, that codes for a protein having domains that share between 37 and 44% amino acid sequence identity and 60% similarity with members of the family of FK506-binding proteins. Tacrolimus 251-256 FK506 binding protein 10 Mus musculus 95-101 7509460-8 1993 These results support the notion that the interaction of drug-immunophilin complexes with calcineurin may be the molecular basis of cyclosporin A/FK506-induced inhibition of CREB/CRE-mediated gene transcription. Tacrolimus 146-151 cAMP responsive element binding protein 1 Rattus norvegicus 174-178 7509460-9 1993 The ability to interfere with CREB/CRE-mediated gene transcription represents a novel mechanism of cyclosporin A/FK506 action which may underlie pharmacological effects and toxic manifestations of these potent immunuosuppressive drugs. Tacrolimus 113-118 cAMP responsive element binding protein 1 Rattus norvegicus 30-34 8235597-2 1993 The DNA-binding specificity of NFAT is conferred by NFATp, a phosphoprotein that is a target for the immunosuppressive compounds cyclosporin A and FK506. Tacrolimus 147-152 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 2 Mus musculus 31-35 8235597-2 1993 The DNA-binding specificity of NFAT is conferred by NFATp, a phosphoprotein that is a target for the immunosuppressive compounds cyclosporin A and FK506. Tacrolimus 147-152 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 2 Mus musculus 52-57 7691614-6 1993 Induction of apoptosis by anti-CD2 mAb was prevented by cyclosporine A and FK 506. Tacrolimus 75-81 CD2 molecule Homo sapiens 31-34 7692637-12 1993 In conclusion, the need for insulin with FK-506 compares favorably to that of previous immunosuppressive regimens, and FK-506 may have a reversible diabetogenic effect that is not dose dependent. Tacrolimus 41-47 insulin Homo sapiens 28-35 7692640-2 1993 FK-506 is known to suppress the transcription of several genes encoding cytokines (e.g., IL-2, IFN-gamma) thought to play an important role in the allograft response. Tacrolimus 0-6 interleukin 2 Mus musculus 89-93 7692640-2 1993 FK-506 is known to suppress the transcription of several genes encoding cytokines (e.g., IL-2, IFN-gamma) thought to play an important role in the allograft response. Tacrolimus 0-6 interferon gamma Mus musculus 95-104 7692640-5 1993 Supernatants from Th2 cells treated with FK-506 showed marked suppression of IL-4 but only moderate suppression of IL-10 levels. Tacrolimus 41-47 interleukin 4 Mus musculus 77-81 7692640-5 1993 Supernatants from Th2 cells treated with FK-506 showed marked suppression of IL-4 but only moderate suppression of IL-10 levels. Tacrolimus 41-47 interleukin 10 Mus musculus 115-120 7692640-8 1993 Similar to results at the protein level, FK-506 suppressed steady state levels of IL-4 mRNA markedly but had a lesser effect on steady state levels of IL-10 mRNA. Tacrolimus 41-47 interleukin 4 Mus musculus 82-86 7692640-8 1993 Similar to results at the protein level, FK-506 suppressed steady state levels of IL-4 mRNA markedly but had a lesser effect on steady state levels of IL-10 mRNA. Tacrolimus 41-47 interleukin 10 Mus musculus 151-156 7692640-9 1993 Furthermore, FK-506 completely abrogated Con A-induced upregulation of IL-4 mRNA, but only slightly suppressed Con A-induced upregulation of IL-10 mRNA. Tacrolimus 13-19 interleukin 4 Mus musculus 71-75 7692640-9 1993 Furthermore, FK-506 completely abrogated Con A-induced upregulation of IL-4 mRNA, but only slightly suppressed Con A-induced upregulation of IL-10 mRNA. Tacrolimus 13-19 interleukin 10 Mus musculus 141-146 7692640-12 1993 Therefore, the ability of FK-506 to differentially suppress the mRNA levels of immunostimulatory cytokines such as IL-2, IL-4, and IFN-gamma more than the mRNA levels of the immunosuppressive cytokine IL-10 suggests that the effective immunosuppression seen in vivo with FK-506 may be a combination of these 2 effects. Tacrolimus 26-32 interleukin 2 Mus musculus 115-119 7692640-12 1993 Therefore, the ability of FK-506 to differentially suppress the mRNA levels of immunostimulatory cytokines such as IL-2, IL-4, and IFN-gamma more than the mRNA levels of the immunosuppressive cytokine IL-10 suggests that the effective immunosuppression seen in vivo with FK-506 may be a combination of these 2 effects. Tacrolimus 26-32 interleukin 4 Mus musculus 121-125 7692640-12 1993 Therefore, the ability of FK-506 to differentially suppress the mRNA levels of immunostimulatory cytokines such as IL-2, IL-4, and IFN-gamma more than the mRNA levels of the immunosuppressive cytokine IL-10 suggests that the effective immunosuppression seen in vivo with FK-506 may be a combination of these 2 effects. Tacrolimus 26-32 interferon gamma Mus musculus 131-140 7692640-12 1993 Therefore, the ability of FK-506 to differentially suppress the mRNA levels of immunostimulatory cytokines such as IL-2, IL-4, and IFN-gamma more than the mRNA levels of the immunosuppressive cytokine IL-10 suggests that the effective immunosuppression seen in vivo with FK-506 may be a combination of these 2 effects. Tacrolimus 26-32 interleukin 10 Mus musculus 201-206 7507316-4 1993 In contrast, rapamycin, a structural analogue of FK 506, interferes with the immune response at a different level, by blocking the response induced by cytokines such as IL-2. Tacrolimus 49-55 interleukin 2 Homo sapiens 169-173 7507316-6 1993 For instance, CsA and FK 506 inhibit the transcription of IL-3, IL-4, IFN gamma, TNF alpha or GM-CSF by activated T cells, and rapamycin has been shown to block the response to various growth factors such as IL-3, IL-4 or IL-6. Tacrolimus 22-28 interleukin 3 Homo sapiens 58-62 7507316-6 1993 For instance, CsA and FK 506 inhibit the transcription of IL-3, IL-4, IFN gamma, TNF alpha or GM-CSF by activated T cells, and rapamycin has been shown to block the response to various growth factors such as IL-3, IL-4 or IL-6. Tacrolimus 22-28 interleukin 4 Homo sapiens 64-68 7507316-6 1993 For instance, CsA and FK 506 inhibit the transcription of IL-3, IL-4, IFN gamma, TNF alpha or GM-CSF by activated T cells, and rapamycin has been shown to block the response to various growth factors such as IL-3, IL-4 or IL-6. Tacrolimus 22-28 interferon gamma Homo sapiens 70-79 7507316-6 1993 For instance, CsA and FK 506 inhibit the transcription of IL-3, IL-4, IFN gamma, TNF alpha or GM-CSF by activated T cells, and rapamycin has been shown to block the response to various growth factors such as IL-3, IL-4 or IL-6. Tacrolimus 22-28 tumor necrosis factor Homo sapiens 81-90 7507316-6 1993 For instance, CsA and FK 506 inhibit the transcription of IL-3, IL-4, IFN gamma, TNF alpha or GM-CSF by activated T cells, and rapamycin has been shown to block the response to various growth factors such as IL-3, IL-4 or IL-6. Tacrolimus 22-28 colony stimulating factor 2 Homo sapiens 94-100 7507316-6 1993 For instance, CsA and FK 506 inhibit the transcription of IL-3, IL-4, IFN gamma, TNF alpha or GM-CSF by activated T cells, and rapamycin has been shown to block the response to various growth factors such as IL-3, IL-4 or IL-6. Tacrolimus 22-28 interleukin 3 Homo sapiens 208-212 7507316-6 1993 For instance, CsA and FK 506 inhibit the transcription of IL-3, IL-4, IFN gamma, TNF alpha or GM-CSF by activated T cells, and rapamycin has been shown to block the response to various growth factors such as IL-3, IL-4 or IL-6. Tacrolimus 22-28 interleukin 4 Homo sapiens 214-218 7507316-6 1993 For instance, CsA and FK 506 inhibit the transcription of IL-3, IL-4, IFN gamma, TNF alpha or GM-CSF by activated T cells, and rapamycin has been shown to block the response to various growth factors such as IL-3, IL-4 or IL-6. Tacrolimus 22-28 interleukin 6 Homo sapiens 222-226 8373400-3 1993 It binds the immunosuppressants FK506 and rapamycin and possesses three FKBP-12 (FK506 binding protein of M(r) 12,000)--like domains (I to III), plus a tail containing a putative calmodulin binding site (domain IV). Tacrolimus 32-37 calmodulin 1 Homo sapiens 179-189 8397339-2 1993 NFAT, a DNA-binding protein required for interleukin-2 gene transcription, is a potential target for calcineurin, cyclosporin A and FK506. Tacrolimus 132-137 interleukin 2 Homo sapiens 41-54 7690248-1 1993 Backbone dynamics of the major tacrolimus (FK506) binding protein (FKBP-12, 107 amino acids) have been studied using 15N relaxation data derived from proton-detected two-dimensional 1H-15N NMR spectroscopy. Tacrolimus 31-41 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 67-74 7690248-1 1993 Backbone dynamics of the major tacrolimus (FK506) binding protein (FKBP-12, 107 amino acids) have been studied using 15N relaxation data derived from proton-detected two-dimensional 1H-15N NMR spectroscopy. Tacrolimus 43-48 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 67-74 8377379-0 1993 CsA, FK506, corticosteroids and rapamycin inhibit TNF alpha production by cultured PTEC. Tacrolimus 5-10 tumor necrosis factor Homo sapiens 50-59 7690315-8 1993 FK506 was found to inhibit the synthesis of IL3 and GM-CSF, whereas rapamycin failed to suppress the cytokine production of eosinophils. Tacrolimus 0-5 interleukin 3 Homo sapiens 44-47 7690315-8 1993 FK506 was found to inhibit the synthesis of IL3 and GM-CSF, whereas rapamycin failed to suppress the cytokine production of eosinophils. Tacrolimus 0-5 colony stimulating factor 2 Homo sapiens 52-58 7689858-2 1993 Recently, we showed that p59 purified from human lymphocytes is an immunophilin (FKBP59) which binds both FK506 and rapamycin. Tacrolimus 106-111 HLA complex P5B Homo sapiens 25-28 7689858-2 1993 Recently, we showed that p59 purified from human lymphocytes is an immunophilin (FKBP59) which binds both FK506 and rapamycin. Tacrolimus 106-111 FKBP prolyl isomerase 4 Homo sapiens 81-87 7689858-4 1993 Here we provide evidence that rabbit uterine p59 also binds FK506 and rapamycin and that p59 or its homologue is associated with nontransformed progesterone receptors of rabbit uterus and chicken oviduct. Tacrolimus 60-65 peptidyl-prolyl cis-trans isomerase FKBP4 Oryctolagus cuniculus 45-48 7689858-8 1993 The association of p63 to the p59 complex was inhibited by FK506 and rapamycin, suggesting that p63 could be a potential target for the immunosuppressive actions of these two drugs. Tacrolimus 59-64 peptidyl-prolyl cis-trans isomerase FKBP4 Oryctolagus cuniculus 30-33 8377379-6 1993 FK506, corticosteroids and rapamycin also inhibited TNF alpha production in a dose dependent fashion, although not as effectively as CsA. Tacrolimus 0-5 tumor necrosis factor Homo sapiens 52-61 8325502-8 1993 The single immunoblot-positive allele was found to contain a mutation altering a specific residue (Tyr89) which is conserved among the known FKBPs, and which, based on the solution and x-ray structures of human FKBP12, has been proposed to be part of a hydrophobic drug-binding pocket for FK506 and Rm. Tacrolimus 289-294 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 211-217 7687429-9 1993 Both immunosuppressive agents enhanced the calcium-dependent release of adrenocorticotropic hormone into the medium, once more, FK506 was 10-fold more potent than cyclosporin A. Tacrolimus 128-133 pro-opiomelanocortin-alpha Mus musculus 72-99 8335913-2 1993 NF-AT is thought to consist of two components: a ubiquitous, inducible nuclear component that we have identified as Fos and Jun proteins, and a preexisting, T cell-specific component (NF-ATp) which is the target for the immunosuppressive agents cyclosporin A (CsA) and FK506. Tacrolimus 269-274 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 2 Mus musculus 0-5 7680613-2 1993 SEB-activated lamina propria T cells produced interleukin-2 and interferon-gamma and T cell activation was accompanied by tissue damage, which was inhibited by FK506. Tacrolimus 160-165 interferon gamma Homo sapiens 64-80 7687744-3 1993 We found that overexpression of cyclophilin A or B or FKBP12 increased T-cell sensitivity to CsA or FK506, respectively, demonstrating that they are able to mediate the inhibitory effects of their respective immunosuppressants in vivo. Tacrolimus 100-105 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 54-60 7687745-7 1993 Amino acid-auxotrophic yeast strains (trp1 his4 leu2) are FK506 sensitive, whereas prototrophic strains (TRP1 his4 leu2, trp1 HIS4 leu2, and trp1 his4 LEU2) are FK506 resistant. Tacrolimus 58-63 phosphoribosylanthranilate isomerase TRP1 Saccharomyces cerevisiae S288C 38-42 7684925-4 1993 Two largely nonpolar, structurally related macrolide ligands, tacrolimus (also known as FK506) and rapamycin, each bind with high affinity to a common site on a small FK506 binding protein (FKBP-12) and inhibit its peptidylprolyl cis-trans-isomerase activity. Tacrolimus 62-72 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 190-197 7684925-4 1993 Two largely nonpolar, structurally related macrolide ligands, tacrolimus (also known as FK506) and rapamycin, each bind with high affinity to a common site on a small FK506 binding protein (FKBP-12) and inhibit its peptidylprolyl cis-trans-isomerase activity. Tacrolimus 88-93 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 190-197 7685382-6 1993 FK-506-dependent MDA formation, studied only in the rat model, paralleled CyA-induced MDA formation but showed greater inhibition with CAT and less inhibition with SOD or GLUT. Tacrolimus 0-6 catalase Rattus norvegicus 135-138 7683633-3 1993 FK506 and CsA also reduced expression of the proto-oncogenes, c-myc and c-fos, but not c-jun and interleukin-2-receptor-alpha (IL-2R alpha) gene in H109 cells. Tacrolimus 0-5 MYC proto-oncogene, bHLH transcription factor Homo sapiens 62-67 7683633-3 1993 FK506 and CsA also reduced expression of the proto-oncogenes, c-myc and c-fos, but not c-jun and interleukin-2-receptor-alpha (IL-2R alpha) gene in H109 cells. Tacrolimus 0-5 Fos proto-oncogene, AP-1 transcription factor subunit Homo sapiens 72-77 7682438-0 1993 FK506 binding to the 56-kilodalton immunophilin (Hsp56) in the glucocorticoid receptor heterocomplex has no effect on receptor folding or function. Tacrolimus 0-5 nuclear receptor subfamily 3, group C, member 1 Mus musculus 63-86 7682438-1 1993 It has recently been reported that the hsp56 component of glucocorticoid receptor heterocomplexes is an immunophilin of the FK506 binding class [Yem, A. W., Tomasselli, A. G., Heinrikson, R. L., Zurcher-Neely, H., Ruff, V. A., Johnson, R. A., & Deibel, M. R. (1992) J. Biol. Tacrolimus 124-129 nuclear receptor subfamily 3, group C, member 1 Mus musculus 58-81 7683935-0 1993 Reversion of the P-glycoprotein-mediated multidrug resistance of cancer cells by FK-506 derivatives. Tacrolimus 81-87 phosphoglycolate phosphatase Mus musculus 17-31 7683935-1 1993 FK-506 is a resistance-modulating agent (RMA) for tumor cells whose multidrug resistance (MDR) involves a P-glycoprotein (Pgp)-mediated anti-cancer drug efflux. Tacrolimus 0-6 phosphoglycolate phosphatase Mus musculus 106-120 7683935-1 1993 FK-506 is a resistance-modulating agent (RMA) for tumor cells whose multidrug resistance (MDR) involves a P-glycoprotein (Pgp)-mediated anti-cancer drug efflux. Tacrolimus 0-6 phosphoglycolate phosphatase Mus musculus 122-125 7681058-0 1993 Potentiation of glucocorticoid receptor-mediated gene expression by the immunophilin ligands FK506 and rapamycin. Tacrolimus 93-98 nuclear receptor subfamily 3 group C member 1 Homo sapiens 16-39 7681058-2 1993 The ability of hsp56 to bind the immunosuppressive macrolide FK506 has led to the speculation that the steroid receptor and immunophilin signal transduction pathways are functionally interrelated. Tacrolimus 61-66 FKBP prolyl isomerase 4 Homo sapiens 15-20 7681058-3 1993 We have tested this idea by assessing the effects of FK506 on glucocorticoid receptor (GR)-mediated expression of the murine mammary tumor virus-chloramphenicol acetyltransferase (MMTV-CAT) reporter plasmid. Tacrolimus 53-58 nuclear receptor subfamily 3, group C, member 1 Mus musculus 62-85 7681058-3 1993 We have tested this idea by assessing the effects of FK506 on glucocorticoid receptor (GR)-mediated expression of the murine mammary tumor virus-chloramphenicol acetyltransferase (MMTV-CAT) reporter plasmid. Tacrolimus 53-58 nuclear receptor subfamily 3, group C, member 1 Mus musculus 87-89 7681058-7 1993 Finally, we provide evidence that FK506 potentiation of GR-mediated gene expression is the result of increased translocation to the nucleus of the GR. Tacrolimus 34-39 nuclear receptor subfamily 3 group C member 1 Homo sapiens 56-58 7681058-7 1993 Finally, we provide evidence that FK506 potentiation of GR-mediated gene expression is the result of increased translocation to the nucleus of the GR. Tacrolimus 34-39 nuclear receptor subfamily 3 group C member 1 Homo sapiens 147-149 7681059-0 1993 Human P-glycoprotein transports cyclosporin A and FK506. Tacrolimus 50-55 ATP binding cassette subfamily B member 1 Homo sapiens 6-20 7681059-4 1993 We were interested to determine whether cyclosporin A and FK506 are substrates for P-glycoprotein to transport, and we studied their transcellular transport. Tacrolimus 58-63 ATP binding cassette subfamily B member 1 Homo sapiens 83-97 7681059-10 1993 These results indicate that P-glycoprotein transports the immunosuppressive agents cyclosporin A and FK506. Tacrolimus 101-106 ATP binding cassette subfamily B member 1 Homo sapiens 28-42 7680241-4 1993 Liquid-suspension-limiting dilution assay with IL-3 showed that FK506 directly stimulated the growth of blood progenitors in a dose-dependent manner with single-hit kinetics. Tacrolimus 64-69 interleukin 3 Homo sapiens 47-51 7680241-5 1993 Liquid-suspension preincubation of blood cells with FK506 before culture in methylcellulose induced a significant increase in the amount of IL-3-supported growth of CFU-GM and BFU-E, whereas initial preincubation with IL-3 and subsequent culture with FK506 plus IL-3 exerted its stimulatory effect only on BFU-E. Tacrolimus 52-57 interleukin 3 Homo sapiens 140-144 7680241-5 1993 Liquid-suspension preincubation of blood cells with FK506 before culture in methylcellulose induced a significant increase in the amount of IL-3-supported growth of CFU-GM and BFU-E, whereas initial preincubation with IL-3 and subsequent culture with FK506 plus IL-3 exerted its stimulatory effect only on BFU-E. Tacrolimus 52-57 interleukin 3 Homo sapiens 218-222 7680241-5 1993 Liquid-suspension preincubation of blood cells with FK506 before culture in methylcellulose induced a significant increase in the amount of IL-3-supported growth of CFU-GM and BFU-E, whereas initial preincubation with IL-3 and subsequent culture with FK506 plus IL-3 exerted its stimulatory effect only on BFU-E. Tacrolimus 52-57 interleukin 3 Homo sapiens 218-222 7680241-5 1993 Liquid-suspension preincubation of blood cells with FK506 before culture in methylcellulose induced a significant increase in the amount of IL-3-supported growth of CFU-GM and BFU-E, whereas initial preincubation with IL-3 and subsequent culture with FK506 plus IL-3 exerted its stimulatory effect only on BFU-E. Tacrolimus 251-256 interleukin 3 Homo sapiens 140-144 7680293-6 1993 FK 506 administration reduced markedly the incidence of infiltrating TCR alpha/beta +, CD5+, CD4+, CD8+, and LFA-1 beta + cells and the expression both of MHC class II antigens and ICAM-1 on MNC, endothelial cells and thyrocytes. Tacrolimus 0-6 similar to T cell receptor V-alpha J-alpha Rattus norvegicus 69-78 7687745-9 1993 FK506 induces GCN4 expression, which is normally induced by amino acid starvation. Tacrolimus 0-5 amino acid starvation-responsive transcription factor GCN4 Saccharomyces cerevisiae S288C 14-18 7689811-0 1993 FK-506 inhibits the IL-2-independent induction of the activation antigen CD 69. Tacrolimus 0-6 interleukin 2 Homo sapiens 20-24 7689811-0 1993 FK-506 inhibits the IL-2-independent induction of the activation antigen CD 69. Tacrolimus 0-6 CD69 molecule Homo sapiens 73-78 7685932-7 1993 FK506 and CsA-treated animals had better survival and diminished neutrophil liver infiltration, as well as MPO and MDA levels. Tacrolimus 0-5 myeloperoxidase Rattus norvegicus 107-110 7685949-0 1993 Effect of FK 506 and cyclosporine on the expression of IL-6 and its receptor on stimulated monocytes. Tacrolimus 10-16 interleukin 6 Homo sapiens 55-59 7684380-8 1993 In addition, FK-506 complexes with FKBP12 proteins from several species all inhibit mammalian calcineurin. Tacrolimus 13-19 FKBP prolyl isomerase 1A Homo sapiens 35-41 7683633-5 1993 These results suggest that the inhibitory effects of FK506 and CsA are independent of IL-2, and are associated with the reduction of c-myc and c-fos gene expression. Tacrolimus 53-58 MYC proto-oncogene, bHLH transcription factor Homo sapiens 133-138 7683633-5 1993 These results suggest that the inhibitory effects of FK506 and CsA are independent of IL-2, and are associated with the reduction of c-myc and c-fos gene expression. Tacrolimus 53-58 Fos proto-oncogene, AP-1 transcription factor subunit Homo sapiens 143-148 7683267-8 1993 Immunocytochemistry demonstrated that FK506 reduced the expression of interferon-gamma induced major histocompatibility complex (MHC) class I on the proximal tubular cells, but had no effect on the expression of the MHC class II antigens or the intercellular adhesion molecule (ICAM-1) on the cultured cells. Tacrolimus 38-43 interferon gamma Homo sapiens 70-86 7683267-8 1993 Immunocytochemistry demonstrated that FK506 reduced the expression of interferon-gamma induced major histocompatibility complex (MHC) class I on the proximal tubular cells, but had no effect on the expression of the MHC class II antigens or the intercellular adhesion molecule (ICAM-1) on the cultured cells. Tacrolimus 38-43 intercellular adhesion molecule 1 Homo sapiens 278-284 7681074-7 1993 The FK506-binding immunophilin FKBP12, as well as calcineurin, are shown to be present in these cells by immunoblotting analysis. Tacrolimus 4-9 FK506 binding protein 1a Mus musculus 18-37 8475567-6 1993 Cyclosporine and FK506 had similar effects on the frequency of IL-5 gene expression in rejecting and nonrejecting allografts. Tacrolimus 17-22 interleukin 5 Homo sapiens 63-67 7683619-11 1993 Furthermore, the PCNA-labeling index 36 hrs after the partial hepatectomy was enhanced by the administration with FK-506 in the FHF mice. Tacrolimus 114-120 proliferating cell nuclear antigen Mus musculus 17-21 7683641-0 1993 FKBP12-FK506 complex inhibits phosphatase activity of two mammalian isoforms of calcineurin irrespective of their substrates or activation mechanisms. Tacrolimus 7-12 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 0-6 7683641-1 1993 The interaction of calcineurin (Ca2+/calmodulin-dependent protein phosphatase) with the potent immunosuppressive agent FK506 and its 12 kDa isoform binding protein (FKBP12) was investigated. Tacrolimus 119-124 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 165-171 7683641-2 1993 The FKBP12-FK506 complex inhibited the Ca2+/calmodulin-stimulated phosphatase activity of each of two calcineurin isoforms, which contain either the catalytic subunit A alpha or A beta (calcineurin A alpha or A beta) of bovine calcineurin. Tacrolimus 11-16 peptidyl-prolyl cis-trans isomerase FKBP1A Bos taurus 4-10 7683641-3 1993 Calcineurin phosphatase activity was inhibited by the FKBP12-FK506 complex irrespective of the substrate or the enzyme activation mechanism. Tacrolimus 61-66 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 54-60 7683641-4 1993 FK506 and FKBP-12 inhibited calcineurin in a concentration-dependent manner, and complete inhibition of the phosphatase activity appeared to require a molar excess of FKBP12-FK506 complex. Tacrolimus 174-179 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 10-17 7683641-4 1993 FK506 and FKBP-12 inhibited calcineurin in a concentration-dependent manner, and complete inhibition of the phosphatase activity appeared to require a molar excess of FKBP12-FK506 complex. Tacrolimus 174-179 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 167-173 7683641-6 1993 Direct binding studies with [3H]dihydro-FK506 suggest that the ratio of FKBP12-FK506 complex to calcineurin in vivo when IL2 production is inhibited is well correlated with the ratio when calcineurin phosphatase activity is inhibited in vitro. Tacrolimus 40-45 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 72-78 7683641-6 1993 Direct binding studies with [3H]dihydro-FK506 suggest that the ratio of FKBP12-FK506 complex to calcineurin in vivo when IL2 production is inhibited is well correlated with the ratio when calcineurin phosphatase activity is inhibited in vitro. Tacrolimus 40-45 interleukin 2 Homo sapiens 121-124 7683641-7 1993 These results suggest that calcineurin is a relevant cellular target of FK506 when bound to FKBP-12. Tacrolimus 72-77 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 92-99 7686193-0 1993 FK 506 pre-treatment is associated with reduced levels of tumor necrosis factor and interleukin 6 following hepatic ischemia/reperfusion. Tacrolimus 0-6 tumor necrosis factor-like Rattus norvegicus 58-79 7686193-0 1993 FK 506 pre-treatment is associated with reduced levels of tumor necrosis factor and interleukin 6 following hepatic ischemia/reperfusion. Tacrolimus 0-6 interleukin 6 Rattus norvegicus 84-97 7686193-8 1993 Based upon these data, it is probable that FK 506 attenuates hepatic ischemia/reperfusion injury, at least in part, by reducing TNF and IL-6 levels. Tacrolimus 43-49 tumor necrosis factor-like Rattus norvegicus 128-131 7686193-8 1993 Based upon these data, it is probable that FK 506 attenuates hepatic ischemia/reperfusion injury, at least in part, by reducing TNF and IL-6 levels. Tacrolimus 43-49 interleukin 6 Rattus norvegicus 136-140 7679116-6 1993 Moreover, dephosphorylation of NF-ATp in cell extracts is inhibited by prior treatment of T cells with the immunosuppressive drugs cyclosporin A or FK506, which inhibit the phosphatase activity of calcineurin when complexed with their specific binding proteins, cyclophilin and FK506-binding protein. Tacrolimus 148-153 nuclear factor of activated T cells 1 Bos taurus 31-37 7679116-7 1993 This work identifies NF-ATp as a DNA-binding phosphoprotein and a target for the drug/immunophilin/calcineurin complexes thought to mediate the inhibition of interleukin-2 gene induction by cyclosporin A and FK506. Tacrolimus 208-213 nuclear factor of activated T cells 1 Bos taurus 21-27 7679116-7 1993 This work identifies NF-ATp as a DNA-binding phosphoprotein and a target for the drug/immunophilin/calcineurin complexes thought to mediate the inhibition of interleukin-2 gene induction by cyclosporin A and FK506. Tacrolimus 208-213 interleukin 2 Bos taurus 158-171 7682200-0 1993 Regulation of liver regeneration by interleukin-2 and its inhibitors: cyclosporine A and FK 506. Tacrolimus 89-95 interleukin 2 Mus musculus 36-49 7682200-6 1993 On the other hand, treatment with CsA and FK506, which inhibit IL-2 production, increased the mitotic indices of the regenerating livers. Tacrolimus 42-47 interleukin 2 Mus musculus 63-67 7682200-8 1993 Based on these results, CsA and FK506 would appear to stimulate liver cell proliferation by suppressing IL-2 production and inhibiting of NK cell activity. Tacrolimus 32-37 interleukin 2 Mus musculus 104-108 7679839-0 1993 Long-term insulin requirement after liver transplantation with FK 506 in American veterans. Tacrolimus 63-69 insulin Homo sapiens 10-17 7678400-4 1993 It was found that C-18 hydroxyl analogues of ascomycin, an analogue of FK-506 also called FR900520, bound tightly to immunophilin FKBP-12, but do not show any immunosuppressive activity in vitro or in vivo despite good bioavailability. Tacrolimus 71-77 FKBP prolyl isomerase 1A Homo sapiens 117-137 8419347-9 1993 The peptidyl prolyl isomerase hsp59 of the FK506 binding class is known to bind to hsp90. Tacrolimus 43-48 heat shock protein 90 alpha family class A member 1 Rattus norvegicus 83-88 7678431-0 1993 Atomic structures of the human immunophilin FKBP-12 complexes with FK506 and rapamycin. Tacrolimus 67-72 FKBP prolyl isomerase 1A Homo sapiens 31-51 7678431-1 1993 High resolution structures for the complexes formed by the immunosuppressive agents FK506 and rapamycin with the human immunophilin FKBP-12 have been determined by X-ray diffraction. Tacrolimus 84-89 FKBP prolyl isomerase 1A Homo sapiens 119-139 7505632-0 1993 ICAM-1 and E-selectin expression in lesional biopsies of psoriasis patients responding to systemic FK 506 therapy. Tacrolimus 99-105 intercellular adhesion molecule 1 Homo sapiens 0-6 7687472-4 1993 As previously found in other systems, induction of this lymphokine by ionomycin + PMA was not inhibited by RAP, although it was highly sensitive to inhibition by FK-506, an immunosuppressive macrolide structurally related to RAP. Tacrolimus 162-168 peroneal muscular atrophy Mus musculus 82-85 7687472-4 1993 As previously found in other systems, induction of this lymphokine by ionomycin + PMA was not inhibited by RAP, although it was highly sensitive to inhibition by FK-506, an immunosuppressive macrolide structurally related to RAP. Tacrolimus 162-168 regulatory associated protein of MTOR, complex 1 Mus musculus 225-228 7687472-5 1993 In contrast, the induction of the same lymphokine by IL-1 alpha + PMA was highly sensitive to RAP but resistant to FK-506. Tacrolimus 115-121 interleukin 1 alpha Mus musculus 53-63 7687472-5 1993 In contrast, the induction of the same lymphokine by IL-1 alpha + PMA was highly sensitive to RAP but resistant to FK-506. Tacrolimus 115-121 peroneal muscular atrophy Mus musculus 66-69 7687472-9 1993 While the inhibitory action of RAP could not be removed by extensive washing of the cells, it was readily reversed by a hundred-fold excess of FK-506 added to the cultures simultaneously with RAP or up to 16-18 h later. Tacrolimus 143-149 regulatory associated protein of MTOR, complex 1 Mus musculus 31-34 7687472-9 1993 While the inhibitory action of RAP could not be removed by extensive washing of the cells, it was readily reversed by a hundred-fold excess of FK-506 added to the cultures simultaneously with RAP or up to 16-18 h later. Tacrolimus 143-149 regulatory associated protein of MTOR, complex 1 Mus musculus 192-195 7687472-11 1993 The inhibition of lymphokine gene expression by RAP takes place at a late stage of the inductive response, and through a mechanism that involves interaction with the same cellular binding proteins as FK-506. Tacrolimus 200-206 regulatory associated protein of MTOR, complex 1 Mus musculus 48-51 7678228-4 1993 In the present report we describe the effects of three immunosuppressive drugs, cyclosporin A (CsA), FK 506, and mycalamide A on mB7-mediated T cell activation. Tacrolimus 101-107 CD52 antigen Mus musculus 129-132 7678228-5 1993 The immunophilin ligands CsA and FK 506 block activation of murine CD4+ T cells by the combination of anti-CD3 mAb and CHO-mB7 cells but do not affect activation by CHO-mB7 cells and PMA. Tacrolimus 33-39 CD52 antigen Mus musculus 123-126 7678231-0 1993 Inhibition of activation-induced changes in the structure of the T cell interleukin-7 receptor by cyclosporin A and FK506. Tacrolimus 116-121 interleukin 7 receptor Homo sapiens 72-94 7678231-7 1993 In this study, the effect of the potent immunosuppressive agents cyclosporin A and FK506 on the activation-induced responsiveness to IL-7-driven proliferation and the concomitant changes in receptor structure have been investigated. Tacrolimus 83-88 interleukin 7 Homo sapiens 133-137 7678231-14 1993 As reported for IL-2R and IL-4R, our data also show that the expression of another T cell growth factor receptor is sensitive to the effects of cyclosporin A and FK506. Tacrolimus 162-167 interleukin 2 receptor subunit alpha Homo sapiens 16-21 7678231-14 1993 As reported for IL-2R and IL-4R, our data also show that the expression of another T cell growth factor receptor is sensitive to the effects of cyclosporin A and FK506. Tacrolimus 162-167 interleukin 4 receptor Homo sapiens 26-31 7509973-2 1993 This study was undertaken to examine the effect of FK 506 on stimulation of endothelin-1 (ET-1) mRNA and secretion of ET-1 in human endothelial cells (EC) compared with the effects of CyA. Tacrolimus 51-57 endothelin 1 Homo sapiens 76-88 7509973-2 1993 This study was undertaken to examine the effect of FK 506 on stimulation of endothelin-1 (ET-1) mRNA and secretion of ET-1 in human endothelial cells (EC) compared with the effects of CyA. Tacrolimus 51-57 endothelin 1 Homo sapiens 90-94 7509973-2 1993 This study was undertaken to examine the effect of FK 506 on stimulation of endothelin-1 (ET-1) mRNA and secretion of ET-1 in human endothelial cells (EC) compared with the effects of CyA. Tacrolimus 51-57 endothelin 1 Homo sapiens 118-122 22827197-1 1993 In vitro studies of FK506 demonstrated that the agent inhibited the T-cell receptormediated signal transduction that results in the transcription of interleukin 2. Tacrolimus 20-25 interleukin 2 Rattus norvegicus 149-162 7507676-0 1993 Living related liver transplantation across ABO blood groups with FK506 and OKT3. Tacrolimus 66-71 ABO, alpha 1-3-N-acetylgalactosaminyltransferase and alpha 1-3-galactosyltransferase Homo sapiens 44-47 7507676-14 1993 The present results suggest that graft livers from living related donors across ABO blood groups can function well with FK506, low-dose steroids, and prophylactic OKT3 without causing lethal complications. Tacrolimus 120-125 ABO, alpha 1-3-N-acetylgalactosaminyltransferase and alpha 1-3-galactosyltransferase Homo sapiens 80-83 1279700-1 1992 Using an FK506 affinity column to identify mammalian immunosuppressant-binding proteins, we identified an immunophilin with an apparent M(r) approximately 55,000, which we have named FKBP52. Tacrolimus 9-14 FKBP prolyl isomerase 4 Homo sapiens 183-189 1279700-4 1992 Recombinant hFKBP52 has peptidyl-prolyl cis-trans isomerase activity that is inhibited by FK506 and rapamycin and an FKBP12-like consensus sequence that probably defines the immunosuppressant-binding site. Tacrolimus 90-95 FKBP prolyl isomerase 4 Homo sapiens 12-19 7680293-6 1993 FK 506 administration reduced markedly the incidence of infiltrating TCR alpha/beta +, CD5+, CD4+, CD8+, and LFA-1 beta + cells and the expression both of MHC class II antigens and ICAM-1 on MNC, endothelial cells and thyrocytes. Tacrolimus 0-6 Cd5 molecule Rattus norvegicus 87-90 7680293-6 1993 FK 506 administration reduced markedly the incidence of infiltrating TCR alpha/beta +, CD5+, CD4+, CD8+, and LFA-1 beta + cells and the expression both of MHC class II antigens and ICAM-1 on MNC, endothelial cells and thyrocytes. Tacrolimus 0-6 Cd4 molecule Rattus norvegicus 93-96 7680293-6 1993 FK 506 administration reduced markedly the incidence of infiltrating TCR alpha/beta +, CD5+, CD4+, CD8+, and LFA-1 beta + cells and the expression both of MHC class II antigens and ICAM-1 on MNC, endothelial cells and thyrocytes. Tacrolimus 0-6 intercellular adhesion molecule 1 Rattus norvegicus 181-187 7680293-10 1993 The results are consistent with a therapeutic effect of FK 506 mediated via interference with CD4+ T lymphocyte function and adhesion molecule-dependent cytotoxic effector mechanisms. Tacrolimus 56-62 Cd4 molecule Rattus norvegicus 94-97 7678356-0 1993 Inhibition of glucose-stimulated insulin release from beta TC3 cells and rodent islets by an analog of FK506. Tacrolimus 103-108 insulin Homo sapiens 33-40 7678356-4 1993 We have studied the effects of an analog of a newer agent (FK506) termed L-683,590 on insulin secretion by an islet tumor line, beta TC3, and rat islets, and compared the effects of this drug to those of cyclosporine, since both cause similar immunosuppression. Tacrolimus 59-64 insulin Homo sapiens 86-93 7692621-8 1993 The analysis of lymphocyte subsets proved the decrease of W3/25: OX8 ratio in both FK506- and cyclosporin-treated groups. Tacrolimus 83-88 Cd4 molecule Rattus norvegicus 58-63 1282000-3 1992 Using this and immunohistochemical staining, we found that the immunosuppressants cyclosporin A and FK506 decreased CD4 expression in cultured murine microglia without causing any significant decrease in cell viability. Tacrolimus 100-105 CD4 antigen Mus musculus 116-119 1281550-0 1992 Transcription of the tumor necrosis factor alpha gene is rapidly induced by anti-immunoglobulin and blocked by cyclosporin A and FK506 in human B cells. Tacrolimus 129-134 tumor necrosis factor Homo sapiens 21-48 1281550-5 1992 Moreover, induction of TNF-alpha gene transcription by anti-immunoglobulin was blocked by the immunosuppressants cyclosporin A and FK506. Tacrolimus 131-136 tumor necrosis factor Homo sapiens 23-32 1281562-6 1992 The damage induced by FK506 and CsA was characterized by a direct cytotoxic effect on tubular cells, as expressed by release of 3H thymidine from prelabeled cells, N-acetyl-beta-D-glucosaminidase release, and cell detachment. Tacrolimus 22-27 O-GlcNAcase Rattus norvegicus 164-195 1281562-12 1992 The concentrations of FK506 or CsA that induced ET-1 secretion were not cytolytic for tubular cells in vitro. Tacrolimus 22-27 endothelin 1 Rattus norvegicus 48-52 1281562-13 1992 FK506- or CsA-treated rats showed an increase in serum level of ET-1 in comparison with the control. Tacrolimus 0-5 endothelin 1 Rattus norvegicus 64-68 7505632-0 1993 ICAM-1 and E-selectin expression in lesional biopsies of psoriasis patients responding to systemic FK 506 therapy. Tacrolimus 99-105 selectin E Homo sapiens 11-21 7505632-5 1993 In contrast, the number of epidermal CD1+ (Langerhans) cells increased in response to FK 506 therapy. Tacrolimus 86-92 CD1c molecule Homo sapiens 37-40 7505632-8 1993 In response to FK 506 treatment, both ICAM-1 and E-selectin expression on blood vessels was reduced consistently but nevertheless persisted, even in individuals exhibiting total clearance of psoriatic lesions. Tacrolimus 15-21 intercellular adhesion molecule 1 Homo sapiens 38-44 7505632-8 1993 In response to FK 506 treatment, both ICAM-1 and E-selectin expression on blood vessels was reduced consistently but nevertheless persisted, even in individuals exhibiting total clearance of psoriatic lesions. Tacrolimus 15-21 selectin E Homo sapiens 49-59 1383226-2 1992 FK-506 binds to a growing family of receptors termed FK-506-binding proteins (FKBPs), the most abundant being a 12-kDa cytosolic receptor, FKBP12. Tacrolimus 0-6 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 139-145 1383226-7 1992 The 110-kDa activity observed in brain extracts appears to be the FKBP12.FK-506.calcineurin (CaN) complex previously reported (Liu, J., Farmer, J., Lane, W., Friedman, J., Weissman, I., and Schreiber, S. (1991) Cell 66, 807-815) while the 110 kDa activity observed in JURKAT cells is a novel FK-506-binding protein. Tacrolimus 73-79 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 66-72 1383222-2 1992 Heat shock protein 56 (hsp56) has been shown to be involved in two cellular pathways, as an immunophilin for FK506 and as a component of steroid receptor complexes. Tacrolimus 109-114 FKBP prolyl isomerase 4 Homo sapiens 0-21 1383222-2 1992 Heat shock protein 56 (hsp56) has been shown to be involved in two cellular pathways, as an immunophilin for FK506 and as a component of steroid receptor complexes. Tacrolimus 109-114 FKBP prolyl isomerase 4 Homo sapiens 23-28 1383226-8 1992 Our characterization of the FKBP12.FK-506.CaN complex reveals a dependence upon calmodulin (CaM) for formation of the complex and demonstrates that the peptidyl-prolyl cis-trans isomerase (PPIase) activity of FKBP12 is not required for binding of FKBP12.FK-506 to CaN or for inhibition of CaN phosphatase activity. Tacrolimus 35-41 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 28-34 1383226-8 1992 Our characterization of the FKBP12.FK-506.CaN complex reveals a dependence upon calmodulin (CaM) for formation of the complex and demonstrates that the peptidyl-prolyl cis-trans isomerase (PPIase) activity of FKBP12 is not required for binding of FKBP12.FK-506 to CaN or for inhibition of CaN phosphatase activity. Tacrolimus 35-41 FKBP prolyl isomerase 5 Homo sapiens 189-195 1383226-8 1992 Our characterization of the FKBP12.FK-506.CaN complex reveals a dependence upon calmodulin (CaM) for formation of the complex and demonstrates that the peptidyl-prolyl cis-trans isomerase (PPIase) activity of FKBP12 is not required for binding of FKBP12.FK-506 to CaN or for inhibition of CaN phosphatase activity. Tacrolimus 35-41 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 209-215 1383226-8 1992 Our characterization of the FKBP12.FK-506.CaN complex reveals a dependence upon calmodulin (CaM) for formation of the complex and demonstrates that the peptidyl-prolyl cis-trans isomerase (PPIase) activity of FKBP12 is not required for binding of FKBP12.FK-506 to CaN or for inhibition of CaN phosphatase activity. Tacrolimus 35-41 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 209-215 1383226-8 1992 Our characterization of the FKBP12.FK-506.CaN complex reveals a dependence upon calmodulin (CaM) for formation of the complex and demonstrates that the peptidyl-prolyl cis-trans isomerase (PPIase) activity of FKBP12 is not required for binding of FKBP12.FK-506 to CaN or for inhibition of CaN phosphatase activity. Tacrolimus 254-260 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 28-34 1383226-8 1992 Our characterization of the FKBP12.FK-506.CaN complex reveals a dependence upon calmodulin (CaM) for formation of the complex and demonstrates that the peptidyl-prolyl cis-trans isomerase (PPIase) activity of FKBP12 is not required for binding of FKBP12.FK-506 to CaN or for inhibition of CaN phosphatase activity. Tacrolimus 254-260 FKBP prolyl isomerase 5 Homo sapiens 189-195 1382988-3 1992 We have previously shown that T cell receptor/CD3-mediated induction of apoptosis in a murine T cell hybridoma is inhibited by the immunosuppressive drugs cyclosporin A (CsA) and FK506. Tacrolimus 179-184 CD3 antigen, epsilon polypeptide Mus musculus 46-49 1384129-4 1992 A similar reduction in motility on vitronectin occurred when cells were treated with the immunosuppressant FK506, which also inhibits calcineurin when bound to its binding protein, FKBP. Tacrolimus 107-112 vitronectin Homo sapiens 35-46 1281674-0 1992 FK506 and rapamycin selectively enhance degradation of IL-2 and GM-CSF mRNA. Tacrolimus 0-5 interleukin 2 Homo sapiens 55-59 1281674-0 1992 FK506 and rapamycin selectively enhance degradation of IL-2 and GM-CSF mRNA. Tacrolimus 0-5 colony stimulating factor 2 Homo sapiens 64-70 1281674-2 1992 Using Northern analyses and promoter-reporter constructs we analyzed the transcriptional and posttranscriptional effects of FK506 and rapamycin on IL-2, GM-CSF, and IL-2R alpha gene expression. Tacrolimus 124-129 interleukin 2 Homo sapiens 147-151 1281674-2 1992 Using Northern analyses and promoter-reporter constructs we analyzed the transcriptional and posttranscriptional effects of FK506 and rapamycin on IL-2, GM-CSF, and IL-2R alpha gene expression. Tacrolimus 124-129 colony stimulating factor 2 Homo sapiens 153-159 1281674-2 1992 Using Northern analyses and promoter-reporter constructs we analyzed the transcriptional and posttranscriptional effects of FK506 and rapamycin on IL-2, GM-CSF, and IL-2R alpha gene expression. Tacrolimus 124-129 interleukin 2 receptor subunit alpha Homo sapiens 165-176 1281674-3 1992 FK506 completely inhibited activation of the IL-2 promoter, but only partially blocked GM-CSF promoter activity. Tacrolimus 0-5 interleukin 2 Homo sapiens 45-49 1381629-8 1992 This is supported by the ability of FK506 and rapamycin to directly compete the binding of the photoaffinity analogue 125I-iodoaryl azidoprazosin to the P-glycoprotein. Tacrolimus 36-41 ATP binding cassette subfamily B member 1 Homo sapiens 153-167 1355105-6 1992 Growth of the cells required activation because cyclosporin A and FK506 blocked stimulator cell-induced IL-2 production and proliferation as well as the spontaneous growth of the lines. Tacrolimus 66-71 interleukin 2 Homo sapiens 104-108 1382293-1 1992 The inhibitory effects of cyclosporin A (CsA) and FK506 on Fc epsilon receptor type I-initiated increases in cytokine mRNA and the expression of their intracellular binding proteins were studied in interleukin 3 (IL-3)-dependent, mouse bone marrow-derived mast cells (BMMCs). Tacrolimus 50-55 interleukin 3 Mus musculus 198-217 1382293-9 1992 The resistance of BMMCs to inhibition of Fc epsilon receptor type I-mediated increases in cytokine mRNA by FK506 is most likely due to their deficiency of FKBP12 and the related inability to inhibit the activity of calcineurin. Tacrolimus 107-112 FK506 binding protein 1a Mus musculus 155-161 1385058-0 1992 Cytochrome P-450 3A enzymes are responsible for biotransformation of FK506 and rapamycin in man and rat. Tacrolimus 69-74 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 0-16 1385058-1 1992 The hepatic cytochrome P-450 responsible for metabolism of the structurally related macrolides FK506 and rapamycin in humans was identified using in vitro studies. Tacrolimus 95-100 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 12-28 1385058-7 1992 It is concluded that in human and rat liver FK506 and rapamycin are metabolized primarily by cytochrome P-450 3A4. Tacrolimus 44-49 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 93-109 1380976-4 1992 FK-506 is known to interact with FK-binding protein-12 (FKBP-12), an abundant cytosolic protein with cis-trans peptidyl-prolyl isomerase activity (PPIase) activity. Tacrolimus 0-6 FKBP prolyl isomerase family member 6 Rattus norvegicus 147-153 1380976-6 1992 Recently, it was found that the complex of FKBP-12 with FK-506, but not with RAP, inhibits the phosphatase activity of calcineurin. Tacrolimus 56-62 FKBP prolyl isomerase 1A Rattus norvegicus 43-50 1380976-4 1992 FK-506 is known to interact with FK-binding protein-12 (FKBP-12), an abundant cytosolic protein with cis-trans peptidyl-prolyl isomerase activity (PPIase) activity. Tacrolimus 0-6 FKBP prolyl isomerase 1A Rattus norvegicus 33-54 1380976-4 1992 FK-506 is known to interact with FK-binding protein-12 (FKBP-12), an abundant cytosolic protein with cis-trans peptidyl-prolyl isomerase activity (PPIase) activity. Tacrolimus 0-6 FKBP prolyl isomerase 1A Rattus norvegicus 56-63 1383612-0 1992 FK-506 inhibits proliferation and IL-4 messenger RNA production by a T-helper 2 cell line. Tacrolimus 0-6 interleukin 4 Homo sapiens 34-38 1384815-1 1992 The immunosuppressive drugs FK506 and cyclosporin A have an identical spectrum of activities with respect to IgE receptor (Fc epsilon RI)-mediated exocytosis from mast cells and T cell receptor-mediated transcription of IL-2. Tacrolimus 28-33 Fc receptor, IgE, high affinity I, alpha polypeptide Mus musculus 123-136 1384815-1 1992 The immunosuppressive drugs FK506 and cyclosporin A have an identical spectrum of activities with respect to IgE receptor (Fc epsilon RI)-mediated exocytosis from mast cells and T cell receptor-mediated transcription of IL-2. Tacrolimus 28-33 interleukin 2 Mus musculus 220-224 1379588-4 1992 We have identified, however, three FKBP12 surface residues (Asp-37, Arg-42, and His-87) proximal to a solvent-exposed segment of bound FK506 that may be direct contacts in the calcineurin complex. Tacrolimus 135-140 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 35-41 1379588-5 1992 Site-directed mutagenesis of two of these residues decreases the affinity of FKBP12-FK506 for calcineurin (Ki) from 6 nM for wild-type FKBP12 to 3.7 microM for a R42K/H87V double mutant, without affecting the peptidylprolyl isomerase activity or FK506 affinity of the mutant protein. Tacrolimus 84-89 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 77-83 1379588-5 1992 Site-directed mutagenesis of two of these residues decreases the affinity of FKBP12-FK506 for calcineurin (Ki) from 6 nM for wild-type FKBP12 to 3.7 microM for a R42K/H87V double mutant, without affecting the peptidylprolyl isomerase activity or FK506 affinity of the mutant protein. Tacrolimus 84-89 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 135-141 1379588-5 1992 Site-directed mutagenesis of two of these residues decreases the affinity of FKBP12-FK506 for calcineurin (Ki) from 6 nM for wild-type FKBP12 to 3.7 microM for a R42K/H87V double mutant, without affecting the peptidylprolyl isomerase activity or FK506 affinity of the mutant protein. Tacrolimus 246-251 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 77-83 1379588-6 1992 These FKBP12 mutations along with several substitutions on FK506 known to affect calcineurin binding form a roughly 100-A2 region of the FKBP12-FK506 complex surface that is likely to be within the calcineurin binding site. Tacrolimus 59-64 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 137-143 1379588-6 1992 These FKBP12 mutations along with several substitutions on FK506 known to affect calcineurin binding form a roughly 100-A2 region of the FKBP12-FK506 complex surface that is likely to be within the calcineurin binding site. Tacrolimus 144-149 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 6-12 1379588-6 1992 These FKBP12 mutations along with several substitutions on FK506 known to affect calcineurin binding form a roughly 100-A2 region of the FKBP12-FK506 complex surface that is likely to be within the calcineurin binding site. Tacrolimus 144-149 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 137-143 1380130-1 1992 The immunophilins cyclophilin and FK506 binding protein (FKBP) are small, predominantly soluble proteins that bind the immunosuppressant drugs cyclosporin A and FK506, respectively, with high affinity, and which seem to mediate their pharmacological actions. Tacrolimus 34-39 FK506-binding protein 12kD Drosophila melanogaster 57-61 1380130-2 1992 The Ca(2+)-dependent protein phosphatase, calcineurin, binds the cyclophilin-cyclosporin A and FKBP-FK506 complexes, indicating that calcineurin might mediate the actions of these drugs. Tacrolimus 100-105 FK506-binding protein 12kD Drosophila melanogaster 95-99 1383612-7 1992 FK-506 markedly inhibits Con A-induced proliferation and IL-4 mRNA production by the T-helper 2 cell line Ly1+2-/9. Tacrolimus 0-6 interleukin 4 Homo sapiens 57-61 1383612-8 1992 The ability of FK-506 to block the proliferation and IL-4 production by this helper cell subset suggests that this effect may contribute to its observed marked immunosuppressive properties in vitro and in vivo. Tacrolimus 15-21 interleukin 4 Homo sapiens 53-57 1380951-3 1992 While 1 microgram/ml CSA and 0.1 microgram/ml FK 506 completely suppressed PHA-stimulated accumulation of mRNA for IL2, IL4, IL9, GM-CSF, TNF-alpha and IFN-gamma in PBMC, flu, keto and TGF-beta failed to inhibit any (except TNF-alpha blocked by TGF-beta). Tacrolimus 46-52 interleukin 2 Homo sapiens 115-118 1279908-3 1992 Yeast FKBP-13 is homologous to human FKBP-13 (52% amino acid identity) and to FKBP-12, the major cytosolic receptor for FK506. Tacrolimus 120-125 FKBP prolyl isomerase 2 Homo sapiens 6-13 1279908-3 1992 Yeast FKBP-13 is homologous to human FKBP-13 (52% amino acid identity) and to FKBP-12, the major cytosolic receptor for FK506. Tacrolimus 120-125 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 78-85 1380951-3 1992 While 1 microgram/ml CSA and 0.1 microgram/ml FK 506 completely suppressed PHA-stimulated accumulation of mRNA for IL2, IL4, IL9, GM-CSF, TNF-alpha and IFN-gamma in PBMC, flu, keto and TGF-beta failed to inhibit any (except TNF-alpha blocked by TGF-beta). Tacrolimus 46-52 interleukin 4 Homo sapiens 120-123 1380951-3 1992 While 1 microgram/ml CSA and 0.1 microgram/ml FK 506 completely suppressed PHA-stimulated accumulation of mRNA for IL2, IL4, IL9, GM-CSF, TNF-alpha and IFN-gamma in PBMC, flu, keto and TGF-beta failed to inhibit any (except TNF-alpha blocked by TGF-beta). Tacrolimus 46-52 interleukin 9 Homo sapiens 125-128 1380951-3 1992 While 1 microgram/ml CSA and 0.1 microgram/ml FK 506 completely suppressed PHA-stimulated accumulation of mRNA for IL2, IL4, IL9, GM-CSF, TNF-alpha and IFN-gamma in PBMC, flu, keto and TGF-beta failed to inhibit any (except TNF-alpha blocked by TGF-beta). Tacrolimus 46-52 colony stimulating factor 2 Homo sapiens 130-136 1380951-3 1992 While 1 microgram/ml CSA and 0.1 microgram/ml FK 506 completely suppressed PHA-stimulated accumulation of mRNA for IL2, IL4, IL9, GM-CSF, TNF-alpha and IFN-gamma in PBMC, flu, keto and TGF-beta failed to inhibit any (except TNF-alpha blocked by TGF-beta). Tacrolimus 46-52 tumor necrosis factor Homo sapiens 138-147 1380951-3 1992 While 1 microgram/ml CSA and 0.1 microgram/ml FK 506 completely suppressed PHA-stimulated accumulation of mRNA for IL2, IL4, IL9, GM-CSF, TNF-alpha and IFN-gamma in PBMC, flu, keto and TGF-beta failed to inhibit any (except TNF-alpha blocked by TGF-beta). Tacrolimus 46-52 interferon gamma Homo sapiens 152-161 1380951-3 1992 While 1 microgram/ml CSA and 0.1 microgram/ml FK 506 completely suppressed PHA-stimulated accumulation of mRNA for IL2, IL4, IL9, GM-CSF, TNF-alpha and IFN-gamma in PBMC, flu, keto and TGF-beta failed to inhibit any (except TNF-alpha blocked by TGF-beta). Tacrolimus 46-52 transforming growth factor beta 1 Homo sapiens 185-193 1380951-3 1992 While 1 microgram/ml CSA and 0.1 microgram/ml FK 506 completely suppressed PHA-stimulated accumulation of mRNA for IL2, IL4, IL9, GM-CSF, TNF-alpha and IFN-gamma in PBMC, flu, keto and TGF-beta failed to inhibit any (except TNF-alpha blocked by TGF-beta). Tacrolimus 46-52 tumor necrosis factor Homo sapiens 224-233 1380951-3 1992 While 1 microgram/ml CSA and 0.1 microgram/ml FK 506 completely suppressed PHA-stimulated accumulation of mRNA for IL2, IL4, IL9, GM-CSF, TNF-alpha and IFN-gamma in PBMC, flu, keto and TGF-beta failed to inhibit any (except TNF-alpha blocked by TGF-beta). Tacrolimus 46-52 transforming growth factor beta 1 Homo sapiens 245-253 1377361-0 1992 FK-506- and CsA-sensitive activation of the interleukin-2 promoter by calcineurin. Tacrolimus 0-6 interleukin 2 Homo sapiens 44-57 1377361-2 1992 The immunosuppressive drugs, cyclosporin A (CsA) and FK-506, prevent T-cell proliferation by inhibiting a Ca(2+)-dependent event required for induction of interleukin-2 transcription. Tacrolimus 53-59 interleukin 2 Homo sapiens 155-168 1377361-6 1992 Here we report that transfection of a calcineurin catalytic subunit increases the 50% inhibitory concentration (IC50) of the immunosuppressants FK-506 and CsA, and that a mutant subunit acts in synergy with phorbol ester alone to activate the interleukin-2 promoter in a drug-sensitive manner. Tacrolimus 144-150 interleukin 2 Homo sapiens 243-256 1377606-3 1992 The structurally related drug FK506 had no effect on pp70S6K activation but at high concentrations reversed the rapamycin-induced block, confirming the requirement for the rapamycin and FK506 receptor, FKBP. Tacrolimus 30-35 FK506 binding protein 1a Mus musculus 202-206 1375189-7 1992 As shown by both Western blots and FK506 binding activity, FKBP-12 was eluted only in the flow-through and wash fractions. Tacrolimus 35-40 FKBP prolyl isomerase 1A Homo sapiens 59-66 1376361-3 1992 In this report, we examined the ability of rapamycin (RAP) to inhibit cytokine production and cytokine-induced proliferation by a factor-dependent murine mast cell line and compared its activity to that of the structurally related macrolide FK506. Tacrolimus 241-246 regulatory associated protein of MTOR, complex 1 Mus musculus 43-52 1379588-0 1992 Charged surface residues of FKBP12 participate in formation of the FKBP12-FK506-calcineurin complex. Tacrolimus 74-79 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 28-34 1379588-0 1992 Charged surface residues of FKBP12 participate in formation of the FKBP12-FK506-calcineurin complex. Tacrolimus 74-79 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 67-73 1379588-1 1992 The mechanism of FK506 immunosuppression has been proposed to proceed by formation of a tight-binding complex with the intracellular 12-kDa FK506-binding protein (FKBP12). Tacrolimus 17-22 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 163-169 1376361-3 1992 In this report, we examined the ability of rapamycin (RAP) to inhibit cytokine production and cytokine-induced proliferation by a factor-dependent murine mast cell line and compared its activity to that of the structurally related macrolide FK506. Tacrolimus 241-246 regulatory associated protein of MTOR, complex 1 Mus musculus 54-57 1376361-8 1992 Because RAP and FK506 are structurally related and yet have divergent biological effects, we examined the ability of RAP to antagonize inhibitory effects of FK506 on mast cell cytokine production and the ability of FK506 to antagonize inhibitory effects of RAP on cytokine-induced mast cell proliferation. Tacrolimus 157-162 regulatory associated protein of MTOR, complex 1 Mus musculus 117-120 1376361-8 1992 Because RAP and FK506 are structurally related and yet have divergent biological effects, we examined the ability of RAP to antagonize inhibitory effects of FK506 on mast cell cytokine production and the ability of FK506 to antagonize inhibitory effects of RAP on cytokine-induced mast cell proliferation. Tacrolimus 157-162 regulatory associated protein of MTOR, complex 1 Mus musculus 117-120 1376361-8 1992 Because RAP and FK506 are structurally related and yet have divergent biological effects, we examined the ability of RAP to antagonize inhibitory effects of FK506 on mast cell cytokine production and the ability of FK506 to antagonize inhibitory effects of RAP on cytokine-induced mast cell proliferation. Tacrolimus 157-162 regulatory associated protein of MTOR, complex 1 Mus musculus 117-120 1376361-8 1992 Because RAP and FK506 are structurally related and yet have divergent biological effects, we examined the ability of RAP to antagonize inhibitory effects of FK506 on mast cell cytokine production and the ability of FK506 to antagonize inhibitory effects of RAP on cytokine-induced mast cell proliferation. Tacrolimus 157-162 regulatory associated protein of MTOR, complex 1 Mus musculus 117-120 1376361-9 1992 The addition of RAP in molar excess reversed inhibition of mast cell cytokine production mediated by FK506, but not that of CSA. Tacrolimus 101-106 regulatory associated protein of MTOR, complex 1 Mus musculus 16-19 1604471-14 1992 The hypersecretory reaction of the beta cell may be of help in further investigations of mechanisms of CsA- and FK506-induced inhibition of insulin release. Tacrolimus 112-117 insulin Canis lupus familiaris 140-147 1375751-3 1992 Two largely nonpolar, immunosuppressive agents, FK506 and rapamycin, each bind with high affinity to a common hydrophobic pocket on a small peptidylproline cis-trans isomerase known as FK506 binding protein (FKBP-12) and inhibit its activity. Tacrolimus 48-53 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 208-215 1375751-4 1992 In an effort to elucidate the structural features of these ligands responsible for the observed energetics, we have undertaken an investigation of the thermodynamics of binding of FK506 and rapamycin to FKBP-12. Tacrolimus 180-185 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 203-210 1375751-6 1992 By analyzing the distribution of changes in solvent-accessible surface area upon binding of FK506 to FKBP-12 from crystallographic data, it is found that 99% of the net surface buried upon binding involves nonpolar groups. Tacrolimus 92-97 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 101-108 1376003-3 1992 A 59-kilodalton member of the FK506- and rapamycin-binding class was found to associate in the absence of these drugs with two heat shock proteins (hsp90 and hsp70) and the glucocorticoid receptor (GR). Tacrolimus 30-35 heat shock protein 90 alpha family class A member 1 Homo sapiens 148-153 1376003-3 1992 A 59-kilodalton member of the FK506- and rapamycin-binding class was found to associate in the absence of these drugs with two heat shock proteins (hsp90 and hsp70) and the glucocorticoid receptor (GR). Tacrolimus 30-35 heat shock protein family A (Hsp70) member 4 Homo sapiens 158-163 1376003-3 1992 A 59-kilodalton member of the FK506- and rapamycin-binding class was found to associate in the absence of these drugs with two heat shock proteins (hsp90 and hsp70) and the glucocorticoid receptor (GR). Tacrolimus 30-35 nuclear receptor subfamily 3 group C member 1 Homo sapiens 173-196 1376003-3 1992 A 59-kilodalton member of the FK506- and rapamycin-binding class was found to associate in the absence of these drugs with two heat shock proteins (hsp90 and hsp70) and the glucocorticoid receptor (GR). Tacrolimus 30-35 nuclear receptor subfamily 3 group C member 1 Homo sapiens 198-200 1374404-4 1992 In humans, FK506 binds to the 12-kDa FK506-binding protein (FKBP12) and blocks calcium-dependent T cell activation. Tacrolimus 11-16 FKBP prolyl isomerase 1A Homo sapiens 30-58 1374404-4 1992 In humans, FK506 binds to the 12-kDa FK506-binding protein (FKBP12) and blocks calcium-dependent T cell activation. Tacrolimus 11-16 FKBP prolyl isomerase 1A Homo sapiens 60-66 1380242-3 1992 Cyclosporin A (CsA) and FK506 inhibit the production of IL-2 in T lymphocytes at the level of gene transcription. Tacrolimus 24-29 interleukin 2 Homo sapiens 56-60 1375171-0 1992 Solution structure of FK506 bound to FKBP-12. Tacrolimus 22-27 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 37-44 1375171-1 1992 The complex of the immunosuppressant FK506 bound to FKBP-12 has been studied in solution using 1H and inverse-detected 13C NMR methods. Tacrolimus 37-42 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 52-59 1373887-5 1992 Both CsA and FK 506 specifically inhibit cellular calcineurin at drug concentrations that inhibit interleukin 2 production in activated T cells. Tacrolimus 13-19 interleukin 2 Homo sapiens 98-111 1374947-0 1992 FK506 as an agonist to induce inhibition of interleukin 2 production. Tacrolimus 0-5 interleukin 2 Homo sapiens 44-57 1374948-8 1992 FK506 pretreatment significantly reduced the serum levels of BUN (P less than 0.02), creatinine (P less than 0.02), and TNF (P less than 0.05) as compared with that seen in controls. Tacrolimus 0-5 tumor necrosis factor Rattus norvegicus 120-123 1374948-11 1992 Based upon these data, it can be concluded that (1) FK506 pretreatment ameliorates the functional renal injury associated with I/R, (2) renal ischemia induces the release of TNF, and (3) FK506 pretreatment results in a significant inhibition of TNF production. Tacrolimus 52-57 tumor necrosis factor Rattus norvegicus 174-177 1374948-11 1992 Based upon these data, it can be concluded that (1) FK506 pretreatment ameliorates the functional renal injury associated with I/R, (2) renal ischemia induces the release of TNF, and (3) FK506 pretreatment results in a significant inhibition of TNF production. Tacrolimus 52-57 tumor necrosis factor Rattus norvegicus 245-248 1380242-6 1992 However, CsA and FK506 inhibit the appearance of DNA binding activity of factors that bind to the NF-AT and AP-1 sites in the IL-2 enhancer. Tacrolimus 17-22 interleukin 2 Homo sapiens 126-130 1380242-7 1992 Since the induction of NF-AT and AP-1 is induced by the same stimuli that stimulate IL-2 production, these results indicate that the immunosuppressant action of CsA and FK506 is exerted at the level of these trans-activating factors. Tacrolimus 169-174 interleukin 2 Homo sapiens 84-88 1371698-4 1992 FKBP25 displays the rotamase activity characteristic of FKBPs; the activity is inhibited by the immunosuppressants rapamycin (Ki = 0.9 nM) and FK506 (Ki = 160 nM), but not cyclosporin A. Tacrolimus 143-148 FKBP prolyl isomerase 3 Bos taurus 0-6 1375932-1 1992 Two FK506 binding proteins of molecular mass 12 kDa (FKBP12) and 13 kDa (FKBP13) have been identified as common cellular receptors of the immunosuppressants FK506 and rapamycin. Tacrolimus 4-9 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 53-59 1375932-1 1992 Two FK506 binding proteins of molecular mass 12 kDa (FKBP12) and 13 kDa (FKBP13) have been identified as common cellular receptors of the immunosuppressants FK506 and rapamycin. Tacrolimus 4-9 FKBP prolyl isomerase 2 Homo sapiens 73-79 1375932-1 1992 Two FK506 binding proteins of molecular mass 12 kDa (FKBP12) and 13 kDa (FKBP13) have been identified as common cellular receptors of the immunosuppressants FK506 and rapamycin. Tacrolimus 157-162 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 53-59 1375932-1 1992 Two FK506 binding proteins of molecular mass 12 kDa (FKBP12) and 13 kDa (FKBP13) have been identified as common cellular receptors of the immunosuppressants FK506 and rapamycin. Tacrolimus 157-162 FKBP prolyl isomerase 2 Homo sapiens 73-79 1375932-6 1992 The PPIase activity of FKBP25 was far more sensitive to inhibition by rapamycin (IC50 = 50 nM) than FK506 (IC50 = 400 nM). Tacrolimus 100-105 FKBP prolyl isomerase 3 Homo sapiens 23-29 1375932-7 1992 PPIase activity of 100 nM FKBP25 was almost completely inhibited by 150 nM rapamycin while only 90% inhibition was achieved by 4 microM FK506. Tacrolimus 136-141 FKBP prolyl isomerase 5 Homo sapiens 0-6 1375932-7 1992 PPIase activity of 100 nM FKBP25 was almost completely inhibited by 150 nM rapamycin while only 90% inhibition was achieved by 4 microM FK506. Tacrolimus 136-141 FKBP prolyl isomerase 3 Homo sapiens 26-32 1375932-8 1992 These data demonstrate that FKBP25 has a higher affinity for rapamycin than for FK506 and suggest that this cellular receptor may be an important target molecule for immunosuppression by rapamycin. Tacrolimus 80-85 FKBP prolyl isomerase 3 Homo sapiens 28-34 1371107-0 1992 The Hsp56 component of steroid receptor complexes binds to immobilized FK506 and shows homology to FKBP-12 and FKBP-13. Tacrolimus 71-76 FKBP prolyl isomerase 4 Homo sapiens 4-9 1378764-0 1992 Cyclosporin A and FK506 prevent the derepression of the IL-2 gene in mitogen-induced primary T lymphocytes. Tacrolimus 18-23 interleukin 2 Homo sapiens 56-60 1378764-3 1992 Cyclosporin A (CsA) and FK506 interfere with normal derepression of the IL-2 gene. Tacrolimus 24-29 interleukin 2 Homo sapiens 72-76 1371107-5 1992 It would appear, therefore, that this 60-kDa protein, or as we refer to it provisionally, "Hsp56," could have the capacity to bind FK506 directly. Tacrolimus 131-136 FKBP prolyl isomerase 4 Homo sapiens 91-96 1371117-1 1992 FK506-binding protein (FKBP) catalyzes the cis-trans isomerization of the peptidyl-prolyl amide bond (the PPIase reaction) and is the major intracellular receptor for the immunosuppressive drugs FK506 and rapamycin. Tacrolimus 0-5 FKBP prolyl isomerase 10 Homo sapiens 106-112 1371158-7 1992 Similarly, FK506 completely inhibited cytokine production by MC/9, partially inhibited cytokine production by MCIII and had differential effects on IL-3/granulocyte-macrophage colony-stimulating factor and IL-2/IL-4 production by MCVI. Tacrolimus 11-16 interleukin 3 Mus musculus 148-152 1371158-7 1992 Similarly, FK506 completely inhibited cytokine production by MC/9, partially inhibited cytokine production by MCIII and had differential effects on IL-3/granulocyte-macrophage colony-stimulating factor and IL-2/IL-4 production by MCVI. Tacrolimus 11-16 interleukin 2 Mus musculus 206-210 1371158-7 1992 Similarly, FK506 completely inhibited cytokine production by MC/9, partially inhibited cytokine production by MCIII and had differential effects on IL-3/granulocyte-macrophage colony-stimulating factor and IL-2/IL-4 production by MCVI. Tacrolimus 11-16 interleukin 4 Mus musculus 211-215 1371623-0 1992 Blockade of interleukin-2 production from cloned T cells by cyclosporine and FK 506 assessed by proliferation assays in vitro. Tacrolimus 77-83 interleukin 2 Homo sapiens 12-25 1371624-0 1992 Enhanced liver regeneration by FK 506 can be blocked by interleukin-1 alpha and interleukin-2. Tacrolimus 31-37 interleukin 1 alpha Homo sapiens 56-75 1371624-0 1992 Enhanced liver regeneration by FK 506 can be blocked by interleukin-1 alpha and interleukin-2. Tacrolimus 31-37 interleukin 2 Homo sapiens 80-93 1375473-8 1992 However, nonimmunosuppressive analogs of CsA and FK-506 are also inhibitory, indicating that inhibition of PPIase activity is not directly implicated in immunosuppression. Tacrolimus 49-55 FKBP prolyl isomerase 5 Homo sapiens 107-113 1371491-8 1992 When the cells were stimulated by phorbol ester (phorbol 12-myristate 13-acetate, PMA) plus calcium ionophore (ionomycin), FK506 and CsA inhibited, in a dose-dependent manner, the production of IL-2, IL-4, IL-5, IFN-gamma and TNF-alpha. Tacrolimus 123-128 interleukin 5 Homo sapiens 206-210 1371491-5 1992 FK506 or CsA inhibited SEA-induced tumour necrosis factor-alpha (TNF-alpha) production both in monocytes (P less than 0.01) and in lymphocytes (P less than 0.001), at a drug concentration of 1-25 ng/ml for FK506 and 100-500 ng/ml for CsA. Tacrolimus 0-5 tumor necrosis factor Homo sapiens 65-74 1371491-5 1992 FK506 or CsA inhibited SEA-induced tumour necrosis factor-alpha (TNF-alpha) production both in monocytes (P less than 0.01) and in lymphocytes (P less than 0.001), at a drug concentration of 1-25 ng/ml for FK506 and 100-500 ng/ml for CsA. Tacrolimus 206-211 tumor necrosis factor Homo sapiens 65-74 1371491-8 1992 When the cells were stimulated by phorbol ester (phorbol 12-myristate 13-acetate, PMA) plus calcium ionophore (ionomycin), FK506 and CsA inhibited, in a dose-dependent manner, the production of IL-2, IL-4, IL-5, IFN-gamma and TNF-alpha. Tacrolimus 123-128 interleukin 2 Homo sapiens 194-198 1371491-8 1992 When the cells were stimulated by phorbol ester (phorbol 12-myristate 13-acetate, PMA) plus calcium ionophore (ionomycin), FK506 and CsA inhibited, in a dose-dependent manner, the production of IL-2, IL-4, IL-5, IFN-gamma and TNF-alpha. Tacrolimus 123-128 interleukin 4 Homo sapiens 200-204 1384862-4 1992 However, the response of the PHA-pulsed T cells to IL-6 was still inhibited by FK-506 or Cs A, but the inhibitory effect gradually decreased as the time in which the PHA-pulsed T cells interacted with IL-6 was prolonged. Tacrolimus 79-85 interleukin 6 Homo sapiens 51-55 1384862-7 1992 It is likely that the two drugs inhibit the expression of lymphokine receptors, by interfering Ca(2+)-related signals and that IL-6 induces T cell proliferation in a different way than IL-2 and IL-4, which are FK-506- and Cs A-sensitive. Tacrolimus 210-216 interleukin 4 Homo sapiens 194-198 1371575-0 1992 Effect of FK506 on insulin secretion in normal dogs. Tacrolimus 10-15 insulin Canis lupus familiaris 19-26 1371575-1 1992 In this report, we describe the effect of FK506 on glucose-mediated insulin release in normal dogs. Tacrolimus 42-47 insulin Canis lupus familiaris 68-75 1371575-9 1992 Insulin secretion after the recovery period remained unchanged in group 1 dogs, but continued to be significantly reduced in group 2 dogs that had received FK506 for 4 weeks. Tacrolimus 156-161 insulin Canis lupus familiaris 0-7 1282197-4 1992 This in vitro synergism of gamma-IFN and FK506 may have clinical application in that low doses of gamma-IFN and FK506 combinations may be effective to correct polyclonal B cell activation of patients with SLE. Tacrolimus 41-46 interferon gamma Mus musculus 98-107 1282197-4 1992 This in vitro synergism of gamma-IFN and FK506 may have clinical application in that low doses of gamma-IFN and FK506 combinations may be effective to correct polyclonal B cell activation of patients with SLE. Tacrolimus 112-117 interferon gamma Mus musculus 27-36 1372739-6 1992 The release of amylase in response to CCK was reduced by FK506 in a dose-related manner (p less than 0.01) and by CS at 25 mg/kg (p less than 0.01). Tacrolimus 57-62 cholecystokinin Rattus norvegicus 38-41 1371491-8 1992 When the cells were stimulated by phorbol ester (phorbol 12-myristate 13-acetate, PMA) plus calcium ionophore (ionomycin), FK506 and CsA inhibited, in a dose-dependent manner, the production of IL-2, IL-4, IL-5, IFN-gamma and TNF-alpha. Tacrolimus 123-128 interferon gamma Homo sapiens 212-221 1380720-7 1992 FK 506 pretreatment reduced the serum levels of BUN (p less than .02), creatinine (p less than .02) and TNF (p less than .05) as compared to that seen in controls. Tacrolimus 0-6 tumor necrosis factor-like Rattus norvegicus 104-107 1380720-8 1992 Based upon these data, it appears that: (a) renal ischemia induces the release of TNF; (b) FK 506 pretreatment inhibits TNF production; and (c) FK 506 reduces renal injury association with I/R. Tacrolimus 91-97 tumor necrosis factor-like Rattus norvegicus 120-123 1380720-8 1992 Based upon these data, it appears that: (a) renal ischemia induces the release of TNF; (b) FK 506 pretreatment inhibits TNF production; and (c) FK 506 reduces renal injury association with I/R. Tacrolimus 144-150 tumor necrosis factor-like Rattus norvegicus 82-85 1721455-0 1991 FK 506 modulates accessory cell adhesion molecule expression and inhibits CD4 lymphocyte adhesion to retinal pigment epithelial cells in vitro: implications for therapy of uveoretinitis. Tacrolimus 0-6 CD4 molecule Homo sapiens 74-77 1721462-0 1991 The ability of myelin basic protein-sensitised leukocytes to adoptively transfer experimental allergic encephalomyelitis following coculture with FK 506, cyclosporine, or prednisolone. Tacrolimus 146-152 myelin basic protein Homo sapiens 15-35 1719972-1 1991 Recently, the amino acid sequence of a 12 Kd endogenous protein inhibitor of protein kinase C (PKC-I 2) has been shown to be identical to that of the 12 KDa receptor for the immunosuppressive drug, FK-506. Tacrolimus 198-204 proline rich transmembrane protein 2 Homo sapiens 77-93 1719972-1 1991 Recently, the amino acid sequence of a 12 Kd endogenous protein inhibitor of protein kinase C (PKC-I 2) has been shown to be identical to that of the 12 KDa receptor for the immunosuppressive drug, FK-506. Tacrolimus 198-204 FKBP prolyl isomerase 1A Homo sapiens 95-102 1930186-1 1991 FKBP-12 is the major T cell binding protein for the immunosuppressive drugs FK506 and rapamycin. Tacrolimus 76-81 FKBP prolyl isomerase 1A Homo sapiens 0-7 1716149-1 1991 FKBP-12, the major T-cell binding protein for the immunosuppressive agents FK506 and rapamycin, catalyzes the interconversion of the cis and trans rotamers of the peptidyl-prolyl amide bond of peptide and protein substrates. Tacrolimus 75-80 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 0-7 14621743-4 1992 Exposure of tubular cells to high concentrations of FK506 or CyA (10, 50 and 100 microM) induced a time- and dose-dependent cell injury in vitro characterized by a direct cytotoxic effect on tubular cells as expressed by release of 3H-thymidine from prelabelled cells, N-acetyl-beta-D-glucosaminidase (NAG) release and cell detachment. Tacrolimus 52-57 O-GlcNAcase Homo sapiens 269-300 14621743-4 1992 Exposure of tubular cells to high concentrations of FK506 or CyA (10, 50 and 100 microM) induced a time- and dose-dependent cell injury in vitro characterized by a direct cytotoxic effect on tubular cells as expressed by release of 3H-thymidine from prelabelled cells, N-acetyl-beta-D-glucosaminidase (NAG) release and cell detachment. Tacrolimus 52-57 O-GlcNAcase Homo sapiens 302-305 14621744-7 1992 The concentrations of FK506 or CyA which induced ET-1 secretion by tubular cells and kidney cells were not cytolytic as assessed by N-acetyl-beta-D-glucosaminidase (NAG) release and lactic dehydrogenase (LDH) release. Tacrolimus 22-27 O-GlcNAcase Homo sapiens 165-168 14621859-3 1992 Treatment with low dose FK 506 in combination with splenectomy (Spx) synergistically prolonged the heart allograft survival in this sensitized rat model. Tacrolimus 24-30 spexin hormone Rattus norvegicus 64-67 1721644-5 1991 FK-506 also inhibited the de novo synthesis of 5-lipoxygenase (sulfidopeptide leukotriene C4) and cyclo-oxygenase (prostaglandin D2) metabolites of arachidonic acid from mast cells challenged with anti-IgE. Tacrolimus 0-6 arachidonate 5-lipoxygenase Homo sapiens 47-61 1721276-0 1991 Effects of FK 506 on human hepatic microsomal cytochrome P-450-dependent drug metabolism in vitro. Tacrolimus 11-17 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 46-62 1721286-0 1991 Inhibition of insulin release by FK 506 and its prevention by rioprostil, a stable prostaglandin E1 analogue. Tacrolimus 33-39 insulin Homo sapiens 14-21 1721310-0 1991 Activation of transcription factor NF kappa B in Jurkat cells is inhibited selectively by FK 506 in a signal-dependent manner. Tacrolimus 90-96 nuclear factor kappa B subunit 1 Homo sapiens 35-45 1721312-0 1991 FK 506, rapamycin, and cyclosporine: effects on IL-4 and IL-10 mRNA levels in a T-helper 2 cell line. Tacrolimus 0-6 interleukin 4 Homo sapiens 48-52 1721312-0 1991 FK 506, rapamycin, and cyclosporine: effects on IL-4 and IL-10 mRNA levels in a T-helper 2 cell line. Tacrolimus 0-6 interleukin 10 Homo sapiens 57-62 1721313-0 1991 Kinetics of early T-cell repopulation in the mouse following syngeneic bone marrow transplantation: FK 506 causes a maturational defect of CD4+ CD8- T cells. Tacrolimus 100-106 CD4 antigen Mus musculus 139-142 1721337-0 1991 FK 506: reversal of humorally mediated rejection following ABO-incompatible liver transplantation. Tacrolimus 0-6 ABO, alpha 1-3-N-acetylgalactosaminyltransferase and alpha 1-3-galactosyltransferase Homo sapiens 59-62 1721394-0 1991 Synexin: a target protein for toxic effects of cyclosporine and FK 506 in endocrine cells. Tacrolimus 64-70 annexin A7 Homo sapiens 0-7 1960417-2 1991 Here we show that the generation of interferon-gamma producing cells (IFN-gamma pc) in rat spleen cell cultures stimulated with concanavalin A (ConA) is dose-dependently inhibited by a wide variety of immunosuppressants such as cyclosporin A, FK506, hydrocortisone, dexamethasone, azathioprine and ART-18, a monoclonal antibody (mAb) with established immunosuppressive activity in organ transplantation and autoimmunity. Tacrolimus 243-248 interferon gamma Rattus norvegicus 36-52 1960417-2 1991 Here we show that the generation of interferon-gamma producing cells (IFN-gamma pc) in rat spleen cell cultures stimulated with concanavalin A (ConA) is dose-dependently inhibited by a wide variety of immunosuppressants such as cyclosporin A, FK506, hydrocortisone, dexamethasone, azathioprine and ART-18, a monoclonal antibody (mAb) with established immunosuppressive activity in organ transplantation and autoimmunity. Tacrolimus 243-248 interferon gamma Rattus norvegicus 70-79 1721767-4 1991 Although full recovery was not observed in FK506, this finding indicated that FK506 as well as CsA inhibit IL2 secretion from HTL403. Tacrolimus 78-83 interleukin 2 Homo sapiens 107-110 1371491-8 1992 When the cells were stimulated by phorbol ester (phorbol 12-myristate 13-acetate, PMA) plus calcium ionophore (ionomycin), FK506 and CsA inhibited, in a dose-dependent manner, the production of IL-2, IL-4, IL-5, IFN-gamma and TNF-alpha. Tacrolimus 123-128 tumor necrosis factor Homo sapiens 226-235 1371491-10 1992 Further stimulation by addition of anti-CD28 mAb to the cultures resulted in an augmented IL-2 and IFN-gamma production which was resistant to both FK506 and CsA. Tacrolimus 148-153 interleukin 2 Homo sapiens 90-94 1371491-10 1992 Further stimulation by addition of anti-CD28 mAb to the cultures resulted in an augmented IL-2 and IFN-gamma production which was resistant to both FK506 and CsA. Tacrolimus 148-153 interferon gamma Homo sapiens 99-108 1371491-12 1992 Depending on the mode of cell activation the two drugs inhibited not only cytokine production in lymphocytes but also antigen-induced monokine (TNF-alpha) production in macrophages, although the optimal immunomodulatory effect of FK506 was achieved at a concentration approximately 50-fold lower than that of CsA. Tacrolimus 230-235 tumor necrosis factor Homo sapiens 144-153 1384862-0 1992 The effects of FK-506 and cyclosporin A on the proliferation of PHA-stimulated T cells in response to IL-2, IL-4 or IL-6. Tacrolimus 15-21 interleukin 2 Homo sapiens 102-106 1384862-0 1992 The effects of FK-506 and cyclosporin A on the proliferation of PHA-stimulated T cells in response to IL-2, IL-4 or IL-6. Tacrolimus 15-21 interleukin 6 Homo sapiens 116-120 1720417-0 1991 The immunosuppressive agent FK506 inhibits in vitro expression of membrane-bound and soluble interleukin-2 receptors on resting but not on activated human lymphocytes. Tacrolimus 28-33 ATP binding cassette subfamily A member 1 Homo sapiens 66-80 1720417-0 1991 The immunosuppressive agent FK506 inhibits in vitro expression of membrane-bound and soluble interleukin-2 receptors on resting but not on activated human lymphocytes. Tacrolimus 28-33 interleukin 2 Homo sapiens 93-106 1720417-4 1991 The membrane-bound IL-2 receptor expression was inhibited by FK506 in resting lymphocytes at a concentration of 1 pmol/l. Tacrolimus 61-66 ATP binding cassette subfamily A member 1 Homo sapiens 4-18 1720417-4 1991 The membrane-bound IL-2 receptor expression was inhibited by FK506 in resting lymphocytes at a concentration of 1 pmol/l. Tacrolimus 61-66 interleukin 2 receptor subunit beta Homo sapiens 19-32 1726895-0 1991 FK506 lacks the ability to inhibit expression of interleukin-2 receptor beta-chain on human lymphocytes. Tacrolimus 0-5 interleukin 2 receptor subunit beta Homo sapiens 49-76 1726895-3 1991 FK506 is a new immunosuppressant known to inhibit synthesis of interleukin 2 and expression of the membrane bound alpha chain. Tacrolimus 0-5 interleukin 2 Homo sapiens 63-76 1911152-9 1991 Unfortunately, one of the most effective ingredients of such combination therapies in animal models (anti-CD4) appears to have its tolerogenic potential abrogated by cyclosporin A and FK-506. Tacrolimus 184-190 CD4 molecule Homo sapiens 106-109 1716797-13 1991 Higher doses of FK506 produced a significant delay in glucose disappearance in groups 3 and 4, and a significant inhibition of glucose-mediated C-peptide response in group 4. Tacrolimus 16-21 insulin Homo sapiens 144-153 1715094-4 1991 An FKBP-rapamycin complex is concluded to be the toxic agent because (i) strains that lack FKBP proline rotamase, encoded by FPR1, were viable and fully resistant to rapamycin and (ii) FK506 antagonized rapamycin toxicity in vivo. Tacrolimus 185-190 peptidylprolyl isomerase FPR1 Saccharomyces cerevisiae S288C 125-129 1722778-9 1991 On the other hand, the number of CD4+ CD8+ thymocytes did not decrease significantly in the 0.3 mg/kg/day-treated group, whereas it did decrease significantly in the 1 mg/kg/day-treated group, decreased further with the increase in dosage of FK-506, and decreased markedly in the 30 mg/kg/day group, The number of CD4-CD8-thymocytes did not show any change, even in the high-dosage groups. Tacrolimus 242-248 CD4 antigen Mus musculus 33-36 1712484-1 1991 Investigations of the actions and interactions of the immunophilin ligands FK506, cyclosporin A (CsA), rapamycin, and 506BD suggest that complexes of FK506 with an FK506-binding protein or of CsA with a cyclophilin (CsA-binding protein) inhibit the T-cell receptor-mediated signal transduction that results in the transcription of interleukin 2. Tacrolimus 150-155 interleukin 2 Rattus norvegicus 331-344 1712901-0 1991 The immunosuppressant FK-506 specifically inhibits mitogen-induced activation of the interleukin-2 promoter and the isolated enhancer elements NFIL-2A and NF-AT1. Tacrolimus 22-28 interleukin 2 Homo sapiens 85-98 1712901-0 1991 The immunosuppressant FK-506 specifically inhibits mitogen-induced activation of the interleukin-2 promoter and the isolated enhancer elements NFIL-2A and NF-AT1. Tacrolimus 22-28 nuclear factor of activated T cells 2 Homo sapiens 155-161 1712901-1 1991 The macrolide FK-506, like the cyclic undecapeptide cyclosporin A (CsA), is a potent immunosuppressant that interferes with the transcriptional activation of several early-phase genes in T lymphocytes, including that for interleukin-2 (IL-2). Tacrolimus 14-20 interleukin 2 Homo sapiens 221-234 1712901-1 1991 The macrolide FK-506, like the cyclic undecapeptide cyclosporin A (CsA), is a potent immunosuppressant that interferes with the transcriptional activation of several early-phase genes in T lymphocytes, including that for interleukin-2 (IL-2). Tacrolimus 14-20 interleukin 2 Homo sapiens 236-240 1712901-2 1991 We compared the effects of FK-506 and CsA on transcription from the 5" upstream activating sequences (UAS) of the human IL-2 gene and several cellular and viral UAS to define cis-acting sites which may be responsive to FK-506. Tacrolimus 27-33 interleukin 2 Homo sapiens 120-124 1712901-7 1991 The induced transcription driven by the IL-2 promoter elements NF-AT1 and NFIL-2A could be blocked completely by FK-506 or CsA. Tacrolimus 113-119 interleukin 2 Homo sapiens 40-44 1712901-7 1991 The induced transcription driven by the IL-2 promoter elements NF-AT1 and NFIL-2A could be blocked completely by FK-506 or CsA. Tacrolimus 113-119 nuclear factor of activated T cells 2 Homo sapiens 63-69 1713687-6 1991 Therefore, the three-dimensional structures of FKBP-12 and the FKBP-12/FK506 complex are likely to be excellent models of the corresponding FKBP-13 structure. Tacrolimus 71-76 FKBP prolyl isomerase 1A Homo sapiens 47-54 1713687-6 1991 Therefore, the three-dimensional structures of FKBP-12 and the FKBP-12/FK506 complex are likely to be excellent models of the corresponding FKBP-13 structure. Tacrolimus 71-76 FKBP prolyl isomerase 1A Homo sapiens 63-70 1713687-6 1991 Therefore, the three-dimensional structures of FKBP-12 and the FKBP-12/FK506 complex are likely to be excellent models of the corresponding FKBP-13 structure. Tacrolimus 71-76 FKBP prolyl isomerase 2 Homo sapiens 140-147 1712484-1 1991 Investigations of the actions and interactions of the immunophilin ligands FK506, cyclosporin A (CsA), rapamycin, and 506BD suggest that complexes of FK506 with an FK506-binding protein or of CsA with a cyclophilin (CsA-binding protein) inhibit the T-cell receptor-mediated signal transduction that results in the transcription of interleukin 2. Tacrolimus 150-155 interleukin 2 Rattus norvegicus 331-344 1715317-0 1991 Comparison of the effects of FK-506, cyclosporin A and rapamycin on IL-2 production. Tacrolimus 29-35 interleukin 2 Homo sapiens 68-72 1717376-1 1991 Cyclosporin (CsA) and FK-506 are structurally distinct fungal metabolites, which exert powerful inhibitory effects on CD4+ T (helper) cell activation and on the secretion of interleukin-2 (IL-2) and other cytokines, including various cell growth factors and interferon-gamma. Tacrolimus 22-28 interleukin 2 Homo sapiens 174-187 1717376-1 1991 Cyclosporin (CsA) and FK-506 are structurally distinct fungal metabolites, which exert powerful inhibitory effects on CD4+ T (helper) cell activation and on the secretion of interleukin-2 (IL-2) and other cytokines, including various cell growth factors and interferon-gamma. Tacrolimus 22-28 interleukin 2 Homo sapiens 189-193 1717376-1 1991 Cyclosporin (CsA) and FK-506 are structurally distinct fungal metabolites, which exert powerful inhibitory effects on CD4+ T (helper) cell activation and on the secretion of interleukin-2 (IL-2) and other cytokines, including various cell growth factors and interferon-gamma. Tacrolimus 22-28 interferon gamma Homo sapiens 258-274 1717376-8 1991 Compared with CsA, the inhibitory action of FK-506 appears more difficult to reverse, e.g., in response to pre-formed IL-2. Tacrolimus 44-50 interleukin 2 Homo sapiens 118-122 1709302-4 1991 The nature of this complex has implications for the mechanism of rotamase catalysis and for the biological actions of FK506 and rapamycin. Tacrolimus 118-123 FKBP prolyl isomerase 10 Homo sapiens 65-73 1715185-0 1991 Cyclosporin A and FK-506 both affect DNA binding of regulatory nuclear proteins to the human interleukin-2 promoter. Tacrolimus 18-24 interleukin 2 Homo sapiens 93-106 1710844-0 1991 Evidence that FK506 and rapamycin block T cell activation at different sites relative to early reversible phosphorylation involving the protein phosphatases PP1 and PP2A. Tacrolimus 14-19 inorganic pyrophosphatase 1 Homo sapiens 157-160 1710844-0 1991 Evidence that FK506 and rapamycin block T cell activation at different sites relative to early reversible phosphorylation involving the protein phosphatases PP1 and PP2A. Tacrolimus 14-19 protein phosphatase 2 phosphatase activator Homo sapiens 165-169 1707760-3 1991 Using measurements of the proliferative response, IL-2 production, and changes in intracellular Ca2+ ([Ca2+]i), we demonstrate that FK-506 exerts its inhibitory effect on early events of T-cell activation in a manner indistinguishable from that of CsA. Tacrolimus 132-138 interleukin 2 Homo sapiens 50-54 1706398-0 1991 FK-506, a potent novel inhibitor of the release of proinflammatory mediators from human Fc epsilon RI+ cells. Tacrolimus 0-6 Fc epsilon receptor Ia Homo sapiens 88-101 1706398-9 1991 IL-3 (3 and 10 ng/ml), but not IL-1 beta (10 and 100 ng/ml), reversed the inhibitory effect of both FK-506 and CsA on basophils challenged with anti-IgE or A23187. Tacrolimus 100-106 interleukin 3 Homo sapiens 0-4 1715185-1 1991 The structurally unrelated immunosuppressive drugs cyclosporin A (Sandimmun) and FK-506 both interfere with the process of T-cell proliferation by blocking the transcription of the T-cell growth factor interleukin-2 (IL-2). Tacrolimus 81-87 interleukin 2 Homo sapiens 202-215 1715185-1 1991 The structurally unrelated immunosuppressive drugs cyclosporin A (Sandimmun) and FK-506 both interfere with the process of T-cell proliferation by blocking the transcription of the T-cell growth factor interleukin-2 (IL-2). Tacrolimus 81-87 interleukin 2 Homo sapiens 217-221 1715185-3 1991 We present evidence that the binding by regulatory nuclear proteins to the kappa B element of the IL-2 promoter is affected negatively by cyclosporin A and FK-506 at concentrations paralleling their immunosuppressive activity in vivo. Tacrolimus 156-162 interleukin 2 Homo sapiens 98-102 1715185-5 1991 FK-506 is 10 to 100 times more potent than cyclosporin A in its ability to inhibit sequence-specific DNA binding and IL-2 production. Tacrolimus 0-6 interleukin 2 Homo sapiens 117-121 1705713-8 1991 Overexpression or disruption of FPR1 confers resistance to growth inhibition by FK 506, suggesting that FKBP is a target for FK 506 in yeast. Tacrolimus 80-86 peptidylprolyl isomerase FPR1 Saccharomyces cerevisiae S288C 32-36 1701825-5 1990 Therefore, CSA and FK506, while chemically different, seem to act upon a similar pathway that leads to IL-2 gene expression, whereas glucocorticoids do not affect this pathway. Tacrolimus 19-24 interleukin 2 Homo sapiens 103-107 1703047-0 1991 Effects of an immunosuppressant, FK506, on interleukin 1 alpha production by human macrophages and a macrophage-like cell line, U937. Tacrolimus 33-38 interleukin 1 alpha Homo sapiens 43-62 1703047-3 1991 FK506 partially suppressed IL-1 alpha release, from macrophage-like U937 cells stimulated with phorbol myristate acetate and from human monocytes and alveolar macrophages activated with lipopolysaccharide, in a dose-dependent manner. Tacrolimus 0-5 interleukin 1 alpha Homo sapiens 27-37 1703047-4 1991 Moreover, it was indicated that FK506 suppressed not only IL-1 release but also IL-1 synthesis itself, by measurement of cell-associated IL-1 alpha of U937 cells. Tacrolimus 32-37 interleukin 1 alpha Homo sapiens 58-62 1703047-4 1991 Moreover, it was indicated that FK506 suppressed not only IL-1 release but also IL-1 synthesis itself, by measurement of cell-associated IL-1 alpha of U937 cells. Tacrolimus 32-37 interleukin 1 alpha Homo sapiens 80-84 1703047-4 1991 Moreover, it was indicated that FK506 suppressed not only IL-1 release but also IL-1 synthesis itself, by measurement of cell-associated IL-1 alpha of U937 cells. Tacrolimus 32-37 interleukin 1 alpha Homo sapiens 137-147 1703047-5 1991 The optimal concentrations of FK506 for suppressing IL-1 alpha did not affect cell viability or proliferation, and were 10- to 100-fold lower than those of cyclosporin A. Tacrolimus 30-35 interleukin 1 alpha Homo sapiens 52-62 1703047-6 1991 It is concluded that FK506 affects macrophage physiology, suppressing IL-1 alpha production significantly. Tacrolimus 21-26 interleukin 1 alpha Homo sapiens 70-80 1705513-1 1991 Structurally unrelated, FK-506 and cyclosporin (CsA) bind to and inhibit the action of distinct cytoplasmic receptors, FK-506-binding protein (FKBP) and cyclophilin (CyP), respectively. Tacrolimus 24-30 peptidylprolyl isomerase G Homo sapiens 153-164 1705513-1 1991 Structurally unrelated, FK-506 and cyclosporin (CsA) bind to and inhibit the action of distinct cytoplasmic receptors, FK-506-binding protein (FKBP) and cyclophilin (CyP), respectively. Tacrolimus 24-30 peptidylprolyl isomerase G Homo sapiens 166-169 1713361-4 1991 FK506 and CsA showed pharmacologic antagonism in inhibiting in vitro proliferation upon phytohemagglutinin, anti-CD3 antibody, and mixed lymphocyte reaction (MLR) stimulation, and interleukin 2 generation by activated normal human peripheral blood lymphocytes. Tacrolimus 0-5 interleukin 2 Homo sapiens 180-193 1705513-4 1991 We have shown that FK-506, like CsA, is able to inhibit T cell activation mediated not only by the T cell receptor-CD3 complex, but also via another surface molecule, CD2. Tacrolimus 19-25 CD2 molecule Homo sapiens 167-170 1707162-0 1991 The immunosuppressives FK 506 and cyclosporin A inhibit the generation of protein factors binding to the two purine boxes of the interleukin 2 enhancer. Tacrolimus 23-29 interleukin 2 Homo sapiens 129-142 1707162-1 1991 Like Cyclosporin A (CsA), the macrolide FK 506 is a potent immunosuppressive that inhibits early steps of T cell activation, including the synthesis of Interleukin 2 (II-2) and numerous other lymphokines. Tacrolimus 40-46 ERCC excision repair 8, CSA ubiquitin ligase complex subunit Homo sapiens 20-23 1707162-1 1991 Like Cyclosporin A (CsA), the macrolide FK 506 is a potent immunosuppressive that inhibits early steps of T cell activation, including the synthesis of Interleukin 2 (II-2) and numerous other lymphokines. Tacrolimus 40-46 interleukin 2 Homo sapiens 152-165 1707162-1 1991 Like Cyclosporin A (CsA), the macrolide FK 506 is a potent immunosuppressive that inhibits early steps of T cell activation, including the synthesis of Interleukin 2 (II-2) and numerous other lymphokines. Tacrolimus 40-46 interleukin 2 Homo sapiens 167-171 1707162-3 1991 At concentrations that block T cell activation, FK 506 and CsA inhibit the proto-enhancer activity of Purine boxes of the II-2 promoter and the generation of lymphocyte-specific factors binding to the Purine boxes. Tacrolimus 48-54 interleukin 2 Homo sapiens 122-126 1721613-11 1991 However, RAP (110 nM) reversed the apoptosis-inhibitory effect of FK-506, even if added 1-2 h after the latter to the cultures. Tacrolimus 66-72 regulatory associated protein of MTOR, complex 1 Mus musculus 9-12 1721613-12 1991 Consistent with this antagonism, RAP also reversed the binding of a radiolabeled derivative of FK-506 in DO-11.10 cells. Tacrolimus 95-101 regulatory associated protein of MTOR, complex 1 Mus musculus 33-36 1702372-1 1990 The effect of administration of FK506 at 1 mg/kg body weight for 14 days on rat lymphoid tissues, especially the thymus, and recovery after discontinuation of treatment, were investigated by the immunoperoxidase technique and flow cytofluorometry using monoclonal antibodies OX6, OX7, OX8, OX18 and W3/25, reactive with rat lymphocytes. Tacrolimus 32-37 Cd4 molecule Rattus norvegicus 299-304 1702372-6 1990 Flow cytometric analysis of the thymus showed that the percentages of cells labelled positively with OX7, OX8 and W3/25 were increased with FK506 treatment, and recovered to the normal level soon after withdrawal. Tacrolimus 140-145 Cd4 molecule Rattus norvegicus 114-119 1702372-7 1990 Furthermore, the peak of fluorescence intensity of OX7+, OX8+ and W3/25+ cells showed a temporary shift to the right during FK506 treatment; however, the peak of fluorescence intensity of OX18+ cells showed a temporary shift to the left. Tacrolimus 124-129 Cd4 molecule Rattus norvegicus 66-71 1702375-6 1990 Either CyA or FK506 significantly reduced the number of cells expressing OX-39 (interleukin-2 receptors) and OX-40. Tacrolimus 14-19 interleukin 2 Mus musculus 80-93 1702375-6 1990 Either CyA or FK506 significantly reduced the number of cells expressing OX-39 (interleukin-2 receptors) and OX-40. Tacrolimus 14-19 tumor necrosis factor receptor superfamily, member 4 Mus musculus 109-114 1702375-8 1990 In contrast, the absolute spleen cell numbers of OX-19+, W3/25+ and OX-8+ cells were significantly reduced in transfused animals given 14 days of FK506 treatment, while the corresponding blood cells were unaffected. Tacrolimus 146-151 AF4/FMR2 family, member 2 Mus musculus 49-54 1702408-3 1990 It was found that spleens from S-antigen-immunized and FK506-treated rats contained a population of Ts cells inhibiting the proliferative responses of S-antigen-sensitized lymphocytes to S-antigen, yet these cells did not affect the proliferative responses of interphotoreceptor retinoid-binding protein (IRBP)-sensitized lymphocytes to IRBP. Tacrolimus 55-60 S-antigen visual arrestin Rattus norvegicus 151-160 1702408-3 1990 It was found that spleens from S-antigen-immunized and FK506-treated rats contained a population of Ts cells inhibiting the proliferative responses of S-antigen-sensitized lymphocytes to S-antigen, yet these cells did not affect the proliferative responses of interphotoreceptor retinoid-binding protein (IRBP)-sensitized lymphocytes to IRBP. Tacrolimus 55-60 S-antigen visual arrestin Rattus norvegicus 151-160 1702408-3 1990 It was found that spleens from S-antigen-immunized and FK506-treated rats contained a population of Ts cells inhibiting the proliferative responses of S-antigen-sensitized lymphocytes to S-antigen, yet these cells did not affect the proliferative responses of interphotoreceptor retinoid-binding protein (IRBP)-sensitized lymphocytes to IRBP. Tacrolimus 55-60 retinol binding protein 3 Rattus norvegicus 260-303 1702408-3 1990 It was found that spleens from S-antigen-immunized and FK506-treated rats contained a population of Ts cells inhibiting the proliferative responses of S-antigen-sensitized lymphocytes to S-antigen, yet these cells did not affect the proliferative responses of interphotoreceptor retinoid-binding protein (IRBP)-sensitized lymphocytes to IRBP. Tacrolimus 55-60 retinol binding protein 3 Rattus norvegicus 305-309 1702408-3 1990 It was found that spleens from S-antigen-immunized and FK506-treated rats contained a population of Ts cells inhibiting the proliferative responses of S-antigen-sensitized lymphocytes to S-antigen, yet these cells did not affect the proliferative responses of interphotoreceptor retinoid-binding protein (IRBP)-sensitized lymphocytes to IRBP. Tacrolimus 55-60 retinol binding protein 3 Rattus norvegicus 337-341 1702408-5 1990 Furthermore, transfer of Ts cells from S-antigen-immunized and FK506-treated rats to naive syngenic rats induced partial inhibition of EAU induction or delay of EAU onset after immunizing the recipient rats with S-antigen. Tacrolimus 63-68 S-antigen visual arrestin Rattus norvegicus 212-221 1702408-7 1990 These data thus indicate that FK506 treatment after S-antigen immunization induces an activation of Ts cells specific to S-antigen and that the Ts cells might contribute, at least in part, to the uniquely prolonged and intensive immunosuppression by FK506. Tacrolimus 30-35 S-antigen visual arrestin Rattus norvegicus 52-61 1702408-7 1990 These data thus indicate that FK506 treatment after S-antigen immunization induces an activation of Ts cells specific to S-antigen and that the Ts cells might contribute, at least in part, to the uniquely prolonged and intensive immunosuppression by FK506. Tacrolimus 30-35 S-antigen visual arrestin Rattus norvegicus 121-130 2123553-2 1990 On the other hand, interleukin 2 (IL-2)-induced signals are blocked by rapamycin but not by FK506. Tacrolimus 92-97 interleukin 2 Homo sapiens 34-38 2123553-5 1990 However, an excess of rapamycin is needed to revert FK506-mediated inhibition of IL-2 production, apoptosis, and transcriptional activation of NF-AT, a T-cell-specific transcription factor necessary for IL-2 gene activation. Tacrolimus 52-57 interleukin 2 Homo sapiens 81-85 1701148-2 1990 First, rats actively immunized with S-antigen were treated with FK 506 only after the onset of EAU. Tacrolimus 64-70 S-antigen visual arrestin Rattus norvegicus 36-45 2123553-5 1990 However, an excess of rapamycin is needed to revert FK506-mediated inhibition of IL-2 production, apoptosis, and transcriptional activation of NF-AT, a T-cell-specific transcription factor necessary for IL-2 gene activation. Tacrolimus 52-57 interleukin 2 Homo sapiens 203-207 2123553-6 1990 Similarly, an excess of FK506 is needed to revert rapamycin-mediated inhibition of IL-2-induced proliferation. Tacrolimus 24-29 interleukin 2 Homo sapiens 83-87 1701570-1 1990 The fungal metabolite FK506 was discovered because it shared an important property, the ability to inhibit production of IL-2, with another well-known immunosuppressive fungal metabolite, CsA. Tacrolimus 22-27 interleukin 2 Homo sapiens 121-125 1702750-5 1990 FK506 caused a dose-dependent inhibition of cell cycle-related induction of locomotor capacity both of anti-CD3-cultured T cells and IL-4-cultured B cells, with an ID50 of less than 1 ng per ml. Tacrolimus 0-5 interleukin 4 Homo sapiens 133-137 1701148-9 1990 The antibody levels to S-antigen, the antigen-specific proliferative responses of lymphocytes, and even the proliferative responses to Con A were markedly suppressed in the rats in which FK 506 was given only during the efferent limb of the immune response. Tacrolimus 187-193 S-antigen visual arrestin Rattus norvegicus 23-32 2282365-10 1990 The FK-506 binding protein also has a PPIase activity, and this activity is inhibited by FK-506. Tacrolimus 4-10 FKBP prolyl isomerase like Homo sapiens 38-44 1695378-2 1990 After the recent discovery that the cyclosporin A-binding protein cyclophilin is identical to peptidylprolyl cis-trans isomerase, a cellular binding protein for FK506 was found to be distinct from cyclophilin but to have the same enzymatic activity. Tacrolimus 161-166 FKBP prolyl isomerase 5 Homo sapiens 94-128 1726093-0 1991 Unexpected up-regulation of gene expression by cyclosporin A and FK-506 in a T-cell lymphoma: both immunosuppressants augment Ly-6E antigen induction by interferon-gamma in the presence of ionomycin. Tacrolimus 65-71 lymphocyte antigen 6 complex, locus E Mus musculus 126-131 1726093-0 1991 Unexpected up-regulation of gene expression by cyclosporin A and FK-506 in a T-cell lymphoma: both immunosuppressants augment Ly-6E antigen induction by interferon-gamma in the presence of ionomycin. Tacrolimus 65-71 interferon gamma Mus musculus 153-169 1726093-6 1991 Cyclosporin A or FK-506 also markedly affected Ly-6E induction when the cultures were co-treated with the calcium ionophore, ionomycin. Tacrolimus 17-23 lymphocyte antigen 6 complex, locus E Mus musculus 47-52 1726093-11 1991 Therefore, through mechanisms apparently related to those involved in their immunosuppressive action, both CsA and FK-506 convert the negative effect of ionomycin on IFN-gamma-mediated Ly-6E induction into an overall positive effect. Tacrolimus 115-121 interferon gamma Mus musculus 166-175 1726093-11 1991 Therefore, through mechanisms apparently related to those involved in their immunosuppressive action, both CsA and FK-506 convert the negative effect of ionomycin on IFN-gamma-mediated Ly-6E induction into an overall positive effect. Tacrolimus 115-121 lymphocyte antigen 6 complex, locus E Mus musculus 185-190 1689353-2 1990 FK-506 acts similarly to cyclosporin A (CsA) and prevents IL-2 production and IL-2R expression. Tacrolimus 0-6 interleukin 2 Mus musculus 58-62 1689353-2 1990 FK-506 acts similarly to cyclosporin A (CsA) and prevents IL-2 production and IL-2R expression. Tacrolimus 0-6 interleukin 2 receptor, alpha chain Mus musculus 78-83 1689353-6 1990 However, in the same system, RAP acted as a potent antagonist of FK-506 suppression. Tacrolimus 65-71 regulatory associated protein of MTOR, complex 1 Mus musculus 29-32 1689353-7 1990 RAP also blocked FK-506- but not CsA-mediated inhibition of IL-2 mRNA induction. Tacrolimus 17-23 regulatory associated protein of MTOR, complex 1 Mus musculus 0-3 1689353-8 1990 By using model systems sensitive to inhibition by RAP but not FK-506 we further demonstrated that FK-506 reciprocally behaves as an antagonist of RAP. Tacrolimus 98-104 regulatory associated protein of MTOR, complex 1 Mus musculus 50-53 1689353-8 1990 By using model systems sensitive to inhibition by RAP but not FK-506 we further demonstrated that FK-506 reciprocally behaves as an antagonist of RAP. Tacrolimus 98-104 regulatory associated protein of MTOR, complex 1 Mus musculus 146-149 1689353-9 1990 In one such model, the stimulation of splenic T cells with IL-2 + PMA, FK-506, but not CsA, reversed the suppressive effect of RAP on proliferation. Tacrolimus 71-77 interleukin 2 Mus musculus 59-63 1689353-9 1990 In one such model, the stimulation of splenic T cells with IL-2 + PMA, FK-506, but not CsA, reversed the suppressive effect of RAP on proliferation. Tacrolimus 71-77 regulatory associated protein of MTOR, complex 1 Mus musculus 127-130 1689353-10 1990 FK-506 also antagonized RAP-mediated inhibition with respect to the induction of Ly-6E Ag expression by IFN in YAC cells. Tacrolimus 0-6 regulatory associated protein of MTOR, complex 1 Mus musculus 24-27 1689353-10 1990 FK-506 also antagonized RAP-mediated inhibition with respect to the induction of Ly-6E Ag expression by IFN in YAC cells. Tacrolimus 0-6 lymphocyte antigen 6 complex, locus E Mus musculus 81-86 1689694-7 1990 FACS analyses of the spleen cells revealed that FK506 reduced the percentage of double negative T cells (Thy-1.2+, Lyt-2-, L3T4-). Tacrolimus 48-53 acyl-CoA synthetase long-chain family member 1 Mus musculus 0-4 1690915-9 1990 In contrast to corresponding PHA-stimulated cells, FK-506-treated alloactivated lymphocytes exhibited reductions in IL-2R, TR and HLA-DR antigen expression, which in the cases of IL-2R and TR were further reduced by combination of FK-506 with low-concentration CsA. Tacrolimus 51-57 interleukin 2 receptor subunit alpha Homo sapiens 116-121 1690915-9 1990 In contrast to corresponding PHA-stimulated cells, FK-506-treated alloactivated lymphocytes exhibited reductions in IL-2R, TR and HLA-DR antigen expression, which in the cases of IL-2R and TR were further reduced by combination of FK-506 with low-concentration CsA. Tacrolimus 51-57 transferrin receptor Homo sapiens 123-125 1690915-9 1990 In contrast to corresponding PHA-stimulated cells, FK-506-treated alloactivated lymphocytes exhibited reductions in IL-2R, TR and HLA-DR antigen expression, which in the cases of IL-2R and TR were further reduced by combination of FK-506 with low-concentration CsA. Tacrolimus 51-57 interleukin 2 receptor subunit alpha Homo sapiens 179-184 1690915-9 1990 In contrast to corresponding PHA-stimulated cells, FK-506-treated alloactivated lymphocytes exhibited reductions in IL-2R, TR and HLA-DR antigen expression, which in the cases of IL-2R and TR were further reduced by combination of FK-506 with low-concentration CsA. Tacrolimus 51-57 transferrin receptor Homo sapiens 189-191 1690097-0 1990 Effects of a novel immunosuppressive agent, FK506, on human B cell activation. Tacrolimus 44-49 B cell linker Homo sapiens 60-77 1689694-7 1990 FACS analyses of the spleen cells revealed that FK506 reduced the percentage of double negative T cells (Thy-1.2+, Lyt-2-, L3T4-). Tacrolimus 48-53 CD8 antigen, alpha chain Mus musculus 115-120 1717008-7 1990 FK506 treatment resulted not only in the highest inhibition of expression of IL-2 receptors on T cells, but also in the prevention of the expression of MHC class II antigens on ocular resident cells. Tacrolimus 0-5 interleukin 2 Rattus norvegicus 77-81 1689226-8 1990 FK-506 also suppressed increases in the small proportion of blood-borne OX-40+ (activated CD4+) cells and OX-39+ (interleukin-2 receptor+) cells in the 7 day period following immunization; thereafter values for activation marker expression between treatment and control groups were similar. Tacrolimus 0-6 interleukin 2 Mus musculus 114-127 1688572-3 1990 FK-506 or CsA also inhibited proliferation, IL-2 production, and IL-2R expression in splenic T cells activated with ionomycin + PMA. Tacrolimus 0-6 interleukin 2 Mus musculus 44-48 1688572-3 1990 FK-506 or CsA also inhibited proliferation, IL-2 production, and IL-2R expression in splenic T cells activated with ionomycin + PMA. Tacrolimus 0-6 interleukin 2 receptor, alpha chain Mus musculus 65-70 1688572-8 1990 The proliferative response induced in D10.G4 cells by IL-1 + ionomycin but not that induced by IL-1 + PMA was sensitive to inhibition by FK-506 and CsA. Tacrolimus 137-143 interleukin 1 complex Mus musculus 54-58 1688572-10 1990 Finally, T cell proliferation driven by IL-2 or IL-4 was found to be relatively resistant to FK-506 or CsA but sensitive to RAP. Tacrolimus 93-99 interleukin 2 Mus musculus 40-44 1688572-10 1990 Finally, T cell proliferation driven by IL-2 or IL-4 was found to be relatively resistant to FK-506 or CsA but sensitive to RAP. Tacrolimus 93-99 interleukin 4 Mus musculus 48-52 33805042-6 2021 Interestingly, drugs widely used to treat skin inflammation, the calcineurin inhibitors tacrolimus and cyclosporine and the glucocorticoid dexamethasone, significantly decreased TRPA1 expression. Tacrolimus 88-98 transient receptor potential cation channel, subfamily A, member 1 Mus musculus 178-183 1696410-8 1990 Exogenous IL-2 or L3T4+ T cells could overcome the immunosuppressive effect of FK506 on the CTL induction of Ly2+ T cells in a secondary MLC. Tacrolimus 79-84 interleukin 2 Mus musculus 10-14 33808965-6 2021 Improved systemic and ovarian immune functions, endometrial progesterone receptor and coreceptor expressions and uterine vascular adaptation to pregnancy were among features of enhanced progesterone-receptor sensitivity in the low-dose tacrolimus-treated mouse model of the disease. Tacrolimus 236-246 progesterone receptor Mus musculus 60-81 33768546-13 2021 The haematocrit (HCT), postoperative time (POD) and CYP3A5*3 genotypes had a significant influence on TAC clearance when combined with WZC. Tacrolimus 102-105 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 52-58 33768546-15 2021 For patients carrying the CYP3A5*3/*3 allele and with 30% HCT, the required TAC dose to achieve target trough concentrations of 10-15 ng/ml was 4 mg twice daily (q12h). Tacrolimus 76-79 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 26-32 33768546-16 2021 For patients with the CYP3A5*3/*3 allele, the required dose was 3 mg TAC q12h when combined with WZC, and for patients with the CYP3A5*1/*1 or *1/*3 allele, the required dose was 4 mg of TAC q12h when co-administered with WZC. Tacrolimus 69-72 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 22-28 33768546-16 2021 For patients with the CYP3A5*3/*3 allele, the required dose was 3 mg TAC q12h when combined with WZC, and for patients with the CYP3A5*1/*1 or *1/*3 allele, the required dose was 4 mg of TAC q12h when co-administered with WZC. Tacrolimus 187-190 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 128-134 33768546-17 2021 WHAT IS NEW AND CONCLUSION: Wuzhi Capsule co-administration and CYP3A5 variants affect the PK of TAC Dosing guidelines are made based on the PPK model to allow individualized administration of TAC, especially when co-administered with WZC. Tacrolimus 97-100 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 64-70 33768546-17 2021 WHAT IS NEW AND CONCLUSION: Wuzhi Capsule co-administration and CYP3A5 variants affect the PK of TAC Dosing guidelines are made based on the PPK model to allow individualized administration of TAC, especially when co-administered with WZC. Tacrolimus 193-196 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 64-70 33777956-0 2021 Treatment With Calcineurin Inhibitor FK506 Attenuates Noise-Induced Hearing Loss. Tacrolimus 37-42 calcineurin binding protein 1 Mus musculus 15-36 33777956-5 2021 In agreement with our previous finding that autophagy marker microtubule-associated protein light chain 3B (LC3B) does not change in OHCs under conditions of moderate-noise-induced permanent threshold shifts, treatment with FK506 increases LC3B immunolabeling in OHCs after exposure to moderate noise. Tacrolimus 224-229 microtubule-associated protein 1 light chain 3 beta Mus musculus 108-112 33777956-5 2021 In agreement with our previous finding that autophagy marker microtubule-associated protein light chain 3B (LC3B) does not change in OHCs under conditions of moderate-noise-induced permanent threshold shifts, treatment with FK506 increases LC3B immunolabeling in OHCs after exposure to moderate noise. Tacrolimus 224-229 microtubule-associated protein 1 light chain 3 beta Mus musculus 240-244 33777956-6 2021 Additionally, prevention of NIHL by treatment with FK506 was partially abolished by pretreatment with LC3B small interfering RNA. Tacrolimus 51-56 microtubule-associated protein 1 light chain 3 beta Mus musculus 102-106 30011421-3 2018 METHODS: In this retrospective case series, we identified consecutive CTD-ILD patients treated with tacrolimus plus intravenous (i.v.) Tacrolimus 100-110 CTD Homo sapiens 70-73 30011421-10 2018 CONCLUSION: In our cohort of CTD-ILD, two courses of pulse dose methylprednisolone therapy followed by prednisone and oral tacrolimus appeared to be well tolerated, and to have multidimensional efficacy. Tacrolimus 123-133 CTD Homo sapiens 29-32 19855314-0 2009 Time of drug administration, CYP3A5 and ABCB1 genotypes, and analytical method influence tacrolimus pharmacokinetics: a population pharmacokinetic study. Tacrolimus 89-99 ATP binding cassette subfamily B member 1 Homo sapiens 40-45 27011912-1 2016 Tacrolimus (Prograf( ), Astellas Pharma Europe Ltd, Staines, United Kingdom; referred to as tacrolimus-BID) is an immunosuppressive agent to prevent and treat allograft rejection in kidney transplant recipients in combination with mycophenolate mofetil, corticosteroids, with or without basiliximab induction. Tacrolimus 0-10 BH3 interacting domain death agonist Homo sapiens 103-106 27011912-1 2016 Tacrolimus (Prograf( ), Astellas Pharma Europe Ltd, Staines, United Kingdom; referred to as tacrolimus-BID) is an immunosuppressive agent to prevent and treat allograft rejection in kidney transplant recipients in combination with mycophenolate mofetil, corticosteroids, with or without basiliximab induction. Tacrolimus 12-19 BH3 interacting domain death agonist Homo sapiens 103-106 27011912-1 2016 Tacrolimus (Prograf( ), Astellas Pharma Europe Ltd, Staines, United Kingdom; referred to as tacrolimus-BID) is an immunosuppressive agent to prevent and treat allograft rejection in kidney transplant recipients in combination with mycophenolate mofetil, corticosteroids, with or without basiliximab induction. Tacrolimus 92-102 BH3 interacting domain death agonist Homo sapiens 103-106 27011912-4 2016 Extended release tacrolimus has similar absorption, distribution, metabolism and excretion to tacrolimus-BID. Tacrolimus 94-104 BH3 interacting domain death agonist Homo sapiens 105-108 27011912-5 2016 Phase I pharmacokinetic trials comparing extended release tacrolimus and tacrolimus-BID have demonstrated a decreased maximum concentration (Cmax) and delayed time to maximum concentration (tmax) with the extended release formulation; however, AUC0-24 was comparable between formulations. Tacrolimus 73-83 BH3 interacting domain death agonist Homo sapiens 84-87 27011912-6 2016 Overall extended release tacrolimus has a very similar safety and efficacy profile to tacrolimus-BID. Tacrolimus 86-96 BH3 interacting domain death agonist Homo sapiens 97-100 19709321-8 2009 Increased tacrolimus half-life and increased dose interval of sirolimus and tacrolimus were due to CYP3A4/5 and/or P-glycoprotein inhibition by protease inhibitors. Tacrolimus 10-20 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 99-105 19709321-8 2009 Increased tacrolimus half-life and increased dose interval of sirolimus and tacrolimus were due to CYP3A4/5 and/or P-glycoprotein inhibition by protease inhibitors. Tacrolimus 10-20 ATP binding cassette subfamily B member 1 Homo sapiens 115-129 19709321-8 2009 Increased tacrolimus half-life and increased dose interval of sirolimus and tacrolimus were due to CYP3A4/5 and/or P-glycoprotein inhibition by protease inhibitors. Tacrolimus 76-86 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 99-105 19709321-8 2009 Increased tacrolimus half-life and increased dose interval of sirolimus and tacrolimus were due to CYP3A4/5 and/or P-glycoprotein inhibition by protease inhibitors. Tacrolimus 76-86 ATP binding cassette subfamily B member 1 Homo sapiens 115-129 17986100-2 2007 We report a 50-year-old Japanese man with anti-MuSK antibody-positive MG, who showed no or poor response to various therapies, including plasmapheresis, corticosteroid, and tacrolimus. Tacrolimus 173-183 muscle associated receptor tyrosine kinase Homo sapiens 47-51 7512015-9 1994 Water-immersion stress significantly increased myeloperoxidase activity in gastric mucosa, and FK506 reduced the increase in myeloperoxidase activity induced by stress. Tacrolimus 95-100 myeloperoxidase Rattus norvegicus 125-140 34785307-2 2022 FK-506 caused a significant attenuation in the proliferation of allogeneic CD4+ T cells and IFN-gamma secreting effector functions. Tacrolimus 0-6 Cd4 molecule Rattus norvegicus 75-78 34785307-2 2022 FK-506 caused a significant attenuation in the proliferation of allogeneic CD4+ T cells and IFN-gamma secreting effector functions. Tacrolimus 0-6 interferon gamma Rattus norvegicus 92-101 34922024-9 2022 In terms of the predictors of GI symptoms, it was determined that mycophenolate mofetil (MMF) was effective in the development of reflux and diarrhoea, cyclosporine in the development of diarrhoea and constipation, and tacrolimus in the development of indigestion, which are (p < 0.05). Tacrolimus 219-229 G protein subunit alpha i1 Homo sapiens 30-32 34688813-0 2022 CYP3A7, CYP3A4, and CYP3A5 genetic polymorphisms in recipients rather than donors influence tacrolimus concentrations in the early stages after liver transplantation. Tacrolimus 92-102 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 0-6 34688813-1 2022 AIM: The purpose of this study was to investigate the effect of CYP3A7, CYP3A4, and CYP3A5 genetic polymorphisms in liver transplant recipients and donors on tacrolimus concentrations in the early stages after liver transplantation. Tacrolimus 158-168 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 64-70 34688813-1 2022 AIM: The purpose of this study was to investigate the effect of CYP3A7, CYP3A4, and CYP3A5 genetic polymorphisms in liver transplant recipients and donors on tacrolimus concentrations in the early stages after liver transplantation. Tacrolimus 158-168 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-78 34688813-1 2022 AIM: The purpose of this study was to investigate the effect of CYP3A7, CYP3A4, and CYP3A5 genetic polymorphisms in liver transplant recipients and donors on tacrolimus concentrations in the early stages after liver transplantation. Tacrolimus 158-168 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 84-90 34688813-4 2022 RESULTS: Recipient CYP3A polymorphisms were associated with tacrolimus concentrations. Tacrolimus 60-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 19-24 34688813-7 2022 Regardless of the genotype of the matched donor, CYP3A7 rs10211, CYP3A4*1G (rs2242480), and CYP3A5*3 (rs776746) polymorphisms of recipients could affect tacrolimus concentrations. Tacrolimus 153-163 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 49-55 34688813-7 2022 Regardless of the genotype of the matched donor, CYP3A7 rs10211, CYP3A4*1G (rs2242480), and CYP3A5*3 (rs776746) polymorphisms of recipients could affect tacrolimus concentrations. Tacrolimus 153-163 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 65-71 34688813-7 2022 Regardless of the genotype of the matched donor, CYP3A7 rs10211, CYP3A4*1G (rs2242480), and CYP3A5*3 (rs776746) polymorphisms of recipients could affect tacrolimus concentrations. Tacrolimus 153-163 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 92-98 34688813-8 2022 For the CYP3A4 rs4646437 polymorphisms, when the donor carried CYP3A4 rs4646437 CC, the recipient CYP3A4 rs4646437 polymorphism was associated with the C0/D of tacrolimus, and when the donor carried CYP3A4 rs4646437 CT/TT genotype, the recipient CYP3A4 rs4646437 polymorphism also affected on tacrolimus C0/D, although the effect was not significant. Tacrolimus 160-170 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 98-104 34688813-8 2022 For the CYP3A4 rs4646437 polymorphisms, when the donor carried CYP3A4 rs4646437 CC, the recipient CYP3A4 rs4646437 polymorphism was associated with the C0/D of tacrolimus, and when the donor carried CYP3A4 rs4646437 CT/TT genotype, the recipient CYP3A4 rs4646437 polymorphism also affected on tacrolimus C0/D, although the effect was not significant. Tacrolimus 293-303 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 246-252 34688813-9 2022 CONCLUSION: The large inter-individual variation in tacrolimus concentrations in the early stages after liver transplantation is influenced by genetic polymorphisms of CYP3A7, CYP3A4, and CYP3A5. Tacrolimus 52-62 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 168-174 34688813-9 2022 CONCLUSION: The large inter-individual variation in tacrolimus concentrations in the early stages after liver transplantation is influenced by genetic polymorphisms of CYP3A7, CYP3A4, and CYP3A5. Tacrolimus 52-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 176-182 34688813-9 2022 CONCLUSION: The large inter-individual variation in tacrolimus concentrations in the early stages after liver transplantation is influenced by genetic polymorphisms of CYP3A7, CYP3A4, and CYP3A5. Tacrolimus 52-62 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 188-194 34688813-11 2022 Therefore, the detection of CYP3A polymorphisms in recipients could help to predict the tacrolimus starting dose in the early stages after liver transplantation. Tacrolimus 88-98 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 28-33 34781138-0 2022 Trans-eQTLs of the CYP3A4 and CYP3A5 associated with tacrolimus trough blood concentration in Chinese renal transplant patients. Tacrolimus 53-63 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 19-25 34781138-0 2022 Trans-eQTLs of the CYP3A4 and CYP3A5 associated with tacrolimus trough blood concentration in Chinese renal transplant patients. Tacrolimus 53-63 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 30-36 34781138-1 2022 This study aimed to systematically investigate trans-eQTLs of CYP3A4 and CYP3A5 affecting tacrolimus trough blood concentrations in Chinese renal transplant patients. Tacrolimus 90-100 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 62-68 34781138-1 2022 This study aimed to systematically investigate trans-eQTLs of CYP3A4 and CYP3A5 affecting tacrolimus trough blood concentrations in Chinese renal transplant patients. Tacrolimus 90-100 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 73-79 34780122-10 2022 Two and three sampling points limited sampling strategies: C0 , C2 , and C10 provide the most reliable and effective LSS for estimation of tacrolimus AUC0-24 in routine clinic use. Tacrolimus 139-149 homeobox C10 Homo sapiens 73-76 34875338-13 2022 The calcineurin inhibitor FK506 exhibited a Drp1-independent function that mitigated mitochondrial dysfunction. Tacrolimus 26-31 dynamin 1 like Homo sapiens 44-48 34875338-14 2022 Finally, we found that FK506 pretreatment ameliorated the neurite growth in neurons treated with TNF and the learning ability of mice after surgery. Tacrolimus 23-28 tumor necrosis factor Mus musculus 97-100 34889045-0 2022 Tacrolimus alleviates LPS-induced AKI by inhibiting TLR4/MyD88/NF-kappaB signalling in mice. Tacrolimus 0-10 toll-like receptor 4 Mus musculus 52-56 34889045-0 2022 Tacrolimus alleviates LPS-induced AKI by inhibiting TLR4/MyD88/NF-kappaB signalling in mice. Tacrolimus 0-10 myeloid differentiation primary response gene 88 Mus musculus 57-62 34889045-0 2022 Tacrolimus alleviates LPS-induced AKI by inhibiting TLR4/MyD88/NF-kappaB signalling in mice. Tacrolimus 0-10 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 63-72 34889045-5 2022 Moreover, the Toll-like receptor 4 (TLR4)/myeloid differential protein-88 (MyD88)/nuclear factor-kappa (NF-kappaB) signalling pathway was also dramatically inhibited by medium- and high-dose TAC administration at 12, 24 and 48 h of LPS treatment mice. Tacrolimus 191-194 toll-like receptor 4 Mus musculus 14-34 34889045-5 2022 Moreover, the Toll-like receptor 4 (TLR4)/myeloid differential protein-88 (MyD88)/nuclear factor-kappa (NF-kappaB) signalling pathway was also dramatically inhibited by medium- and high-dose TAC administration at 12, 24 and 48 h of LPS treatment mice. Tacrolimus 191-194 toll-like receptor 4 Mus musculus 36-40 34889045-5 2022 Moreover, the Toll-like receptor 4 (TLR4)/myeloid differential protein-88 (MyD88)/nuclear factor-kappa (NF-kappaB) signalling pathway was also dramatically inhibited by medium- and high-dose TAC administration at 12, 24 and 48 h of LPS treatment mice. Tacrolimus 191-194 myeloid differentiation primary response gene 88 Mus musculus 75-80 34889045-5 2022 Moreover, the Toll-like receptor 4 (TLR4)/myeloid differential protein-88 (MyD88)/nuclear factor-kappa (NF-kappaB) signalling pathway was also dramatically inhibited by medium- and high-dose TAC administration at 12, 24 and 48 h of LPS treatment mice. Tacrolimus 191-194 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 104-113 34889045-7 2022 Our findings indicate that TAC has protective effects against LPS-induced AKI by inhibiting TLR4/MyD88/NF-kappaB signalling pathway and podocyte dysfunction, providing another potential therapeutic effects for the LPS-induced SA-AKI. Tacrolimus 27-30 toll-like receptor 4 Mus musculus 92-96 34889045-7 2022 Our findings indicate that TAC has protective effects against LPS-induced AKI by inhibiting TLR4/MyD88/NF-kappaB signalling pathway and podocyte dysfunction, providing another potential therapeutic effects for the LPS-induced SA-AKI. Tacrolimus 27-30 myeloid differentiation primary response gene 88 Mus musculus 97-102 34889045-7 2022 Our findings indicate that TAC has protective effects against LPS-induced AKI by inhibiting TLR4/MyD88/NF-kappaB signalling pathway and podocyte dysfunction, providing another potential therapeutic effects for the LPS-induced SA-AKI. Tacrolimus 27-30 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 103-112 34583027-1 2022 BACKGROUND: CYP3A5 and CYP3A4 are the predominant enzymes responsible for tacrolimus metabolism, however only a proportion of the population expresses CYP3A5 secondary to genetic variation. Tacrolimus 74-84 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 12-18 34793770-0 2022 The mTOR inhibitor everolimus attenuates tacrolimus-induced renal interstitial fibrosis in rats. Tacrolimus 41-51 mechanistic target of rapamycin kinase Rattus norvegicus 4-8 34793770-2 2022 The mammalian target of rapamycin (mTOR) inhibitor, everolimus, is an immunosuppressant used together with tacrolimus. Tacrolimus 107-117 mechanistic target of rapamycin kinase Homo sapiens 4-33 34793770-2 2022 The mammalian target of rapamycin (mTOR) inhibitor, everolimus, is an immunosuppressant used together with tacrolimus. Tacrolimus 107-117 mechanistic target of rapamycin kinase Homo sapiens 35-39 34793770-7 2022 KEY FINDINGS: Tacrolimus administration increased predominant profibrotic cytokine transforming growth factor-beta (TGF-beta) and fibroblast activation marker alpha-smooth muscle actin (alpha-SMA) expression and promoted the infiltration of macrophages in the kidney cortex, resulting in renal interstitial fibrosis in rats. Tacrolimus 14-24 transforming growth factor alpha Rattus norvegicus 116-124 34793770-7 2022 KEY FINDINGS: Tacrolimus administration increased predominant profibrotic cytokine transforming growth factor-beta (TGF-beta) and fibroblast activation marker alpha-smooth muscle actin (alpha-SMA) expression and promoted the infiltration of macrophages in the kidney cortex, resulting in renal interstitial fibrosis in rats. Tacrolimus 14-24 actin gamma 2, smooth muscle Rattus norvegicus 159-184 34793770-8 2022 Tacrolimus increased serum creatinine, blood urea nitrogen, kidney injury molecule-1 (KIM-1), and kidney injuries, such as tubular dilation, vacuolization, and glomerular atrophy. Tacrolimus 0-10 hepatitis A virus cellular receptor 1 Rattus norvegicus 60-84 34793770-8 2022 Tacrolimus increased serum creatinine, blood urea nitrogen, kidney injury molecule-1 (KIM-1), and kidney injuries, such as tubular dilation, vacuolization, and glomerular atrophy. Tacrolimus 0-10 hepatitis A virus cellular receptor 1 Rattus norvegicus 86-91 34800514-0 2022 Impact of the ACE2 activator xanthenone on tacrolimus nephrotoxicity: Modulation of uric acid/ERK/p38 MAPK and Nrf2/SOD3/GCLC signaling pathways. Tacrolimus 43-53 angiotensin converting enzyme 2 Homo sapiens 14-18 34800514-0 2022 Impact of the ACE2 activator xanthenone on tacrolimus nephrotoxicity: Modulation of uric acid/ERK/p38 MAPK and Nrf2/SOD3/GCLC signaling pathways. Tacrolimus 43-53 mitogen-activated protein kinase 1 Homo sapiens 94-97 34800514-0 2022 Impact of the ACE2 activator xanthenone on tacrolimus nephrotoxicity: Modulation of uric acid/ERK/p38 MAPK and Nrf2/SOD3/GCLC signaling pathways. Tacrolimus 43-53 NFE2 like bZIP transcription factor 2 Homo sapiens 111-115 34800514-0 2022 Impact of the ACE2 activator xanthenone on tacrolimus nephrotoxicity: Modulation of uric acid/ERK/p38 MAPK and Nrf2/SOD3/GCLC signaling pathways. Tacrolimus 43-53 superoxide dismutase 3 Homo sapiens 116-120 34800514-0 2022 Impact of the ACE2 activator xanthenone on tacrolimus nephrotoxicity: Modulation of uric acid/ERK/p38 MAPK and Nrf2/SOD3/GCLC signaling pathways. Tacrolimus 43-53 glutamate-cysteine ligase catalytic subunit Homo sapiens 121-125 34800514-8 2022 Relative protein expressions of p-ERK/ERK and p-p38 MAPK/p38 MAPK inflammatory signals were downregulated upon xanthenone administration with tacrolimus. Tacrolimus 142-152 mitogen-activated protein kinase 1 Homo sapiens 34-37 34800514-8 2022 Relative protein expressions of p-ERK/ERK and p-p38 MAPK/p38 MAPK inflammatory signals were downregulated upon xanthenone administration with tacrolimus. Tacrolimus 142-152 mitogen-activated protein kinase 1 Homo sapiens 38-41 34800514-9 2022 In addition, xanthenone reinforced antioxidant defense against tacrolimus by enhancing protein expression of the transcription factor Nrf2 with subsequently increased mRNA expressions of the antioxidants SOD3 and GCLC. Tacrolimus 63-73 NFE2 like bZIP transcription factor 2 Homo sapiens 134-138 34583027-1 2022 BACKGROUND: CYP3A5 and CYP3A4 are the predominant enzymes responsible for tacrolimus metabolism, however only a proportion of the population expresses CYP3A5 secondary to genetic variation. Tacrolimus 74-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 23-29 34583027-2 2022 CYP3A5 is expressed in both the intestine and the liver and has been shown to impact both oral tacrolimus bioavailability and metabolism. Tacrolimus 95-105 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 34583027-4 2022 OBJECTIVE: The objective of this study was to evaluate the impact of CYP3A5 genotype as well as other pharmacogenes on IV tacrolimus exposure to determine whether the current genotype-guided dosing recommendations are appropriate for this formulation. Tacrolimus 122-132 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 69-75 34583027-5 2022 Additionally, this study aimed to investigate dose conversion requirements among CYP3A5 genotypes when converting from IV to PO tacrolimus. Tacrolimus 128-138 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 81-87 34583027-12 2022 RESULTS: CYP3A5 and CYP3A4 genotypes were significantly associated with the IV C/D with CYP3A5 expressers having 20% lower and CYP3A4 rapid metabolizers having 20% lower tacrolimus exposure. Tacrolimus 170-180 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 9-15 34583027-12 2022 RESULTS: CYP3A5 and CYP3A4 genotypes were significantly associated with the IV C/D with CYP3A5 expressers having 20% lower and CYP3A4 rapid metabolizers having 20% lower tacrolimus exposure. Tacrolimus 170-180 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 20-26 34583027-12 2022 RESULTS: CYP3A5 and CYP3A4 genotypes were significantly associated with the IV C/D with CYP3A5 expressers having 20% lower and CYP3A4 rapid metabolizers having 20% lower tacrolimus exposure. Tacrolimus 170-180 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 127-133 34977362-7 2021 AT-induced Bdnf mRNA expression was completely blocked by d-(-)-2-Amino-5-phosphonopentanoic acid but partially blocked by nicardipine, U0126, and FK506. Tacrolimus 147-152 brain-derived neurotrophic factor Rattus norvegicus 11-15 34809463-0 2021 Leveraging Fungal and Human Calcineurin-Inhibitor Structures, Biophysical Data, and Dynamics To Design Selective and Nonimmunosuppressive FK506 Analogs. Tacrolimus 138-143 calcineurin binding protein 1 Homo sapiens 28-49 34809463-3 2021 Harnessing fungal calcineurin-inhibitor crystal structures, we recently developed a less immunosuppressive FK506 analog, APX879, with broad-spectrum antifungal activity and demonstrable efficacy in a murine model of invasive fungal infection. Tacrolimus 107-112 calcineurin binding protein 1 Mus musculus 18-39 34809463-5 2021 To this end, we characterized high-resolution structures of the Mucor circinelloides FKBP12 bound to FK506 and of the Aspergillus fumigatus, M. circinelloides, and human FKBP12 proteins bound to the FK506 analog APX879, which exhibits enhanced selectivity for fungal pathogens. Tacrolimus 101-106 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 85-91 34809463-5 2021 To this end, we characterized high-resolution structures of the Mucor circinelloides FKBP12 bound to FK506 and of the Aspergillus fumigatus, M. circinelloides, and human FKBP12 proteins bound to the FK506 analog APX879, which exhibits enhanced selectivity for fungal pathogens. Tacrolimus 199-204 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 170-176 34809463-12 2021 By combining structural, genetic, biophysical, and in silico methodologies, we pinpoint regions of the FK506 scaffold and a less immunosuppressive analog, APX879, centered around the C15 to C18 and C36 to C37 positions that could be altered with selective extensions and/or deletions to enhance fungal selectivity. Tacrolimus 103-108 Bardet-Biedl syndrome 9 Homo sapiens 190-193 34912030-2 2021 While expression of ARNT can be pharmacologically induced by sub-immunosuppressive doses of FK506 or by GPI1046, its anti-fibrotic activity is only realized when ARNT-ARNT homodimers form, as opposed to formation of ARNT-AHR or ARNT-HIF1alpha heterodimers. Tacrolimus 92-97 aryl hydrocarbon receptor nuclear translocator Mus musculus 20-24 34912030-2 2021 While expression of ARNT can be pharmacologically induced by sub-immunosuppressive doses of FK506 or by GPI1046, its anti-fibrotic activity is only realized when ARNT-ARNT homodimers form, as opposed to formation of ARNT-AHR or ARNT-HIF1alpha heterodimers. Tacrolimus 92-97 aryl hydrocarbon receptor nuclear translocator Mus musculus 167-171 34912030-6 2021 In murine models of kidney fibrosis, and also of liver fibrosis, combinations of FK506 or GPI1046 (to induce ARNT expression) with LB100 (to enhance ARNT homodimerization) elicit additive anti-fibrotic activities. Tacrolimus 81-86 aryl hydrocarbon receptor nuclear translocator Mus musculus 109-113 34912030-6 2021 In murine models of kidney fibrosis, and also of liver fibrosis, combinations of FK506 or GPI1046 (to induce ARNT expression) with LB100 (to enhance ARNT homodimerization) elicit additive anti-fibrotic activities. Tacrolimus 81-86 aryl hydrocarbon receptor nuclear translocator Mus musculus 149-153 34911620-4 2022 The aim of this study was to determine retinal GCL thickness by means of OCT, analyzing the proportion of affected segments in individuals exposed to tacrolimus compared with a control group. Tacrolimus 150-160 germ cell-less 1, spermatogenesis associated Homo sapiens 47-50 34911620-10 2022 Linear regression analysis showed the presence of GCL segments with decreased thickness to be associated with the duration of exposure to tacrolimus (P = .036) and the time in dialysis before kidney transplant (P = .030). Tacrolimus 138-148 germ cell-less 1, spermatogenesis associated Homo sapiens 50-53 34911620-11 2022 CONCLUSION: Although this is a preliminary study, OCT scanning could serve to detect the neurotoxic effect of tacrolimus on the retinal GCL and central nervous system in renal transplant recipients. Tacrolimus 110-120 germ cell-less 1, spermatogenesis associated Homo sapiens 136-139 34950647-9 2021 Compared with the free drug at the same concentration, FK506 liposomes effectively inhibited vascular endothelial growth factor-induced green fluorescent protein-transduced human umbilical vein endothelial cell migration and tube formation in vitro. Tacrolimus 55-60 vascular endothelial growth factor A Homo sapiens 93-127 34956169-0 2021 Lactobacillus acidophilus Supplementation Exerts a Synergistic Effect on Tacrolimus Efficacy by Modulating Th17/Treg Balance in Lupus-Prone Mice via the SIGNR3 Pathway. Tacrolimus 73-83 CD209d antigen Mus musculus 153-159 34871120-12 2022 CONCLUSIONS: Reduced early tacrolimus exposure, facilitated by IL-2RA induction, was associated with reduced risk for HCC recurrence among patients outside Milan criteria. Tacrolimus 27-37 interleukin 2 receptor subunit alpha Homo sapiens 63-69 34938174-6 2021 We found that CYP3A5*3/*3 carriers required lower doses of TAC. Tacrolimus 59-62 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 14-20 34938174-7 2021 In TAC treated patients, most CYP3A5*3/*3 carriers presented higher C0/D and a high proportion of patients with C0 levels outside the therapeutic range relative to other genotypes. Tacrolimus 3-6 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 30-36 34797182-0 2021 Stratification of atopic dermatitis patients by patterns of response to proactive therapy with topical tacrolimus: low serum IgE levels and inadequately controlled disease activity at the start of treatment predict its failure. Tacrolimus 103-113 immunoglobulin heavy constant epsilon Homo sapiens 125-128 34859357-0 2022 The impact of cytochrome P450 3A5 genotype on early tacrolimus metabolism and clinical outcomes in lung transplant recipients. Tacrolimus 52-62 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 14-33 34859357-3 2022 Aim We aim to investigate the influence of cytochrome P450 3A5 (CYP3A5) genotypes on early post-LTx Tac metabolism and whether it is affected by concomitant use of azole antifungals. Tacrolimus 100-103 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 43-62 34859357-3 2022 Aim We aim to investigate the influence of cytochrome P450 3A5 (CYP3A5) genotypes on early post-LTx Tac metabolism and whether it is affected by concomitant use of azole antifungals. Tacrolimus 100-103 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 64-70 34859357-14 2022 Conclusion CYP3A5 genotype could affect Tac metabolism early after LTx. Tacrolimus 40-43 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 11-17 34797182-3 2021 In this study, we stratified AD patients by patterns of response to remission maintenance therapy (proactive therapy) with topical tacrolimus, a typical TCI. Tacrolimus 131-141 transcobalamin 1 Homo sapiens 153-156 34673300-0 2021 Combination of matrine and tacrolimus alleviates acute rejection in murine heart transplantation by inhibiting DCs maturation through ROS/ERK/NF-kappaB pathway. Tacrolimus 27-37 mitogen-activated protein kinase 1 Mus musculus 138-141 34432902-10 2021 FK506 dampened HS-induced loss of MTP and elevation of caspase-3 activity significantly (p<0.05). Tacrolimus 0-5 caspase 3 Rattus norvegicus 55-64 34432902-12 2021 The maintenance of the MTP and protection against caspase-3 mediated endothelial cell barrier disruption are possible mechanisms by which FK506 attenuates HS-induced hyperpermeability. Tacrolimus 138-143 caspase 3 Rattus norvegicus 50-59 34735949-0 2021 Computational validation of ABCB1 gene polymorphism and its effect on tacrolimus dose concentration/levels in renal transplant individuals of South India. Tacrolimus 70-80 ATP binding cassette subfamily B member 1 Homo sapiens 28-33 34120305-8 2021 Furthermore, the frequency of granzyme B+CD19+B cells correlated with the level of alanine aminotransferase instead of tacrolimus. Tacrolimus 119-129 CD19 molecule Homo sapiens 41-45 34673300-0 2021 Combination of matrine and tacrolimus alleviates acute rejection in murine heart transplantation by inhibiting DCs maturation through ROS/ERK/NF-kappaB pathway. Tacrolimus 27-37 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 142-151 34339091-6 2021 RESULTS: Despite persistent low tacrolimus trough levels in GSD1b patients, none of these children developed TCMR within 1 month after LDLT (GSD1b: 0/11 (0%) vs. BA: 86/273 (31.5%), p = .038). Tacrolimus 32-42 solute carrier family 37 member 4 Homo sapiens 60-65 34402788-1 2021 OBJECTIVE: The calcineurin inhibitor tacrolimus has been widely used to prevent allograft rejection after transplantation. Tacrolimus 37-47 calcineurin binding protein 1 Homo sapiens 15-36 34342024-1 2021 WHAT IS KNOWN AND OBJECTIVE: Tacrolimus (FK506), an effective and potent calcineurin inhibitor, is the cornerstone of immunosuppression after kidney transplantation. Tacrolimus 29-39 calcineurin binding protein 1 Homo sapiens 73-94 34342024-1 2021 WHAT IS KNOWN AND OBJECTIVE: Tacrolimus (FK506), an effective and potent calcineurin inhibitor, is the cornerstone of immunosuppression after kidney transplantation. Tacrolimus 41-46 calcineurin binding protein 1 Homo sapiens 73-94 34342024-11 2021 The CYP3A5 genotype showed clearly associated with tacrolimus C0 /D, whereas no significant difference was observed in patients with CYP3A4*1B, CYP3A4*22, ABCB1, ABCC2, POR*28 or PXR alleles. Tacrolimus 51-61 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 4-10 34695450-9 2021 Finally, an inhibitor of calcineurin,FK506, further increased Dicer1 protein compared to Abetao treatment alone. Tacrolimus 37-42 dicer 1, ribonuclease III Homo sapiens 62-68 34905302-2 2022 The main objective of this trial was to investigate whether tacrolimus IPV decreases after switching patients from IR-tacrolimus to either ER-tacrolimus or LCP-tacrolimus. Tacrolimus 60-70 kelch domain containing 2 Homo sapiens 156-159 34905302-2 2022 The main objective of this trial was to investigate whether tacrolimus IPV decreases after switching patients from IR-tacrolimus to either ER-tacrolimus or LCP-tacrolimus. Tacrolimus 160-170 kelch domain containing 2 Homo sapiens 156-159 34905302-8 2022 The IPV of LCP-tacrolimus (20.1%) was not significantly different from the IPV of ER-tacrolimus (16.5%) (%-difference +3.6%, 95%-CI -0.1%-7.3%, p=0.06). Tacrolimus 15-25 kelch domain containing 2 Homo sapiens 11-14 34905302-9 2022 In conclusion, the IPV did not decrease after switching from immediate-release tacrolimus to either ER-tacrolimus or LCP-tacrolimus. Tacrolimus 121-131 kelch domain containing 2 Homo sapiens 117-120 34339091-10 2021 CONCLUSIONS: We found that GSD1b recipients were more likely to develop postoperative bloodstream infection than recipients with BA but did not experience TCMR despite low tacrolimus levels in the early post-LDLT period. Tacrolimus 172-182 solute carrier family 37 member 4 Homo sapiens 27-32 34847842-11 2021 The officially accepted mTOR inhibitors that have undergone clinical testing are sirolimus, everolimus, temsirolimus, and tacrolimus. Tacrolimus 122-132 mechanistic target of rapamycin kinase Homo sapiens 24-28 34016023-8 2021 Finally, the risk of alopecia (p = 0.008), infection (p = 0.045), leukocytosis (p = 0.002), and elevated ALT/AST (p = 0.011) in TAC group was significantly lower than CTX group, whereas TAC was associated with an increased risk of tremor than CTX (p = 0.010). Tacrolimus 128-131 solute carrier family 17 member 5 Homo sapiens 109-112 34854174-3 2022 Tacrolimus can cause islet cell damage and decrease in insulin secretion which can lead to post-transplant diabetes mellitus and rarely diabetic ketoacidosis. Tacrolimus 0-10 insulin Homo sapiens 55-62 34668283-5 2021 With increasing concentrations of tacrolimus, there was a trend to reduction in the release of IL-2 (p = 0.0137), and IFN-gamma (p = 0.0147) in response to peptide stimulation. Tacrolimus 34-44 interleukin 2 Homo sapiens 95-99 34775880-3 2021 Calcineurin inhibitor tacrolimus (FK506) attenuated the MDI-GSH conjugate-mediated induction of CCL2, CCL3, CCL5, and CXCL8/IL8 but not others. Tacrolimus 22-32 chemokine (C-C motif) ligand 2 Mus musculus 96-100 34775880-3 2021 Calcineurin inhibitor tacrolimus (FK506) attenuated the MDI-GSH conjugate-mediated induction of CCL2, CCL3, CCL5, and CXCL8/IL8 but not others. Tacrolimus 22-32 chemokine (C-C motif) ligand 3 Mus musculus 102-106 34775880-3 2021 Calcineurin inhibitor tacrolimus (FK506) attenuated the MDI-GSH conjugate-mediated induction of CCL2, CCL3, CCL5, and CXCL8/IL8 but not others. Tacrolimus 22-32 chemokine (C-C motif) ligand 5 Mus musculus 108-112 34775880-3 2021 Calcineurin inhibitor tacrolimus (FK506) attenuated the MDI-GSH conjugate-mediated induction of CCL2, CCL3, CCL5, and CXCL8/IL8 but not others. Tacrolimus 22-32 chemokine (C-X-C motif) ligand 15 Mus musculus 124-127 34775880-3 2021 Calcineurin inhibitor tacrolimus (FK506) attenuated the MDI-GSH conjugate-mediated induction of CCL2, CCL3, CCL5, and CXCL8/IL8 but not others. Tacrolimus 34-39 chemokine (C-C motif) ligand 2 Mus musculus 96-100 34775880-3 2021 Calcineurin inhibitor tacrolimus (FK506) attenuated the MDI-GSH conjugate-mediated induction of CCL2, CCL3, CCL5, and CXCL8/IL8 but not others. Tacrolimus 34-39 chemokine (C-C motif) ligand 3 Mus musculus 102-106 34775880-3 2021 Calcineurin inhibitor tacrolimus (FK506) attenuated the MDI-GSH conjugate-mediated induction of CCL2, CCL3, CCL5, and CXCL8/IL8 but not others. Tacrolimus 34-39 chemokine (C-C motif) ligand 5 Mus musculus 108-112 34775880-3 2021 Calcineurin inhibitor tacrolimus (FK506) attenuated the MDI-GSH conjugate-mediated induction of CCL2, CCL3, CCL5, and CXCL8/IL8 but not others. Tacrolimus 34-39 chemokine (C-X-C motif) ligand 15 Mus musculus 124-127 34775880-4 2021 Transfection of either miR-inhibitor-206-3p or miR-inhibitor-381-3p in macrophages induced chemokine CCL2, CCL3, CCL5, and CXCL8 transcription, whereas FK506 attenuated the miR-inhibitor-206-3p or miR-inhibitor-381-3p-mediated effects. Tacrolimus 152-157 microRNA 615 Mus musculus 23-26 34775880-4 2021 Transfection of either miR-inhibitor-206-3p or miR-inhibitor-381-3p in macrophages induced chemokine CCL2, CCL3, CCL5, and CXCL8 transcription, whereas FK506 attenuated the miR-inhibitor-206-3p or miR-inhibitor-381-3p-mediated effects. Tacrolimus 152-157 microRNA 615 Mus musculus 47-50 34775880-4 2021 Transfection of either miR-inhibitor-206-3p or miR-inhibitor-381-3p in macrophages induced chemokine CCL2, CCL3, CCL5, and CXCL8 transcription, whereas FK506 attenuated the miR-inhibitor-206-3p or miR-inhibitor-381-3p-mediated effects. Tacrolimus 152-157 microRNA 615 Mus musculus 173-176 34775880-4 2021 Transfection of either miR-inhibitor-206-3p or miR-inhibitor-381-3p in macrophages induced chemokine CCL2, CCL3, CCL5, and CXCL8 transcription, whereas FK506 attenuated the miR-inhibitor-206-3p or miR-inhibitor-381-3p-mediated effects. Tacrolimus 152-157 microRNA 615 Mus musculus 197-200 34534579-4 2021 The yeast Fpr1 (FK506-sensitive proline rotamase) is a homologue of the mammalian prolyl isomerase FKBP12 (FK506-binding protein of 12 kDa). Tacrolimus 16-21 peptidylprolyl isomerase FPR1 Saccharomyces cerevisiae S288C 10-14 34534579-4 2021 The yeast Fpr1 (FK506-sensitive proline rotamase) is a homologue of the mammalian prolyl isomerase FKBP12 (FK506-binding protein of 12 kDa). Tacrolimus 16-21 FKBP prolyl isomerase 1A Homo sapiens 99-105 34534579-4 2021 The yeast Fpr1 (FK506-sensitive proline rotamase) is a homologue of the mammalian prolyl isomerase FKBP12 (FK506-binding protein of 12 kDa). Tacrolimus 16-21 FKBP prolyl isomerase 1A Homo sapiens 107-138 34916931-8 2021 We found that CYP3A5*3 polymorphism was the single most strongly associated factor determining the tacrolimus C0/D in blood at all three time points (p < 0.001). Tacrolimus 99-109 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 14-20 34834375-7 2021 In multivariate analysis, the log Cmin/dose of tacrolimus was significantly and positively associated with the hematocrit, ALAT, and CRP concentrations. Tacrolimus 47-57 C-reactive protein Homo sapiens 133-136 34838267-2 2021 This prospective cohort study was to explore the effectiveness and safety of tacrolimus for treatment of IgA (Immunoglobulin A) nephropathy patients. Tacrolimus 77-87 CD79a molecule Homo sapiens 105-108 34838267-2 2021 This prospective cohort study was to explore the effectiveness and safety of tacrolimus for treatment of IgA (Immunoglobulin A) nephropathy patients. Tacrolimus 77-87 CD79a molecule Homo sapiens 110-126 34834375-8 2021 CRP concentrations were higher (p = 0.003) for patients with tacrolimus overexposure (i.e., tacrolimus Cmin > 15 microg/L) (median CRP (10th-90th percentiles): 27 mg/L (3-149 mg/L), n = 91) than they were for patients with a tacrolimus Cmin <= 15 microg/L (13 mg/mL (3-95 mg/L), n = 1482)). Tacrolimus 61-71 C-reactive protein Homo sapiens 0-3 34834375-8 2021 CRP concentrations were higher (p = 0.003) for patients with tacrolimus overexposure (i.e., tacrolimus Cmin > 15 microg/L) (median CRP (10th-90th percentiles): 27 mg/L (3-149 mg/L), n = 91) than they were for patients with a tacrolimus Cmin <= 15 microg/L (13 mg/mL (3-95 mg/L), n = 1482)). Tacrolimus 92-102 C-reactive protein Homo sapiens 0-3 34834375-9 2021 CRP in the fourth quartile (49 to 334 mg/L) was associated with a 2.6-fold increased risk of tacrolimus Cmin overexposure. Tacrolimus 93-103 C-reactive protein Homo sapiens 0-3 34607938-9 2021 In vitro treatment of healthy CD4+ and CD8+ T cells with tacrolimus abrogated the proliferation and cytokine (INF-gamma, IL-2, and TNF-alpha) secretion associated with the type 1 inflammatory phenotype observed in pre- and post-PTx rejectors. Tacrolimus 57-67 CD4 molecule Homo sapiens 30-33 34824543-5 2021 Results: The CYP3A5 genotype was clearly associated with dose-adjusted trough blood tacrolimus concentrations (C0/D), whereas no significant difference was observed in patients with the CYP3A4*1B, CYP3A4*22, ABCB1, ABCC2, POR*28 or PXR alleles. Tacrolimus 84-94 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 13-19 34824543-9 2021 Conclusion: Clinical factors, medication, and CYP-enzyme polymorphisms accounted for tacrolimus concentration variability in kidney transplantation recipients. Tacrolimus 85-95 peptidylprolyl isomerase G Homo sapiens 46-49 34607938-9 2021 In vitro treatment of healthy CD4+ and CD8+ T cells with tacrolimus abrogated the proliferation and cytokine (INF-gamma, IL-2, and TNF-alpha) secretion associated with the type 1 inflammatory phenotype observed in pre- and post-PTx rejectors. Tacrolimus 57-67 CD8a molecule Homo sapiens 39-42 34607938-9 2021 In vitro treatment of healthy CD4+ and CD8+ T cells with tacrolimus abrogated the proliferation and cytokine (INF-gamma, IL-2, and TNF-alpha) secretion associated with the type 1 inflammatory phenotype observed in pre- and post-PTx rejectors. Tacrolimus 57-67 interleukin 2 Homo sapiens 121-125 34607938-9 2021 In vitro treatment of healthy CD4+ and CD8+ T cells with tacrolimus abrogated the proliferation and cytokine (INF-gamma, IL-2, and TNF-alpha) secretion associated with the type 1 inflammatory phenotype observed in pre- and post-PTx rejectors. Tacrolimus 57-67 tumor necrosis factor Homo sapiens 131-140 34732168-11 2021 A more significant reduction of MuSK-ab titers was observed in patients receiving TAC or RTX plus Pred than those receiving AZA plus Pred. Tacrolimus 82-85 muscle associated receptor tyrosine kinase Homo sapiens 32-36 34830130-10 2021 Differential effects of FK506-binding immunophilins, FKBP4 and FKBP5, contribute to the efficiency of glucocorticoids under stress resilience. Tacrolimus 24-29 FKBP prolyl isomerase 4 Homo sapiens 53-58 34830130-10 2021 Differential effects of FK506-binding immunophilins, FKBP4 and FKBP5, contribute to the efficiency of glucocorticoids under stress resilience. Tacrolimus 24-29 FKBP prolyl isomerase 5 Homo sapiens 63-68 34648292-3 2021 However, CYP3A5 preferentially metabolizes several clinically prescribed drugs, such as tacrolimus. Tacrolimus 88-98 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 9-15 34648292-4 2021 Genetic polymorphism in CYP3A5 makes race-based dosing adjustment of tacrolimus necessary to minimize acute rejection after organ transplantation. Tacrolimus 69-79 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 24-30 34133842-0 2021 Effects of Postoperative Day and NR1I2 on Tacrolimus Clearance in Chinese Liver Transplant Recipients-A Population Model Approach. Tacrolimus 42-52 nuclear receptor subfamily 1 group I member 2 Homo sapiens 33-38 34133842-10 2021 To our knowledge, this is the first report indicating NR1I2 rs2276707 genotypes is another biomarker impacting tacrolimus clearance in liver transplant recipients. Tacrolimus 111-121 nuclear receptor subfamily 1 group I member 2 Homo sapiens 54-59 34133842-11 2021 The NR1I2 gene polymorphism may affect the in vivo behavior of tacrolimus by regulating gene expression. Tacrolimus 63-73 nuclear receptor subfamily 1 group I member 2 Homo sapiens 4-9 34690808-9 2021 Diminished expression of the FK506 binding protein, FKBP12.6, may also contribute. Tacrolimus 29-34 FKBP prolyl isomerase 1B Homo sapiens 52-60 34709766-0 2021 The CYP3A5 genotypes of both liver transplant recipients and donors influence the time-dependent recovery of tacrolimus clearance during the early stage following transplantation. Tacrolimus 109-119 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 4-10 34668283-5 2021 With increasing concentrations of tacrolimus, there was a trend to reduction in the release of IL-2 (p = 0.0137), and IFN-gamma (p = 0.0147) in response to peptide stimulation. Tacrolimus 34-44 interferon gamma Homo sapiens 118-127 34841735-5 2021 The increased percentage of senescent CD8+ CD57+ T lineages and less responsive T cell receptor (TCR) pathway in the FK506 group indicate better graft acceptance. Tacrolimus 117-122 CD8a molecule Homo sapiens 38-41 34841735-5 2021 The increased percentage of senescent CD8+ CD57+ T lineages and less responsive T cell receptor (TCR) pathway in the FK506 group indicate better graft acceptance. Tacrolimus 117-122 beta-1,3-glucuronyltransferase 1 Homo sapiens 43-47 34841735-6 2021 Meanwhile, percentages of regulatory T cells (Tregs) and expression of CTLA-4 were both up to two-fold higher in the RAPA group, suggesting the inconsistent reactivation potential of the FK506 and RAPA groups when an anti-tumour or anti-infection immune response is concerned. Tacrolimus 187-192 cytotoxic T-lymphocyte associated protein 4 Homo sapiens 71-77 34662453-0 2021 Tacrolimus ameliorates podocyte injury by restoring FK506 binding protein 12 (FKBP12) at actin cytoskeleton. Tacrolimus 0-10 FKBP prolyl isomerase 1A Homo sapiens 52-76 34662453-0 2021 Tacrolimus ameliorates podocyte injury by restoring FK506 binding protein 12 (FKBP12) at actin cytoskeleton. Tacrolimus 0-10 FKBP prolyl isomerase 1A Homo sapiens 78-84 34662453-1 2021 FKBP12 was identified as a binding protein of tacrolimus (Tac). Tacrolimus 46-56 FKBP prolyl isomerase 1A Homo sapiens 0-6 34662453-1 2021 FKBP12 was identified as a binding protein of tacrolimus (Tac). Tacrolimus 58-61 FKBP prolyl isomerase 1A Homo sapiens 0-6 34662453-2 2021 Tac binds to FKBP12 and exhibits immunosuppressive effects in T cells. Tacrolimus 0-3 FKBP prolyl isomerase 1A Homo sapiens 13-19 34662453-13 2021 Tac treatment to the normal cells increased the expression of FKBP12 at F-actin in processes and enhanced process formation. Tacrolimus 0-3 FKBP prolyl isomerase 1A Homo sapiens 62-68 34662453-14 2021 Tac enhanced the interaction of FKBP12 with synaptopodin. Tacrolimus 0-3 FKBP prolyl isomerase 1A Homo sapiens 32-38 34662453-15 2021 These observations suggested that FKBP12 at actin cytoskeleton participates in the maintenance of processes, and Tac treatment ameliorates podocyte injury by restoring FKBP12 at actin cytoskeleton. Tacrolimus 113-116 FKBP prolyl isomerase 1A Homo sapiens 168-174 34435330-0 2021 Tacrolimus Decreases Cognitive Function by Impairing Hippocampal Synaptic Balance: a Possible Role of Klotho. Tacrolimus 0-10 klotho Mus musculus 102-108 34435330-4 2021 Furthermore, tacrolimus caused synaptic imbalance, as demonstrated by decreased excitatory synapses and increased inhibitory synapses, and downregulated Klotho in a dose-dependent manner; the downregulation of Klotho was localized to excitatory hippocampal synapses. Tacrolimus 13-23 klotho Mus musculus 153-159 34435330-4 2021 Furthermore, tacrolimus caused synaptic imbalance, as demonstrated by decreased excitatory synapses and increased inhibitory synapses, and downregulated Klotho in a dose-dependent manner; the downregulation of Klotho was localized to excitatory hippocampal synapses. Tacrolimus 13-23 klotho Mus musculus 210-216 34435330-5 2021 Moreover, tacrolimus increased oxidative stress and was associated with activation of the PI3K/AKT pathway in the hippocampus. Tacrolimus 10-20 thymoma viral proto-oncogene 1 Mus musculus 95-98 34435330-6 2021 These results indicate that tacrolimus impairs cognitive function via synaptic imbalance, and that these processes are associated with Klotho downregulation at synapses through tacrolimus-induced oxidative stress in the hippocampus. Tacrolimus 28-38 klotho Mus musculus 135-141 34435330-6 2021 These results indicate that tacrolimus impairs cognitive function via synaptic imbalance, and that these processes are associated with Klotho downregulation at synapses through tacrolimus-induced oxidative stress in the hippocampus. Tacrolimus 177-187 klotho Mus musculus 135-141 34725418-0 2021 CYP3A-status is associated with blood concentration and dose-requirement of tacrolimus in heart transplant recipients. Tacrolimus 76-86 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-5 34725418-1 2021 High inter-individual variability in tacrolimus clearance is attributed to genetic polymorphisms of CYP3A enzymes. Tacrolimus 37-47 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 100-105 34725418-2 2021 However, due to CYP3A phenoconversion induced by non-genetic factors, continuous changes in tacrolimus-metabolizing capacity entail frequent dose-refinement for optimal immunosuppression. Tacrolimus 92-102 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 16-21 34725418-4 2021 In low CYP3A4 expressers carrying CYP3A5*3/*3, the dose-corrected tacrolimus level was significantly higher than in normal CYP3A4 expressers or in those with CYP3A5*1. Tacrolimus 66-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 7-13 34725418-4 2021 In low CYP3A4 expressers carrying CYP3A5*3/*3, the dose-corrected tacrolimus level was significantly higher than in normal CYP3A4 expressers or in those with CYP3A5*1. Tacrolimus 66-76 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 34-40 34725418-5 2021 Modification of the initial tacrolimus dose was required for all patients: dose reduction by 20% for low CYP3A4 expressers, a 40% increase for normal expressers and a 2.4-fold increase for CYP3A5*1 carriers. Tacrolimus 28-38 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 105-111 34725418-5 2021 Modification of the initial tacrolimus dose was required for all patients: dose reduction by 20% for low CYP3A4 expressers, a 40% increase for normal expressers and a 2.4-fold increase for CYP3A5*1 carriers. Tacrolimus 28-38 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 189-195 34725418-7 2021 The fluctuation of CYP3A4 expression and tacrolimus blood concentration (C0/D) was found to be associated with tapering and cessation of corticosteroid in CYP3A5 non-expressers, but not in those carrying CYP3A5*1. Tacrolimus 41-51 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 155-161 34725418-8 2021 Although monitoring of tacrolimus blood concentration cannot be omitted, assaying recipients" CYP3A-status can guide optimization of the initial tacrolimus dose, and can facilitate personalized tacrolimus therapy during steroid withdrawal in the late post-operative period. Tacrolimus 145-155 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 94-99 34269803-8 2021 This synonymous variant in P-glycoprotein may influence the risk of CMV reactivation by altering the efflux of cyclosporine and tacrolimus from donor lymphocytes. Tacrolimus 128-138 ATP binding cassette subfamily B member 1 Homo sapiens 27-41 34708436-11 2022 Furthermore, a larger proportion of patients in the CYP3A5 expression groups required Tac dose adjustment to achieve a therapeutic effect and were given Tac with WZC. Tacrolimus 86-89 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 52-58 34708436-11 2022 Furthermore, a larger proportion of patients in the CYP3A5 expression groups required Tac dose adjustment to achieve a therapeutic effect and were given Tac with WZC. Tacrolimus 153-156 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 52-58 34500058-7 2021 Tacrolimus was loaded into MSNs and the particles were characterized for particle size (TEM and DLS), zeta potential (DLS), solubility studies, FTIR, TGA, XRD, BET and cytotoxicity studies. Tacrolimus 0-10 delta/notch-like EGF repeat containing Mus musculus 160-163 34788922-0 2021 (The effect of CYP3A5 gene polymorphism on tacrolimus concentration and adverse events in patients undergoing allogeneic hematopoietic stem cell transplantation). Tacrolimus 43-53 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 15-21 34788922-8 2021 Conclusion: CYP3A5 genotype-directed administration may help achieve the target blood concentration of tacrolimus after HSCT more quickly, reduce the incidence of severe aGVHD, and improve the efficacy of transplantation. Tacrolimus 103-113 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 12-18 34683143-1 2021 The pharmacokinetic variability of tacrolimus can be partly explained by CYP3A5 activity. Tacrolimus 35-45 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 73-79 34683143-13 2021 Our study raised some issues about specific therapeutic tacrolimus C0 targets for CYP3A5*1/- patients and suggests to set up randomized control studies in this specific population. Tacrolimus 56-66 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 82-88 34352707-5 2021 Tacrolimus trough levels increased only 0.3 ng/mL upon conversion in the CYP3A5*3/*3 group: 5.8 (3.4-7.2) vs 6.1 (3.8-7.9); p = 0.06. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 73-79 34228988-0 2021 Combination of mesenchymal stem cells and FK506 prolongs heart allograft survival by inhibiting TBK1/IRF3-regulated-IFN-gamma production. Tacrolimus 42-47 TANK-binding kinase 1 Mus musculus 96-100 34228988-0 2021 Combination of mesenchymal stem cells and FK506 prolongs heart allograft survival by inhibiting TBK1/IRF3-regulated-IFN-gamma production. Tacrolimus 42-47 interferon regulatory factor 3 Mus musculus 101-105 34228988-0 2021 Combination of mesenchymal stem cells and FK506 prolongs heart allograft survival by inhibiting TBK1/IRF3-regulated-IFN-gamma production. Tacrolimus 42-47 interferon gamma Mus musculus 116-125 34228988-6 2021 Thereafter, in vitro and in vivo experiments were conducted to identify the mechanisms regarding MSC and FK506 combination (MF group) use in regulating IFN-gamma signaling. Tacrolimus 105-110 interferon gamma Mus musculus 152-161 34228988-11 2021 Combination use of MSC and FK506 can prolong graft survival, possibly by down-regulating TBK1/IRF3 phosphorylation, thus reducing IFN-gamma production to prevent infiltration of inflammatory cells in the graft and extend graft survival. Tacrolimus 27-32 TANK-binding kinase 1 Mus musculus 89-93 34228988-11 2021 Combination use of MSC and FK506 can prolong graft survival, possibly by down-regulating TBK1/IRF3 phosphorylation, thus reducing IFN-gamma production to prevent infiltration of inflammatory cells in the graft and extend graft survival. Tacrolimus 27-32 interferon regulatory factor 3 Mus musculus 94-98 34228988-11 2021 Combination use of MSC and FK506 can prolong graft survival, possibly by down-regulating TBK1/IRF3 phosphorylation, thus reducing IFN-gamma production to prevent infiltration of inflammatory cells in the graft and extend graft survival. Tacrolimus 27-32 interferon gamma Mus musculus 130-139 34481645-1 2021 Calcineurin-inhibitor induced pain syndrome (CIPS) also called the "symmetrical bone syndrome" is a condition describing reversible lower extremity pain in patients after organ transplantation who are receiving calcineurin inhibitors, especially tacrolimus. Tacrolimus 246-256 calcineurin binding protein 1 Homo sapiens 0-21 34575860-4 2021 We hypothesized that CsA and Tac induce functional defects and activate an inflammatory cascade via NF-kappaB signaling in ECFCs. Tacrolimus 29-32 nuclear factor kappa B subunit 1 Homo sapiens 100-109 34575860-11 2021 Furthermore, CsA and Tac led to NF-kappaB p65 subunit phosphorylation and nuclear translocation. Tacrolimus 21-24 RELA proto-oncogene, NF-kB subunit Homo sapiens 32-45 34575860-12 2021 Pharmacological inhibition of NF-kappaB by parthenolide diminished CsA- and Tac-mediated proinflammatory effects. Tacrolimus 76-79 nuclear factor kappa B subunit 1 Homo sapiens 30-39 34217824-2 2021 A FK506/HP-beta-CD inclusion compound was prepared by grinding to increase drug solubility. Tacrolimus 2-7 adrenocortical dysplasia Mus musculus 11-18 34217824-3 2021 To address the side- effects in non-target organs and systemic toxicity of FK506, pH-responsive Eudragit S100 (ES100) and hyaluronic acid (HA) with high affinity to CD44 receptor were adsorbed onto the surface of chitosan (CS) nanoparticles loaded with FK506/HP-beta-CD through electrostatic interactions to obtain FK506@ES100/HA/CS/HP-beta-CD nanoparticles (FK506@EHCh NPs). Tacrolimus 315-320 CD44 antigen Mus musculus 165-169 34217824-3 2021 To address the side- effects in non-target organs and systemic toxicity of FK506, pH-responsive Eudragit S100 (ES100) and hyaluronic acid (HA) with high affinity to CD44 receptor were adsorbed onto the surface of chitosan (CS) nanoparticles loaded with FK506/HP-beta-CD through electrostatic interactions to obtain FK506@ES100/HA/CS/HP-beta-CD nanoparticles (FK506@EHCh NPs). Tacrolimus 315-320 adrenocortical dysplasia Mus musculus 262-269 34217824-3 2021 To address the side- effects in non-target organs and systemic toxicity of FK506, pH-responsive Eudragit S100 (ES100) and hyaluronic acid (HA) with high affinity to CD44 receptor were adsorbed onto the surface of chitosan (CS) nanoparticles loaded with FK506/HP-beta-CD through electrostatic interactions to obtain FK506@ES100/HA/CS/HP-beta-CD nanoparticles (FK506@EHCh NPs). Tacrolimus 359-364 adrenocortical dysplasia Mus musculus 336-343 34217824-5 2021 FK506@EHCh NPs significantly suppressed secretion of TNF-alpha, IL-1beta and IL-6 by LPS-activated Raw 264.7 macrophages. Tacrolimus 0-5 tumor necrosis factor Mus musculus 53-62 34217824-5 2021 FK506@EHCh NPs significantly suppressed secretion of TNF-alpha, IL-1beta and IL-6 by LPS-activated Raw 264.7 macrophages. Tacrolimus 0-5 interleukin 1 alpha Mus musculus 64-72 34217824-5 2021 FK506@EHCh NPs significantly suppressed secretion of TNF-alpha, IL-1beta and IL-6 by LPS-activated Raw 264.7 macrophages. Tacrolimus 0-5 interleukin 6 Mus musculus 77-81 34511980-6 2021 Our final model identified creatinine clearance rate, hematocrit, Wuzhi capsule dose, CYP3A5*3 genetic polymorphisms, and tacrolimus daily dose as significant covariates for tacrolimus clearance, with the value of 14.4 L h-1, and the between-subject variability (BSV) was 25.4%. Tacrolimus 174-184 procollagen-lysine,2-oxoglutarate 5-dioxygenase 1 Homo sapiens 219-224 34278483-0 2021 Tacrolimus inhibits insulin release and promotes apoptosis of Min6 cells through the inhibition of the PI3K/Akt/mTOR pathway. Tacrolimus 0-10 thymoma viral proto-oncogene 1 Mus musculus 108-111 34620272-3 2021 Cytochrome-P450 (CYP) isoenzymes CYP3A4 and CYP3A5, as well P-glycoprotein (P-gp) are involved in TAC bioavailability. Tacrolimus 98-101 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 0-15 34620272-3 2021 Cytochrome-P450 (CYP) isoenzymes CYP3A4 and CYP3A5, as well P-glycoprotein (P-gp) are involved in TAC bioavailability. Tacrolimus 98-101 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 17-20 34620272-3 2021 Cytochrome-P450 (CYP) isoenzymes CYP3A4 and CYP3A5, as well P-glycoprotein (P-gp) are involved in TAC bioavailability. Tacrolimus 98-101 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 33-39 34620272-3 2021 Cytochrome-P450 (CYP) isoenzymes CYP3A4 and CYP3A5, as well P-glycoprotein (P-gp) are involved in TAC bioavailability. Tacrolimus 98-101 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 44-50 34620272-3 2021 Cytochrome-P450 (CYP) isoenzymes CYP3A4 and CYP3A5, as well P-glycoprotein (P-gp) are involved in TAC bioavailability. Tacrolimus 98-101 ATP binding cassette subfamily B member 1 Homo sapiens 60-74 34136903-0 2021 A 24-Hour Extended Calibration Strategy for Quantitating Tacrolimus Concentrations by Liquid Chromatography-Tandem Mass Spectrometry. Tacrolimus 57-67 immunoglobulin kappa variable 2-23 (pseudogene) Homo sapiens 0-4 34136903-5 2021 A 24-h extended calibration of LC-MS/MS tacrolimus was designed and validated to reduce calibrator usage, improve turnaround time, and provide a more efficient workflow for urgent requests. Tacrolimus 40-50 immunoglobulin kappa variable 2-23 (pseudogene) Homo sapiens 0-4 34278483-13 2021 Furthermore, the western blotting results suggested that tacrolimus had no significant effects on the expression levels of total PI3K, Akt and mTOR proteins (P>0.05), but 25 and 50 ng/ml tacrolimus could significantly inhibit the expression levels of p-Akt and p-mTOR (P<0.01). Tacrolimus 187-197 thymoma viral proto-oncogene 1 Mus musculus 253-256 34278483-13 2021 Furthermore, the western blotting results suggested that tacrolimus had no significant effects on the expression levels of total PI3K, Akt and mTOR proteins (P>0.05), but 25 and 50 ng/ml tacrolimus could significantly inhibit the expression levels of p-Akt and p-mTOR (P<0.01). Tacrolimus 187-197 mechanistic target of rapamycin kinase Mus musculus 263-267 34278483-14 2021 In conclusion, tacrolimus decreased the activity and insulin secretion of pancreatic beta cells and induced the apoptosis of islet beta cells by inhibiting the mRNA expression levels of PI3K, Akt and mTOR and reducing the phosphorylation of Akt and mTOR proteins in the PI3K/Akt/mTOR signaling pathway, which may ultimately lead to the occurrence of diabetes mellitus, and may be considered as one of the specific mechanisms of PTDM caused by tacrolimus. Tacrolimus 15-25 thymoma viral proto-oncogene 1 Mus musculus 192-195 34278483-14 2021 In conclusion, tacrolimus decreased the activity and insulin secretion of pancreatic beta cells and induced the apoptosis of islet beta cells by inhibiting the mRNA expression levels of PI3K, Akt and mTOR and reducing the phosphorylation of Akt and mTOR proteins in the PI3K/Akt/mTOR signaling pathway, which may ultimately lead to the occurrence of diabetes mellitus, and may be considered as one of the specific mechanisms of PTDM caused by tacrolimus. Tacrolimus 15-25 mechanistic target of rapamycin kinase Mus musculus 200-204 34278483-14 2021 In conclusion, tacrolimus decreased the activity and insulin secretion of pancreatic beta cells and induced the apoptosis of islet beta cells by inhibiting the mRNA expression levels of PI3K, Akt and mTOR and reducing the phosphorylation of Akt and mTOR proteins in the PI3K/Akt/mTOR signaling pathway, which may ultimately lead to the occurrence of diabetes mellitus, and may be considered as one of the specific mechanisms of PTDM caused by tacrolimus. Tacrolimus 15-25 thymoma viral proto-oncogene 1 Mus musculus 241-244 34278483-14 2021 In conclusion, tacrolimus decreased the activity and insulin secretion of pancreatic beta cells and induced the apoptosis of islet beta cells by inhibiting the mRNA expression levels of PI3K, Akt and mTOR and reducing the phosphorylation of Akt and mTOR proteins in the PI3K/Akt/mTOR signaling pathway, which may ultimately lead to the occurrence of diabetes mellitus, and may be considered as one of the specific mechanisms of PTDM caused by tacrolimus. Tacrolimus 15-25 mechanistic target of rapamycin kinase Mus musculus 249-253 34278483-14 2021 In conclusion, tacrolimus decreased the activity and insulin secretion of pancreatic beta cells and induced the apoptosis of islet beta cells by inhibiting the mRNA expression levels of PI3K, Akt and mTOR and reducing the phosphorylation of Akt and mTOR proteins in the PI3K/Akt/mTOR signaling pathway, which may ultimately lead to the occurrence of diabetes mellitus, and may be considered as one of the specific mechanisms of PTDM caused by tacrolimus. Tacrolimus 15-25 thymoma viral proto-oncogene 1 Mus musculus 275-278 34278483-14 2021 In conclusion, tacrolimus decreased the activity and insulin secretion of pancreatic beta cells and induced the apoptosis of islet beta cells by inhibiting the mRNA expression levels of PI3K, Akt and mTOR and reducing the phosphorylation of Akt and mTOR proteins in the PI3K/Akt/mTOR signaling pathway, which may ultimately lead to the occurrence of diabetes mellitus, and may be considered as one of the specific mechanisms of PTDM caused by tacrolimus. Tacrolimus 15-25 mechanistic target of rapamycin kinase Mus musculus 279-283 34278483-14 2021 In conclusion, tacrolimus decreased the activity and insulin secretion of pancreatic beta cells and induced the apoptosis of islet beta cells by inhibiting the mRNA expression levels of PI3K, Akt and mTOR and reducing the phosphorylation of Akt and mTOR proteins in the PI3K/Akt/mTOR signaling pathway, which may ultimately lead to the occurrence of diabetes mellitus, and may be considered as one of the specific mechanisms of PTDM caused by tacrolimus. Tacrolimus 443-453 thymoma viral proto-oncogene 1 Mus musculus 192-195 34278483-14 2021 In conclusion, tacrolimus decreased the activity and insulin secretion of pancreatic beta cells and induced the apoptosis of islet beta cells by inhibiting the mRNA expression levels of PI3K, Akt and mTOR and reducing the phosphorylation of Akt and mTOR proteins in the PI3K/Akt/mTOR signaling pathway, which may ultimately lead to the occurrence of diabetes mellitus, and may be considered as one of the specific mechanisms of PTDM caused by tacrolimus. Tacrolimus 443-453 mechanistic target of rapamycin kinase Mus musculus 200-204 34278483-14 2021 In conclusion, tacrolimus decreased the activity and insulin secretion of pancreatic beta cells and induced the apoptosis of islet beta cells by inhibiting the mRNA expression levels of PI3K, Akt and mTOR and reducing the phosphorylation of Akt and mTOR proteins in the PI3K/Akt/mTOR signaling pathway, which may ultimately lead to the occurrence of diabetes mellitus, and may be considered as one of the specific mechanisms of PTDM caused by tacrolimus. Tacrolimus 443-453 thymoma viral proto-oncogene 1 Mus musculus 241-244 34278483-14 2021 In conclusion, tacrolimus decreased the activity and insulin secretion of pancreatic beta cells and induced the apoptosis of islet beta cells by inhibiting the mRNA expression levels of PI3K, Akt and mTOR and reducing the phosphorylation of Akt and mTOR proteins in the PI3K/Akt/mTOR signaling pathway, which may ultimately lead to the occurrence of diabetes mellitus, and may be considered as one of the specific mechanisms of PTDM caused by tacrolimus. Tacrolimus 443-453 mechanistic target of rapamycin kinase Mus musculus 249-253 34278483-14 2021 In conclusion, tacrolimus decreased the activity and insulin secretion of pancreatic beta cells and induced the apoptosis of islet beta cells by inhibiting the mRNA expression levels of PI3K, Akt and mTOR and reducing the phosphorylation of Akt and mTOR proteins in the PI3K/Akt/mTOR signaling pathway, which may ultimately lead to the occurrence of diabetes mellitus, and may be considered as one of the specific mechanisms of PTDM caused by tacrolimus. Tacrolimus 443-453 thymoma viral proto-oncogene 1 Mus musculus 275-278 34278483-14 2021 In conclusion, tacrolimus decreased the activity and insulin secretion of pancreatic beta cells and induced the apoptosis of islet beta cells by inhibiting the mRNA expression levels of PI3K, Akt and mTOR and reducing the phosphorylation of Akt and mTOR proteins in the PI3K/Akt/mTOR signaling pathway, which may ultimately lead to the occurrence of diabetes mellitus, and may be considered as one of the specific mechanisms of PTDM caused by tacrolimus. Tacrolimus 443-453 mechanistic target of rapamycin kinase Mus musculus 279-283 34931247-1 2021 OBJECTIVES: We retrospectively compared the therapeutic effects of combination therapy with prednisolone (PSL) and oral tacrolimus (TAC) or azathioprine (AZA) on progressive interstitial pneumonia with systemic sclerosis (SSc-PIP). Tacrolimus 120-130 prolactin induced protein Homo sapiens 226-229 34931247-7 2021 CONCLUSION: The inhibitory effect of PSL and TAC combination therapy on the progression of fibrosis in SSc-PIP may be superior to that of PSL and AZA in the long period. Tacrolimus 45-48 prolactin induced protein Homo sapiens 107-110 34483924-5 2021 We present the case of a 16-year-old girl with kidney and liver transplant in whom low concentrations of tacrolimus in the context of low hematocrit led to significant increase in the dosage of tacrolimus and participate, along with a genetic polymorphism of ABCB1, in nephrotoxicity. Tacrolimus 105-115 ATP binding cassette subfamily B member 1 Homo sapiens 259-264 34144106-4 2021 Among many immunosuppressants, tacrolimus (FK506) is one of the most potent interleukin-2 (IL-2)-mediated T-cell proliferation blockers. Tacrolimus 31-41 interleukin 2 Mus musculus 76-89 34144106-4 2021 Among many immunosuppressants, tacrolimus (FK506) is one of the most potent interleukin-2 (IL-2)-mediated T-cell proliferation blockers. Tacrolimus 31-41 interleukin 2 Mus musculus 91-95 34144106-4 2021 Among many immunosuppressants, tacrolimus (FK506) is one of the most potent interleukin-2 (IL-2)-mediated T-cell proliferation blockers. Tacrolimus 43-48 interleukin 2 Mus musculus 76-89 34144106-4 2021 Among many immunosuppressants, tacrolimus (FK506) is one of the most potent interleukin-2 (IL-2)-mediated T-cell proliferation blockers. Tacrolimus 43-48 interleukin 2 Mus musculus 91-95 34144106-8 2021 Interestingly, FK506-M at very low-doses (equivalent to 150 to 2400 ng FK506 per recipient) was found to inhibit the infiltration of immune cells into grafts and reduce serum IL-1beta levels, thereby improving graft survival times dose-dependently. Tacrolimus 15-20 interleukin 1 alpha Mus musculus 175-183 34144106-8 2021 Interestingly, FK506-M at very low-doses (equivalent to 150 to 2400 ng FK506 per recipient) was found to inhibit the infiltration of immune cells into grafts and reduce serum IL-1beta levels, thereby improving graft survival times dose-dependently. Tacrolimus 71-76 interleukin 1 alpha Mus musculus 175-183 34278483-0 2021 Tacrolimus inhibits insulin release and promotes apoptosis of Min6 cells through the inhibition of the PI3K/Akt/mTOR pathway. Tacrolimus 0-10 mechanistic target of rapamycin kinase Mus musculus 112-116 34278483-1 2021 As a calcineurin inhibitor, tacrolimus is commonly used as a first-line immunosuppressant in organ transplant recipients. Tacrolimus 28-38 calcineurin binding protein 1 Mus musculus 5-26 34278483-5 2021 The aim of the present study was to investigate whether the PI3K/Akt/mTOR signaling pathway served an important role in the pathogenesis of PTDM induced by tacrolimus. Tacrolimus 156-166 thymoma viral proto-oncogene 1 Mus musculus 65-68 34278483-5 2021 The aim of the present study was to investigate whether the PI3K/Akt/mTOR signaling pathway served an important role in the pathogenesis of PTDM induced by tacrolimus. Tacrolimus 156-166 mechanistic target of rapamycin kinase Mus musculus 69-73 34278483-7 2021 The effects of tacrolimus on the insulin secretion and the activity of caspase-3 of Min6 cells stimulated by glucose exposure were measured by ELISA. Tacrolimus 15-25 caspase 3 Mus musculus 71-80 34278483-9 2021 The effects of tacrolimus on the mRNA expression levels of PI3K, Akt and mTOR were detected by reverse transcription-quantitative PCR (RT-qPCR), whereas the protein expression levels of PI3K, Akt, mTOR, phosphorylated (p)-AKT and p-mTOR in Min6 cells were assessed using western blotting. Tacrolimus 15-25 thymoma viral proto-oncogene 1 Mus musculus 65-68 34278483-9 2021 The effects of tacrolimus on the mRNA expression levels of PI3K, Akt and mTOR were detected by reverse transcription-quantitative PCR (RT-qPCR), whereas the protein expression levels of PI3K, Akt, mTOR, phosphorylated (p)-AKT and p-mTOR in Min6 cells were assessed using western blotting. Tacrolimus 15-25 mechanistic target of rapamycin kinase Mus musculus 73-77 34278483-9 2021 The effects of tacrolimus on the mRNA expression levels of PI3K, Akt and mTOR were detected by reverse transcription-quantitative PCR (RT-qPCR), whereas the protein expression levels of PI3K, Akt, mTOR, phosphorylated (p)-AKT and p-mTOR in Min6 cells were assessed using western blotting. Tacrolimus 15-25 thymoma viral proto-oncogene 1 Mus musculus 222-225 34278483-11 2021 Moreover, 50 ng/ml tacrolimus markedly increased the activity of caspase-3 by 175.1% (P<0.05), it also decreased the SOD activity (P<0.01) and increased MDA levels (P<0.05). Tacrolimus 19-29 caspase 3 Mus musculus 65-74 34278483-12 2021 The RT-qPCR results demonstrated that the mRNA expression levels of PI3K, Akt and mTOR were downregulated by 25 and 50 ng/ml tacrolimus (P<0.01). Tacrolimus 125-135 thymoma viral proto-oncogene 1 Mus musculus 74-77 34278483-12 2021 The RT-qPCR results demonstrated that the mRNA expression levels of PI3K, Akt and mTOR were downregulated by 25 and 50 ng/ml tacrolimus (P<0.01). Tacrolimus 125-135 mechanistic target of rapamycin kinase Mus musculus 82-86 34362271-3 2022 OBJECTIVE: To detect genotypes of cytochrome P450 3A5 (CYP3A5) and ABCB1 in kidney transplant patients and establish initial daily tacrolimus dosing formula based on genotypes of CYP3A5 and ABCB1 and patients" clinical parameters. Tacrolimus 131-141 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 34-53 34362271-3 2022 OBJECTIVE: To detect genotypes of cytochrome P450 3A5 (CYP3A5) and ABCB1 in kidney transplant patients and establish initial daily tacrolimus dosing formula based on genotypes of CYP3A5 and ABCB1 and patients" clinical parameters. Tacrolimus 131-141 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 179-185 34342774-3 2021 FKBP2 (FKBP13) and FKBP1 (FKBP12), known as immunophilins, are binding proteins for rapamycin and FK506, which are immunosuppressive drugs. Tacrolimus 98-103 FKBP prolyl isomerase 2 Homo sapiens 0-5 34342774-3 2021 FKBP2 (FKBP13) and FKBP1 (FKBP12), known as immunophilins, are binding proteins for rapamycin and FK506, which are immunosuppressive drugs. Tacrolimus 98-103 FKBP prolyl isomerase 1A Homo sapiens 19-24 34342774-5 2021 Within the 15 mammalian FKBPs known, FKBP1 is merely the only one proven to form complexes with rapamycin and FK506 in the cytosol and facilitate their T cells immunosuppressive effects, FKBP2 is a luminal protein of the endoplasmic reticulum (ER) and is reported to take part in protein folding in the ER. Tacrolimus 110-115 FKBP prolyl isomerase 1A Homo sapiens 37-42 34488389-11 2021 However, the expression of Bcl-2 increased when HC-030031, pifithrin-alpha, or FK506 was used alone, and HC-030031 combined with pifithrin-alpha or FK506 further improved the expression of Bcl-2. Tacrolimus 79-84 BCL2 apoptosis regulator Homo sapiens 27-32 34488389-11 2021 However, the expression of Bcl-2 increased when HC-030031, pifithrin-alpha, or FK506 was used alone, and HC-030031 combined with pifithrin-alpha or FK506 further improved the expression of Bcl-2. Tacrolimus 148-153 BCL2 apoptosis regulator Homo sapiens 27-32 34488389-11 2021 However, the expression of Bcl-2 increased when HC-030031, pifithrin-alpha, or FK506 was used alone, and HC-030031 combined with pifithrin-alpha or FK506 further improved the expression of Bcl-2. Tacrolimus 148-153 BCL2 apoptosis regulator Homo sapiens 189-194 34129685-1 2021 This study investigated the effect of CYP3A5 phenotype on time in therapeutic range (TTR) of tacrolimus post-transplant in pediatric patients. Tacrolimus 93-103 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 38-44 34403416-5 2021 IgAN recipients, who were maintained with a regimen containing tacrolimus, experienced recurrence less frequently, compared to those maintained with cyclosporine (p = 0.01). Tacrolimus 63-73 IGAN1 Homo sapiens 0-4 34403416-9 2021 Tacrolimus, as part of the KTx maintenance therapy, was associated with lower rates of IgAN recurrence in the graft, compared to the rate cyclosporine. Tacrolimus 0-10 IGAN1 Homo sapiens 87-91 34804426-3 2021 The cytotoxic effect of TAC and protective effect of EAF co-treatment were studied in MDCK cell lines by measuring ROS, LPO, and NO levels; collagen accumulation, effect on mitochondrial membrane integrity and cell cycle analysis were studied. Tacrolimus 24-27 lactoperoxidase Canis lupus familiaris 120-123 34804426-6 2021 Further, ROS (P<0.05), LPO and NO (P<0.001), were significantly reduced with EAF co-treatment compared with TAC individually treated cells. Tacrolimus 108-111 lactoperoxidase Canis lupus familiaris 23-26 34804426-7 2021 TAC induced mitochondrial membrane integrity loss was found to be significantly reduced in co-treated cells, as measured by rhodamine123 (P<0.05) and translocation of cytochrome c (P<0.001) from nucleus to cytoplasm, and caspase 3 release (P<0.001). Tacrolimus 0-3 cytochrome c, somatic Canis lupus familiaris 167-179 34804426-7 2021 TAC induced mitochondrial membrane integrity loss was found to be significantly reduced in co-treated cells, as measured by rhodamine123 (P<0.05) and translocation of cytochrome c (P<0.001) from nucleus to cytoplasm, and caspase 3 release (P<0.001). Tacrolimus 0-3 caspase 3 Canis lupus familiaris 221-230 34439942-8 2021 We observed decreased levels of prolactin (11.9 ng/mL) and cortisol (87.4 mug/mL) in patients under tacrolimus-based therapy. Tacrolimus 100-110 prolactin Homo sapiens 32-41 34367377-14 2021 Serum protein expressions of IL-17 (p = 0.0017), IL-18 (p = 0.0036), IFN-gamma (p = 0.0102), and MMP-9 (p = 0.0194) were significantly decreased in the allograft+tacrolimus+azithromycin group compared to the allograft group. Tacrolimus 162-172 interleukin 17A Mus musculus 29-34 34367377-14 2021 Serum protein expressions of IL-17 (p = 0.0017), IL-18 (p = 0.0036), IFN-gamma (p = 0.0102), and MMP-9 (p = 0.0194) were significantly decreased in the allograft+tacrolimus+azithromycin group compared to the allograft group. Tacrolimus 162-172 interleukin 18 Mus musculus 49-54 34367377-14 2021 Serum protein expressions of IL-17 (p = 0.0017), IL-18 (p = 0.0036), IFN-gamma (p = 0.0102), and MMP-9 (p = 0.0194) were significantly decreased in the allograft+tacrolimus+azithromycin group compared to the allograft group. Tacrolimus 162-172 interferon gamma Mus musculus 69-78 34367377-14 2021 Serum protein expressions of IL-17 (p = 0.0017), IL-18 (p = 0.0036), IFN-gamma (p = 0.0102), and MMP-9 (p = 0.0194) were significantly decreased in the allograft+tacrolimus+azithromycin group compared to the allograft group. Tacrolimus 162-172 matrix metallopeptidase 9 Mus musculus 97-102 34335631-7 2021 In that group, absolute CD4+CD25+CD127-Foxp3+ Tregs were negatively associated with steroid dose and tacrolimus trough levels (r=-0.377, p = 0.021, n=37; r=-0.43, p=0.033, n=25, respectively), opposite to IL-10+ Bregs, whose frequency apparently was not negatively affected by potent immunosuppression early posttransplant. Tacrolimus 101-111 CD4 molecule Homo sapiens 24-27 34289186-4 2022 The goal of this study was to investigate the extent to which FK506 loaded biomimetic sponges support functional muscle regeneration and fracture healing in a composite trauma model involving VML injury to the tibialis anterior muscle and osteotomy (OST) to the tibia. Tacrolimus 62-67 MCF.2 cell line derived transforming sequence like Homo sapiens 250-253 34289186-5 2022 In this model, implantation of the FK-506 loaded biomimetic sponges limited the extent of inflammation while increasing the total number of myofibers, mean myofiber cross-sectional area, myosin-to-collagen ratio, and peak isometric torque compared to untreated VML+OST muscles on day 28. Tacrolimus 35-41 myosin heavy chain 14 Homo sapiens 187-193 34377239-14 2021 CONCLUSION: The combination of ultra-low dose rituximab and low dose tacrolimus is more effective in inducing proteinuria response, improving eGFR and serum albumin in non-responsive iMN patients than standard tacrolimus monotherapy. Tacrolimus 69-79 albumin Homo sapiens 151-164 34335631-7 2021 In that group, absolute CD4+CD25+CD127-Foxp3+ Tregs were negatively associated with steroid dose and tacrolimus trough levels (r=-0.377, p = 0.021, n=37; r=-0.43, p=0.033, n=25, respectively), opposite to IL-10+ Bregs, whose frequency apparently was not negatively affected by potent immunosuppression early posttransplant. Tacrolimus 101-111 interleukin 2 receptor subunit alpha Homo sapiens 28-32 34335631-7 2021 In that group, absolute CD4+CD25+CD127-Foxp3+ Tregs were negatively associated with steroid dose and tacrolimus trough levels (r=-0.377, p = 0.021, n=37; r=-0.43, p=0.033, n=25, respectively), opposite to IL-10+ Bregs, whose frequency apparently was not negatively affected by potent immunosuppression early posttransplant. Tacrolimus 101-111 interleukin 7 receptor Homo sapiens 33-38 34335631-7 2021 In that group, absolute CD4+CD25+CD127-Foxp3+ Tregs were negatively associated with steroid dose and tacrolimus trough levels (r=-0.377, p = 0.021, n=37; r=-0.43, p=0.033, n=25, respectively), opposite to IL-10+ Bregs, whose frequency apparently was not negatively affected by potent immunosuppression early posttransplant. Tacrolimus 101-111 forkhead box P3 Homo sapiens 39-44 34189904-6 2021 Western blot and immunofluorescence revealed that incorporation of CL in a lipid bilayer ameliorated the docking of CEF-FK506-nilotinib-GSH-CL-liposomes at alpha-synuclein (alpha-syn), indicating a better targeting capability of the liposomes to degenerated neurons. Tacrolimus 120-125 synuclein alpha Homo sapiens 156-171 34290503-6 2021 TAC@MD-alpha-TOC also showed significantly enhanced anti-arthritic activity compared with free TAC, as reflected by improved clinical scores and decreased IL-6 and TNF-alpha levels in serum and synovial fluids. Tacrolimus 0-3 interleukin-6 Chlorocebus sabaeus 155-159 34290503-8 2021 Chondrogenic differentiation abilities of TAC@MD-alpha-TOC were proved by increased serum and synovial fluid levels of SOX9 mRNA and protein expression. Tacrolimus 42-45 transcription factor SOX-9 Chlorocebus sabaeus 119-123 34189904-6 2021 Western blot and immunofluorescence revealed that incorporation of CL in a lipid bilayer ameliorated the docking of CEF-FK506-nilotinib-GSH-CL-liposomes at alpha-synuclein (alpha-syn), indicating a better targeting capability of the liposomes to degenerated neurons. Tacrolimus 120-125 synuclein alpha Homo sapiens 173-182 34285488-2 2021 Wuzhi capsule (WZC) could improve tacrolimus blood concentration by inhibiting the metabolism of cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp). Tacrolimus 34-44 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-115 34306041-9 2021 CYP3A4*22 was shown to significantly influence the pharmacokinetics of several drugs, with currently being most thoroughly investigated tacrolimus, cyclosporine, and statins. Tacrolimus 136-146 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 34619854-11 2021 Tacrolimus inhibited the proliferation of CD8+T cells when IL-2 concentration was 20.0,200.0 and 2 000.0 U/ml (P<0.05). Tacrolimus 0-10 CD8a molecule Homo sapiens 42-45 34619854-12 2021 The expression of perforin in CD8+T cells of SAA patients treated with tacrolimus was significantly lower than that in blank control group and IL-2 group ((2.25+-0.76)%, (6.70+-0.82)% vs (9.10+-1.90)%,all P<0.05). Tacrolimus 71-81 CD8a molecule Homo sapiens 30-33 34619854-13 2021 The level of IFN-gamma in CD8+T cells group after applying tacrolimus was significantly lower than that in the blank control group (P<0.05). Tacrolimus 59-69 interferon gamma Homo sapiens 13-22 34619854-13 2021 The level of IFN-gamma in CD8+T cells group after applying tacrolimus was significantly lower than that in the blank control group (P<0.05). Tacrolimus 59-69 CD8a molecule Homo sapiens 26-29 34619854-15 2021 The expression of perforin in CD8+T cells in tacrolimus group was significantly lower than that in SAA group ((18. Tacrolimus 45-55 CD8a molecule Homo sapiens 30-33 34236044-7 2021 OX40 immunoPET signals also reflected the subject"s immunosuppression level with tacrolimus in this study. Tacrolimus 81-91 tumor necrosis factor receptor superfamily, member 4 Mus musculus 0-4 34290611-0 2021 CYP3A5 Genotype-Dependent Drug-Drug Interaction Between Tacrolimus and Nifedipine in Chinese Renal Transplant Patients. Tacrolimus 56-66 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 34290611-2 2021 Nifedipine, frequently prescribed for hypertension, is a competitive CYP3A5 inhibitor which can inhibit tacrolimus metabolism. Tacrolimus 104-114 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 69-75 34290611-3 2021 The objective of this study was to investigate whether CYP3A5 genotype could influence tacrolimus-nifedipine DDI in Chinese renal transplant patients. Tacrolimus 87-97 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 55-61 34290611-9 2021 Results: In this study, a significant DDI between tacrolimus and nifedipine with respect to the CYP3A5*3 polymorphism was confirmed. Tacrolimus 50-60 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 96-102 34290611-12 2021 The co-administrated nifedipine and CYP3A5*3/*3 homozygotes significantly increased tacrolimus concentrations in multivariate line regression analysis. Tacrolimus 84-94 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 36-42 34290611-13 2021 Discussion: A CYP3A5 genotype-dependent DDI was found between tacrolimus and nifedipine. Tacrolimus 62-72 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 14-20 34165588-0 2021 FK506 ameliorates osteoporosis caused by osteoblast apoptosis via suppressing the activated CaN/NFAT pathway during oxidative stress. Tacrolimus 0-5 nuclear factor of activated T-cells 5 Rattus norvegicus 96-100 34165588-9 2021 FK-506 inhibited the oxidative stress and apoptosis by suppressing the activated CaN/NFAT pathway. Tacrolimus 0-6 nuclear factor of activated T-cells 5 Rattus norvegicus 85-89 34165588-12 2021 Briefly, low dose of FK-506 inhibited the oxidative stress by suppressing the activated CaN/NFAT pathway, while high dose of that further inhibited the oxidative stress by suppressing the CaN/NFAT pathway. Tacrolimus 21-27 nuclear factor of activated T-cells 5 Rattus norvegicus 92-96 34165588-12 2021 Briefly, low dose of FK-506 inhibited the oxidative stress by suppressing the activated CaN/NFAT pathway, while high dose of that further inhibited the oxidative stress by suppressing the CaN/NFAT pathway. Tacrolimus 21-27 nuclear factor of activated T-cells 5 Rattus norvegicus 192-196 34165588-13 2021 CONCLUSION: FK-506 ameliorates osteoporosis resulted from osteoblastic apoptosis which caused by suppressing the activated CaN/NFAT pathway during oxidative stress. Tacrolimus 12-18 nuclear factor of activated T-cells 5 Rattus norvegicus 127-131 34241984-2 2022 Persons carrying at least one copy of the wild-type allele, defined as CYP3A5 expressers, exhibit higher clearance and lower trough concentrations of tacrolimus than homozygous nonexpressers, and this difference may affect alloimmunization and allograft function. Tacrolimus 150-160 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 71-77 34241984-5 2022 During the first 3 years after transplant, CYP3A5 expressers tended to have lower tacrolimus trough levels than non-expressers, even though their tacrolimus dosage was as much as 80% higher. Tacrolimus 82-92 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 43-49 34241984-10 2022 CONCLUSIONS: Early detection of CYP3A5 expressers, enabling genotype-based dose adjustment of tacrolimus immediately after renal transplant, may be a useful strategy for reducing the risk of de novo DSA production and antibody-mediated rejection. Tacrolimus 94-104 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 32-38 34168412-0 2021 Early serum albumin changes in patients with ulcerative colitis treated with tacrolimus will predict clinical outcome. Tacrolimus 77-87 albumin Homo sapiens 12-19 34168412-2 2021 AIM: To examine serum albumin (Alb) level as a prognostic factor for the therapeutic effect of tacrolimus in clinical practice. Tacrolimus 95-105 albumin Homo sapiens 22-29 34168412-2 2021 AIM: To examine serum albumin (Alb) level as a prognostic factor for the therapeutic effect of tacrolimus in clinical practice. Tacrolimus 95-105 albumin Homo sapiens 31-34 34168412-8 2021 In the Kaplan-Meier analysis, a week 2/week 0 Alb ratio <= 1 had a significantly higher failure rate than that of > 1; Cox proportional hazard regression analysis also showed that a week 2/week 0 Alb ratio <= 1 was an independent prognostic factor for failure within 3 mo after the start of tacrolimus treatment. Tacrolimus 291-301 albumin Homo sapiens 46-49 34168412-8 2021 In the Kaplan-Meier analysis, a week 2/week 0 Alb ratio <= 1 had a significantly higher failure rate than that of > 1; Cox proportional hazard regression analysis also showed that a week 2/week 0 Alb ratio <= 1 was an independent prognostic factor for failure within 3 mo after the start of tacrolimus treatment. Tacrolimus 291-301 albumin Homo sapiens 196-199 34168412-9 2021 CONCLUSION: A week 2/week 0 Alb ratio <= 1 predicts failure within 3 mo of tacrolimus administration for UC. Tacrolimus 75-85 albumin Homo sapiens 28-31 34130909-2 2022 Each of the compounds are substrates of CYP3A4/5, the cytochrome P450 enzyme family for which tacrolimus is also a substrate. Tacrolimus 94-104 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 40-48 34108576-7 2021 A multivariable Cox regression model confirmed that high tacrolimus IPV was an independent risk factor for graft failure in the high risk group (HR, 2.90; 95% CI, 1.42-5.95, P = 0.004). Tacrolimus 57-67 cytochrome c oxidase subunit 8A Homo sapiens 16-19 34085919-1 2021 We report a case of neurotoxicity as a side effect of a calcineurin inhibitor (tacrolimus), which is used as an immunosuppressive drug after liver transplant. Tacrolimus 79-89 calcineurin binding protein 1 Homo sapiens 56-77 34090756-9 2022 Immunohistochemical caspase-3 evaluation of the axon area revealed a significant difference between group 2 (PRFM alone; 8.67 +- 0.029) and group 3 (PRFM plus topical tacrolimus; 4.42 +- 0.028) (P = 0.001). Tacrolimus 167-177 caspase 3 Rattus norvegicus 20-29 34150686-1 2021 Background: The calcineurin inhibitor (CNI) tacrolimus (TAC) is a cornerstone agent in immunosuppressive therapy in pediatric liver transplantation (LTX). Tacrolimus 44-54 calcineurin binding protein 1 Homo sapiens 16-37 34150686-1 2021 Background: The calcineurin inhibitor (CNI) tacrolimus (TAC) is a cornerstone agent in immunosuppressive therapy in pediatric liver transplantation (LTX). Tacrolimus 56-59 calcineurin binding protein 1 Homo sapiens 16-37 34077419-4 2021 Under nutrient-replete conditions, SRMS phosphorylates the PHLPP scaffold FK506-binding protein 51 (FKBP51), disrupts the FKBP51-PHLPP complex, and promotes FKBP51 degradation through the ubiquitin-proteasome pathway. Tacrolimus 74-79 src-related kinase lacking C-terminal regulatory tyrosine and N-terminal myristylation sites Homo sapiens 35-39 34077419-4 2021 Under nutrient-replete conditions, SRMS phosphorylates the PHLPP scaffold FK506-binding protein 51 (FKBP51), disrupts the FKBP51-PHLPP complex, and promotes FKBP51 degradation through the ubiquitin-proteasome pathway. Tacrolimus 74-79 PH domain and leucine rich repeat protein phosphatase 1 Homo sapiens 59-64 33149056-1 2021 BACKGROUND: The calcineurin inhibitor tacrolimus is a narrow therapeutic index medication, which requires therapeutic drug monitoring to optimize dose on the basis of systemic exposure. Tacrolimus 38-48 calcineurin binding protein 1 Homo sapiens 16-37 33729741-10 2021 Patients lacking detectable SARS-CoV-2-specific CD4 response by month 6 were more likely to be under tacrolimus (100.0% versus 66.7%; P-value = 0.087) and to have received tocilizumab for the previous COVID-19 episode (40.0% versus 0.0%; P-value = 0.087). Tacrolimus 101-111 CD4 molecule Homo sapiens 48-51 34072036-4 2021 Glucocorticoid signaling is mediated via glucocorticoid receptors, 11beta-hydroxysteroid dehydrogenases, and the FK506-binding immunophilins, Fkbp4 and Fkbp5. Tacrolimus 113-118 FK506 binding protein 4 Mus musculus 142-147 34072036-4 2021 Glucocorticoid signaling is mediated via glucocorticoid receptors, 11beta-hydroxysteroid dehydrogenases, and the FK506-binding immunophilins, Fkbp4 and Fkbp5. Tacrolimus 113-118 FK506 binding protein 5 Mus musculus 152-157 34285488-2 2021 Wuzhi capsule (WZC) could improve tacrolimus blood concentration by inhibiting the metabolism of cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp). Tacrolimus 34-44 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 117-122 34285488-2 2021 Wuzhi capsule (WZC) could improve tacrolimus blood concentration by inhibiting the metabolism of cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp). Tacrolimus 34-44 ATP binding cassette subfamily B member 1 Homo sapiens 128-142 34285488-2 2021 Wuzhi capsule (WZC) could improve tacrolimus blood concentration by inhibiting the metabolism of cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp). Tacrolimus 34-44 ATP binding cassette subfamily B member 1 Homo sapiens 144-148 34095318-0 2021 Tacrolimus Protects Podocytes from Apoptosis via Downregulation of TRPC6 in Diabetic Nephropathy. Tacrolimus 0-10 transient receptor potential cation channel, subfamily C, member 6 Rattus norvegicus 67-72 34095318-10 2021 Decreased expression of nephrin and increased expression of TRPC6, cleaved-caspase-3, and bax/bcl-2 ratios were found in podocytes, along with higher apoptotic percentage, while tacrolimus intervention counteracted the effect of HG on podocytes. Tacrolimus 178-188 transient receptor potential cation channel, subfamily C, member 6 Rattus norvegicus 60-65 34095318-11 2021 Our results suggest that tacrolimus protects podocytes during the progression of type 2 diabetic nephropathy, possibly ameliorating podocyte apoptosis by downregulating the expression of TRPC6. Tacrolimus 25-35 transient receptor potential cation channel, subfamily C, member 6 Rattus norvegicus 187-192 34145119-11 2021 Aspartate aminotransferase was identified to be the main covariate that influences tacrolimus CL/F. Tacrolimus 83-93 crooked neck pre-mRNA splicing factor 1 Homo sapiens 94-98 34525930-1 2021 BACKGROUND: Although the pharmacokinetic variability of Tacrolimus (Tac) metabolism is primarily influenced by CYP3A5 genotypes, the potential effect according to CYP3A5 polymorphisms in Tac extended-release (Tac-ER) and immediate-release (Tac-IR) and between these formulations" conversion needs further investigation. Tacrolimus 56-66 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 111-117 34104149-0 2021 Influence of ABCB1 gene polymorphism on concentration to dose ratio and adverse effects of tacrolimus in Pakistani liver transplant recipients. Tacrolimus 91-101 ATP binding cassette subfamily B member 1 Homo sapiens 13-18 34104149-1 2021 Objective: To evaluate the possible association of ABCB1 single nucleotide polymorphism (SNPs) of the ABCB1 gene with tacrolimus dosages, concentration-to-dose ratios (CDR) and adverse effects in Pakistani liver transplant recipients. Tacrolimus 118-128 ATP binding cassette subfamily B member 1 Homo sapiens 51-56 34104149-1 2021 Objective: To evaluate the possible association of ABCB1 single nucleotide polymorphism (SNPs) of the ABCB1 gene with tacrolimus dosages, concentration-to-dose ratios (CDR) and adverse effects in Pakistani liver transplant recipients. Tacrolimus 118-128 ATP binding cassette subfamily B member 1 Homo sapiens 102-107 34104149-8 2021 Results: ABCB1 rs1045642 CC genotype showed lower tacrolimus CDR as compared to CT and TT genotype in the first week of the post-transplantation period (p=0.02). Tacrolimus 50-60 ATP binding cassette subfamily B member 1 Homo sapiens 9-14 34104149-10 2021 Conclusion: Identification of ABCB1 rs1045642 polymorphism may shorten the time to achieve optimum levels of tacrolimus during dose titration. Tacrolimus 109-119 ATP binding cassette subfamily B member 1 Homo sapiens 30-35 34104149-11 2021 ABCB1 polymorphism rs1045642, rs2032582 and rs1128503 may predict adverse effects in liver transplant recipients receiving tacrolimus. Tacrolimus 123-133 ATP binding cassette subfamily B member 1 Homo sapiens 0-5 34570631-4 2021 In contrast, treatment with tacrolimus or mycophenolate led to reduced expression of functional molecule GITR in CB-Tregs, impaired their viability, proliferation and mitochondrial metabolism. Tacrolimus 28-38 TNF receptor superfamily member 18 Homo sapiens 105-109 34735755-4 2021 The topical formulation of tacrolimus is a well-known FDAapproved anti-T cell agent that was recently identified as a potent activator of ALK1, which is involved in several processes and functions including angiogenesis. Tacrolimus 27-37 secretory leukocyte peptidase inhibitor Homo sapiens 138-142 35396676-0 2022 Interactions with the CYP3A inhibitor voriconazole differ between extended-LCP- and immediate-release tacrolimus formulations. Tacrolimus 102-112 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 22-27 34535212-0 2021 Effect of tacrolimus on the expression of Park7 in glomerular podocytes injured by puromycin aminonucleoside. Tacrolimus 10-20 Parkinson disease (autosomal recessive, early onset) 7 Mus musculus 42-47 34535212-14 2021 Compared with the PAN group, the FK506 group had a significant reduction in the mRNA expression level of Park7 at all time points (P<0.01). Tacrolimus 33-38 Parkinson disease (autosomal recessive, early onset) 7 Mus musculus 105-110 34535212-16 2021 Compared with the PAN group, the FK506 group had a significant reduction in the protein expression level of Park7 at all time points (P<0.01). Tacrolimus 33-38 Parkinson disease (autosomal recessive, early onset) 7 Mus musculus 108-113 34535212-18 2021 Compared with the PAN group, the FK506 group had a significant improvement in the distribution of Park7 protein. Tacrolimus 33-38 Parkinson disease (autosomal recessive, early onset) 7 Mus musculus 98-103 34535212-20 2021 FK506 can downregulate the mRNA and protein expression of Park7 in the model of MPC-5 injury, maintain cellular homeostasis, reduce proteinuria, and delay glomerulosclerosis. Tacrolimus 0-5 Parkinson disease (autosomal recessive, early onset) 7 Mus musculus 58-63 35389944-0 2022 Composite CYP3A phenotypes influence tacrolimus dose-adjusted concentration in lung transplant recipients. Tacrolimus 37-47 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 10-15 35389944-1 2022 OBJECTIVES: Interpatient variability in tacrolimus pharmacokinetics is attributed to metabolism by cytochrome P-450 3A4/5 isoenzymes (encoded by CYP3A4 and CYP3A5). Tacrolimus 40-50 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 99-121 35389944-1 2022 OBJECTIVES: Interpatient variability in tacrolimus pharmacokinetics is attributed to metabolism by cytochrome P-450 3A4/5 isoenzymes (encoded by CYP3A4 and CYP3A5). Tacrolimus 40-50 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 145-151 35389944-1 2022 OBJECTIVES: Interpatient variability in tacrolimus pharmacokinetics is attributed to metabolism by cytochrome P-450 3A4/5 isoenzymes (encoded by CYP3A4 and CYP3A5). Tacrolimus 40-50 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 156-162 35389944-2 2022 Guidelines for adjusting tacrolimus based on CYP3A5 test results are published; however, CYP3A4 variants also contribute to the variability in tacrolimus pharmacokinetics. Tacrolimus 25-35 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 45-51 35389944-2 2022 Guidelines for adjusting tacrolimus based on CYP3A5 test results are published; however, CYP3A4 variants also contribute to the variability in tacrolimus pharmacokinetics. Tacrolimus 143-153 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 45-51 35389944-2 2022 Guidelines for adjusting tacrolimus based on CYP3A5 test results are published; however, CYP3A4 variants also contribute to the variability in tacrolimus pharmacokinetics. Tacrolimus 143-153 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-95 35389944-4 2022 The objective of this study is to investigate the impact of both increased and decreased function CYP3A variants on weight and dose-adjusted tacrolimus concentration (C0/D). Tacrolimus 141-151 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 98-103 35389944-13 2022 CONCLUSION: These data indicate that a composite CYP3A phenotype incorporating both increase and decrease variant information from CYP3A4 in addition to CYP3A5 may significantly influence tacrolimus C0/D during the early postoperative period. Tacrolimus 188-198 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 49-54 35389944-13 2022 CONCLUSION: These data indicate that a composite CYP3A phenotype incorporating both increase and decrease variant information from CYP3A4 in addition to CYP3A5 may significantly influence tacrolimus C0/D during the early postoperative period. Tacrolimus 188-198 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 131-137 35389944-13 2022 CONCLUSION: These data indicate that a composite CYP3A phenotype incorporating both increase and decrease variant information from CYP3A4 in addition to CYP3A5 may significantly influence tacrolimus C0/D during the early postoperative period. Tacrolimus 188-198 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 153-159 35060126-0 2022 Reg3g ameliorates Tacrolimus-induced pancreatic beta-cell dysfunction by restoring mitochondrial function in murine models. Tacrolimus 18-28 regenerating islet-derived 3 gamma Mus musculus 0-5 35060126-3 2022 Here, we aim to investigate the potential role of Reg3g in reversing Tac-induced beta-cell dysfunction and NODM in mice. Tacrolimus 69-72 regenerating islet-derived 3 gamma Mus musculus 50-55 35060126-4 2022 EXPERIMENTAL APPROACH: Circulating REG3A (the human homolog of mouse Reg3g) of patients treated with Tac after heart transplantation (HT) was detected. Tacrolimus 101-104 regenerating family member 3 alpha Homo sapiens 35-40 35060126-4 2022 EXPERIMENTAL APPROACH: Circulating REG3A (the human homolog of mouse Reg3g) of patients treated with Tac after heart transplantation (HT) was detected. Tacrolimus 101-104 regenerating islet-derived 3 gamma Mus musculus 69-74 35060126-9 2022 Moreover, Reg3g restored GSIS suppressed by Tac in beta-cells through improving mitochondrial functions, including increased MMP, mitochondria calcium uptake, ATP production, OCR, and contributing to an intact mitochondrial morphology. Tacrolimus 44-47 regenerating family member 3 gamma Homo sapiens 10-15 35060126-10 2022 Mechanically, Reg3g increased accumulation of pSTAT3(Ser727) in mitochondria by activating ERK1/2-STAT3 signaling pathway, leading to restoration of Tac-induced mitochondrial impairment. Tacrolimus 149-152 regenerating family member 3 gamma Homo sapiens 14-19 35060126-10 2022 Mechanically, Reg3g increased accumulation of pSTAT3(Ser727) in mitochondria by activating ERK1/2-STAT3 signaling pathway, leading to restoration of Tac-induced mitochondrial impairment. Tacrolimus 149-152 mitogen-activated protein kinase 3 Mus musculus 91-97 35060126-10 2022 Mechanically, Reg3g increased accumulation of pSTAT3(Ser727) in mitochondria by activating ERK1/2-STAT3 signaling pathway, leading to restoration of Tac-induced mitochondrial impairment. Tacrolimus 149-152 signal transducer and activator of transcription 3 Mus musculus 98-103 35060126-11 2022 Finally, Reg3g overexpression also effectively mitigated Tac-induced NODM in mice. Tacrolimus 57-60 regenerating islet-derived 3 gamma Mus musculus 9-14 35060126-12 2022 CONCLUSION AND IMPLICATIONS: Reg3g can significantly ameliorate Tac-induced beta-cell dysfunction by restoring mitochondrial function in a pSTAT3(Ser727)-dependent manner. Tacrolimus 64-67 regenerating islet-derived 3 gamma Mus musculus 29-34 35060126-13 2022 Our observations identify a novel Reg3g-mediated mechanism that is involved in Tac-induced NODM, and establish the novel role of Reg3g in reversing Tac-induced beta-cell dysfunction. Tacrolimus 79-82 regenerating islet-derived 3 gamma Mus musculus 34-39 35060126-13 2022 Our observations identify a novel Reg3g-mediated mechanism that is involved in Tac-induced NODM, and establish the novel role of Reg3g in reversing Tac-induced beta-cell dysfunction. Tacrolimus 79-82 regenerating islet-derived 3 gamma Mus musculus 129-134 35060126-13 2022 Our observations identify a novel Reg3g-mediated mechanism that is involved in Tac-induced NODM, and establish the novel role of Reg3g in reversing Tac-induced beta-cell dysfunction. Tacrolimus 148-151 regenerating islet-derived 3 gamma Mus musculus 129-134 35294797-3 2022 In experimental Sprague Dawley rat model of TAC-induced DM and nephrotoxicity, dual inhibition of DPP4 and SGLT2 significantly decreased blood glucose level, HbA1C and increased plasma insulin levels and pancreatic islet size compared with each drug. Tacrolimus 44-47 dipeptidylpeptidase 4 Rattus norvegicus 98-102 35294797-3 2022 In experimental Sprague Dawley rat model of TAC-induced DM and nephrotoxicity, dual inhibition of DPP4 and SGLT2 significantly decreased blood glucose level, HbA1C and increased plasma insulin levels and pancreatic islet size compared with each drug. Tacrolimus 44-47 solute carrier family 5 member 2 Rattus norvegicus 107-112 35294797-3 2022 In experimental Sprague Dawley rat model of TAC-induced DM and nephrotoxicity, dual inhibition of DPP4 and SGLT2 significantly decreased blood glucose level, HbA1C and increased plasma insulin levels and pancreatic islet size compared with each drug. Tacrolimus 44-47 insulin Homo sapiens 185-192 35294797-6 2022 In in vitro study, TAC decreased the cell viability of human kidney-2(HK-2) cells and insulin-secreting beta-cell-derived line(INS-1) cells. Tacrolimus 19-22 insulin Homo sapiens 86-93 35294797-7 2022 SGLT2i protected TAC-induced cell death in HK-2 cells, but not in INS-1 cells. Tacrolimus 17-20 solute carrier family 5 member 2 Rattus norvegicus 0-5 35322385-0 2022 Correction to: The impact of IL-10 and CYP3A5 gene polymorphisms on dose-adjusted trough blood tacrolimus concentrations in early post-renal transplant recipients. Tacrolimus 95-105 interleukin 10 Homo sapiens 29-34 35322385-0 2022 Correction to: The impact of IL-10 and CYP3A5 gene polymorphisms on dose-adjusted trough blood tacrolimus concentrations in early post-renal transplant recipients. Tacrolimus 95-105 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 39-45 35426036-1 2022 The FK506-binding protein 51 (FKBP51) binds progesterone receptor (PR), glucocorticoid receptor (GR), and androgen receptor (AR) to coregulate their transcriptional activity. Tacrolimus 4-9 progesterone receptor Homo sapiens 44-65 35426036-1 2022 The FK506-binding protein 51 (FKBP51) binds progesterone receptor (PR), glucocorticoid receptor (GR), and androgen receptor (AR) to coregulate their transcriptional activity. Tacrolimus 4-9 progesterone receptor Homo sapiens 67-69 35426036-1 2022 The FK506-binding protein 51 (FKBP51) binds progesterone receptor (PR), glucocorticoid receptor (GR), and androgen receptor (AR) to coregulate their transcriptional activity. Tacrolimus 4-9 nuclear receptor subfamily 3 group C member 1 Homo sapiens 72-95 35426036-1 2022 The FK506-binding protein 51 (FKBP51) binds progesterone receptor (PR), glucocorticoid receptor (GR), and androgen receptor (AR) to coregulate their transcriptional activity. Tacrolimus 4-9 nuclear receptor subfamily 3 group C member 1 Homo sapiens 97-99 35426036-1 2022 The FK506-binding protein 51 (FKBP51) binds progesterone receptor (PR), glucocorticoid receptor (GR), and androgen receptor (AR) to coregulate their transcriptional activity. Tacrolimus 4-9 androgen receptor Homo sapiens 106-123 35426036-1 2022 The FK506-binding protein 51 (FKBP51) binds progesterone receptor (PR), glucocorticoid receptor (GR), and androgen receptor (AR) to coregulate their transcriptional activity. Tacrolimus 4-9 androgen receptor Homo sapiens 125-127 35604094-3 2022 FK506 (tacrolimus) is a naturally produced macrocyclic compound that inhibits calcineurin by binding to the immunophilin FKBP12. Tacrolimus 0-5 FKBP prolyl isomerase 1A Homo sapiens 108-127 35604094-3 2022 FK506 (tacrolimus) is a naturally produced macrocyclic compound that inhibits calcineurin by binding to the immunophilin FKBP12. Tacrolimus 7-17 FKBP prolyl isomerase 1A Homo sapiens 108-127 35604094-6 2022 We now report high-resolution protein crystal structures of fungal FKBP12 and a human truncated calcineurin-FKBP12 bound to a natural FK506 analog, FK520 (ascomycin). Tacrolimus 134-139 FKBP prolyl isomerase 1A Homo sapiens 67-73 35604094-6 2022 We now report high-resolution protein crystal structures of fungal FKBP12 and a human truncated calcineurin-FKBP12 bound to a natural FK506 analog, FK520 (ascomycin). Tacrolimus 134-139 FKBP prolyl isomerase 1A Homo sapiens 108-114 35604094-10 2022 Furthermore, molecular dynamic simulations performed with JH-FK-05 binding to fungal and human FKBP12 identified additional residues outside the C-22 and C-21 positions that could be modified to generate novel FK506 analogs with improved antifungal activity. Tacrolimus 210-215 FKBP prolyl isomerase 1A Homo sapiens 95-101 35604094-10 2022 Furthermore, molecular dynamic simulations performed with JH-FK-05 binding to fungal and human FKBP12 identified additional residues outside the C-22 and C-21 positions that could be modified to generate novel FK506 analogs with improved antifungal activity. Tacrolimus 210-215 TBL1X/Y related 1 Homo sapiens 154-158 35136987-10 2022 These results indicated that intermittently blocking TCR signal by tacrolimus can promote anti-tumor immunity and inhibit the tumor growth in melanoma-bearing mice, inhibiting the transcription of several exhaustion-related genes, such as Nr4a1 and Ctla4. Tacrolimus 67-77 nuclear receptor subfamily 4, group A, member 1 Mus musculus 239-244 35136987-10 2022 These results indicated that intermittently blocking TCR signal by tacrolimus can promote anti-tumor immunity and inhibit the tumor growth in melanoma-bearing mice, inhibiting the transcription of several exhaustion-related genes, such as Nr4a1 and Ctla4. Tacrolimus 67-77 cytotoxic T-lymphocyte-associated protein 4 Mus musculus 249-254 35629245-6 2022 SNPs in CYP3A5*3 were significantly associated with greater dose-adjusted cyclosporine and tacrolimus concentrations. Tacrolimus 91-101 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 8-14 35629245-7 2022 SNPs in POR*28 were observed with significantly lower dose-adjusted concentrations, particularly with cyclosporine and tacrolimus. Tacrolimus 119-129 cytochrome p450 oxidoreductase Homo sapiens 8-11 35599203-4 2022 Tacrolimus is metabolized by the cytochrome P450 3A4 enzyme system. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 33-52 35578566-1 2022 BACKGROUND Tacrolimus is a calcineurin inhibitor (CNI) commonly used as an immunosuppressant to prevent the rejection of organ transplants. Tacrolimus 11-21 calcineurin binding protein 1 Homo sapiens 27-48 35580897-5 2022 In a treatment approach, we partially reversed vascular pathology by BMPR2-targeted treatment with FK506 in vitro and in vivo. Tacrolimus 99-104 bone morphogenetic protein receptor, type II (serine/threonine kinase) Mus musculus 69-74 35578867-0 2022 Impact of POR*28 Variant on Tacrolimus Pharmacokinetics in Kidney Transplant Patients with Different CYP3A5 Genotypes. Tacrolimus 28-38 cytochrome p450 oxidoreductase Homo sapiens 10-13 35578867-3 2022 Although the relationship between CYP3A5 polymorphisms and TAC pharmacokinetics (PK) is well established, the effects of other genetic variants on TAC metabolism, such as POR*28, still remain uncertain. Tacrolimus 147-150 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 34-40 35549669-9 2022 Tacrolimus pretreatment prevented increases in the interleukin (IL)-6-to-IL-10 ratio, vascular cell adhesion molecule-1, circulating levels of IL-1beta, IL-6-to-IL-10 ratio and glycocalyx-derived molecules. Tacrolimus 0-10 interleukin 6 Sus scrofa 51-69 35549669-9 2022 Tacrolimus pretreatment prevented increases in the interleukin (IL)-6-to-IL-10 ratio, vascular cell adhesion molecule-1, circulating levels of IL-1beta, IL-6-to-IL-10 ratio and glycocalyx-derived molecules. Tacrolimus 0-10 IL10 Sus scrofa 73-78 35549669-9 2022 Tacrolimus pretreatment prevented increases in the interleukin (IL)-6-to-IL-10 ratio, vascular cell adhesion molecule-1, circulating levels of IL-1beta, IL-6-to-IL-10 ratio and glycocalyx-derived molecules. Tacrolimus 0-10 vascular cell adhesion molecule 1 Sus scrofa 86-119 35549669-9 2022 Tacrolimus pretreatment prevented increases in the interleukin (IL)-6-to-IL-10 ratio, vascular cell adhesion molecule-1, circulating levels of IL-1beta, IL-6-to-IL-10 ratio and glycocalyx-derived molecules. Tacrolimus 0-10 interleukin 1 alpha Sus scrofa 143-151 35549669-9 2022 Tacrolimus pretreatment prevented increases in the interleukin (IL)-6-to-IL-10 ratio, vascular cell adhesion molecule-1, circulating levels of IL-1beta, IL-6-to-IL-10 ratio and glycocalyx-derived molecules. Tacrolimus 0-10 interleukin 6 Sus scrofa 153-157 35549669-9 2022 Tacrolimus pretreatment prevented increases in the interleukin (IL)-6-to-IL-10 ratio, vascular cell adhesion molecule-1, circulating levels of IL-1beta, IL-6-to-IL-10 ratio and glycocalyx-derived molecules. Tacrolimus 0-10 IL10 Sus scrofa 161-166 35549669-10 2022 Tacrolimus partially decreased apoptosis (Bax-to-Bcl2 ratio (p=0.07) and the number of apoptotic cells in the lungs (p<0.05)) but failed to improve LIS. Tacrolimus 0-10 apoptosis regulator BAX Sus scrofa 42-45 35549669-10 2022 Tacrolimus partially decreased apoptosis (Bax-to-Bcl2 ratio (p=0.07) and the number of apoptotic cells in the lungs (p<0.05)) but failed to improve LIS. Tacrolimus 0-10 apoptosis regulator Bcl-2 Sus scrofa 49-53 35570009-0 2022 Renal Cyp3a5-Expressing Genotype Decreases Tacrolimus-to-Dose Ratio in Small Cohort of Renal Transplant Recipients-Preliminary Report. Tacrolimus 43-53 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 6-12 35570009-1 2022 BACKGROUND: Previous reports have established that patient CYP3A5 allelic variability may be the most important genetic contributor to interindividual variation in tacrolimus exposure in renal transplant recipients. Tacrolimus 164-174 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 59-65 35570009-3 2022 The aim of this study was to investigate the role of the renal CYP3A5 genotype in tacrolimus concentration-to-dose ratio within 3 years posttransplant. Tacrolimus 82-92 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 63-69 35570009-4 2022 METHODS: A retrospective cohort study of 90 renal transplant recipients and their donors evaluated the effect of the CYP3A5 single-nucleotide polymorphism (rs776746) on tacrolimus exposure. Tacrolimus 169-179 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 117-123 35570009-6 2022 RESULTS: A significant effect of CYP3A5 expression on tacrolimus exposure was observed in both donors (mean +- SD: 23.8 +- 7.9 vs 32.6 +- 7.4 ng/mL/mg, respectively; P < .001) and recipients (mean +- SD: 27.1 +- 8.0 vs 32.2 +- 7.9 ng/mL/mg, respectively; P = .034) and was lower when CYP3A5 enzyme occurred. Tacrolimus 54-64 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 33-39 35570009-6 2022 RESULTS: A significant effect of CYP3A5 expression on tacrolimus exposure was observed in both donors (mean +- SD: 23.8 +- 7.9 vs 32.6 +- 7.4 ng/mL/mg, respectively; P < .001) and recipients (mean +- SD: 27.1 +- 8.0 vs 32.2 +- 7.9 ng/mL/mg, respectively; P = .034) and was lower when CYP3A5 enzyme occurred. Tacrolimus 54-64 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 284-290 35570009-7 2022 Thus, new groups were formed: the group in which at least 1 of the pairs, donor or recipient, had a CYP3A5 expressing allele (n = 23) had lower exposure to tacrolimus compared with nonexpressors (n = 67; mean +- SD: 26.2 +- 7.6 vs 33.2 +- 7.4 ng/mL/mg, respectively; P < .001). Tacrolimus 156-166 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 100-106 35570009-9 2022 Nonexpressors receiving kidneys with the CYP3A5*1 allele may benefit from higher tacrolimus doses to hasten achievement of target drug concentrations. Tacrolimus 81-91 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 41-47 35536394-15 2022 CONCLUSIONS: The CYP3A5 and ABCB1 genotypes impact TAC exposure in PBMCs, which may further alter the effects of TAC. Tacrolimus 51-54 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 17-23 35536394-15 2022 CONCLUSIONS: The CYP3A5 and ABCB1 genotypes impact TAC exposure in PBMCs, which may further alter the effects of TAC. Tacrolimus 51-54 ATP binding cassette subfamily B member 1 Homo sapiens 28-33 35536394-15 2022 CONCLUSIONS: The CYP3A5 and ABCB1 genotypes impact TAC exposure in PBMCs, which may further alter the effects of TAC. Tacrolimus 113-116 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 17-23 35536394-15 2022 CONCLUSIONS: The CYP3A5 and ABCB1 genotypes impact TAC exposure in PBMCs, which may further alter the effects of TAC. Tacrolimus 113-116 ATP binding cassette subfamily B member 1 Homo sapiens 28-33 35537812-0 2022 Tacrolimus-binding protein FKBP8 directs myosin light chain kinase-dependent barrier regulation and is a potential therapeutic target in Crohn"s disease. Tacrolimus 0-10 FKBP prolyl isomerase 8 Homo sapiens 27-32 35537812-0 2022 Tacrolimus-binding protein FKBP8 directs myosin light chain kinase-dependent barrier regulation and is a potential therapeutic target in Crohn"s disease. Tacrolimus 0-10 myosin light chain kinase Homo sapiens 41-66 35537812-8 2022 RESULTS: MLCK1 interacted specifically with the tacrolimus-binding FKBP8 PPI domain. Tacrolimus 48-58 myosin light chain kinase Homo sapiens 9-14 35537812-8 2022 RESULTS: MLCK1 interacted specifically with the tacrolimus-binding FKBP8 PPI domain. Tacrolimus 48-58 FKBP prolyl isomerase 8 Homo sapiens 67-72 35537812-10 2022 MLCK1-FKBP8 binding was blocked by tacrolimus, which reversed TNF-induced MLCK1-FKBP8 interactions, MLCK1 recruitment and barrier loss in vitro and in vivo. Tacrolimus 35-45 myosin light chain kinase Homo sapiens 0-5 35537812-10 2022 MLCK1-FKBP8 binding was blocked by tacrolimus, which reversed TNF-induced MLCK1-FKBP8 interactions, MLCK1 recruitment and barrier loss in vitro and in vivo. Tacrolimus 35-45 FKBP prolyl isomerase 8 Homo sapiens 6-11 35537812-10 2022 MLCK1-FKBP8 binding was blocked by tacrolimus, which reversed TNF-induced MLCK1-FKBP8 interactions, MLCK1 recruitment and barrier loss in vitro and in vivo. Tacrolimus 35-45 myosin light chain kinase Homo sapiens 74-79 35537812-10 2022 MLCK1-FKBP8 binding was blocked by tacrolimus, which reversed TNF-induced MLCK1-FKBP8 interactions, MLCK1 recruitment and barrier loss in vitro and in vivo. Tacrolimus 35-45 FKBP prolyl isomerase 8 Homo sapiens 80-85 35537812-10 2022 MLCK1-FKBP8 binding was blocked by tacrolimus, which reversed TNF-induced MLCK1-FKBP8 interactions, MLCK1 recruitment and barrier loss in vitro and in vivo. Tacrolimus 35-45 myosin light chain kinase Homo sapiens 100-105 35537812-12 2022 CONCLUSION: Binding to FKBP8, which can be blocked by tacrolimus, is required for MLCK1 recruitment to intercellular junctions and downstream events leading to immune-mediated barrier loss. Tacrolimus 54-64 FKBP prolyl isomerase 8 Homo sapiens 23-28 35537812-12 2022 CONCLUSION: Binding to FKBP8, which can be blocked by tacrolimus, is required for MLCK1 recruitment to intercellular junctions and downstream events leading to immune-mediated barrier loss. Tacrolimus 54-64 myosin light chain kinase Homo sapiens 82-87 35508891-9 2022 Although urine beta2-microglobulin significantly decreased following 2 months of treatment with all medications, efficacy was greater with tacrolimus than with cyclophosphamide and MMF (P < 0.001). Tacrolimus 139-149 beta-2-microglobulin Homo sapiens 15-34 35238110-10 2022 Different studies have consistently shown that CYP3A5 expressers require a higher tacrolimus dose and take longer time to achieve target blood tacrolimus levels than nonexpressers. Tacrolimus 82-92 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 47-53 35238110-10 2022 Different studies have consistently shown that CYP3A5 expressers require a higher tacrolimus dose and take longer time to achieve target blood tacrolimus levels than nonexpressers. Tacrolimus 143-153 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 47-53 35212883-1 2022 PURPOSE: Recent studies suggest that FK506 binding protein 51 (FKBP51), a negative regulator of glucocorticoid response, encoded by FKBP5, may influence insulin action. Tacrolimus 37-42 FKBP prolyl isomerase 5 Homo sapiens 132-137 35212883-1 2022 PURPOSE: Recent studies suggest that FK506 binding protein 51 (FKBP51), a negative regulator of glucocorticoid response, encoded by FKBP5, may influence insulin action. Tacrolimus 37-42 insulin Homo sapiens 153-160 35508605-0 2022 The importance of CYP2C19 genotype in tacrolimus dose optimization when concomitant with voriconazole in heart transplant recipients. Tacrolimus 38-48 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 18-25 35508605-8 2022 Besides, the fold changes of tacrolimus dose were associated with CYP2C19 genotype, which was found to be significantly lower in CYP2C19 extensive metabolizers than that in CYP2C19 intermediate metabolizers or poor metabolizers (4.06+-1.85 vs 5.49+-2.47, p=0.0031). Tacrolimus 29-39 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 66-73 35508605-8 2022 Besides, the fold changes of tacrolimus dose were associated with CYP2C19 genotype, which was found to be significantly lower in CYP2C19 extensive metabolizers than that in CYP2C19 intermediate metabolizers or poor metabolizers (4.06+-1.85 vs 5.49+-2.47, p=0.0031). Tacrolimus 29-39 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 129-136 35508605-8 2022 Besides, the fold changes of tacrolimus dose were associated with CYP2C19 genotype, which was found to be significantly lower in CYP2C19 extensive metabolizers than that in CYP2C19 intermediate metabolizers or poor metabolizers (4.06+-1.85 vs 5.49+-2.47, p=0.0031). Tacrolimus 29-39 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 173-180 35508605-10 2022 Moreover, CYP2C19 genotype and hematocrit acted as independent predicting factors for tacrolimus dose modification after voriconazole co-therapy. Tacrolimus 86-96 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 10-17 35508605-12 2022 CYP2C19 genotype and hematocrit should be considered in tailoring tacrolimus dose. Tacrolimus 66-76 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 0-7 35563498-0 2022 Physosmotic Induction of Chondrogenic Maturation Is TGF-beta Dependent and Enhanced by Calcineurin Inhibitor FK506. Tacrolimus 109-114 transforming growth factor alpha Homo sapiens 52-60 35563498-12 2022 While hyperosmolarity alone facilitates TGF-beta superfamily signaling, FK506 further enhances signaling by releasing the FKBP12 break from the type I receptor to improve collagenous marker expression. Tacrolimus 72-77 transforming growth factor alpha Homo sapiens 40-48 35563498-12 2022 While hyperosmolarity alone facilitates TGF-beta superfamily signaling, FK506 further enhances signaling by releasing the FKBP12 break from the type I receptor to improve collagenous marker expression. Tacrolimus 72-77 FKBP prolyl isomerase 1A pseudogene 2 Homo sapiens 122-128 35090967-2 2022 FKBP8 is a member of the FK506-binding proteins family (FKBP) usually found in mitochondria and the endoplasmic reticulum. Tacrolimus 25-30 FKBP prolyl isomerase 8 Homo sapiens 0-5 35395919-2 2022 In the present study, we established a population pharmacokinetic model to explore the effect of combined use of Wuzhi capsules/echinocandins and the patients" biochemical parameters such as hematocrit on blood concentrations and target doses of tacrolimus in renal transplant patients with different CYP3A5 genotypes. Tacrolimus 246-256 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 301-307 35487881-1 2022 AIMS: To investigate the effects of ABCB1 DNA methylation in donors on individual differences in tacrolimus blood concentrations following liver transplantation. Tacrolimus 97-107 ATP binding cassette subfamily B member 1 Homo sapiens 36-41 35487881-7 2022 RESULTS: Genome-wide methylation sequencing and pyrosequencing analyses showed that the methylation levels of three ABCB1 CpG sites (cg12501229, cg00634941, and cg05496710) were significantly different between groups with different tacrolimus concentration/dose (C0 /D) ratios. Tacrolimus 232-242 ATP binding cassette subfamily B member 1 Homo sapiens 116-121 35487881-8 2022 ABCB1 mRNA expression in donor livers was found to be positively correlated with tacrolimus C0 /D ratio (r = 0.458, P < 0.05). Tacrolimus 81-91 ATP binding cassette subfamily B member 1 Homo sapiens 0-5 35466485-14 2022 CYP3A5 expressors with high IPV of Tac showed worse outcomes, while the CYP3A5 polymorphism had no impact on IPV of Tac. Tacrolimus 35-38 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 35439353-9 2022 Compared to healthy subjects, the associated geometric mean ratios GMR (90% CI) for apixaban Cmax , AUC0-tlast and AUC0-inf were 197%(153, 295), 244%(184, 323) and 224%(170, 295) for transplant recipients on tacrolimus. Tacrolimus 208-218 colony stimulating factor 2 receptor subunit alpha Homo sapiens 67-70 35562875-0 2022 Examination of the Impact of CYP3A4/5 on Drug-Drug Interaction between Schizandrol A/Schizandrol B and Tacrolimus (FK-506): A Physiologically Based Pharmacokinetic Modeling Approach. Tacrolimus 103-113 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 29-37 35562875-0 2022 Examination of the Impact of CYP3A4/5 on Drug-Drug Interaction between Schizandrol A/Schizandrol B and Tacrolimus (FK-506): A Physiologically Based Pharmacokinetic Modeling Approach. Tacrolimus 115-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 29-37 35562875-2 2022 Due to their inhibitory effects on cytochrome P450 (CYP) 3A enzymes, SZA/SZB may display drug-drug interaction (DDI) with tacrolimus. Tacrolimus 122-132 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 35-59 35562875-6 2022 Moreover, our PBPK model predicted that multiple doses of SZB would increase tacrolimus exposure by 26% and 57% in CYP3A5 expressers and non-expressers, respectively. Tacrolimus 77-87 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 115-121 35066448-0 2022 Exogenous pancreatic kininogenase protects against tacrolimus-induced renal injury by inhibiting PI3K/AKT signaling: The role of bradykinin receptors. Tacrolimus 51-61 thymoma viral proto-oncogene 1 Mus musculus 102-105 35066448-9 2022 TAC-induced oxidative stress was closely associated with endoplasmic reticulum stress and mitochondrial dysfunction, resulting in excessive programmed cell death (apoptosis and autophagy) that was significantly abrogated by concurrent PK interference with PI3K/AKT signaling. Tacrolimus 0-3 thymoma viral proto-oncogene 1 Mus musculus 261-264 35091292-3 2022 The co-chaperone FK506 binding protein 51 (FKBP51) is a negative regulator of the GC receptor (GR), is highly stress responsive, and its polymorphisms have been repeatedly associated with stress-related disorders and dysfunctions in humans and rodents. Tacrolimus 17-22 FK506 binding protein 5 Mus musculus 43-49 35428510-2 2022 The enzyme encoded by the CYP3A5 gene can regulate the metabolism of tacrolimus, and the polymorphism of the CYP3A5 gene regulates the enzyme function. Tacrolimus 69-79 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 26-32 35428510-2 2022 The enzyme encoded by the CYP3A5 gene can regulate the metabolism of tacrolimus, and the polymorphism of the CYP3A5 gene regulates the enzyme function. Tacrolimus 69-79 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 109-115 35244772-1 2022 FK506-binding protein 51 (encoded by Fkpb51, also known as Fkbp5) has been associated with stress-related mental illness. Tacrolimus 0-5 FK506 binding protein 5 Mus musculus 59-64 35487881-9 2022 After treatment with 5-Aza-2-Dc, the methylation levels of the ABCB1 CpG sites in HepG2 cells significantly decreased, and this was confirmed by pyrosequencing; there was also a significant increase in ABCB1 transcription, which induced a decrease in intracellular tacrolimus concentrations. Tacrolimus 265-275 ATP binding cassette subfamily B member 1 Homo sapiens 63-68 35487881-9 2022 After treatment with 5-Aza-2-Dc, the methylation levels of the ABCB1 CpG sites in HepG2 cells significantly decreased, and this was confirmed by pyrosequencing; there was also a significant increase in ABCB1 transcription, which induced a decrease in intracellular tacrolimus concentrations. Tacrolimus 265-275 ATP binding cassette subfamily B member 1 Homo sapiens 202-207 35487881-10 2022 CONCLUSIONS: ABCB1 CpG site methylation affects tacrolimus metabolism in humans by regulating ABCB1 expression. Tacrolimus 48-58 ATP binding cassette subfamily B member 1 Homo sapiens 13-18 35487881-10 2022 CONCLUSIONS: ABCB1 CpG site methylation affects tacrolimus metabolism in humans by regulating ABCB1 expression. Tacrolimus 48-58 ATP binding cassette subfamily B member 1 Homo sapiens 94-99 35487881-11 2022 Therefore, ABCB1 DNA methylation in donor livers might be an important epigenetic factor that affects tacrolimus blood concentrations following liver transplantation. Tacrolimus 102-112 ATP binding cassette subfamily B member 1 Homo sapiens 11-16 35428708-1 2022 OBJECTIVE: The calcineurin inhibitor tacrolimus has been approved in Japan for the treatment of interstitial pneumonia in patients with polymyositis (PM) and dermatomyositis (DM). Tacrolimus 37-47 calcineurin binding protein 1 Homo sapiens 15-36 35456020-6 2022 Recombinant human FKBP11 was able to refold IgG antibody in vitro and inhibited by FK506, strongly supporting a function as antibody peptidyl-prolyl cis-trans isomerase. Tacrolimus 83-88 FKBP prolyl isomerase 11 Homo sapiens 18-24 35220592-10 2022 We also revealed the influence of genetic polymorphism of CYP3A5, POD, and a combination of COR on tacrolimus PK. Tacrolimus 99-109 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 58-64 35358111-5 2022 CD3+ T lymphocytes and CD14+ monocytes were isolated from PBMCs, and their intracellular tacrolimus concentrations were measured. Tacrolimus 89-99 CD14 molecule Homo sapiens 23-27 35395919-7 2022 CYP3A5 genotypes and co-administration of Wuzhi capsules, as well as time after renal transplantation and hematocrit, were important factors affecting the clearance of tacrolimus. Tacrolimus 168-178 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 35395919-9 2022 The Monte Carlo simulation indicated the following recommended doses of tacrolimus alone: 0.14 mg kg-1 d-1 for genotype CYP3A5*1*1, 0.12 mg kg-1 d-1 for CYP3A5*1*3, and 0.10 mg kg-1 d-1 for CYP3A5*3*3. Tacrolimus 72-82 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 120-126 35395919-9 2022 The Monte Carlo simulation indicated the following recommended doses of tacrolimus alone: 0.14 mg kg-1 d-1 for genotype CYP3A5*1*1, 0.12 mg kg-1 d-1 for CYP3A5*1*3, and 0.10 mg kg-1 d-1 for CYP3A5*3*3. Tacrolimus 72-82 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 153-159 35395919-9 2022 The Monte Carlo simulation indicated the following recommended doses of tacrolimus alone: 0.14 mg kg-1 d-1 for genotype CYP3A5*1*1, 0.12 mg kg-1 d-1 for CYP3A5*1*3, and 0.10 mg kg-1 d-1 for CYP3A5*3*3. Tacrolimus 72-82 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 190-196 35395919-10 2022 For patients receiving the combination with Wuzhi capsules, the recommended doses of tacrolimus were 0.10 mg kg-1 d-1 for CYP3A5*1*1, 0.08 mg kg-1 d-1 for CYP3A5*1*3, and 0.06 mg kg-1 d-1 for CYP3A5*3*3 genotypes. Tacrolimus 85-95 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 122-128 35395919-10 2022 For patients receiving the combination with Wuzhi capsules, the recommended doses of tacrolimus were 0.10 mg kg-1 d-1 for CYP3A5*1*1, 0.08 mg kg-1 d-1 for CYP3A5*1*3, and 0.06 mg kg-1 d-1 for CYP3A5*3*3 genotypes. Tacrolimus 85-95 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 155-161 35395919-10 2022 For patients receiving the combination with Wuzhi capsules, the recommended doses of tacrolimus were 0.10 mg kg-1 d-1 for CYP3A5*1*1, 0.08 mg kg-1 d-1 for CYP3A5*1*3, and 0.06 mg kg-1 d-1 for CYP3A5*3*3 genotypes. Tacrolimus 85-95 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 192-198 35395919-12 2022 For early kidney transplant recipients receiving tacrolimus treatment, not only body weight, but also CYP3A5 genotypes and drugs used in combination should be considered when determining the target dose of tacrolimus. Tacrolimus 206-216 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 102-108 35180322-4 2022 We elucidate the influence of CYP3A5 and MDR1 genetic polymorphisms on the WZC dose by maintaining Ctrough of TAC in Chinese healthy volunteers. Tacrolimus 110-113 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 30-36 35202484-2 2022 Genetic variation within the CYP3A5 gene locus impacts the metabolism of several clinically important drugs, including the immunosuppressants tacrolimus, sirolimus, cyclosporine, and the benzodiazepine midazolam. Tacrolimus 142-152 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 29-35 35202484-3 2022 Variable CYP3A5 activity is of clinical importance regarding tacrolimus metabolism. Tacrolimus 61-71 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 9-15 35180322-6 2022 The plasma TAC level in volunteers with high CYP3A5 expression was greatly lower than that in those with mutant CYP3A5. Tacrolimus 11-14 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 45-51 35180322-6 2022 The plasma TAC level in volunteers with high CYP3A5 expression was greatly lower than that in those with mutant CYP3A5. Tacrolimus 11-14 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 112-118 35132839-4 2022 METHODS: Trough(C0) and 1.5-hour blood levels (C1.5) of tacrolimus were measured in 95 kidney transplantation recipients. Tacrolimus 56-66 placenta associated 8 Homo sapiens 47-51 35143096-8 2022 CONCLUSIONS: Tacrolimus is the standard immunosuppression after LT and can be used in combination with other drugs such as corticosteroids and MMF, and in association with anti-IL2 receptor antibody (IL2Ra) induction. Tacrolimus 13-23 interleukin 2 receptor subunit beta Homo sapiens 177-189 35143096-8 2022 CONCLUSIONS: Tacrolimus is the standard immunosuppression after LT and can be used in combination with other drugs such as corticosteroids and MMF, and in association with anti-IL2 receptor antibody (IL2Ra) induction. Tacrolimus 13-23 interleukin 2 receptor subunit alpha Homo sapiens 200-205 35143096-10 2022 Low dose or delayed introduction of tacrolimus in association with corticosteroids and MMF and/or anti-IL2Ra induction can be used to reduce acute kidney injury. Tacrolimus 36-46 interleukin 2 receptor subunit alpha Homo sapiens 103-108 35132839-15 2022 Single nucleotide variants s in ABCB1 gene might influence the flat pattern peaks of tacrolimus absorption. Tacrolimus 85-95 ATP binding cassette subfamily B member 1 Homo sapiens 32-37 34993577-0 2022 Tacrolimus induces remission in refractory and relapsing lupus nephritis by decreasing P-glycoprotein expression and function on peripheral blood lymphocytes. Tacrolimus 0-10 ATP binding cassette subfamily B member 1 Homo sapiens 87-101 35129440-7 2022 As previous studies reported that tacrolimus treatment lead to a decrease of the measured plasma activity of lipoprotein lipase (LPL), we hypothesized that tacrolimus or related metabolites could also interfere by direct inhibition of LPL involved in TG analytical method used. Tacrolimus 34-44 lipoprotein lipase Homo sapiens 109-127 35129440-7 2022 As previous studies reported that tacrolimus treatment lead to a decrease of the measured plasma activity of lipoprotein lipase (LPL), we hypothesized that tacrolimus or related metabolites could also interfere by direct inhibition of LPL involved in TG analytical method used. Tacrolimus 34-44 lipoprotein lipase Homo sapiens 129-132 35129440-7 2022 As previous studies reported that tacrolimus treatment lead to a decrease of the measured plasma activity of lipoprotein lipase (LPL), we hypothesized that tacrolimus or related metabolites could also interfere by direct inhibition of LPL involved in TG analytical method used. Tacrolimus 34-44 lipoprotein lipase Homo sapiens 235-238 35129440-7 2022 As previous studies reported that tacrolimus treatment lead to a decrease of the measured plasma activity of lipoprotein lipase (LPL), we hypothesized that tacrolimus or related metabolites could also interfere by direct inhibition of LPL involved in TG analytical method used. Tacrolimus 156-166 lipoprotein lipase Homo sapiens 109-127 35129440-7 2022 As previous studies reported that tacrolimus treatment lead to a decrease of the measured plasma activity of lipoprotein lipase (LPL), we hypothesized that tacrolimus or related metabolites could also interfere by direct inhibition of LPL involved in TG analytical method used. Tacrolimus 156-166 lipoprotein lipase Homo sapiens 129-132 35129440-7 2022 As previous studies reported that tacrolimus treatment lead to a decrease of the measured plasma activity of lipoprotein lipase (LPL), we hypothesized that tacrolimus or related metabolites could also interfere by direct inhibition of LPL involved in TG analytical method used. Tacrolimus 156-166 lipoprotein lipase Homo sapiens 235-238 35103348-10 2022 The novel CYP3A5*3*6*7 metabolic composite was the significant covariate accounting for 15%-19% of tacrolimus variability in dose (p = 0.002); AUC0-12 h * (p < 0.001), and Cl (p < 0.001). Tacrolimus 99-109 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 10-16 35103348-11 2022 CONCLUSIONS: Tacrolimus pharmacokinetics and adverse effects were different among stable kidney transplant recipient groups based upon race and sex with interpatient variability associated with the CYP3A5*3*6*7 metabolic composite. Tacrolimus 13-23 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 198-204 35126949-8 2022 The CNI dosage of tacrolimus group and cyclosporine A group was compared before and after MMF. Tacrolimus 18-28 5'-nucleotidase, cytosolic IA Homo sapiens 4-7 35126949-10 2022 Experimental results showed that there were 16 cases (14.55%) of CNI-related renal damage in lung transplant recipients and different immunosuppressants, including 10 cases (11.36%) in males, 6 cases (27.27%) in females, 11 cases (12.09%) in tacrolimus group, and 5 cases (26.32%) in cyclosporine A group. Tacrolimus 242-252 5'-nucleotidase, cytosolic IA Homo sapiens 65-68 35213993-0 2022 Association of P450 Oxidoreductase Gene Polymorphism with Tacrolimus Pharmacokinetics in Renal Transplant Recipients: A Systematic Review and Meta-Analysis. Tacrolimus 58-68 cytochrome p450 oxidoreductase Homo sapiens 15-34 35213993-1 2022 There are conflicting results regarding the effect of the P450 oxidoreductase (POR) *28 genotype on the tacrolimus (TAC) pharmacokinetics (PKs) during the early post-transplantation period in adult renal transplant recipients. Tacrolimus 104-114 cytochrome p450 oxidoreductase Homo sapiens 58-77 35213993-1 2022 There are conflicting results regarding the effect of the P450 oxidoreductase (POR) *28 genotype on the tacrolimus (TAC) pharmacokinetics (PKs) during the early post-transplantation period in adult renal transplant recipients. Tacrolimus 104-114 cytochrome p450 oxidoreductase Homo sapiens 79-82 35213993-1 2022 There are conflicting results regarding the effect of the P450 oxidoreductase (POR) *28 genotype on the tacrolimus (TAC) pharmacokinetics (PKs) during the early post-transplantation period in adult renal transplant recipients. Tacrolimus 116-119 cytochrome p450 oxidoreductase Homo sapiens 58-77 35213993-1 2022 There are conflicting results regarding the effect of the P450 oxidoreductase (POR) *28 genotype on the tacrolimus (TAC) pharmacokinetics (PKs) during the early post-transplantation period in adult renal transplant recipients. Tacrolimus 116-119 cytochrome p450 oxidoreductase Homo sapiens 79-82 35213993-2 2022 Thus, we characterized the impact of POR*28 on TAC PKs. Tacrolimus 47-50 cytochrome p450 oxidoreductase Homo sapiens 37-40 35213993-3 2022 We conducted a systematic review on the association between POR*28 and PKs of TAC in adult renal transplant recipients. Tacrolimus 78-81 cytochrome p450 oxidoreductase Homo sapiens 60-63 35126303-6 2021 The proportion of CD19+CD24hiCD38hi/CD19+ and CD19+CD5+CD1dhi/CD19+ lymphocyte subsets increased significantly after TAC therapy (p = 0.010 and p < 0.001). Tacrolimus 117-120 CD19 molecule Homo sapiens 18-22 35126303-6 2021 The proportion of CD19+CD24hiCD38hi/CD19+ and CD19+CD5+CD1dhi/CD19+ lymphocyte subsets increased significantly after TAC therapy (p = 0.010 and p < 0.001). Tacrolimus 117-120 CD24 molecule Homo sapiens 23-27 35126303-6 2021 The proportion of CD19+CD24hiCD38hi/CD19+ and CD19+CD5+CD1dhi/CD19+ lymphocyte subsets increased significantly after TAC therapy (p = 0.010 and p < 0.001). Tacrolimus 117-120 CD19 molecule Homo sapiens 36-40 35126303-6 2021 The proportion of CD19+CD24hiCD38hi/CD19+ and CD19+CD5+CD1dhi/CD19+ lymphocyte subsets increased significantly after TAC therapy (p = 0.010 and p < 0.001). Tacrolimus 117-120 CD19 molecule Homo sapiens 46-50 35126303-6 2021 The proportion of CD19+CD24hiCD38hi/CD19+ and CD19+CD5+CD1dhi/CD19+ lymphocyte subsets increased significantly after TAC therapy (p = 0.010 and p < 0.001). Tacrolimus 117-120 CD5 molecule Homo sapiens 51-54 35126303-6 2021 The proportion of CD19+CD24hiCD38hi/CD19+ and CD19+CD5+CD1dhi/CD19+ lymphocyte subsets increased significantly after TAC therapy (p = 0.010 and p < 0.001). Tacrolimus 117-120 CD19 molecule Homo sapiens 62-66 35126303-7 2021 The proportion of CD19+BAFFR+, CD19+IFN-gamma+, and CD19+IL-10+ subsets decreased significantly after TAC therapy (p = 0.015, 0.018, and 0.042, respectively). Tacrolimus 102-105 CD19 molecule Homo sapiens 18-22 35126303-7 2021 The proportion of CD19+BAFFR+, CD19+IFN-gamma+, and CD19+IL-10+ subsets decreased significantly after TAC therapy (p = 0.015, 0.018, and 0.042, respectively). Tacrolimus 102-105 TNF receptor superfamily member 13C Homo sapiens 23-28 35126303-7 2021 The proportion of CD19+BAFFR+, CD19+IFN-gamma+, and CD19+IL-10+ subsets decreased significantly after TAC therapy (p = 0.015, 0.018, and 0.042, respectively). Tacrolimus 102-105 CD19 molecule Homo sapiens 31-35 35126303-7 2021 The proportion of CD19+BAFFR+, CD19+IFN-gamma+, and CD19+IL-10+ subsets decreased significantly after TAC therapy (p = 0.015, 0.018, and 0.042, respectively). Tacrolimus 102-105 interferon gamma Homo sapiens 36-45 35126303-7 2021 The proportion of CD19+BAFFR+, CD19+IFN-gamma+, and CD19+IL-10+ subsets decreased significantly after TAC therapy (p = 0.015, 0.018, and 0.042, respectively). Tacrolimus 102-105 CD19 molecule Homo sapiens 52-56 35126303-7 2021 The proportion of CD19+BAFFR+, CD19+IFN-gamma+, and CD19+IL-10+ subsets decreased significantly after TAC therapy (p = 0.015, 0.018, and 0.042, respectively). Tacrolimus 102-105 interleukin 10 Homo sapiens 57-62 35126303-9 2021 Conclusion: Possibly through increasing regulatory B and suppressing BAFFR+ B and interferon (IFN)-gamma+ B subsets, TAC could decrease relapse. Tacrolimus 117-120 interferon gamma Homo sapiens 82-104 34516654-10 2022 Administration of prednisolone and tacrolimus quickly alleviated the symptoms and the CK level returned to normal. Tacrolimus 35-45 cytidine/uridine monophosphate kinase 1 Homo sapiens 86-88 34651654-4 2022 Treatment with prednisolone (PSL), mycophenolate mofetil (MMF), and tacrolimus (TAC) resulted in improved SLE activity and glucose intolerance with the reduction of anti-insulin receptor autoantibodies. Tacrolimus 68-78 insulin receptor Homo sapiens 170-186 34651654-4 2022 Treatment with prednisolone (PSL), mycophenolate mofetil (MMF), and tacrolimus (TAC) resulted in improved SLE activity and glucose intolerance with the reduction of anti-insulin receptor autoantibodies. Tacrolimus 80-83 insulin receptor Homo sapiens 170-186 34993577-2 2022 Tacrolimus is a P-gp inhibitor and hence, may overcome this resistance. Tacrolimus 0-10 ATP binding cassette subfamily B member 1 Homo sapiens 16-20 34993577-5 2022 Expression and function of P-gp on PBL was measured by flow cytometry (as relative fluorescence index, RFI and Rhodamine dye efflux assay) before and 3 months after tacrolimus therapy. Tacrolimus 165-175 ATP binding cassette subfamily B member 1 Homo sapiens 27-31 34993577-10 2022 Tacrolimus achieves renal response in refractory/relapsing proliferative LN patients which may be partly related to overcoming P-glycoprotein mediated treatment unresponsiveness. Tacrolimus 0-10 ATP binding cassette subfamily B member 1 Homo sapiens 127-141 2471685-0 1989 The immunosuppressant FK-506, like cyclosporins and didemnin B, inhibits calmodulin-dependent phosphorylation of the elongation factor 2 in vitro and biological effects of the phorbol ester TPA on mouse skin in vivo. Tacrolimus 22-28 eukaryotic translation elongation factor 2 Mus musculus 117-136 2483716-1 1989 Nanomolar concentrations of the novel immunosuppressive drug FK-506 inhibit the proliferation of human T lymphocytes in vitro induced by mitogenic lectins or by monoclonal antibodies directed against the CD3 or CD2 surface antigens. Tacrolimus 61-67 CD2 molecule Homo sapiens 211-214 35413717-10 2022 Tacrolimus treatment ameliorated mesangial alterations by suppressing the expressions of Th17-related cytokines such as IL-17 and IL-6. Tacrolimus 0-10 interleukin 17A Rattus norvegicus 120-125 35413717-10 2022 Tacrolimus treatment ameliorated mesangial alterations by suppressing the expressions of Th17-related cytokines such as IL-17 and IL-6. Tacrolimus 0-10 interleukin 6 Rattus norvegicus 130-134 35110472-0 2022 Pharmacokinetics of tacrolimus following an overdose in a patient with extreme obesity and genotype CYP3A5*3/*3: a case report. Tacrolimus 20-30 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 100-106 2472451-1 1989 FK506, a neutral macrolide with immunosuppressive properties, was shown to selectively and rapidly inhibit the accumulation of IL-2 mRNA, as well as the mRNAs of other early (E) phase T cell activation genes such as IL-3, IL-4, GM-CSF, TNF alpha, IFN-gamma, and c-myc in activated human peripheral blood T cells. Tacrolimus 0-5 interleukin 2 Homo sapiens 127-131 2472451-1 1989 FK506, a neutral macrolide with immunosuppressive properties, was shown to selectively and rapidly inhibit the accumulation of IL-2 mRNA, as well as the mRNAs of other early (E) phase T cell activation genes such as IL-3, IL-4, GM-CSF, TNF alpha, IFN-gamma, and c-myc in activated human peripheral blood T cells. Tacrolimus 0-5 interleukin 3 Homo sapiens 216-220 2472451-1 1989 FK506, a neutral macrolide with immunosuppressive properties, was shown to selectively and rapidly inhibit the accumulation of IL-2 mRNA, as well as the mRNAs of other early (E) phase T cell activation genes such as IL-3, IL-4, GM-CSF, TNF alpha, IFN-gamma, and c-myc in activated human peripheral blood T cells. Tacrolimus 0-5 interleukin 4 Homo sapiens 222-226 2472451-1 1989 FK506, a neutral macrolide with immunosuppressive properties, was shown to selectively and rapidly inhibit the accumulation of IL-2 mRNA, as well as the mRNAs of other early (E) phase T cell activation genes such as IL-3, IL-4, GM-CSF, TNF alpha, IFN-gamma, and c-myc in activated human peripheral blood T cells. Tacrolimus 0-5 colony stimulating factor 2 Homo sapiens 228-234 2472451-1 1989 FK506, a neutral macrolide with immunosuppressive properties, was shown to selectively and rapidly inhibit the accumulation of IL-2 mRNA, as well as the mRNAs of other early (E) phase T cell activation genes such as IL-3, IL-4, GM-CSF, TNF alpha, IFN-gamma, and c-myc in activated human peripheral blood T cells. Tacrolimus 0-5 tumor necrosis factor Homo sapiens 236-245 2472451-1 1989 FK506, a neutral macrolide with immunosuppressive properties, was shown to selectively and rapidly inhibit the accumulation of IL-2 mRNA, as well as the mRNAs of other early (E) phase T cell activation genes such as IL-3, IL-4, GM-CSF, TNF alpha, IFN-gamma, and c-myc in activated human peripheral blood T cells. Tacrolimus 0-5 interferon gamma Homo sapiens 247-256 2472451-1 1989 FK506, a neutral macrolide with immunosuppressive properties, was shown to selectively and rapidly inhibit the accumulation of IL-2 mRNA, as well as the mRNAs of other early (E) phase T cell activation genes such as IL-3, IL-4, GM-CSF, TNF alpha, IFN-gamma, and c-myc in activated human peripheral blood T cells. Tacrolimus 0-5 MYC proto-oncogene, bHLH transcription factor Homo sapiens 262-267 2472451-2 1989 The activity of FK506, when compared to Cyclosporin A, another immunosuppressant, was 10 to 100x more potent in its ability to inhibit IL-2 mRNA synthesis. Tacrolimus 16-21 interleukin 2 Homo sapiens 135-139 2472451-3 1989 FK506 inhibited IL-2 mRNA accumulation in Con A, Con A plus PMA, Ionomycin plus PMA, anti-CD3, and anti-CD3 plus PMA activated T cells. Tacrolimus 0-5 interleukin 2 Homo sapiens 16-20 2472451-6 1989 The effect of FK506 on inducible genes in non-T and non-lymphoid human cells was studied in LPS-induced monocytes and PMA or IL-1 activated synovial fibroblasts. Tacrolimus 14-19 interleukin 1 alpha Homo sapiens 125-129 2472451-8 1989 Nuclear run-off transcription studies indicate that FK506 inhibits transcription of the IL-2 gene. Tacrolimus 52-57 interleukin 2 Homo sapiens 88-92 2471685-1 1989 Similar to previous observations with cyclosporins and didemnin B, the novel immunosuppressant FK-506 inhibits the Ca2+/calmodulin-dependent phosphorylation of the eukaryotic elongation factor 2 of protein synthesis in vitro and biological effects of the phorbol ester TPA on mouse skin in vivo. Tacrolimus 95-101 eukaryotic translation elongation factor 2 Mus musculus 175-194 2465593-4 1989 FK506 inhibited in a dose-dependent manner both interleukin 2 and gamma-interferon secretion of PBMC stimulated with PHA. Tacrolimus 0-5 interleukin 2 Homo sapiens 48-61 2465593-5 1989 Complete inhibition was obtained at the concentration of 0.25 nM of FK506 for IL-2 and 1 nM of FK506 for gamma-IFN production. Tacrolimus 68-73 interleukin 2 Homo sapiens 78-82 2458329-11 1988 Therefore, as with cyclosporine, as demonstrated in our previous study, FK506 has the capacity to induce immunological unresponsiveness specific to the S-antigen. Tacrolimus 72-77 S-antigen visual arrestin Rattus norvegicus 152-161 3291267-3 1988 The introduction of new drugs such as FK 506, some of which are clearly synergistic with CsA, could ameliorate past problems with drug toxicity. Tacrolimus 38-44 ERCC excision repair 8, CSA ubiquitin ligase complex subunit Homo sapiens 89-92 2463974-6 1988 Both humoral and cellular immune response to MBP were completely suppressed in rats treated with FK506. Tacrolimus 97-102 myelin basic protein Rattus norvegicus 45-48 2442255-8 1987 On the other hand, it was found that FK506 inhibited both IL-2 secretion and IL-2 receptor expression of BC.21 after stimulation with the specific antigen. Tacrolimus 37-42 interleukin 2 Mus musculus 58-62 2442255-8 1987 On the other hand, it was found that FK506 inhibited both IL-2 secretion and IL-2 receptor expression of BC.21 after stimulation with the specific antigen. Tacrolimus 37-42 interleukin 2 Mus musculus 77-81 33512727-0 2021 Tacrolimus (FK506) treatment protects allergen, IL-5, and IL-13-induced mucosal eosinophilia. Tacrolimus 0-10 interleukin 5 Homo sapiens 48-52 33866281-0 2021 CYP3A5*3 polymorphism and age affect tacrolimus blood trough concentration in myasthenia gravis patients. Tacrolimus 37-47 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 33866281-8 2021 Thus, CYP3A5*3 polymorphism and age should be considered in optimizing the initial dose of tacrolimus for MG treatment. Tacrolimus 91-101 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 6-12 33386894-0 2021 The influence of recipient SLCO1B1 rs2291075 polymorphism on tacrolimus dose-corrected trough concentration in the early period after liver transplantation. Tacrolimus 61-71 solute carrier organic anion transporter family member 1B1 Homo sapiens 27-34 33386894-1 2021 PURPOSE: To explore the relationship between rs2291075 polymorphism in SLCO1B1 gene, which encodes an influx transmembrane protein transporter, and tacrolimus dose-corrected trough concentration (C/D, ng ml-1 mg-1 kg-1) in the early period after liver transplantation. Tacrolimus 148-158 solute carrier organic anion transporter family member 1B1 Homo sapiens 71-78 33386894-5 2021 RESULTS: The combined analysis of donor and recipient CYP3A5 rs776746 could distinguish the metabolic phenotype of tacrolimus into three groups: fast elimination (FE), intermediate elimination (IE), and slow elimination (SE), which was entitled the FIS classification system. Tacrolimus 115-125 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 54-60 33386894-5 2021 RESULTS: The combined analysis of donor and recipient CYP3A5 rs776746 could distinguish the metabolic phenotype of tacrolimus into three groups: fast elimination (FE), intermediate elimination (IE), and slow elimination (SE), which was entitled the FIS classification system. Tacrolimus 115-125 long intergenic non-protein coding RNA 1554 Homo sapiens 249-252 33838305-1 2021 Tacrolimus (FK506), a calcineurin inhibitor, is an effective immunosuppressive agent mainly used to lower the risk of organ rejection after allogeneic organ transplant. Tacrolimus 0-10 calcineurin binding protein 1 Rattus norvegicus 22-43 33838305-1 2021 Tacrolimus (FK506), a calcineurin inhibitor, is an effective immunosuppressive agent mainly used to lower the risk of organ rejection after allogeneic organ transplant. Tacrolimus 12-17 calcineurin binding protein 1 Rattus norvegicus 22-43 33512727-0 2021 Tacrolimus (FK506) treatment protects allergen, IL-5, and IL-13-induced mucosal eosinophilia. Tacrolimus 0-10 interleukin 13 Homo sapiens 58-63 33512727-0 2021 Tacrolimus (FK506) treatment protects allergen, IL-5, and IL-13-induced mucosal eosinophilia. Tacrolimus 12-17 interleukin 5 Homo sapiens 48-52 33512727-0 2021 Tacrolimus (FK506) treatment protects allergen, IL-5, and IL-13-induced mucosal eosinophilia. Tacrolimus 12-17 interleukin 13 Homo sapiens 58-63 33512727-2 2021 Herein, we present evidence that pre-and post- intraperitoneal administration of tacrolimus (FK506) is very effective in reducing CCR3/SigleF+ eosinophils in Aspergillus-challenged asthma and EoE, CD2-IL-5 induced global eosinophilia and DOX regulated IL-13 induced asthma. Tacrolimus 81-91 C-C motif chemokine receptor 3 Homo sapiens 130-134 33512727-2 2021 Herein, we present evidence that pre-and post- intraperitoneal administration of tacrolimus (FK506) is very effective in reducing CCR3/SigleF+ eosinophils in Aspergillus-challenged asthma and EoE, CD2-IL-5 induced global eosinophilia and DOX regulated IL-13 induced asthma. Tacrolimus 81-91 CD2 molecule Homo sapiens 197-200 33512727-2 2021 Herein, we present evidence that pre-and post- intraperitoneal administration of tacrolimus (FK506) is very effective in reducing CCR3/SigleF+ eosinophils in Aspergillus-challenged asthma and EoE, CD2-IL-5 induced global eosinophilia and DOX regulated IL-13 induced asthma. Tacrolimus 81-91 interleukin 5 Homo sapiens 201-205 33512727-2 2021 Herein, we present evidence that pre-and post- intraperitoneal administration of tacrolimus (FK506) is very effective in reducing CCR3/SigleF+ eosinophils in Aspergillus-challenged asthma and EoE, CD2-IL-5 induced global eosinophilia and DOX regulated IL-13 induced asthma. Tacrolimus 81-91 interleukin 13 Homo sapiens 252-257 33512727-2 2021 Herein, we present evidence that pre-and post- intraperitoneal administration of tacrolimus (FK506) is very effective in reducing CCR3/SigleF+ eosinophils in Aspergillus-challenged asthma and EoE, CD2-IL-5 induced global eosinophilia and DOX regulated IL-13 induced asthma. Tacrolimus 93-98 C-C motif chemokine receptor 3 Homo sapiens 130-134 33512727-2 2021 Herein, we present evidence that pre-and post- intraperitoneal administration of tacrolimus (FK506) is very effective in reducing CCR3/SigleF+ eosinophils in Aspergillus-challenged asthma and EoE, CD2-IL-5 induced global eosinophilia and DOX regulated IL-13 induced asthma. Tacrolimus 93-98 CD2 molecule Homo sapiens 197-200 33512727-2 2021 Herein, we present evidence that pre-and post- intraperitoneal administration of tacrolimus (FK506) is very effective in reducing CCR3/SigleF+ eosinophils in Aspergillus-challenged asthma and EoE, CD2-IL-5 induced global eosinophilia and DOX regulated IL-13 induced asthma. Tacrolimus 93-98 interleukin 5 Homo sapiens 201-205 33512727-2 2021 Herein, we present evidence that pre-and post- intraperitoneal administration of tacrolimus (FK506) is very effective in reducing CCR3/SigleF+ eosinophils in Aspergillus-challenged asthma and EoE, CD2-IL-5 induced global eosinophilia and DOX regulated IL-13 induced asthma. Tacrolimus 93-98 interleukin 13 Homo sapiens 252-257 33512727-4 2021 Additionally, we also performed ELISA and Western blot analyses to show that tacrolimus treatment also reduces the levels of eosinophil-specific cytokines IL-4, IL-5, IL-13, TGF-beta, eosinophil-specific chemokines Eotaxin-1, Eotaxin-2, and progenitors target RCAN1 mRNA levels. Tacrolimus 77-87 interleukin 4 Homo sapiens 155-159 33512727-4 2021 Additionally, we also performed ELISA and Western blot analyses to show that tacrolimus treatment also reduces the levels of eosinophil-specific cytokines IL-4, IL-5, IL-13, TGF-beta, eosinophil-specific chemokines Eotaxin-1, Eotaxin-2, and progenitors target RCAN1 mRNA levels. Tacrolimus 77-87 interleukin 5 Homo sapiens 161-165 33512727-4 2021 Additionally, we also performed ELISA and Western blot analyses to show that tacrolimus treatment also reduces the levels of eosinophil-specific cytokines IL-4, IL-5, IL-13, TGF-beta, eosinophil-specific chemokines Eotaxin-1, Eotaxin-2, and progenitors target RCAN1 mRNA levels. Tacrolimus 77-87 interleukin 13 Homo sapiens 167-172 33512727-4 2021 Additionally, we also performed ELISA and Western blot analyses to show that tacrolimus treatment also reduces the levels of eosinophil-specific cytokines IL-4, IL-5, IL-13, TGF-beta, eosinophil-specific chemokines Eotaxin-1, Eotaxin-2, and progenitors target RCAN1 mRNA levels. Tacrolimus 77-87 transforming growth factor alpha Homo sapiens 174-182 33512727-4 2021 Additionally, we also performed ELISA and Western blot analyses to show that tacrolimus treatment also reduces the levels of eosinophil-specific cytokines IL-4, IL-5, IL-13, TGF-beta, eosinophil-specific chemokines Eotaxin-1, Eotaxin-2, and progenitors target RCAN1 mRNA levels. Tacrolimus 77-87 C-C motif chemokine ligand 11 Homo sapiens 215-224 33512727-4 2021 Additionally, we also performed ELISA and Western blot analyses to show that tacrolimus treatment also reduces the levels of eosinophil-specific cytokines IL-4, IL-5, IL-13, TGF-beta, eosinophil-specific chemokines Eotaxin-1, Eotaxin-2, and progenitors target RCAN1 mRNA levels. Tacrolimus 77-87 C-C motif chemokine ligand 24 Homo sapiens 226-235 33512727-4 2021 Additionally, we also performed ELISA and Western blot analyses to show that tacrolimus treatment also reduces the levels of eosinophil-specific cytokines IL-4, IL-5, IL-13, TGF-beta, eosinophil-specific chemokines Eotaxin-1, Eotaxin-2, and progenitors target RCAN1 mRNA levels. Tacrolimus 77-87 regulator of calcineurin 1 Homo sapiens 260-265 33512727-6 2021 Mechanistically, we show that tacrolimus in vitro treatment inhibited bone marrow derived eosinophil proliferation and viability by promoting eosinophils apoptosis that may be associated with down regulation of RCAN1. Tacrolimus 30-40 regulator of calcineurin 1 Homo sapiens 211-216 33512727-7 2021 Taken together, we provide in vivo and in vitro evidence that tacrolimus ameliorates eosinophil levels and associated pathogenesis in allergen-, IL-5- and IL-13-induced EoE, EG, and asthma pathogenesis. Tacrolimus 62-72 interleukin 5 Mus musculus 145-149 33512727-7 2021 Taken together, we provide in vivo and in vitro evidence that tacrolimus ameliorates eosinophil levels and associated pathogenesis in allergen-, IL-5- and IL-13-induced EoE, EG, and asthma pathogenesis. Tacrolimus 62-72 interleukin 13 Mus musculus 155-160 33830489-3 2021 We report three cases of cobicistat-tacrolimus co-administration, two of which also include the co-administration of mTOR inhibitors, in HIV-positive patients undergoing SOT (2 kidney and 1 liver recipient). Tacrolimus 36-46 mechanistic target of rapamycin kinase Homo sapiens 117-121 34058078-0 2021 Association of CYP3A5 polymorphisms and parathyroid hormone with blood level of tacrolimus in patients with end-stage renal disease. Tacrolimus 80-90 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 15-21 33386894-8 2021 A model consisting of tacrolimus daily dose, total bilirubin, FIS classification, and recipient SLCO1B1 rs2291075 could predict tacrolimus C/D ratios in the convalescence phase by multivariate analysis. Tacrolimus 128-138 long intergenic non-protein coding RNA 1554 Homo sapiens 62-65 33386894-8 2021 A model consisting of tacrolimus daily dose, total bilirubin, FIS classification, and recipient SLCO1B1 rs2291075 could predict tacrolimus C/D ratios in the convalescence phase by multivariate analysis. Tacrolimus 128-138 solute carrier organic anion transporter family member 1B1 Homo sapiens 96-103 33386894-10 2021 Recipient SLCO1B1 rs2291075 genotype had significant effect on tacrolimus C/D ratios in convalescence phase (p = 0.0300) and stationary phase (p = 0.0400) in subgroup, which excluded the interference come from donor and recipient CYP3A5 rs776746. Tacrolimus 63-73 solute carrier organic anion transporter family member 1B1 Homo sapiens 10-17 33386894-11 2021 CONCLUSION: SLCO1B1 rs2291075 could be a novel genetic locus associated with tacrolimus metabolism. Tacrolimus 77-87 solute carrier organic anion transporter family member 1B1 Homo sapiens 12-19 33386894-12 2021 The combined analysis of donor and recipient CYP3A5 rs776746, recipient SLCO1B1 rs2291075 genotypes, could be helpful to guide the personalized administration of tacrolimus in early period after liver transplantation. Tacrolimus 162-172 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 45-51 33386894-12 2021 The combined analysis of donor and recipient CYP3A5 rs776746, recipient SLCO1B1 rs2291075 genotypes, could be helpful to guide the personalized administration of tacrolimus in early period after liver transplantation. Tacrolimus 162-172 solute carrier organic anion transporter family member 1B1 Homo sapiens 72-79 33398393-0 2021 CYP3A5 and PPARA genetic variants are associated with low trough concentration to dose ratio of tacrolimus in kidney transplant recipients. Tacrolimus 96-106 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 33398393-0 2021 CYP3A5 and PPARA genetic variants are associated with low trough concentration to dose ratio of tacrolimus in kidney transplant recipients. Tacrolimus 96-106 peroxisome proliferator activated receptor alpha Homo sapiens 11-16 33398393-2 2021 This study is aimed at assessing the impact of allelic variants of CYP3A5 and PPARA genes on the pharmacokinetics (PK) of TAC in Brazilian kidney transplant recipients in the first-year post-transplant. Tacrolimus 122-125 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 67-73 33398393-2 2021 This study is aimed at assessing the impact of allelic variants of CYP3A5 and PPARA genes on the pharmacokinetics (PK) of TAC in Brazilian kidney transplant recipients in the first-year post-transplant. Tacrolimus 122-125 peroxisome proliferator activated receptor alpha Homo sapiens 78-83 33386894-6 2021 Tacrolimus C/D ratios of recipient SLCO1B1 rs2291075 CT and TT carriers were very close and were significantly lower than those of recipient SLCO1B1 rs2291075 CC genotype carriers in convalescence phase (p = 0.0195) and in stationary phase (p = 0.0152). Tacrolimus 0-10 solute carrier organic anion transporter family member 1B1 Homo sapiens 35-42 33649515-0 2021 Functional CYP3A variants affecting tacrolimus trough blood concentrations in Chinese renal transplant recipients. Tacrolimus 36-46 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 11-16 33649515-2 2021 We analyzed the association between 58 single nucleotide polymorphisms (SNPs) across the CYP3A gene cluster and the log-transformed tacrolimus concentration/dose ratio (log (C0/D)) in 819 renal transplant recipients (Discovery cohort). Tacrolimus 132-142 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-94 33649515-6 2021 Nine SNPs were significantly associated with tacrolimus log (C0/D) after adjustment for CYP3A5*3 and clinical factors. Tacrolimus 45-55 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 88-94 33649515-10 2021 CYP3A7*2, rs4646450, and rs3823812 are proposed as functional SNPs affecting tacrolimus trough blood concentrations in Chinese renal transplant recipients. Tacrolimus 77-87 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 0-6 34057812-5 2022 Treatment of prostate cancer cells with FK506, which binds to the FK1 domain of FKBPs, or with MJC13, an inhibitor of FKBP52-AR signaling, also inhibited AR dimer formation. Tacrolimus 40-45 androgen receptor Homo sapiens 154-156 34058078-0 2021 Association of CYP3A5 polymorphisms and parathyroid hormone with blood level of tacrolimus in patients with end-stage renal disease. Tacrolimus 80-90 parathyroid hormone Homo sapiens 40-59 34058078-1 2021 Because tacrolimus is predominantly metabolized by CYP3A, the blood concentration/dose (C/D) ratio is affected by CYP3A5 polymorphism. Tacrolimus 8-18 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 51-56 34058078-1 2021 Because tacrolimus is predominantly metabolized by CYP3A, the blood concentration/dose (C/D) ratio is affected by CYP3A5 polymorphism. Tacrolimus 8-18 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 114-120 34058078-4 2021 In this study, we examined the influence of CYP3A5 polymorphism on and association of serum intact-PTH (iPTH) level with blood tacrolimus concentration in patients with end-stage renal disease just before kidney transplantation. Tacrolimus 127-137 parathyroid hormone Homo sapiens 99-102 34058078-7 2021 The blood tacrolimus C/D (per body weight) ratio was significantly lower in CYP3A5 expressors than that in CYP3A5 nonexpressors. Tacrolimus 10-20 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 76-82 34058078-9 2021 A multiple logistic regression analysis by stepwise selection identified CYP3A5 polymorphism and serum iPTH level as significant factors associated with tacrolimus C/D. Tacrolimus 153-163 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 73-79 34042216-6 2021 The cyclosporine actions appear to be a class rather than a drug effect because similar exacerbation of LPS nephrotoxicity was observed in rats treated with tacrolimus, another calcineurin inhibitor (CNI). Tacrolimus 157-167 calcineurin binding protein 1 Rattus norvegicus 177-198 34046945-7 2021 After mTOR initiation, 50% of patients were reduced or weaned off tacrolimus and 13.7% off prednisone. Tacrolimus 66-76 mechanistic target of rapamycin kinase Homo sapiens 6-10 34042216-7 2021 Moreover, the deteriorated renal outcomes in LPS/tacrolimus-treated rats were reduced after castration or androgen receptor blockade by flutamide. Tacrolimus 49-59 androgen receptor Rattus norvegicus 106-123 34048854-4 2021 OBJECTIVE: We sought to evaluate whether ocular lesions that FADS mice spontaneously develop are similar to those of AKC patients and to estimate the efficacy of topical treatments with tacrolimus and betamethasone for FADS mice using a novel biomarker for allergic conjunctival disease, tear periostin. Tacrolimus 186-196 periostin, osteoblast specific factor Mus musculus 293-302 33977768-3 2021 Time dependent study was conducted using primary rat hepatocytes treated with TAC (36 microM) for 6, 12, 24 and 48 h. Western blot analysis was performed using cell lysate in order to analyze the regulation of HH pathway proteins including HHIP, SMO, PTCH, IHH, SHH, and GLI transcription factors. Tacrolimus 78-81 Hedgehog-interacting protein Rattus norvegicus 240-244 34006401-9 2021 The wounds treated with 0.03% tacrolimus showed weak labeling for smooth muscle actin, a higher proportion of mucin absence, strong staining for Verhoeff when compared to the controls. Tacrolimus 30-40 actin Oryctolagus cuniculus 80-85 34006401-8 2021 RESULTS: The wounds treated with 0.1% tacrolimus showed weak labeling and a lower percentage of labeling for smooth muscle actin, a higher proportion of mucin absence, weak staining, fine and organized fibers for Gomori"s Trichrome, strong staining and organized fibers for Verhoeff when compared to controls. Tacrolimus 38-48 actin Oryctolagus cuniculus 123-128 33977768-3 2021 Time dependent study was conducted using primary rat hepatocytes treated with TAC (36 microM) for 6, 12, 24 and 48 h. Western blot analysis was performed using cell lysate in order to analyze the regulation of HH pathway proteins including HHIP, SMO, PTCH, IHH, SHH, and GLI transcription factors. Tacrolimus 78-81 smoothened, frizzled class receptor Rattus norvegicus 246-249 33963666-7 2021 The calcineurin inhibitor (CNI) tacrolimus is the mainstay of immunosuppression but can result in AKI. Tacrolimus 32-42 calcineurin binding protein 1 Homo sapiens 4-25 33977768-3 2021 Time dependent study was conducted using primary rat hepatocytes treated with TAC (36 microM) for 6, 12, 24 and 48 h. Western blot analysis was performed using cell lysate in order to analyze the regulation of HH pathway proteins including HHIP, SMO, PTCH, IHH, SHH, and GLI transcription factors. Tacrolimus 78-81 patched 1 Rattus norvegicus 251-255 33977768-3 2021 Time dependent study was conducted using primary rat hepatocytes treated with TAC (36 microM) for 6, 12, 24 and 48 h. Western blot analysis was performed using cell lysate in order to analyze the regulation of HH pathway proteins including HHIP, SMO, PTCH, IHH, SHH, and GLI transcription factors. Tacrolimus 78-81 Indian hedgehog signaling molecule Rattus norvegicus 257-260 33977768-3 2021 Time dependent study was conducted using primary rat hepatocytes treated with TAC (36 microM) for 6, 12, 24 and 48 h. Western blot analysis was performed using cell lysate in order to analyze the regulation of HH pathway proteins including HHIP, SMO, PTCH, IHH, SHH, and GLI transcription factors. Tacrolimus 78-81 sonic hedgehog signaling molecule Rattus norvegicus 262-265 33977768-3 2021 Time dependent study was conducted using primary rat hepatocytes treated with TAC (36 microM) for 6, 12, 24 and 48 h. Western blot analysis was performed using cell lysate in order to analyze the regulation of HH pathway proteins including HHIP, SMO, PTCH, IHH, SHH, and GLI transcription factors. Tacrolimus 78-81 GLI family zinc finger 1 Rattus norvegicus 271-274 33938785-11 2021 FK506 therapy restored cardiac BMP signaling, reduced RV fibrosis in a BMP-dependent manner independent from its immunosuppressive effect, preserved RV capillarization and improved RV function and strain over the time-course of disease. Tacrolimus 0-5 bone morphogenetic protein receptor, type II (serine/threonine kinase) Mus musculus 31-34 33952632-2 2021 In this study, we tested the hypothesis that tacrolimus, a calcineurin inhibitor, prevents age-associated microstructural atrophy, which we measured using higher-order diffusion MRI, in the middle-aged beagle brain (n = 30, male and female). Tacrolimus 45-55 calcineurin binding protein 1 Homo sapiens 59-80 33952632-8 2021 In this study, we show that administration of the calcineurin inhibitor, tacrolimus, over one year prevents age and AD-associated microstructural changes in the hippocampus, parahippocampal cortex, and prefrontal cortex of the middle-aged beagle brain, with no noticeable adverse effects. Tacrolimus 73-83 calcineurin binding protein 1 Homo sapiens 50-71 33938785-0 2021 Improving Right Ventricular Function by Increasing BMP Signaling with FK506. Tacrolimus 70-75 bone morphogenetic protein receptor, type II (serine/threonine kinase) Mus musculus 51-54 33938785-2 2021 In pre-clinical models, pharmacological activation of bone morphogenetic protein (BMP) signaling with FK506 (Tacrolimus) improved RV function by decreasing RV afterload. Tacrolimus 102-107 bone morphogenetic protein receptor, type II (serine/threonine kinase) Mus musculus 82-85 33938785-2 2021 In pre-clinical models, pharmacological activation of bone morphogenetic protein (BMP) signaling with FK506 (Tacrolimus) improved RV function by decreasing RV afterload. Tacrolimus 109-119 bone morphogenetic protein receptor, type II (serine/threonine kinase) Mus musculus 82-85 33938785-5 2021 We hypothesized that increasing cardiac BMP signaling with FK506 improves RV structure and function in a model of fixed RV afterload after pulmonary artery banding (PAB). Tacrolimus 59-64 bone morphogenetic protein receptor, type II (serine/threonine kinase) Mus musculus 40-43 33711846-9 2021 While ACE2 level increased in the groups receiving a combination of tacrolimus and losartan or captopril, the level of increase was insignificant, compared to the group treated with tacrolimus alone. Tacrolimus 68-78 angiotensin I converting enzyme 2 Rattus norvegicus 6-10 33711846-12 2021 CONCLUSION: According to this study, tacrolimus increased the BUN and Cr levels while decreasing the ACE2 levels. Tacrolimus 37-47 angiotensin I converting enzyme 2 Rattus norvegicus 101-105 33716110-4 2021 In the first part of this study, we demonstrated in vitro that tacrolimus and cyclosporine were able to affect viability, inhibit leucocyte proliferation and suppress il2 expression in vitro. Tacrolimus 63-73 interleukin 2 Oncorhynchus mykiss 167-170 33716110-5 2021 In in vivo experiments, both doses of tacrolimus (0.5 and 1.5 mg/kg) and the lower dose of cyclosporine (20 mg/kg) significantly inhibited the expression of il2 in head kidney, three days post-injection. Tacrolimus 38-48 interleukin 2 Oncorhynchus mykiss 157-160 33716110-10 2021 il2 expression in head kidney was also suppressed in grafted animals treated with tacrolimus compared to non-treated group. Tacrolimus 82-92 interleukin 2 Oncorhynchus mykiss 0-3 33962777-1 2021 Tacrolimus, an immunosuppressant prescribed to reduce the risk of organ rejection, is metabolized by cytochrome P450 and is a substrate for P-glycoprotein. Tacrolimus 0-10 ATP binding cassette subfamily B member 1 Homo sapiens 140-154 33383132-10 2021 CONCLUSIONS: NFATC2 rs150348438, rs6013219, rs1052653, and NFATC1 rs754093, ranking high in scoring, significantly affected the post-transplant eGFR and the incidence of pneumonia, acute rejection, and nephrotoxicity in renal transplant patients taking tacrolimus. Tacrolimus 253-263 nuclear factor of activated T cells 2 Homo sapiens 13-19 33938785-11 2021 FK506 therapy restored cardiac BMP signaling, reduced RV fibrosis in a BMP-dependent manner independent from its immunosuppressive effect, preserved RV capillarization and improved RV function and strain over the time-course of disease. Tacrolimus 0-5 bone morphogenetic protein receptor, type II (serine/threonine kinase) Mus musculus 71-74 33938785-13 2021 Mechanistically, FK506 required ALK1 in hCFs as BMPR2 co-receptor to reduce TGFbeta1-induced proliferation and collagen production. Tacrolimus 17-22 secretory leukocyte peptidase inhibitor Homo sapiens 32-36 33938785-13 2021 Mechanistically, FK506 required ALK1 in hCFs as BMPR2 co-receptor to reduce TGFbeta1-induced proliferation and collagen production. Tacrolimus 17-22 bone morphogenetic protein receptor, type II (serine/threonine kinase) Mus musculus 48-53 33938785-13 2021 Mechanistically, FK506 required ALK1 in hCFs as BMPR2 co-receptor to reduce TGFbeta1-induced proliferation and collagen production. Tacrolimus 17-22 transforming growth factor beta 1 Homo sapiens 76-84 33938785-14 2021 Our study demonstrates that increasing cardiac BMP signaling with FK506 improves RV structure and function independent from its previously described beneficial effects on pulmonary vascular remodeling. Tacrolimus 66-71 bone morphogenetic protein receptor, type II (serine/threonine kinase) Mus musculus 47-50 33185367-7 2021 Tacrolimus/m-TOR inhibitors were reduced by 50% and all antimetabolites were discontinued. Tacrolimus 0-10 RAR related orphan receptor C Homo sapiens 13-16 33516819-6 2021 In addition, tacrolimus treatment combined with IR injury increased histological injury (tubular vacuolation, glomerulosclerosis and interstitial fibrosis), as well as alpha-smooth muscle actin (alpha-SMA), transforming growth factor-beta (TGF-beta), and kidney injury molecule-1 (KIM-1) expression in the renal cortex. Tacrolimus 13-23 actin gamma 2, smooth muscle Rattus norvegicus 168-193 33516819-6 2021 In addition, tacrolimus treatment combined with IR injury increased histological injury (tubular vacuolation, glomerulosclerosis and interstitial fibrosis), as well as alpha-smooth muscle actin (alpha-SMA), transforming growth factor-beta (TGF-beta), and kidney injury molecule-1 (KIM-1) expression in the renal cortex. Tacrolimus 13-23 transforming growth factor alpha Rattus norvegicus 240-248 33516819-6 2021 In addition, tacrolimus treatment combined with IR injury increased histological injury (tubular vacuolation, glomerulosclerosis and interstitial fibrosis), as well as alpha-smooth muscle actin (alpha-SMA), transforming growth factor-beta (TGF-beta), and kidney injury molecule-1 (KIM-1) expression in the renal cortex. Tacrolimus 13-23 hepatitis A virus cellular receptor 1 Rattus norvegicus 255-279 33516819-6 2021 In addition, tacrolimus treatment combined with IR injury increased histological injury (tubular vacuolation, glomerulosclerosis and interstitial fibrosis), as well as alpha-smooth muscle actin (alpha-SMA), transforming growth factor-beta (TGF-beta), and kidney injury molecule-1 (KIM-1) expression in the renal cortex. Tacrolimus 13-23 hepatitis A virus cellular receptor 1 Rattus norvegicus 281-286 33996955-0 2021 Case Report: Clinical Remission in a Cat With Severe Bilateral Eosinophilic Keratitis Receiving Combined Immunosuppressive Therapy (Triamcinolone Acetonide and Tacrolimus). Tacrolimus 160-170 catalase Homo sapiens 37-40 33925140-9 2021 Indeed, blockade of the CXCL10 receptor CXCR3 at the time of tacrolimus withdrawal prevented CD8+ T cell infiltration and the regression of SCC. Tacrolimus 61-71 chemokine (C-X-C motif) ligand 10 Mus musculus 24-30 33925140-9 2021 Indeed, blockade of the CXCL10 receptor CXCR3 at the time of tacrolimus withdrawal prevented CD8+ T cell infiltration and the regression of SCC. Tacrolimus 61-71 chemokine (C-X-C motif) receptor 3 Mus musculus 40-45 33896035-9 2021 CONCLUSION: Our data support the quick conversion to tacrolimus in the condition of persistent low CSA levels with acceptable efficacy and safety. Tacrolimus 53-63 ERCC excision repair 8, CSA ubiquitin ligase complex subunit Homo sapiens 99-102 33896348-7 2021 CONCLUSIONS: The inhibitory effect of PSL and TAC combination therapy on the progression of fibrosis in SSc-PIP may be superior to that of PSL and AZA in the long period. Tacrolimus 46-49 prolactin induced protein Homo sapiens 108-111 33887727-0 2021 Outcomes of Interleukin-2 Receptor Antagonist Induction Therapy in Standard-Risk Renal Transplant Recipients Maintained on Tacrolimus: A Systematic Review and Meta-Analysis. Tacrolimus 123-133 interleukin 2 receptor subunit alpha Homo sapiens 12-45 33887167-7 2021 Tac group showed the highest expression of caspase-3. Tacrolimus 0-3 caspase 3 Rattus norvegicus 43-52 33883562-9 2021 Consistent with these data, expression levels of genes encoding lysyl hydroxylase 2 (LH2) and its molecular chaperone FK506-binding protein 65 were both significantly increased in neoplastic samples. Tacrolimus 118-123 procollagen-lysine,2-oxoglutarate 5-dioxygenase 2 Homo sapiens 64-83 33883562-9 2021 Consistent with these data, expression levels of genes encoding lysyl hydroxylase 2 (LH2) and its molecular chaperone FK506-binding protein 65 were both significantly increased in neoplastic samples. Tacrolimus 118-123 procollagen-lysine,2-oxoglutarate 5-dioxygenase 2 Homo sapiens 85-88 33882512-5 2021 For in vitro assessment, human renal epithelium HK-2 cells were cultured under serum starvation conditions or with tacrolimus.The administration of SLPI (250 mug/kg, i.p) reduced elevated plasma creatinine and blood urea nitrogen levels, tissue myeloperoxidase content, and acute tubular necrosis induced by kidney damage. Tacrolimus 115-125 secretory leukocyte peptidase inhibitor Homo sapiens 148-152 33865397-8 2021 Moreover, HGC-TAC administration regulated renal injury via the TGF-beta1/MAPK/NF-kappaB signaling pathway. Tacrolimus 14-17 transforming growth factor, beta 1 Mus musculus 64-73 33571621-3 2021 A thin-film hydration method was used to encapsulate TAC within the chitosan-based amphiphile: N-palmitoyl-N-monomethyl-N,N-dimethyl-N,N,N-trimethyl-6-O-glycolchitosan (Molecular Envelope Technology - MET) in an aqueous formulation. Tacrolimus 53-56 hepatocyte growth factor receptor Oryctolagus cuniculus 201-204 33936035-7 2021 Through gene set enrichment analysis, we found that this subpopulation is similar to virus-specific CD8+ T cells and T cells that mediate acute rejection in patients using tacrolimus and belatacept, a selective costimulation blocker. Tacrolimus 172-182 CD8a molecule Homo sapiens 100-103 33853841-2 2021 The vast majority of patients are treated with the calcineurin inhibitor tacrolimus as the primary agent in combination with mycophenolate, with or without corticosteroids. Tacrolimus 73-83 calcineurin binding protein 1 Homo sapiens 51-72 33847343-8 2021 The combination of vedolizumab with tacrolimus further reduced the number of infiltrating CD3+ T cells and CD68+ monocytes/macrophages and was superior in ameliorating intestinal inflammation when compared to vedolizumab monotreatment. Tacrolimus 36-46 CD68 molecule Homo sapiens 107-111 33920149-0 2021 Relationship between CYP3A5 Polymorphism and Tacrolimus Blood Concentration Changes in Allogeneic Hematopoietic Stem Cell Transplant Recipients during Continuous Infusion. Tacrolimus 45-55 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 21-27 33920149-1 2021 A polymorphism in the gene encoding the metabolic enzyme cytochrome P450 family 3 subfamily A member 5 (CYP3A5) is a particularly influential factor in the use of tacrolimus in Japanese patients. Tacrolimus 163-173 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 57-102 33920149-1 2021 A polymorphism in the gene encoding the metabolic enzyme cytochrome P450 family 3 subfamily A member 5 (CYP3A5) is a particularly influential factor in the use of tacrolimus in Japanese patients. Tacrolimus 163-173 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 104-110 33920149-2 2021 Those who are homozygotic for the *3 mutation lack CYP3A5 activity, which results in substantial individual differences in tacrolimus metabolism. Tacrolimus 123-133 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 51-57 33920149-3 2021 The aim of this study was to analyze the relationship between individual differences in tacrolimus blood concentration changes and CYP3A5 polymorphisms in allogeneic hematopoietic stem cell transplantation recipients during the period of increasing blood concentration of the drug following treatment onset. Tacrolimus 88-98 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 131-137 33920149-7 2021 This study reveals the effects of CYP3A5 polymorphism on continuous changes in tacrolimus blood concentration. Tacrolimus 79-89 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 34-40 32986876-0 2021 Clinical significance of personalized tacrolimus dosing by adjusting to donor CYP3A-status in liver transplant recipients. Tacrolimus 38-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 78-83 32986876-1 2021 AIMS: Donor"s CYP3A-status (CYP3A5 genotype and CYP3A4 expression) can provide prognostic information regarding tacrolimus-metabolizing capacity of the liver graft and initial tacrolimus dosing for therapeutic blood concentrations in liver transplants. Tacrolimus 112-122 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-19 32986876-1 2021 AIMS: Donor"s CYP3A-status (CYP3A5 genotype and CYP3A4 expression) can provide prognostic information regarding tacrolimus-metabolizing capacity of the liver graft and initial tacrolimus dosing for therapeutic blood concentrations in liver transplants. Tacrolimus 112-122 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 28-34 32986876-1 2021 AIMS: Donor"s CYP3A-status (CYP3A5 genotype and CYP3A4 expression) can provide prognostic information regarding tacrolimus-metabolizing capacity of the liver graft and initial tacrolimus dosing for therapeutic blood concentrations in liver transplants. Tacrolimus 112-122 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 48-54 32986876-1 2021 AIMS: Donor"s CYP3A-status (CYP3A5 genotype and CYP3A4 expression) can provide prognostic information regarding tacrolimus-metabolizing capacity of the liver graft and initial tacrolimus dosing for therapeutic blood concentrations in liver transplants. Tacrolimus 176-186 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-19 32986876-1 2021 AIMS: Donor"s CYP3A-status (CYP3A5 genotype and CYP3A4 expression) can provide prognostic information regarding tacrolimus-metabolizing capacity of the liver graft and initial tacrolimus dosing for therapeutic blood concentrations in liver transplants. Tacrolimus 176-186 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 28-34 32986876-2 2021 The present work prospectively investigated whether CYP3A-status guided tacrolimus therapy has any potential clinical benefit for recipients in the early post-operative period. Tacrolimus 72-82 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 52-57 32986876-3 2021 METHODS: The contribution of preliminary assaying of donor CYP3A-status to the optimization of initial tacrolimus therapy and to the reduction of adverse events (acute rejection, infection, nephrotoxicity) was investigated in 112 liver transplant recipients (CYPtest group) comparing to 101 control patients on tacrolimus concentration guided therapy. Tacrolimus 103-113 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 59-64 33756310-14 2021 One study found that for each 5 ng/mL per year of tacrolimus exposure, defined by consecutive AUC, eGFR declined by 1.3 mL/min/1.73m2 (p < 0.001). Tacrolimus 50-60 epidermal growth factor receptor Homo sapiens 99-103 32761929-8 2021 Further, in a gene expression analysis of infected Kupffer cells, the TREM-1 pathway was the one with the most significant downregulation after tacrolimus treatment. Tacrolimus 144-154 triggering receptor expressed on myeloid cells 1 Mus musculus 70-76 32761929-11 2021 Our results indicate that tacrolimus treatment has a significant impact directly on Kupffer cells and on TREM-1, thereby compromising their capacity to fend off infections. Tacrolimus 26-36 triggering receptor expressed on myeloid cells 1 Mus musculus 105-111 33887167-4 2021 Tac group showed significantly lower expression of HO-1. Tacrolimus 0-3 heme oxygenase 1 Rattus norvegicus 51-55 33967795-16 2021 Conclusions: These results support that CYP3A5 and UGT1A9 genotyping in pediatric recipients might be useful and advisable to guide TAC and MPA dosing and monitoring in children that undergo kidney transplantation. Tacrolimus 132-135 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 40-46 33967795-16 2021 Conclusions: These results support that CYP3A5 and UGT1A9 genotyping in pediatric recipients might be useful and advisable to guide TAC and MPA dosing and monitoring in children that undergo kidney transplantation. Tacrolimus 132-135 UDP glucuronosyltransferase family 1 member A9 Homo sapiens 51-57 33894161-0 2021 Phenotypic screen identifies calcineurin-sparing FK506 analogs as BMP potentiators for treatment of acute kidney injury. Tacrolimus 49-54 bone morphogenetic protein 1 Homo sapiens 66-69 33894161-4 2021 We performed a high-throughput phenotypic screen and identified a series of FK506 analogs that act as potent BMP potentiators by sequestering FKBP12 from BMP type I receptors. Tacrolimus 76-81 bone morphogenetic protein 1 Homo sapiens 109-112 33894161-4 2021 We performed a high-throughput phenotypic screen and identified a series of FK506 analogs that act as potent BMP potentiators by sequestering FKBP12 from BMP type I receptors. Tacrolimus 76-81 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 142-148 33873145-4 2021 We observed that in a 4-Nitroquinoline N-oxide (4NQO)-induced oral carcinogenesis model, tacrolimus treatment was associated with a significantly lower ratio of cancer formation (52.94% vs. 90%) and a lower proportion of Ki67 and proliferation cell nuclear antigen (PCNA) -positive cells in lesion areas (P < 0.001). Tacrolimus 89-99 proliferating cell nuclear antigen Homo sapiens 230-271 33873145-9 2021 Tacrolimus induced G1/S phase arrest and significantly downregulated the expression of cyclinD1, cyclinE1, and c-Myc. Tacrolimus 0-10 cyclin D1 Homo sapiens 87-95 33873145-9 2021 Tacrolimus induced G1/S phase arrest and significantly downregulated the expression of cyclinD1, cyclinE1, and c-Myc. Tacrolimus 0-10 cyclin E1 Homo sapiens 97-105 33873145-9 2021 Tacrolimus induced G1/S phase arrest and significantly downregulated the expression of cyclinD1, cyclinE1, and c-Myc. Tacrolimus 0-10 MYC proto-oncogene, bHLH transcription factor Homo sapiens 111-116 33873145-10 2021 These results suggest that tacrolimus induces G1/S phase arrest via inhibition of cyclinD1, cyclinE1, and c-Myc expression and retards oral cell carcinogenesis in vitro and in vivo. Tacrolimus 27-37 cyclin D1 Homo sapiens 82-90 33873145-10 2021 These results suggest that tacrolimus induces G1/S phase arrest via inhibition of cyclinD1, cyclinE1, and c-Myc expression and retards oral cell carcinogenesis in vitro and in vivo. Tacrolimus 27-37 cyclin E1 Homo sapiens 92-100 33873145-10 2021 These results suggest that tacrolimus induces G1/S phase arrest via inhibition of cyclinD1, cyclinE1, and c-Myc expression and retards oral cell carcinogenesis in vitro and in vivo. Tacrolimus 27-37 MYC proto-oncogene, bHLH transcription factor Homo sapiens 106-111 33597150-8 2021 PD1 upregulation is accentuated in the presence of rapamycin but prevented by tacrolimus. Tacrolimus 78-88 programmed cell death 1 Homo sapiens 0-3 33166580-7 2021 Anti-PLA2R titers showed a significant decrease in both groups but the proportion of anti-PLA2R-positive patients who achieved immunological response (depletion of anti-PLA2R antibodies) was significantly higher at three and six months in the corticosteroid-cyclophosphamide group (77% and 92%, respectively), as compared to the tacrolimus-rituximab group (45% and 70%, respectively). Tacrolimus 329-339 phospholipase A2 receptor 1 Homo sapiens 90-95 33166580-7 2021 Anti-PLA2R titers showed a significant decrease in both groups but the proportion of anti-PLA2R-positive patients who achieved immunological response (depletion of anti-PLA2R antibodies) was significantly higher at three and six months in the corticosteroid-cyclophosphamide group (77% and 92%, respectively), as compared to the tacrolimus-rituximab group (45% and 70%, respectively). Tacrolimus 329-339 phospholipase A2 receptor 1 Homo sapiens 90-95 33027230-12 2021 Obesity, high mycophenolate mofetil daily dose at M3, and CYP3A5 expression were independently associated with higher tacrolimus exposure. Tacrolimus 118-128 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 58-64 33754647-0 2021 Effects of Tacrolimus on c-Fos in Hippocampus and Memory Performances in Streptozotocin Model of Alzheimer"s Disease of Rats. Tacrolimus 11-21 Fos proto-oncogene, AP-1 transcription factor subunit Rattus norvegicus 25-30 33754647-4 2021 Our hypothesis is that a calcineurin inhibitor, tacrolimus, could prevent the accumulation and the decrease of the neuronal cells. Tacrolimus 48-58 calcineurin binding protein 1 Rattus norvegicus 25-46 33724664-4 2021 Utilizing a combination of in vitro techniques and a mouse model of CNI nephrotoxicity, we found that the CNIs, cyclosporine A (CsA) and tacrolimus (TAC), share a similar mechanism of tubular epithelial kidney cell injury, including mitochondrial dysfunction and release of High Mobility Group Box I (HMGB1). Tacrolimus 137-147 high mobility group box 1 Mus musculus 301-306 33724664-4 2021 Utilizing a combination of in vitro techniques and a mouse model of CNI nephrotoxicity, we found that the CNIs, cyclosporine A (CsA) and tacrolimus (TAC), share a similar mechanism of tubular epithelial kidney cell injury, including mitochondrial dysfunction and release of High Mobility Group Box I (HMGB1). Tacrolimus 149-152 high mobility group box 1 Mus musculus 301-306 33732042-11 2021 The results of the GSE84908 data analysis showed that after tacrolimus treatment, the expression of DAAM1 was significantly increased (p = 0.015). Tacrolimus 60-70 dishevelled associated activator of morphogenesis 1 Homo sapiens 100-105 33746516-0 2021 Evaluating the Impact of CYP3A5 Genotype on Post-Transplant Healthcare Resource Utilization in Pediatric Renal and Heart Transplant Recipients Receiving Tacrolimus. Tacrolimus 153-163 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 25-31 33746516-1 2021 Purpose: CYP3A5 genotype is a significant contributor to inter-individual tacrolimus exposure and may impact the time required to achieve therapeutic concentrations and number of tacrolimus dose adjustments in transplant patients. Tacrolimus 74-84 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 9-15 33746516-1 2021 Purpose: CYP3A5 genotype is a significant contributor to inter-individual tacrolimus exposure and may impact the time required to achieve therapeutic concentrations and number of tacrolimus dose adjustments in transplant patients. Tacrolimus 179-189 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 9-15 33746516-11 2021 CYP3A5 genotype was not associated with any outcomes in renal transplant, however, a CYP3A5 expresser phenotype was a predictor of more dose changes, more tacrolimus concentrations, longer length of stay, and higher total charges in heart transplant recipients. Tacrolimus 155-165 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 85-91 33746516-14 2021 Conclusion: CYP3A5 genotype may predict healthcare resource utilization in the first year post-transplant, although this may be mitigated by differences in tacrolimus management. Tacrolimus 156-166 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 12-18 33751414-0 2021 Clinical Impact of the Adaptation of Initial Tacrolimus Dosing to the CYP3A5 Genotype After Kidney Transplantation: Systematic Review and Meta-Analysis of Randomized Controlled Trials. Tacrolimus 45-55 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 70-76 33692448-12 2021 Gal-9 can be regarded as a new biomarker for evaluating RA activity and therapeutic effect, including TAC. Tacrolimus 102-105 galectin 9 Homo sapiens 0-5 33248001-0 2021 Temporary decrease in tacrolimus clearance in cytochrome P450 3A5 non-expressors early after living donor kidney transplantation: Effect of interleukin 6-induced suppression of the cytochrome P450 3A gene. Tacrolimus 22-32 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 46-65 33248001-4 2021 The blood tacrolimus concentration per dose ratio (C/D) temporarily increased post-kidney transplantation on days 3 to 4 only in CYP3A5 non-expressors. Tacrolimus 10-20 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 129-135 33248001-8 2021 We hypothesise that CYP3A5 non-expressors might exhibit a temporary decrease in the oral clearance of tacrolimus via an increase in serum IL-6 concentrations early after kidney transplantation. Tacrolimus 102-112 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 20-26 33248001-8 2021 We hypothesise that CYP3A5 non-expressors might exhibit a temporary decrease in the oral clearance of tacrolimus via an increase in serum IL-6 concentrations early after kidney transplantation. Tacrolimus 102-112 interleukin 6 Homo sapiens 138-142 32749698-0 2021 Roles of BATF/JUN/IRF4 complex in tacrolimus mediated immunosuppression on Tfh cells in acute rejection after liver transplantation. Tacrolimus 34-44 basic leucine zipper ATF-like transcription factor Rattus norvegicus 9-13 32749698-0 2021 Roles of BATF/JUN/IRF4 complex in tacrolimus mediated immunosuppression on Tfh cells in acute rejection after liver transplantation. Tacrolimus 34-44 interferon regulatory factor 4 Rattus norvegicus 18-22 32749698-4 2021 This study aimed to explore the role of the BATF/JUN/IRF4 complex in rejection after LTx by treatment with Tac. Tacrolimus 107-110 basic leucine zipper ATF-like transcription factor Rattus norvegicus 44-48 32749698-4 2021 This study aimed to explore the role of the BATF/JUN/IRF4 complex in rejection after LTx by treatment with Tac. Tacrolimus 107-110 interferon regulatory factor 4 Rattus norvegicus 53-57 32749698-8 2021 The results demonstrated that Tac prolonged the allografts survival and attenuated inflammation injury, and decreased the percentage frequencies of T follicular helper (Tfh) cells in peripheral blood mononuclear cells and inhibited B-cell lymphoma 6 (Bcl-6) and IL-6 expression in Tfh cells. Tacrolimus 30-33 BCL6, transcription repressor Rattus norvegicus 251-256 32749698-8 2021 The results demonstrated that Tac prolonged the allografts survival and attenuated inflammation injury, and decreased the percentage frequencies of T follicular helper (Tfh) cells in peripheral blood mononuclear cells and inhibited B-cell lymphoma 6 (Bcl-6) and IL-6 expression in Tfh cells. Tacrolimus 30-33 interleukin 6 Rattus norvegicus 262-266 32749698-10 2021 In conclusion, the attenuation of rejection injury may be dependent on the NFAT-BATF/JUN/IRF4-IL-21 axis, and the BATF/JUN/IRF4 complex participates in the inhibition of IL-21-producing Tfh cells after treatment with Tac. Tacrolimus 217-220 basic leucine zipper ATF-like transcription factor Rattus norvegicus 114-118 32749698-10 2021 In conclusion, the attenuation of rejection injury may be dependent on the NFAT-BATF/JUN/IRF4-IL-21 axis, and the BATF/JUN/IRF4 complex participates in the inhibition of IL-21-producing Tfh cells after treatment with Tac. Tacrolimus 217-220 interferon regulatory factor 4 Rattus norvegicus 123-127 32749698-10 2021 In conclusion, the attenuation of rejection injury may be dependent on the NFAT-BATF/JUN/IRF4-IL-21 axis, and the BATF/JUN/IRF4 complex participates in the inhibition of IL-21-producing Tfh cells after treatment with Tac. Tacrolimus 217-220 interleukin 21 Rattus norvegicus 170-175 33732042-12 2021 Conclusion: Tacrolimus may inhibit the human immune response by affecting the expression of DAAM1 in liver transplant patients. Tacrolimus 12-22 dishevelled associated activator of morphogenesis 1 Homo sapiens 92-97 33673653-0 2021 Investigation of the Impact of CYP3A5 Polymorphism on Drug-Drug Interaction between Tacrolimus and Schisantherin A/Schisandrin A Based on Physiologically-Based Pharmacokinetic Modeling. Tacrolimus 84-94 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 31-37 32541562-5 2021 As we enter the fourth decade of tacrolimus use, newer studies utilizing of novel combinations (as with the mammalian target of rapamycin (mTOR) inhibitor, everolimus, and T-cell co-stimulation blockade with belatacept) offer potential for enhanced benefits. Tacrolimus 33-43 mechanistic target of rapamycin kinase Homo sapiens 108-137 33673653-8 2021 An optimized physiologically-based pharmacokinetic (PBPK) model integrated with CYP3A5 polymorphism was successfully established, providing more insights regarding the long-term DDI between tacrolimus and Wuzhi capsules in patients with different CYP3A5 genotypes. Tacrolimus 190-200 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 80-86 33673653-8 2021 An optimized physiologically-based pharmacokinetic (PBPK) model integrated with CYP3A5 polymorphism was successfully established, providing more insights regarding the long-term DDI between tacrolimus and Wuzhi capsules in patients with different CYP3A5 genotypes. Tacrolimus 190-200 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 247-253 33692688-0 2021 Commentary: The Clinical Impact of the C0/D Ratio and the CYP3A5 Genotype on Outcome in Tacrolimus Treated Kidney Transplant Recipients. Tacrolimus 88-98 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 58-64 33638630-0 2021 CD28 confers CD4+ T cells with resistance to cyclosporin A and tacrolimus but to different degrees. Tacrolimus 63-73 CD4 molecule Homo sapiens 13-16 33638630-9 2021 RESULTS: Anti-CD28 mAb conferred CD4+ T cells with resistance to both CSA and TAC, and CD28"s effect on the latter was approximately twice that on the former. Tacrolimus 78-81 CD4 molecule Homo sapiens 33-36 33638630-11 2021 The addition of LPS to culture containing DCs seemed to make CD4+ T cells slightly resistant to TAC but not to CSA. Tacrolimus 96-99 CD4 molecule Homo sapiens 61-64 33654003-0 2021 Unraveling the Genomic Architecture of the CYP3A Locus and ADME Genes for Personalized Tacrolimus Dosing. Tacrolimus 87-97 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-48 33637323-7 2021 We also found the higher frequency of Eomes+dCD4+T cells from miscarriage in response to cyclosporine, tacrolimus, Trophoblasts, and HTR8/SVneo cell line, might provide new strategy for therapy to promote maternal-fetal tolerance and prevent pregnancy loss. Tacrolimus 103-113 eomesodermin Homo sapiens 38-43 33539328-8 2021 The patient had several FSGS relapses that were treated by different combinations of plasmapheresis, pulse steroid, mycophenolic acid, tacrolimus, prednisolone, IVIG, and IV rituximab. Tacrolimus 135-145 actinin alpha 4 Homo sapiens 24-28 32908236-0 2021 Correction: Influence of CYP3A polymorphisms on tacrolimus pharmacokinetics in kidney transplant recipients. Tacrolimus 48-58 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 25-30 33348024-0 2021 Multiple microRNAs regulate tacrolimus metabolism through CYP3A5. Tacrolimus 28-38 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 58-64 33348024-1 2021 The CYP3A5 gene polymorphism accounts for the majority of inter-individual variability in tacrolimus pharmacokinetics. Tacrolimus 90-100 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 4-10 33604334-10 2020 In cultured podocytes, FK506 activated OSR1/SPAK, increased lamellipodia, accelerated cell migration, and promoted traction force. Tacrolimus 23-28 serine/threonine kinase 39 Mus musculus 44-48 33604334-11 2020 These actions of FK506 were reduced by depletion of WNK1. Tacrolimus 17-22 WNK lysine deficient protein kinase 1 Mus musculus 52-56 33093072-3 2021 From December 2016 to October 2019, five vitiligo patients from Peking Union Medical College Hospital were treated with simvastatin and tacrolimus. Tacrolimus 136-146 VAMAS6 Homo sapiens 41-49 33654003-6 2021 RESULTS: GWAS verified that CYP3A5*3 is the only common variant associated with TAC PK variability in Koreans. Tacrolimus 80-83 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 28-34 33654003-7 2021 We detected several CYP3A5 and CYP3A4 rare variants which could potentially affect TAC metabolism. Tacrolimus 83-86 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 20-26 33654003-7 2021 We detected several CYP3A5 and CYP3A4 rare variants which could potentially affect TAC metabolism. Tacrolimus 83-86 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-37 33654003-10 2021 Gene-based association tests in the 61 absorption, distribution, metabolism, and excretion (ADME) genes revealed that CYP1A1 are associated with additional TAC PK variability: CYP1A1 rare variant carriers among CYP3A5 poor metabolizers showed lower TAC trough levels than the noncarrier controls. Tacrolimus 156-159 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 118-124 33654003-10 2021 Gene-based association tests in the 61 absorption, distribution, metabolism, and excretion (ADME) genes revealed that CYP1A1 are associated with additional TAC PK variability: CYP1A1 rare variant carriers among CYP3A5 poor metabolizers showed lower TAC trough levels than the noncarrier controls. Tacrolimus 156-159 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 176-182 33654003-10 2021 Gene-based association tests in the 61 absorption, distribution, metabolism, and excretion (ADME) genes revealed that CYP1A1 are associated with additional TAC PK variability: CYP1A1 rare variant carriers among CYP3A5 poor metabolizers showed lower TAC trough levels than the noncarrier controls. Tacrolimus 156-159 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 211-217 33572801-7 2021 The 2.17 A structure of this ALK2-FKBP12.6 complex bound to the inhibitor dorsomorphin showed FKBP12.6 binding to the GS domain of ALK2 in a manner equivalent to the FKBP12 complex, with ALK2 residues Phe198 and Leu199 extending into the FK506-binding pocket of FKBP12.6. Tacrolimus 238-243 activin A receptor type 1 Homo sapiens 29-33 32843687-0 2021 Influence CYP3A polymorphisms on tacrolimus pharmacokinetics in kidney transplant recipients. Tacrolimus 33-43 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 10-15 32843687-3 2021 This study aimed to determine, in kidney transplant patients, the influence of different genotypic clusters involving these SNPs CYP3A4*1B, CYP3A4*22, and CYP3A5*3 on Tacrolimus bioavailability during the first (PTP1) and the second (PTP2) posttransplant phase (PT). Tacrolimus 167-177 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 129-135 32843687-3 2021 This study aimed to determine, in kidney transplant patients, the influence of different genotypic clusters involving these SNPs CYP3A4*1B, CYP3A4*22, and CYP3A5*3 on Tacrolimus bioavailability during the first (PTP1) and the second (PTP2) posttransplant phase (PT). Tacrolimus 167-177 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 140-146 32843687-3 2021 This study aimed to determine, in kidney transplant patients, the influence of different genotypic clusters involving these SNPs CYP3A4*1B, CYP3A4*22, and CYP3A5*3 on Tacrolimus bioavailability during the first (PTP1) and the second (PTP2) posttransplant phase (PT). Tacrolimus 167-177 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 155-161 33572801-7 2021 The 2.17 A structure of this ALK2-FKBP12.6 complex bound to the inhibitor dorsomorphin showed FKBP12.6 binding to the GS domain of ALK2 in a manner equivalent to the FKBP12 complex, with ALK2 residues Phe198 and Leu199 extending into the FK506-binding pocket of FKBP12.6. Tacrolimus 238-243 FKBP prolyl isomerase 1B Homo sapiens 34-42 33572801-7 2021 The 2.17 A structure of this ALK2-FKBP12.6 complex bound to the inhibitor dorsomorphin showed FKBP12.6 binding to the GS domain of ALK2 in a manner equivalent to the FKBP12 complex, with ALK2 residues Phe198 and Leu199 extending into the FK506-binding pocket of FKBP12.6. Tacrolimus 238-243 FKBP prolyl isomerase 1B Homo sapiens 94-102 33572801-7 2021 The 2.17 A structure of this ALK2-FKBP12.6 complex bound to the inhibitor dorsomorphin showed FKBP12.6 binding to the GS domain of ALK2 in a manner equivalent to the FKBP12 complex, with ALK2 residues Phe198 and Leu199 extending into the FK506-binding pocket of FKBP12.6. Tacrolimus 238-243 activin A receptor type 1 Homo sapiens 131-135 33572801-7 2021 The 2.17 A structure of this ALK2-FKBP12.6 complex bound to the inhibitor dorsomorphin showed FKBP12.6 binding to the GS domain of ALK2 in a manner equivalent to the FKBP12 complex, with ALK2 residues Phe198 and Leu199 extending into the FK506-binding pocket of FKBP12.6. Tacrolimus 238-243 FKBP prolyl isomerase 1A Homo sapiens 34-40 33572801-7 2021 The 2.17 A structure of this ALK2-FKBP12.6 complex bound to the inhibitor dorsomorphin showed FKBP12.6 binding to the GS domain of ALK2 in a manner equivalent to the FKBP12 complex, with ALK2 residues Phe198 and Leu199 extending into the FK506-binding pocket of FKBP12.6. Tacrolimus 238-243 activin A receptor type 1 Homo sapiens 131-135 33572801-7 2021 The 2.17 A structure of this ALK2-FKBP12.6 complex bound to the inhibitor dorsomorphin showed FKBP12.6 binding to the GS domain of ALK2 in a manner equivalent to the FKBP12 complex, with ALK2 residues Phe198 and Leu199 extending into the FK506-binding pocket of FKBP12.6. Tacrolimus 238-243 FKBP prolyl isomerase 1B Homo sapiens 94-102 32555441-0 2021 L-Carnitine protects against tacrolimus-induced renal injury by attenuating programmed cell death via PI3K/AKT/PTEN signaling. Tacrolimus 29-39 AKT serine/threonine kinase 1 Rattus norvegicus 107-110 33515077-0 2021 Correction to: CYP3A5 and CYP3A7 genetic polymorphisms affect tacrolimus concentration in pediatric patients with nephrotic syndrome. Tacrolimus 62-72 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 15-21 33515077-0 2021 Correction to: CYP3A5 and CYP3A7 genetic polymorphisms affect tacrolimus concentration in pediatric patients with nephrotic syndrome. Tacrolimus 62-72 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 26-32 33534527-0 2021 COMMENTARY: Unraveling the Genomic Architecture of the CYP3A Locus and ADME Genes for Personalized Tacrolimus Dosing. Tacrolimus 99-109 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 55-60 33536919-0 2020 Astragaloside IV Alleviates Tacrolimus-Induced Chronic Nephrotoxicity via p62-Keap1-Nrf2 Pathway. Tacrolimus 28-38 nucleoporin 62 Homo sapiens 74-77 33536919-0 2020 Astragaloside IV Alleviates Tacrolimus-Induced Chronic Nephrotoxicity via p62-Keap1-Nrf2 Pathway. Tacrolimus 28-38 kelch like ECH associated protein 1 Homo sapiens 78-83 33536919-0 2020 Astragaloside IV Alleviates Tacrolimus-Induced Chronic Nephrotoxicity via p62-Keap1-Nrf2 Pathway. Tacrolimus 28-38 NFE2 like bZIP transcription factor 2 Homo sapiens 84-88 33431785-0 2021 Suppression of Allograft Fibrosis by Regulation of Mammalian Target of Rapamycin-Related Protein Expression in Kidney-Transplanted Recipients Treated with Everolimus and Reduced Tacrolimus. Tacrolimus 178-188 mechanistic target of rapamycin kinase Homo sapiens 51-80 33432012-1 2021 Tacrolimus (TAC) pharmacokinetics is influenced by the donor CYP3A5 genotype and the age of pediatric liver recipients. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 61-67 33432012-1 2021 Tacrolimus (TAC) pharmacokinetics is influenced by the donor CYP3A5 genotype and the age of pediatric liver recipients. Tacrolimus 12-15 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 61-67 33432012-6 2021 TAC concentration/weight-adjusted dose ratio was significantly lower in recipients from CYP3A5*1/*3 donors or with extra-large (GRWR > 5%) or large (GRWR 3-5%) grafts. Tacrolimus 0-3 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 88-94 33432012-9 2021 In conclusion, TAC starting dose could be guided according to the donor CYP3A5 genotype and GRWR, allowing for a quicker achievement of target concentrations and eventually reducing the risk of rejection. Tacrolimus 15-18 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 72-78 33422095-5 2021 In this study, we identified a significant increase in the expression of miRNA-690 (miR-690) in the medial prefrontal cortex (mPFC) of FK506-binding protein 51 knock-out (Fkbp5 KO) mice. Tacrolimus 135-140 FK506 binding protein 5 Mus musculus 171-176 32555441-0 2021 L-Carnitine protects against tacrolimus-induced renal injury by attenuating programmed cell death via PI3K/AKT/PTEN signaling. Tacrolimus 29-39 phosphatase and tensin homolog Rattus norvegicus 111-115 32555441-10 2021 Human kidney proximal tubular epithelial cells (HK-2 cells) were treated with TAC (50 mug/mL) in vitro, which induced production of intracellular reactive oxygen species and expression of an array of genes controlling programmed cell death (pyroptosis, apoptosis, and autophagy) through interfering with PI3K/AKT/PTEN signaling. Tacrolimus 78-81 AKT serine/threonine kinase 1 Homo sapiens 309-312 32956624-5 2021 We developed a vector-free clustered regularly interspaced short palindromic repeats (CRISPR)-Cas9-based good manufacturing practice (GMP)-compliant protocol that efficiently targets and knocks out the gene for the adaptor protein FK506-binding protein 12 (FKBP12), required for the immunosuppressive function of tacrolimus. Tacrolimus 313-323 FKBP prolyl isomerase 1A Homo sapiens 231-255 33220920-7 2021 Particularly, tacrolimus, an inhibitor of phosphatase calcineurin, strongly suppressed the CYP11B2 expression even at 10 nM. Tacrolimus 14-24 cytochrome P450 family 11 subfamily B member 2 Homo sapiens 91-98 33790106-0 2021 The Optimal Dose of Tacrolimus in Combination Therapy with an Anti-TNFalpha Antibody in a Mouse Colitis Model. Tacrolimus 20-30 tumor necrosis factor Mus musculus 67-75 33348024-2 2021 We found that the basal expression of CYP3A5 in donor grafts also played a significant role in tacrolimus metabolism under the same genetic conditions after pediatric liver transplantation. Tacrolimus 95-105 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 38-44 33348024-6 2021 We found that these miRNAs inhibited tacrolimus metabolism that was dependent on CYP3A5. Tacrolimus 37-47 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 81-87 33348024-8 2021 Luciferase reporter assays and functional studies showed that miR-26b-5p inhibited tacrolimus metabolism by directly regulating CYP3A5, while miR-29a-5p, miR-99a-5p, and miR-532-5p targeted HNF4alpha, NR1I3, and NR1I2, respectively, in turn regulating the downstream expression of CYP3A5; the corresponding target gene siRNAs markedly abolished the effects caused by miRNA inhibitors. Tacrolimus 83-93 microRNA 26b Homo sapiens 62-69 33348024-8 2021 Luciferase reporter assays and functional studies showed that miR-26b-5p inhibited tacrolimus metabolism by directly regulating CYP3A5, while miR-29a-5p, miR-99a-5p, and miR-532-5p targeted HNF4alpha, NR1I3, and NR1I2, respectively, in turn regulating the downstream expression of CYP3A5; the corresponding target gene siRNAs markedly abolished the effects caused by miRNA inhibitors. Tacrolimus 83-93 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 128-134 33348024-9 2021 Also, the expression of miR-29a-3p, miR-99a-5p, miR-532-5p, and miR-26b-5p in donor grafts were negatively correlated with tacrolimus C/D following pediatric liver transplantation. Tacrolimus 123-133 microRNA 532 Homo sapiens 48-55 33348024-9 2021 Also, the expression of miR-29a-3p, miR-99a-5p, miR-532-5p, and miR-26b-5p in donor grafts were negatively correlated with tacrolimus C/D following pediatric liver transplantation. Tacrolimus 123-133 microRNA 26b Homo sapiens 64-71 32555441-10 2021 Human kidney proximal tubular epithelial cells (HK-2 cells) were treated with TAC (50 mug/mL) in vitro, which induced production of intracellular reactive oxygen species and expression of an array of genes controlling programmed cell death (pyroptosis, apoptosis, and autophagy) through interfering with PI3K/AKT/PTEN signaling. Tacrolimus 78-81 phosphatase and tensin homolog Homo sapiens 313-317 32803289-7 2021 Subpopulation carrying CYP3A4*1G, CYP3A5*1, ABCB1-3435TT, or SLCO1B3-699AA was presented with enhanced increment in tacrolimus C0/D by 38.8-102.9%. Tacrolimus 116-126 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 23-29 33618532-10 2021 RESULTS: In our study, serum MCP-1 levels were significantly higher in cyclosporine and tacrolimus groups than in sirolimus (p<0.05). Tacrolimus 88-98 C-C motif chemokine ligand 2 Homo sapiens 29-34 32803289-7 2021 Subpopulation carrying CYP3A4*1G, CYP3A5*1, ABCB1-3435TT, or SLCO1B3-699AA was presented with enhanced increment in tacrolimus C0/D by 38.8-102.9%. Tacrolimus 116-126 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 34-40 32803289-7 2021 Subpopulation carrying CYP3A4*1G, CYP3A5*1, ABCB1-3435TT, or SLCO1B3-699AA was presented with enhanced increment in tacrolimus C0/D by 38.8-102.9%. Tacrolimus 116-126 ATP binding cassette subfamily B member 1 Homo sapiens 44-49 32803289-7 2021 Subpopulation carrying CYP3A4*1G, CYP3A5*1, ABCB1-3435TT, or SLCO1B3-699AA was presented with enhanced increment in tacrolimus C0/D by 38.8-102.9%. Tacrolimus 116-126 solute carrier organic anion transporter family member 1B3 Homo sapiens 61-68 32803289-8 2021 CONCLUSION: Moderate effect of diltiazem on tacrolimus sparing, which might relate to the polymorphisms of CYP3A4, CYP3A5, ABCB1, and SLCO1B3, was documented. Tacrolimus 44-54 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 107-113 32803289-8 2021 CONCLUSION: Moderate effect of diltiazem on tacrolimus sparing, which might relate to the polymorphisms of CYP3A4, CYP3A5, ABCB1, and SLCO1B3, was documented. Tacrolimus 44-54 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 115-121 32803289-8 2021 CONCLUSION: Moderate effect of diltiazem on tacrolimus sparing, which might relate to the polymorphisms of CYP3A4, CYP3A5, ABCB1, and SLCO1B3, was documented. Tacrolimus 44-54 ATP binding cassette subfamily B member 1 Homo sapiens 123-128 32803289-8 2021 CONCLUSION: Moderate effect of diltiazem on tacrolimus sparing, which might relate to the polymorphisms of CYP3A4, CYP3A5, ABCB1, and SLCO1B3, was documented. Tacrolimus 44-54 solute carrier organic anion transporter family member 1B3 Homo sapiens 134-141 33631989-7 2021 FK506 clearly decreased the numbers of Th17 cells and FoxP3+IL-17+ cells. Tacrolimus 0-5 forkhead box P3 Homo sapiens 54-59 33631989-7 2021 FK506 clearly decreased the numbers of Th17 cells and FoxP3+IL-17+ cells. Tacrolimus 0-5 interleukin 17A Homo sapiens 60-65 33631989-8 2021 The proliferation capacity of cells was also inhibited by FK506, which had a greater effect on FoxP3- cells than FoxP3+ cells. Tacrolimus 58-63 forkhead box P3 Homo sapiens 95-100 33631989-8 2021 The proliferation capacity of cells was also inhibited by FK506, which had a greater effect on FoxP3- cells than FoxP3+ cells. Tacrolimus 58-63 forkhead box P3 Homo sapiens 113-118 33631989-10 2021 Our study provides that FK506 reduced the number of FoxP3low CD45RA- T cells (FrIII) by inhibiting its proliferation. Tacrolimus 24-29 forkhead box P3 Homo sapiens 52-57 33631989-10 2021 Our study provides that FK506 reduced the number of FoxP3low CD45RA- T cells (FrIII) by inhibiting its proliferation. Tacrolimus 24-29 protein tyrosine phosphatase receptor type C Homo sapiens 61-67 32238515-11 2021 Urine protein:creatinine ratio, serum anti-dsDNA antibody levels, complement C3 levels, and steroid-sparing effect were all significantly improved from 4 weeks after tacrolimus treatment initiation (p<0.001), and were sustained over 5 years. Tacrolimus 166-176 complement C3 Homo sapiens 66-79 33790106-2 2021 However, the optimal dose of TAC in combination therapy with anti-TNFalpha antibodies (TAC + anti-TNFalpha therapy) remains unclear. Tacrolimus 29-32 tumor necrosis factor Mus musculus 98-106 33790106-8 2021 The nuclear expression of NFATc1 was inversely proportional to the administered doses of TAC. Tacrolimus 89-92 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 26-32 33790106-10 2021 The serum concentration of anti-TNFalpha antibodies in the high-dose TAC + anti-TNFalpha therapy was significantly higher than those in the other groups. Tacrolimus 69-72 tumor necrosis factor Mus musculus 32-40 33790106-11 2021 Low-dose TAC exerted its immunosuppressive effect on T-cells, and additionally, high-dose TAC maintained the serum anti-TNFalpha antibody concentration. Tacrolimus 90-93 tumor necrosis factor Mus musculus 120-128 33790106-12 2021 When administered in combination with anti-TNFalpha antibodies, the dose of TAC should be adjusted according to the disease severity. Tacrolimus 76-79 tumor necrosis factor Mus musculus 43-51 33135259-1 2021 Post-Transplant Diabetes Mellitus (PTDM) shows a relationship with risk factors including obesity and tacrolimus-based immunosuppression, which decreases pancreatic insulin secretion. Tacrolimus 102-112 solute carrier family 35 member G1 Homo sapiens 0-4 32768638-3 2020 However, WZ possesses a biphasic effect on regulating CYP3A (the major metabolizing enzyme of tacrolimus), which could induce the mRNA and protein expression after long-term treatment while transiently inhibit the activity of CYP3A. Tacrolimus 94-104 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 54-59 33368914-0 2021 Age and sex determine conversion from immediate-release to extended-release tacrolimus in a multi-center cohort of Canadian pediatric renal transplant recipients. Tacrolimus 76-86 renin binding protein Homo sapiens 0-3 33363168-0 2020 FK506 Induces the TGF-beta1/Smad 3 Pathway Independently of Calcineurin Inhibition to Prevent Intervertebral Disk Degeneration. Tacrolimus 0-5 transforming growth factor, beta 1 Rattus norvegicus 18-27 33363168-0 2020 FK506 Induces the TGF-beta1/Smad 3 Pathway Independently of Calcineurin Inhibition to Prevent Intervertebral Disk Degeneration. Tacrolimus 0-5 SMAD family member 3 Rattus norvegicus 28-34 33363168-10 2020 FK506 could attenuate NP degeneration induced by IL-1beta. Tacrolimus 0-5 interleukin 1 alpha Rattus norvegicus 49-57 33363168-11 2020 Furthermore, FK506 exerted its function via TGFbeta/Smad3 activation instead of through calcineurin inhibition. Tacrolimus 13-18 transforming growth factor alpha Rattus norvegicus 44-51 33363168-11 2020 Furthermore, FK506 exerted its function via TGFbeta/Smad3 activation instead of through calcineurin inhibition. Tacrolimus 13-18 SMAD family member 3 Rattus norvegicus 52-57 33363168-12 2020 Inhibition of the TGF-beta pathway prevented the protective effect of FK506 on IVD degeneration. Tacrolimus 70-75 transforming growth factor alpha Rattus norvegicus 18-26 33363168-13 2020 In an in vivo study, FK506 injection reversed the development of rat caudal IVD degeneration influenced by Smad3. Tacrolimus 21-26 SMAD family member 3 Rattus norvegicus 107-112 33363168-14 2020 Conclusion: Our current study demonstrates the positive effect of FK506 on delaying the degeneration of IVD via the TGFbeta/Smad3 pathway. Tacrolimus 66-71 SMAD family member 3 Rattus norvegicus 124-129 33019979-11 2020 In addition, podocyte apoptosis induced by HDAC4 overexpression was effectively rescued by FK506, a pharmacological inhibitor of CaN, which was accompanied by decreased Bax and increased Bcl-2 expression. Tacrolimus 91-96 histone deacetylase 4 Homo sapiens 43-48 33019979-11 2020 In addition, podocyte apoptosis induced by HDAC4 overexpression was effectively rescued by FK506, a pharmacological inhibitor of CaN, which was accompanied by decreased Bax and increased Bcl-2 expression. Tacrolimus 91-96 BCL2 associated X, apoptosis regulator Homo sapiens 169-172 33019979-11 2020 In addition, podocyte apoptosis induced by HDAC4 overexpression was effectively rescued by FK506, a pharmacological inhibitor of CaN, which was accompanied by decreased Bax and increased Bcl-2 expression. Tacrolimus 91-96 BCL2 apoptosis regulator Homo sapiens 187-192 32768638-3 2020 However, WZ possesses a biphasic effect on regulating CYP3A (the major metabolizing enzyme of tacrolimus), which could induce the mRNA and protein expression after long-term treatment while transiently inhibit the activity of CYP3A. Tacrolimus 94-104 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 226-231 33278239-0 2021 High Intra-Patient Variability in Tacrolimus Exposure Calculated over a Long Period Is Associated with De Novo Donor-Specific Antibody Development and/or Late Rejection in Thai Kidney Transplant Patients Receiving Concomitant CYP3A4/5 Inhibitors. Tacrolimus 34-44 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 226-234 33273604-4 2020 Administration of FK506, a calcineurin inhibitor, in the heterozygous fetuses improved bone mineral content (BMC) of the neonates, although it did not save the neonates from the lethal effects of the mutation, whereas rapamycin, an mTOR inhibitor, reduced BMC, suggesting that mTOR signaling is involved in the bone mineralization of heterozygous mutants. Tacrolimus 18-23 calcineurin binding protein 1 Mus musculus 27-48 33273604-4 2020 Administration of FK506, a calcineurin inhibitor, in the heterozygous fetuses improved bone mineral content (BMC) of the neonates, although it did not save the neonates from the lethal effects of the mutation, whereas rapamycin, an mTOR inhibitor, reduced BMC, suggesting that mTOR signaling is involved in the bone mineralization of heterozygous mutants. Tacrolimus 18-23 mechanistic target of rapamycin kinase Mus musculus 232-236 33273604-4 2020 Administration of FK506, a calcineurin inhibitor, in the heterozygous fetuses improved bone mineral content (BMC) of the neonates, although it did not save the neonates from the lethal effects of the mutation, whereas rapamycin, an mTOR inhibitor, reduced BMC, suggesting that mTOR signaling is involved in the bone mineralization of heterozygous mutants. Tacrolimus 18-23 mechanistic target of rapamycin kinase Mus musculus 277-281 32956634-2 2020 Among the seven mTOR inhibitors evaluated, tacrolimus (TAC) showed significant dose- and time-dependent killing of cultured protoscoleces and cysts in vitro. Tacrolimus 43-53 mechanistic target of rapamycin kinase Homo sapiens 16-20 32956634-2 2020 Among the seven mTOR inhibitors evaluated, tacrolimus (TAC) showed significant dose- and time-dependent killing of cultured protoscoleces and cysts in vitro. Tacrolimus 55-58 mechanistic target of rapamycin kinase Homo sapiens 16-20 32956634-6 2020 We further observed that the ATP levels and glucose content of cysts reduced upon TAC treatment, indicating that inhibiting mTORC1 activity possibly affects glucose metabolism in the cysts of mice. Tacrolimus 82-85 CREB regulated transcription coactivator 1 Mus musculus 124-130 32828804-0 2020 Proof that the high molecular weight immunophilin FKBP52 mediates the in vivo neuroregenerative effect of the macrolide FK506. Tacrolimus 120-125 FK506 binding protein 4 Mus musculus 37-56 33188441-5 2020 A tacrolimus trough > 2.5 ng/mL was recently shown to be associated with a lower risk of PEP in liver transplant patients undergoing ERCP. Tacrolimus 2-12 prolyl endopeptidase Homo sapiens 89-92 33202516-12 2020 Conclusion: In tacrolimus-based immunosuppressive drugs regimen, impaired insulin secretory function for reduced insulin sensitivity contributed to the development of PTDM than insulin resistance during 1 year after transplantation. Tacrolimus 15-25 insulin Homo sapiens 74-81 33202516-12 2020 Conclusion: In tacrolimus-based immunosuppressive drugs regimen, impaired insulin secretory function for reduced insulin sensitivity contributed to the development of PTDM than insulin resistance during 1 year after transplantation. Tacrolimus 15-25 insulin Homo sapiens 113-120 32828804-6 2020 The experimental evidence demonstrates that the neurotrophic actions of FK506 are the consequence of its binding to FKBP52, whereas FK506 interaction with the close-related partner immunophilin FKBP51 antagonises the function of FKBP52. Tacrolimus 72-77 FK506 binding protein 4 Mus musculus 116-122 32828804-6 2020 The experimental evidence demonstrates that the neurotrophic actions of FK506 are the consequence of its binding to FKBP52, whereas FK506 interaction with the close-related partner immunophilin FKBP51 antagonises the function of FKBP52. Tacrolimus 132-137 FK506 binding protein 4 Mus musculus 229-235 32712713-11 2020 CONCLUSIONS: Flucloxacillin decreases tacrolimus trough levels, possibly through a CYP3A4 and/or P-gp-inducing effect. Tacrolimus 38-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 83-89 32712713-11 2020 CONCLUSIONS: Flucloxacillin decreases tacrolimus trough levels, possibly through a CYP3A4 and/or P-gp-inducing effect. Tacrolimus 38-48 ATP binding cassette subfamily B member 1 Homo sapiens 97-101 33125703-0 2020 A twist in the ABC: Regulation of ABC transporter trafficking and transport by FK506-binding proteins. Tacrolimus 79-84 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 34-49 33125703-2 2020 Yet, recent accumulating evidence implicates FK506-binding proteins (FKBPs), a type of peptidylprolyl cis-trans isomerase (PPIase) proteins, in ABC transporter regulation. Tacrolimus 45-50 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 144-159 33039969-3 2020 The aim of the study was to examine the correlation between tacrolimus (TAC) dose and genetic variation for interleukin-10 (IL-10) and its effect on the therapeutic outcome. Tacrolimus 60-70 interleukin 10 Homo sapiens 108-122 33039969-3 2020 The aim of the study was to examine the correlation between tacrolimus (TAC) dose and genetic variation for interleukin-10 (IL-10) and its effect on the therapeutic outcome. Tacrolimus 60-70 interleukin 10 Homo sapiens 124-129 33039969-3 2020 The aim of the study was to examine the correlation between tacrolimus (TAC) dose and genetic variation for interleukin-10 (IL-10) and its effect on the therapeutic outcome. Tacrolimus 72-75 interleukin 10 Homo sapiens 108-122 33039969-3 2020 The aim of the study was to examine the correlation between tacrolimus (TAC) dose and genetic variation for interleukin-10 (IL-10) and its effect on the therapeutic outcome. Tacrolimus 72-75 interleukin 10 Homo sapiens 124-129 33039969-8 2020 The analysis of the correlation between TAC dose and IL-10 genetic variation for the -1082A > G polymorphism revealed that patients with the AA genotype required lower immunosuppressive drug doses (AA: 3.54 +- 2.38 mg/day vs AG: 6.18 +- 5.10 mg/day, GG: 4.44 +- 3.01 mg/day). Tacrolimus 40-43 interleukin 10 Homo sapiens 53-58 33039969-10 2020 The results of the study indicated that the IL-10 -1082A > G polymorphism may in fact influence the TAC dose. Tacrolimus 100-103 interleukin 10 Homo sapiens 44-49 33322998-0 2020 Effects of tacrolimus on autophagy protein LC3 in puromycin-damaged mouse podocytes. Tacrolimus 11-21 microtubule-associated protein 1 light chain 3 alpha Mus musculus 43-46 33322998-6 2020 The low level of LC3 mRNA observed in untreated podocytes was decreased by puromycin treatment; however, levels of LC3 mRNA were higher in the FK506 group versus PAN group. Tacrolimus 143-148 microtubule-associated protein 1 light chain 3 alpha Mus musculus 17-20 33322998-6 2020 The low level of LC3 mRNA observed in untreated podocytes was decreased by puromycin treatment; however, levels of LC3 mRNA were higher in the FK506 group versus PAN group. Tacrolimus 143-148 microtubule-associated protein 1 light chain 3 alpha Mus musculus 115-118 33322998-9 2020 Cytoplasmic LC3-related fluorescence intensity was stronger in control and FK506 podocytes versus the PAN group. Tacrolimus 75-80 microtubule-associated protein 1 light chain 3 alpha Mus musculus 12-15 33322998-10 2020 CONCLUSIONS: Tacrolimus inhibited puromycin-induced mouse podocyte damage by regulating LC3 expression and enhancing autophagy. Tacrolimus 13-23 microtubule-associated protein 1 light chain 3 alpha Mus musculus 88-91 32180132-7 2020 IFN-gamma potently enhanced TNFA, IL12, HLADRA1 and LRRK2 expression, which was suppressed by FK506, a calcineurin-specific inhibitor, but further enhanced by LRRK2-specific kinase inhibitor (GSK2578215A). Tacrolimus 94-99 interferon gamma Homo sapiens 0-9 32180132-7 2020 IFN-gamma potently enhanced TNFA, IL12, HLADRA1 and LRRK2 expression, which was suppressed by FK506, a calcineurin-specific inhibitor, but further enhanced by LRRK2-specific kinase inhibitor (GSK2578215A). Tacrolimus 94-99 tumor necrosis factor Homo sapiens 28-32 32180132-7 2020 IFN-gamma potently enhanced TNFA, IL12, HLADRA1 and LRRK2 expression, which was suppressed by FK506, a calcineurin-specific inhibitor, but further enhanced by LRRK2-specific kinase inhibitor (GSK2578215A). Tacrolimus 94-99 major histocompatibility complex, class II, DR alpha Homo sapiens 40-47 32180132-7 2020 IFN-gamma potently enhanced TNFA, IL12, HLADRA1 and LRRK2 expression, which was suppressed by FK506, a calcineurin-specific inhibitor, but further enhanced by LRRK2-specific kinase inhibitor (GSK2578215A). Tacrolimus 94-99 leucine rich repeat kinase 2 Homo sapiens 52-57 32180132-9 2020 CD14+ monocytes from G2019S and R1441C LRRK2 mutated PD cases and carriers show no changes in IFN-gamma responses for TNFA or IL12, reduced response for HLADRA1, and enhanced responses for LRRK2 in FK506-sensitive manner. Tacrolimus 198-203 CD14 molecule Homo sapiens 0-4 32393842-5 2020 Among patients receiving tacrolimus/sirolimus, nivolumab-exposed patients had a higher incidence of severe aGVHD and a more effector T-cell profile compared with anti-PD-1-naive patients. Tacrolimus 25-35 programmed cell death 1 Homo sapiens 167-171 32600641-11 2020 CONCLUSIONS: Our findings suggest that EVR-based regimens with tacrolimus and corticosteroid therapy for de novo KT reduce the recurrence of IgAN compared with MMF-based regimens with tacrolimus and corticosteroid therapy. Tacrolimus 63-73 IGAN1 Homo sapiens 141-145 32453653-0 2020 Effects of CYP3A5, ABCB1 and POR*28 polymorphisms on pharmacokinetics of tacrolimus in the early period after renal transplantation. Tacrolimus 73-83 cytochrome p450 oxidoreductase Homo sapiens 29-32 32453653-2 2020 We aimed to establish a population pharmacokinetic (PK) model of tacrolimus and identify clinical covariates, especially the genetic polymorphisms of CYP3A5, ABCB1 and POR*28 that affected the PK to prevent fluctuation in the trough concentration of tacrolimus during the early period after renal transplantation. Tacrolimus 65-75 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 150-156 32453653-2 2020 We aimed to establish a population pharmacokinetic (PK) model of tacrolimus and identify clinical covariates, especially the genetic polymorphisms of CYP3A5, ABCB1 and POR*28 that affected the PK to prevent fluctuation in the trough concentration of tacrolimus during the early period after renal transplantation. Tacrolimus 65-75 ATP binding cassette subfamily B member 1 Homo sapiens 158-163 32453653-2 2020 We aimed to establish a population pharmacokinetic (PK) model of tacrolimus and identify clinical covariates, especially the genetic polymorphisms of CYP3A5, ABCB1 and POR*28 that affected the PK to prevent fluctuation in the trough concentration of tacrolimus during the early period after renal transplantation. Tacrolimus 65-75 cytochrome p450 oxidoreductase Homo sapiens 168-171 32453653-2 2020 We aimed to establish a population pharmacokinetic (PK) model of tacrolimus and identify clinical covariates, especially the genetic polymorphisms of CYP3A5, ABCB1 and POR*28 that affected the PK to prevent fluctuation in the trough concentration of tacrolimus during the early period after renal transplantation. Tacrolimus 250-260 cytochrome p450 oxidoreductase Homo sapiens 168-171 32453653-14 2020 CYP3A5 genotype, post-operative day and hematocrit were confirmed as critical PK factors of tacrolimus. Tacrolimus 92-102 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 33312896-2 2020 In order to expand successful renal transplant care to children and adolescents at the lowest possible cost, our pediatric renal transplant clinic uses a post-transplant tacrolimus-sparing strategy via inhibition of CYP3A4. Tacrolimus 170-180 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 216-222 33207690-1 2020 The protective effects of alpha-1 antitrypsin (AAT) in tacrolimus (TAC)-induced renal injury was evaluated in a rat model. Tacrolimus 55-65 serpin family A member 1 Rattus norvegicus 47-50 33207690-1 2020 The protective effects of alpha-1 antitrypsin (AAT) in tacrolimus (TAC)-induced renal injury was evaluated in a rat model. Tacrolimus 67-70 serpin family A member 1 Rattus norvegicus 47-50 33207690-3 2020 The TAC with AAT group was cotreated with daily subcutaneous injections of TAC and intraperitoneal injections of AAT (80 mg/kg) for four weeks. Tacrolimus 4-7 serpin family A member 1 Rattus norvegicus 13-16 33207690-3 2020 The TAC with AAT group was cotreated with daily subcutaneous injections of TAC and intraperitoneal injections of AAT (80 mg/kg) for four weeks. Tacrolimus 4-7 serpin family A member 1 Rattus norvegicus 113-116 33207690-4 2020 The effects of AAT on TAC-induced renal injury were evaluated using serum biochemistry, histopathology, and Western blotting. Tacrolimus 22-25 serpin family A member 1 Rattus norvegicus 15-18 33207690-7 2020 Immunohistochemical staining for inflammation (osteopontin and ED-1 staining) revealed improved interstitial inflammation in the TAC with AAT group compared to that in the TAC group. Tacrolimus 129-132 serpin family A member 1 Rattus norvegicus 138-141 33207690-8 2020 The TAC treatment increased renal apoptosis compared to the control treatment, based on the results of increased immunohistochemical staining of terminal deoxynucleotidyl transferase-mediated dUTP nick-end labeling (TUNEL), increased caspase-3 activity, and lower Bcl-2 to Bad expression ratio. Tacrolimus 4-7 caspase 3 Rattus norvegicus 234-243 33207690-8 2020 The TAC treatment increased renal apoptosis compared to the control treatment, based on the results of increased immunohistochemical staining of terminal deoxynucleotidyl transferase-mediated dUTP nick-end labeling (TUNEL), increased caspase-3 activity, and lower Bcl-2 to Bad expression ratio. Tacrolimus 4-7 BCL2, apoptosis regulator Rattus norvegicus 264-269 33207690-10 2020 AAT protects against TAC-induced renal injury via antifibrotic, anti-inflammatory, and antiapoptotic effects. Tacrolimus 21-24 serpin family A member 1 Rattus norvegicus 0-3 33188441-9 2020 Tacrolimus is a promising potential agent to prevent PEP but needs further clinical study. Tacrolimus 0-10 prolyl endopeptidase Homo sapiens 53-56 33206751-8 2020 Moreover, the drug combination of mycophenolate mofetil and tacrolimus greatly reduced the expression levels of serum TGF-beta1 and cystatin C. Tacrolimus 60-70 transforming growth factor beta 1 Homo sapiens 118-127 33206751-8 2020 Moreover, the drug combination of mycophenolate mofetil and tacrolimus greatly reduced the expression levels of serum TGF-beta1 and cystatin C. Tacrolimus 60-70 cystatin C Homo sapiens 132-142 32783100-8 2020 Studies related variability in tacrolimus whole blood clearance among transplant recipients to either cytochrome P450 (CYP) 3A5 genotype (41%), days post-transplant (30%), or hematocrit (29%). Tacrolimus 31-41 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 102-127 33000210-8 2020 The expression levels of TGF-beta1, SMAD3 and CTGF, as well as their concentrations in the culture supernatant, were significantly downregulated in the tacrolimus group compared with the paraquat group. Tacrolimus 152-162 transforming growth factor, beta 1 Rattus norvegicus 25-34 32894758-0 2020 Differential effects of voclosporin and tacrolimus on insulin secretion from human islets. Tacrolimus 40-50 insulin Homo sapiens 54-61 32894758-7 2020 TAC, but not VCS, caused a significant impairment of 15 mM glucose-stimulated and 30 mM KCl-stimulated insulin secretion. Tacrolimus 0-3 insulin Homo sapiens 103-110 32894758-11 2020 Clinically relevant doses of TAC, but not VCS, directly inhibit insulin secretion from human islets, likely via transcriptional control of exocytosis machinery. Tacrolimus 29-32 insulin Homo sapiens 64-71 33275448-5 2020 Expression of miR-155-5p and miR-223-3p correlated with tacrolimus dose (p < 0.05), miR-223-3p with serum creatinine (p < 0.05), and miR-223-3p and miR-1228-3p with blood leukocytes (p < 0.05). Tacrolimus 56-66 microRNA 155 Homo sapiens 14-21 32738395-6 2020 Knock down of CYP2E1 mRNA using specific shRNA, FK506, a Calcineurin inhibitor, and Mdivi-1, a DRP1 inhibitor, ameliorated alcohol-induced mitochondrial retrograde signaling, and hepatic steatosis. Tacrolimus 48-53 cytochrome P450 family 2 subfamily E member 1 Homo sapiens 14-20 33000210-0 2020 Effects of tacrolimus on the TGF-beta1/SMAD signaling pathway in paraquat-exposed rat alveolar type II epithelial cells. Tacrolimus 11-21 transforming growth factor, beta 1 Rattus norvegicus 29-38 33000210-8 2020 The expression levels of TGF-beta1, SMAD3 and CTGF, as well as their concentrations in the culture supernatant, were significantly downregulated in the tacrolimus group compared with the paraquat group. Tacrolimus 152-162 SMAD family member 3 Rattus norvegicus 36-41 33000210-8 2020 The expression levels of TGF-beta1, SMAD3 and CTGF, as well as their concentrations in the culture supernatant, were significantly downregulated in the tacrolimus group compared with the paraquat group. Tacrolimus 152-162 cellular communication network factor 2 Rattus norvegicus 46-50 33000210-9 2020 However, both the concentration and expression levels of SMAD7 were significantly upregulated in the tacrolimus group compared with the paraquat group. Tacrolimus 101-111 SMAD family member 7 Rattus norvegicus 57-62 33000210-10 2020 In conclusion, tacrolimus can reduce the levels of TGF-beta1, SMAD3 and CTGF, increase the level of SMAD7 in TGF-beta1 signaling pathway and protect the development of pulmonary fibrosis in paraquat exposed alveolar epithelial cells. Tacrolimus 15-25 transforming growth factor, beta 1 Rattus norvegicus 51-60 33000210-10 2020 In conclusion, tacrolimus can reduce the levels of TGF-beta1, SMAD3 and CTGF, increase the level of SMAD7 in TGF-beta1 signaling pathway and protect the development of pulmonary fibrosis in paraquat exposed alveolar epithelial cells. Tacrolimus 15-25 SMAD family member 3 Rattus norvegicus 62-67 33000210-10 2020 In conclusion, tacrolimus can reduce the levels of TGF-beta1, SMAD3 and CTGF, increase the level of SMAD7 in TGF-beta1 signaling pathway and protect the development of pulmonary fibrosis in paraquat exposed alveolar epithelial cells. Tacrolimus 15-25 cellular communication network factor 2 Rattus norvegicus 72-76 33000210-10 2020 In conclusion, tacrolimus can reduce the levels of TGF-beta1, SMAD3 and CTGF, increase the level of SMAD7 in TGF-beta1 signaling pathway and protect the development of pulmonary fibrosis in paraquat exposed alveolar epithelial cells. Tacrolimus 15-25 SMAD family member 7 Rattus norvegicus 100-105 33000210-10 2020 In conclusion, tacrolimus can reduce the levels of TGF-beta1, SMAD3 and CTGF, increase the level of SMAD7 in TGF-beta1 signaling pathway and protect the development of pulmonary fibrosis in paraquat exposed alveolar epithelial cells. Tacrolimus 15-25 transforming growth factor, beta 1 Rattus norvegicus 109-118 32687845-6 2020 Then the role of calcineurin (CnA)-mediated Drp1 signaling pathway on KGN cells was confirmed by treating with Mdivi-1 or FK506T. Tacrolimus 122-127 utrophin Homo sapiens 44-48 32622856-2 2020 The original member of this family, FKBP12, is a well-known binding partner for the immunosuppressive drugs tacrolimus (FK506) and sirolimus (rapamycin). Tacrolimus 108-118 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 36-42 32622856-2 2020 The original member of this family, FKBP12, is a well-known binding partner for the immunosuppressive drugs tacrolimus (FK506) and sirolimus (rapamycin). Tacrolimus 120-125 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 36-42 33350247-1 2020 The purpose of this study was to investigate the inhibitory effects of the main active components of Salviae Miltiorrhizae Radix et Rhizoma on the metabolism of tacrolimus mediated by CYP3 A4/5 enzyme, so as to predict the potential drug-drug interaction(DDI) in clinical use. Tacrolimus 161-171 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 184-193 33350247-5 2020 The results showed that dihydrotanshinone I had a strong inhibitory effect on the metabolism of tacrolimus in both HLM and rCYP3 A4/5 enzyme systems, and the inhibitory potential IC_(50) in HLM was 6.0 mumol L~(-1), while the other four active components of Salviae Miltiorrhizae Radix et Rhizoma exhibited relatively weak inhibition on CYP3 A4/5 activity with inhibition rate less than 30% at 10 mumol L~(-1). Tacrolimus 96-106 oxysterol binding protein 2 Homo sapiens 115-118 33350247-5 2020 The results showed that dihydrotanshinone I had a strong inhibitory effect on the metabolism of tacrolimus in both HLM and rCYP3 A4/5 enzyme systems, and the inhibitory potential IC_(50) in HLM was 6.0 mumol L~(-1), while the other four active components of Salviae Miltiorrhizae Radix et Rhizoma exhibited relatively weak inhibition on CYP3 A4/5 activity with inhibition rate less than 30% at 10 mumol L~(-1). Tacrolimus 96-106 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 124-133 33195437-5 2020 Two small molecules FK506 and rapamycin bind to FKBP12 immunophilin and the resulting complexes (FK506-FKBP12 and rapamycin-FKBP12) target calcineurin and TOR, respectively in both humans and fungi. Tacrolimus 20-25 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 48-54 33149706-14 2020 FK506 use has significantly (P<0.01) increased biomarkers levels of cystatin C (325% and 477%), urea (177% and 245%), MDA (1253%), except calcineurin B1 that has decreased (97%). Tacrolimus 0-5 cystatin C Rattus norvegicus 68-78 33195437-5 2020 Two small molecules FK506 and rapamycin bind to FKBP12 immunophilin and the resulting complexes (FK506-FKBP12 and rapamycin-FKBP12) target calcineurin and TOR, respectively in both humans and fungi. Tacrolimus 20-25 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 103-109 33195437-5 2020 Two small molecules FK506 and rapamycin bind to FKBP12 immunophilin and the resulting complexes (FK506-FKBP12 and rapamycin-FKBP12) target calcineurin and TOR, respectively in both humans and fungi. Tacrolimus 20-25 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 103-109 33195437-5 2020 Two small molecules FK506 and rapamycin bind to FKBP12 immunophilin and the resulting complexes (FK506-FKBP12 and rapamycin-FKBP12) target calcineurin and TOR, respectively in both humans and fungi. Tacrolimus 20-25 RAR related orphan receptor C Homo sapiens 155-158 33195437-5 2020 Two small molecules FK506 and rapamycin bind to FKBP12 immunophilin and the resulting complexes (FK506-FKBP12 and rapamycin-FKBP12) target calcineurin and TOR, respectively in both humans and fungi. Tacrolimus 97-102 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 48-54 33195437-5 2020 Two small molecules FK506 and rapamycin bind to FKBP12 immunophilin and the resulting complexes (FK506-FKBP12 and rapamycin-FKBP12) target calcineurin and TOR, respectively in both humans and fungi. Tacrolimus 97-102 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 103-109 33195437-5 2020 Two small molecules FK506 and rapamycin bind to FKBP12 immunophilin and the resulting complexes (FK506-FKBP12 and rapamycin-FKBP12) target calcineurin and TOR, respectively in both humans and fungi. Tacrolimus 97-102 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 103-109 33195437-5 2020 Two small molecules FK506 and rapamycin bind to FKBP12 immunophilin and the resulting complexes (FK506-FKBP12 and rapamycin-FKBP12) target calcineurin and TOR, respectively in both humans and fungi. Tacrolimus 97-102 RAR related orphan receptor C Homo sapiens 155-158 33195437-8 2020 The current review highlights FK506/rapamycin-FKBP12 interactions with calcineurin/TOR kinase in human and fungi, and development of non-immunosuppressive analogs of FK506, rapamycin, and novel small molecules in inhibition of fungal calcineurin and TOR kinase. Tacrolimus 30-35 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 46-52 33195437-8 2020 The current review highlights FK506/rapamycin-FKBP12 interactions with calcineurin/TOR kinase in human and fungi, and development of non-immunosuppressive analogs of FK506, rapamycin, and novel small molecules in inhibition of fungal calcineurin and TOR kinase. Tacrolimus 30-35 RAR related orphan receptor C Homo sapiens 83-86 33195437-8 2020 The current review highlights FK506/rapamycin-FKBP12 interactions with calcineurin/TOR kinase in human and fungi, and development of non-immunosuppressive analogs of FK506, rapamycin, and novel small molecules in inhibition of fungal calcineurin and TOR kinase. Tacrolimus 30-35 RAR related orphan receptor C Homo sapiens 250-253 32749395-4 2020 The LN distribution study showed that both DiR and FK506 were delivered into the LNs effectively via GM-mediated transport after 24 h and were present in the LNs for at least 48 h. The FK506-loaded GM (GM-FK506) significantly prolonged allograft survival compared with the PBS group (mean survival time, 17.8 +- 1.9 versus 7.3 +- 1.0 days; P < 0.01), and marked decreased the acute rejection grade. Tacrolimus 185-190 arginine vasopressin receptor 2 Homo sapiens 43-46 33067715-1 2020 AIM: The high doses of oral tacrolimus (TAC) (1,2) necessary to prevent acute rejection (AR) after vascularized composite allotransplantation (VCA) are associated with systemic adverse effects. Tacrolimus 28-38 ferredoxin reductase Rattus norvegicus 89-91 33067715-1 2020 AIM: The high doses of oral tacrolimus (TAC) (1,2) necessary to prevent acute rejection (AR) after vascularized composite allotransplantation (VCA) are associated with systemic adverse effects. Tacrolimus 40-43 ferredoxin reductase Rattus norvegicus 89-91 33067715-3 2020 However, the short-term use of topical TAC (Protopic ), as an off-label adjunct to oral TAC, to treat AR episodes pro re nata (PRN), has yielded inconsistent results. Tacrolimus 39-42 ferredoxin reductase Rattus norvegicus 102-104 32749395-5 2020 Furthermore, T cell infiltration, and secretion of IL-2 and IFN-gamma were dramatically reduced in the GM-FK506 group. Tacrolimus 106-111 interleukin 2 Homo sapiens 51-55 32749395-5 2020 Furthermore, T cell infiltration, and secretion of IL-2 and IFN-gamma were dramatically reduced in the GM-FK506 group. Tacrolimus 106-111 interferon gamma Homo sapiens 60-69 32945359-10 2020 TAC inhibited HMC proliferation by affecting the Smad2 signaling pathway. Tacrolimus 0-3 SMAD family member 2 Homo sapiens 49-54 32728937-8 2020 Meanwhile, tacrolimus-treated ITP mice displayed a significant decrease in the mRNA expression of T-bet and plasma level of IFN-gamma and IL-12p70 compared with ITP mice but without differences when compared with normal mice. Tacrolimus 11-21 T-box 21 Mus musculus 98-103 32728937-8 2020 Meanwhile, tacrolimus-treated ITP mice displayed a significant decrease in the mRNA expression of T-bet and plasma level of IFN-gamma and IL-12p70 compared with ITP mice but without differences when compared with normal mice. Tacrolimus 11-21 interferon gamma Mus musculus 124-133 32728937-9 2020 Furthermore, the expression of GATA3, Foxp3, and plasma level of IL-4 and TGF-beta were upregulated in tacrolimus-treated ITP mice without significant differences to normal mice (except TGF-beta). Tacrolimus 103-113 GATA binding protein 3 Mus musculus 31-36 32728937-9 2020 Furthermore, the expression of GATA3, Foxp3, and plasma level of IL-4 and TGF-beta were upregulated in tacrolimus-treated ITP mice without significant differences to normal mice (except TGF-beta). Tacrolimus 103-113 forkhead box P3 Mus musculus 38-43 32728937-9 2020 Furthermore, the expression of GATA3, Foxp3, and plasma level of IL-4 and TGF-beta were upregulated in tacrolimus-treated ITP mice without significant differences to normal mice (except TGF-beta). Tacrolimus 103-113 interleukin 4 Mus musculus 65-69 32728937-9 2020 Furthermore, the expression of GATA3, Foxp3, and plasma level of IL-4 and TGF-beta were upregulated in tacrolimus-treated ITP mice without significant differences to normal mice (except TGF-beta). Tacrolimus 103-113 transforming growth factor alpha Mus musculus 74-82 32728937-9 2020 Furthermore, the expression of GATA3, Foxp3, and plasma level of IL-4 and TGF-beta were upregulated in tacrolimus-treated ITP mice without significant differences to normal mice (except TGF-beta). Tacrolimus 103-113 transforming growth factor alpha Mus musculus 186-194 32888708-0 2020 Effect of ABCB1 3435C>T Genetic Polymorphism on Pharmacokinetic Variables of Tacrolimus in Adult Renal Transplant Recipients: a Systematic Review and Meta-analysis. Tacrolimus 77-87 ATP binding cassette subfamily B member 1 Homo sapiens 10-15 32888708-1 2020 PURPOSE: Tacrolimus is the substrate of multidrug-resistance 1 (ABCB1). Tacrolimus 9-19 ATP binding cassette subfamily B member 1 Homo sapiens 40-62 32888708-1 2020 PURPOSE: Tacrolimus is the substrate of multidrug-resistance 1 (ABCB1). Tacrolimus 9-19 ATP binding cassette subfamily B member 1 Homo sapiens 64-69 32888708-2 2020 However, the effect of ABCB1 C3435T polymorphism on pharmacokinetic variables of tacrolimus is controversial in different studies. Tacrolimus 81-91 ATP binding cassette subfamily B member 1 Homo sapiens 23-28 32888708-3 2020 This meta-analysis was conducted to explore the relationship between ABCB1 3435C>T genetic polymorphism and pharmacokinetic variables of tacrolimus. Tacrolimus 137-147 ATP binding cassette subfamily B member 1 Homo sapiens 69-74 32888708-6 2020 The study explored the relationship between ABCB1 3435C>T genetic polymorphism and pharmacokinetic variables of tacrolimus stratified according to time of posttransplantation, ethnicity, methods of concentration measurement, and the initial doses of tacrolimus. Tacrolimus 112-122 ATP binding cassette subfamily B member 1 Homo sapiens 44-49 32888708-9 2020 The subgroup analysis then revealed that the tacrolimus concentration/weight-adjusted daily dose ratio of ABCB1 3435T carriers was significantly higher than that of the ABCB1 3435CC group at 1 and 6 months. Tacrolimus 45-55 ATP binding cassette subfamily B member 1 Homo sapiens 106-111 32888708-10 2020 Meanwhile, ABCB1 3435CT and TT both had a higher tacrolimus concentration/weight-adjusted daily dose ratio compared with ABCB1 3435CC. Tacrolimus 49-59 ATP binding cassette subfamily B member 1 Homo sapiens 11-16 32888708-11 2020 IMPLICATIONS: Our meta-analysis identified that the ABCB1 3435C>T genetic polymorphism affected the pharmacokinetic variables of tacrolimus in adult renal transplant recipients. Tacrolimus 129-139 ATP binding cassette subfamily B member 1 Homo sapiens 52-57 32985896-9 2020 Results: Examination of the 15 SNPs and several clinical factors identified the CYP3A5 genotype (p = 5.6 x 10-11) and hemoglobin (p = 8.4 x 10-10) as the most significant determinants of tacrolimus C0/D. Tacrolimus 187-197 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 80-86 32985896-11 2020 Conclusion: A new classification and regression tree model was developed for establishing the starting dose of tacrolimus based on the CYP3A5 genotype and hemoglobin values. Tacrolimus 111-121 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 135-141 32992801-0 2020 Conjunctival Injection Reduction in Patients with Atopic Keratoconjunctivitis Due to Synergic Effect of Bovine Enteric-Coated Lactoferrin in 0.1% Tacrolimus Ophthalmic Suspension. Tacrolimus 146-156 lactotransferrin Bos taurus 126-137 33127654-5 2020 RESULTS: In two embodiments of our strategy, we fuse the chronically endocytosing domain of human folate receptor alpha to either a murine scFv that binds fluorescein or human FK506 binding protein that binds FK506, thereby creating a fusion receptor composed of largely human components. Tacrolimus 209-214 folate receptor alpha Homo sapiens 98-119 32247597-1 2020 BACKGROUND: The aim of the study was to assess bioavailability aspects of tacrolimus formulations during conversion from twice-daily (TAC BID) to once-daily (TAC OD) formulation in 89 stable kidney transplant recipients. Tacrolimus 74-84 BH3 interacting domain death agonist Homo sapiens 138-141 32247597-9 2020 CONCLUSIONS: Conversion from TAC BID to TAC OD is associated with a significant increase in tacrolimus dose during the first 3 months. Tacrolimus 92-102 BH3 interacting domain death agonist Homo sapiens 33-36 32307148-1 2020 INTRODUCTION: After kidney transplantation (KTx) in patients with diagnosed cancers, calcineurin inhibitor tacrolimus (TAC) is replaced by sirolimus or everolimus (EV). Tacrolimus 107-117 calcineurin binding protein 1 Homo sapiens 85-106 32307148-1 2020 INTRODUCTION: After kidney transplantation (KTx) in patients with diagnosed cancers, calcineurin inhibitor tacrolimus (TAC) is replaced by sirolimus or everolimus (EV). Tacrolimus 119-122 calcineurin binding protein 1 Homo sapiens 85-106 32971783-2 2020 The objective of this study was to estimate the frequency of CYP3A5 genetic polymorphisms and their relationship with tacrolimus requirements in the pediatric population. Tacrolimus 118-128 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 61-67 32945964-4 2020 Here, we characterized the function of two FK506-binding proteins, namely, FKBP15-1 and FKBP15-2, in Arabidopsis. Tacrolimus 43-48 FK506-binding protein 15 kD-1 Arabidopsis thaliana 75-83 32945964-4 2020 Here, we characterized the function of two FK506-binding proteins, namely, FKBP15-1 and FKBP15-2, in Arabidopsis. Tacrolimus 43-48 FK506- and rapamycin-binding protein 15 kD-2 Arabidopsis thaliana 88-96 33193695-9 2020 In addition, for the first time, our results suggested several antiviral drugs, such as FK506, with molecular binding energies of -11.06 and -10.1 kcal/mol with ACE2 and the spike protein, respectively, could be potentially used to prevent SARS-CoV-2 and remains to further validation. Tacrolimus 88-93 angiotensin converting enzyme 2 Homo sapiens 161-165 33193695-9 2020 In addition, for the first time, our results suggested several antiviral drugs, such as FK506, with molecular binding energies of -11.06 and -10.1 kcal/mol with ACE2 and the spike protein, respectively, could be potentially used to prevent SARS-CoV-2 and remains to further validation. Tacrolimus 88-93 surface glycoprotein Severe acute respiratory syndrome coronavirus 2 174-179 32907953-6 2020 We also demonstrate that, in contrast to the case with Saccharomyces cerevisiae, NCS1 expression in C. neoformans is regulated by the calcineurin pathway via the transcription factor Crz1, as NCS1 expression is reduced by FK506 treatment and CRZ1 deletion. Tacrolimus 222-227 neuronal calcium sensor 1 Mus musculus 81-85 32907953-6 2020 We also demonstrate that, in contrast to the case with Saccharomyces cerevisiae, NCS1 expression in C. neoformans is regulated by the calcineurin pathway via the transcription factor Crz1, as NCS1 expression is reduced by FK506 treatment and CRZ1 deletion. Tacrolimus 222-227 neuronal calcium sensor 1 Mus musculus 192-196 32911703-0 2020 Effect of CYP3A5 on the Once-Daily Tacrolimus Conversion in Stable Liver Transplant Patients. Tacrolimus 35-45 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 10-16 32911703-1 2020 Cytochrome P450 (CYP) 3A5 polymorphism influences tacrolimus metabolism, but its effect on the drug pharmacokinetics in liver transplant recipients switched to once-daily extended-release formulation remains unknown. Tacrolimus 50-60 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-25 32911703-2 2020 The aim of this study is to analyze the effect of CYP3A5 polymorphism on liver function after once-daily tacrolimus conversion in liver transplant patients. Tacrolimus 105-115 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 50-56 32911703-12 2020 CYP3A5 genotyping in liver transplant recipients leads to prediction of pharmacokinetics after switching from a twice-daily regimen to a once-daily dosage form, which makes it possible to establish an appropriate dose of tacrolimus. Tacrolimus 221-231 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 32817992-0 2020 Tacrolimus Improves the Implantation Rate in Patients with Elevated Th1/2 Helper Cell Ratio and Repeated Implantation Failure (RIF). Tacrolimus 0-10 negative elongation factor complex member C/D Homo sapiens 68-73 33061827-9 2020 Tacrolimus therapy-induced methylation and overexpression of NFAT5 could significantly reduce the expression of G0S2 in AChR MG patients. Tacrolimus 0-10 G0/G1 switch 2 Homo sapiens 112-116 33061827-12 2020 Therefore, G0S2 could be an immune regulatory factor in both AChR MG occurrence and treatment with tacrolimus. Tacrolimus 99-109 G0/G1 switch 2 Homo sapiens 11-15 32243709-6 2020 The butyrate-GRP43-GLP-1 pathway in the intestine crypts may involve in the pathogenesis of normalization of hyperglycemia caused by the tacrolimus. Tacrolimus 137-147 glucagon Mus musculus 19-24 32243709-7 2020 Therefore, tacrolimus affects glucose metabolism through the butyrate-associated GLP-1 pathway in the gut, and oral supplementation with butyrate provides new insights for the prevention and treatment of tacrolimus-induced hyperglycemia in transplant recipients. Tacrolimus 11-21 glucagon Mus musculus 81-86 33145270-0 2020 Differential expression of genes related to calcineurin and mTOR signaling and regulatory miRNAs in peripheral blood from kidney recipients under tacrolimus-based therapy. Tacrolimus 146-156 mechanistic target of rapamycin kinase Homo sapiens 60-64 33145270-10 2020 Conclusions: The expression of PPP3CA, MTOR and miR-99a in the peripheral blood of renal recipients is influenced by tacrolimus-based therapy and by PPP3CA and MTOR variants. Tacrolimus 117-127 protein phosphatase 3 catalytic subunit alpha Homo sapiens 31-37 33145270-10 2020 Conclusions: The expression of PPP3CA, MTOR and miR-99a in the peripheral blood of renal recipients is influenced by tacrolimus-based therapy and by PPP3CA and MTOR variants. Tacrolimus 117-127 mechanistic target of rapamycin kinase Homo sapiens 39-43 33145270-10 2020 Conclusions: The expression of PPP3CA, MTOR and miR-99a in the peripheral blood of renal recipients is influenced by tacrolimus-based therapy and by PPP3CA and MTOR variants. Tacrolimus 117-127 microRNA 99a Homo sapiens 48-55 33145270-10 2020 Conclusions: The expression of PPP3CA, MTOR and miR-99a in the peripheral blood of renal recipients is influenced by tacrolimus-based therapy and by PPP3CA and MTOR variants. Tacrolimus 117-127 mechanistic target of rapamycin kinase Homo sapiens 160-164 32563057-6 2020 Systemic MDSC plus FK-506 therapy was found to have a significant anti-psoriatic effect in the murine model, to reduce levels of pro-inflammatory cytokines Th1 cytokines (TNF-alpha and IFN-gamma) and Th17 cytokines (IL-17A and IL-23) in serum and skin. Tacrolimus 19-25 tumor necrosis factor Mus musculus 171-180 32563057-6 2020 Systemic MDSC plus FK-506 therapy was found to have a significant anti-psoriatic effect in the murine model, to reduce levels of pro-inflammatory cytokines Th1 cytokines (TNF-alpha and IFN-gamma) and Th17 cytokines (IL-17A and IL-23) in serum and skin. Tacrolimus 19-25 interferon gamma Mus musculus 185-194 32563057-6 2020 Systemic MDSC plus FK-506 therapy was found to have a significant anti-psoriatic effect in the murine model, to reduce levels of pro-inflammatory cytokines Th1 cytokines (TNF-alpha and IFN-gamma) and Th17 cytokines (IL-17A and IL-23) in serum and skin. Tacrolimus 19-25 interleukin 17A Mus musculus 216-222 32563057-6 2020 Systemic MDSC plus FK-506 therapy was found to have a significant anti-psoriatic effect in the murine model, to reduce levels of pro-inflammatory cytokines Th1 cytokines (TNF-alpha and IFN-gamma) and Th17 cytokines (IL-17A and IL-23) in serum and skin. Tacrolimus 19-25 interleukin 23, alpha subunit p19 Mus musculus 227-232 32779844-0 2020 Tacrolimus ameliorates tubulointerstitial inflammation in diabetic nephropathy via inhibiting the NFATc1/TRPC6 pathway. Tacrolimus 0-10 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 98-104 32779844-0 2020 Tacrolimus ameliorates tubulointerstitial inflammation in diabetic nephropathy via inhibiting the NFATc1/TRPC6 pathway. Tacrolimus 0-10 transient receptor potential cation channel, subfamily C, member 6 Mus musculus 105-110 32779844-7 2020 The expression of NFATc1 and TRPC6 also increased in the kidneys of db/db mice and HK-2 cells with high glucose (HG), while TAC inhibited these effects. Tacrolimus 124-127 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 18-24 32779844-9 2020 Furthermore, HG-induced TRPC6 expression was inhibited by NFATc1 siRNA, while NFATc1 nuclear translocation was inhibited by TAC, but was restored by TRPC6 plasmid in HK-2 cells under HG conditions. Tacrolimus 124-127 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 78-84 32779844-10 2020 These findings suggest that TAC ameliorates tubulointerstitial inflammation in DN through NFATc1/TRPC6 feedback loop. Tacrolimus 28-31 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 90-96 32779844-10 2020 These findings suggest that TAC ameliorates tubulointerstitial inflammation in DN through NFATc1/TRPC6 feedback loop. Tacrolimus 28-31 transient receptor potential cation channel, subfamily C, member 6 Mus musculus 97-102 32552577-1 2020 INTRODUCTION: Although the association between CYP3A5 gene polymorphism and tacrolimus dosing requirements was well established, the impact on how CYP3A5 genotype affects the acute rejection and long-term renal function in patients who received kidney transplants and were treated with tacrolimus remained controversial. Tacrolimus 286-296 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 147-153 32552577-7 2020 Mean daily tacrolimus dose in the CYP3A5 expressers and nonexpressers was 0.08 (0.03) and 0.05 (0.02) mg/kg, respectively (P < .01). Tacrolimus 11-21 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 34-40 32878009-1 2020 FK506 Induces Ligand-Independent Activation of the Bone Morphogenetic Protein Pathway and Osteogenesis. Tacrolimus 0-5 bone morphogenetic protein 1 Homo sapiens 51-77 32983131-2 2020 Methods: To understand the biology of Tfr cells in kidney transplant patients treated with tacrolimus and mycophenolate mofetil (MMF) combination immunosuppression, we measured circulating (c)Tfh and cTfr cells in peripheral blood by flow cytometry in n = 211 kidney transplant recipients. Tacrolimus 91-101 transferrin receptor Homo sapiens 38-41 32848803-0 2020 CYP3A5 Gene-Guided Tacrolimus Treatment of Living-Donor Egyptian Kidney Transplanted Patients. Tacrolimus 19-29 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 32848803-2 2020 Part of interindividual and interethnic differences in the response of patients to tacrolimus is attributed to polymorphisms at CYP3A5 metabolic enzyme. Tacrolimus 83-93 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 128-134 32848803-3 2020 CYP3A5 gene expression status is associated with tacrolimus dose requirement in renal transplant recipients. Tacrolimus 49-59 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 32848803-5 2020 Secondly, we evaluated the influence of the CYP3A5 gene variant on tacrolimus doses required for these patients as well on dose-adjusted tacrolimus trough-concentrations. Tacrolimus 67-77 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 44-50 32848803-7 2020 Additionally, our results showed that, mean tacrolimus daily requirements for heterozygous patients (CYP3A5*1/*3) were significantly higher compared to homozygous patients (CYP3A5*3/*3) during the first year after kidney transplantation. Tacrolimus 44-54 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 101-107 32821416-14 2020 Finally, we offer a simplified approach that can aid in distinguishing between a primary psychiatric diagnosis versus tacrolimus-associated psychosis. Tacrolimus 118-128 activation induced cytidine deaminase Homo sapiens 49-52 32621968-7 2020 Hematocrit, postoperative days, tacrolimus daily dose, voriconazole concomitant therapy, and CYP3A5*3 genotype were identified as significant covariates for tacrolimus clearance. Tacrolimus 157-167 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 93-99 32933627-14 2020 CYP3A5 genotyping has a certain guiding significance for determining the dosage of tacrolimus. Tacrolimus 83-93 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 32825653-7 2020 All SSD1 disruptants displayed susceptibility to the calcineurin inhibitor FK506, similar to fks1 . Tacrolimus 75-80 mRNA-binding translational repressor SSD1 Saccharomyces cerevisiae S288C 4-8 32848803-8 2020 Conclusion: This is the first study in Egypt contributing to the individualization of tacrolimus dosing in Egyptian patients, informed by the CYP3A5 genotype. Tacrolimus 86-96 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 142-148 32849848-0 2020 Beyond Single Nucleotide Polymorphisms: CYP3A5*3*6*7 Composite and ABCB1 Haplotype Associations to Tacrolimus Pharmacokinetics in Black and White Renal Transplant Recipients. Tacrolimus 99-109 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 40-46 32849848-0 2020 Beyond Single Nucleotide Polymorphisms: CYP3A5*3*6*7 Composite and ABCB1 Haplotype Associations to Tacrolimus Pharmacokinetics in Black and White Renal Transplant Recipients. Tacrolimus 99-109 ATP binding cassette subfamily B member 1 Homo sapiens 67-72 32849848-1 2020 Interpatient variability in tacrolimus pharmacokinetics is attributed to metabolism by cytochrome P-450 3A5 (CYP3A5) isoenzymes and membrane transport by P-glycoprotein. Tacrolimus 28-38 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 87-107 32849848-1 2020 Interpatient variability in tacrolimus pharmacokinetics is attributed to metabolism by cytochrome P-450 3A5 (CYP3A5) isoenzymes and membrane transport by P-glycoprotein. Tacrolimus 28-38 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 109-115 32849848-1 2020 Interpatient variability in tacrolimus pharmacokinetics is attributed to metabolism by cytochrome P-450 3A5 (CYP3A5) isoenzymes and membrane transport by P-glycoprotein. Tacrolimus 28-38 ATP binding cassette subfamily B member 1 Homo sapiens 154-168 32849848-3 2020 Tacrolimus pharmacokinetics was investigated in 65 stable Black and Caucasian post-renal transplant patients by assessing the effects of multiple alleles in both CYP3A5 and ABCB1. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 162-168 32849848-3 2020 Tacrolimus pharmacokinetics was investigated in 65 stable Black and Caucasian post-renal transplant patients by assessing the effects of multiple alleles in both CYP3A5 and ABCB1. Tacrolimus 0-10 ATP binding cassette subfamily B member 1 Homo sapiens 173-178 32849848-6 2020 Finally, a combined analysis using both CYP3A5 and ABCB1 polymorphisms was developed to assess their inter-related influence on tacrolimus pharmacokinetics. Tacrolimus 128-138 ATP binding cassette subfamily B member 1 Homo sapiens 51-56 32849848-13 2020 The ABCB1 haplotype analysis detected significant associations of the wildtype 1236T-2677T-3435T haplotype to tacrolimus dose (P = 0.03), CL (P = 0.023), CL/LBW (P = 0.022), and AUC* (P = 0.078). Tacrolimus 110-120 ATP binding cassette subfamily B member 1 Homo sapiens 4-9 32849848-14 2020 Finally, analysis combining CYP3A5 and ABCB1 genotypes indicated that the presence of the ABCB1 3435 T allele significantly reduced tacrolimus clearance for all three CPY3A5 metabolic composite groups. Tacrolimus 132-142 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 28-34 32849848-14 2020 Finally, analysis combining CYP3A5 and ABCB1 genotypes indicated that the presence of the ABCB1 3435 T allele significantly reduced tacrolimus clearance for all three CPY3A5 metabolic composite groups. Tacrolimus 132-142 ATP binding cassette subfamily B member 1 Homo sapiens 39-44 32849848-14 2020 Finally, analysis combining CYP3A5 and ABCB1 genotypes indicated that the presence of the ABCB1 3435 T allele significantly reduced tacrolimus clearance for all three CPY3A5 metabolic composite groups. Tacrolimus 132-142 ATP binding cassette subfamily B member 1 Homo sapiens 90-95 32849848-15 2020 Genotypic associations of tacrolimus pharmacokinetics can be improved by using the novel composite CYP3A5*3*4*5 and ABCB1 haplotypes. Tacrolimus 26-36 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 99-105 32849848-15 2020 Genotypic associations of tacrolimus pharmacokinetics can be improved by using the novel composite CYP3A5*3*4*5 and ABCB1 haplotypes. Tacrolimus 26-36 ATP binding cassette subfamily B member 1 Homo sapiens 116-121 32849848-16 2020 Consideration of multiple alleles using CYP3A5 metabolic composites and drug transporter ABCB1 haplotypes provides a more comprehensive appraisal of genetic factors contributing to interpatient variability in tacrolimus pharmacokinetics among Whites and Blacks. Tacrolimus 209-219 ATP binding cassette subfamily B member 1 Homo sapiens 89-94 32817992-4 2020 Results Tacrolimus significantly increased the expression of LIF, IL-10, and IL-17 and decreased the expression of IL-4, IFN-gamma, and the IFN-gamma/IL-10 ratio in RIF patients. Tacrolimus 8-18 LIF interleukin 6 family cytokine Homo sapiens 61-64 32817992-4 2020 Results Tacrolimus significantly increased the expression of LIF, IL-10, and IL-17 and decreased the expression of IL-4, IFN-gamma, and the IFN-gamma/IL-10 ratio in RIF patients. Tacrolimus 8-18 interleukin 10 Homo sapiens 66-71 32817992-4 2020 Results Tacrolimus significantly increased the expression of LIF, IL-10, and IL-17 and decreased the expression of IL-4, IFN-gamma, and the IFN-gamma/IL-10 ratio in RIF patients. Tacrolimus 8-18 interleukin 17A Homo sapiens 77-82 32170643-10 2020 CONCLUSIONS: For patients with the CYP3A5*3*3 allele, the required tacrolimus dose for 75% of subjects to achieve target trough concentrations of 4.8-15 ng/mL was 2 mg every 12 h (q12h). Tacrolimus 67-77 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 35-41 32817992-4 2020 Results Tacrolimus significantly increased the expression of LIF, IL-10, and IL-17 and decreased the expression of IL-4, IFN-gamma, and the IFN-gamma/IL-10 ratio in RIF patients. Tacrolimus 8-18 interleukin 4 Homo sapiens 115-119 32170643-11 2020 For patients with the CYP3A5*1*1 allele, the required dose was 2 mg tacrolimus q12h with a Wuzhi capsule, and for patients with the CYP3A5*1*3 allele, the required dose was 3 mg of tacrolimus q12h or 4 mg q24h co-administered with a Wuzhi capsule. Tacrolimus 68-78 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 22-28 32817992-4 2020 Results Tacrolimus significantly increased the expression of LIF, IL-10, and IL-17 and decreased the expression of IL-4, IFN-gamma, and the IFN-gamma/IL-10 ratio in RIF patients. Tacrolimus 8-18 interferon gamma Homo sapiens 121-130 32817992-4 2020 Results Tacrolimus significantly increased the expression of LIF, IL-10, and IL-17 and decreased the expression of IL-4, IFN-gamma, and the IFN-gamma/IL-10 ratio in RIF patients. Tacrolimus 8-18 interferon gamma Homo sapiens 140-149 32817992-4 2020 Results Tacrolimus significantly increased the expression of LIF, IL-10, and IL-17 and decreased the expression of IL-4, IFN-gamma, and the IFN-gamma/IL-10 ratio in RIF patients. Tacrolimus 8-18 interleukin 10 Homo sapiens 150-155 32301802-7 2020 These data support that the antimelanoma effect of FK506 and FK520 is partially mediated by inhibiting the oncogenic factor NFAT3, suggesting that therapeutics based on NFAT3 inhibition may be effective in clinical melanoma treatment. Tacrolimus 51-56 nuclear factor of activated T cells 4 Homo sapiens 124-129 32301802-7 2020 These data support that the antimelanoma effect of FK506 and FK520 is partially mediated by inhibiting the oncogenic factor NFAT3, suggesting that therapeutics based on NFAT3 inhibition may be effective in clinical melanoma treatment. Tacrolimus 51-56 nuclear factor of activated T cells 4 Homo sapiens 169-174 32301802-6 2020 Mechanistic studies revealed that FK506 or FK520 blocked the nuclear translocation and reduced the transcriptional activity of NFAT3. Tacrolimus 34-39 nuclear factor of activated T cells 4 Homo sapiens 127-132 32736525-0 2020 FK506 induces lung lymphatic endothelial cell senescence and downregulates LYVE-1 expression, with associated decreased hyaluronan uptake. Tacrolimus 0-5 lymphatic vessel endothelial hyaluronan receptor 1 Homo sapiens 75-81 31902946-7 2020 Tacrolimus C0/D was higher in CYP3A5 nonexpressers than in CYP3A5 expressers (p = 0.003). Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 30-36 31902946-7 2020 Tacrolimus C0/D was higher in CYP3A5 nonexpressers than in CYP3A5 expressers (p = 0.003). Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 59-65 31902946-8 2020 ACTN4 rs62121818, MYH9 rs2239781, CYP3A5*3, and age explained 20.5% interindividual variability of tacrolimus concentration in the total cohort. Tacrolimus 99-109 actinin alpha 4 Homo sapiens 0-5 31902946-8 2020 ACTN4 rs62121818, MYH9 rs2239781, CYP3A5*3, and age explained 20.5% interindividual variability of tacrolimus concentration in the total cohort. Tacrolimus 99-109 myosin heavy chain 9 Homo sapiens 18-22 31902946-9 2020 In CYP3A5 nonexpressers, ACTN4 rs62121818 and MYH9 rs2239781 together explained 14.6% variation of tacrolimus C0/D. Tacrolimus 99-109 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 3-9 31902946-9 2020 In CYP3A5 nonexpressers, ACTN4 rs62121818 and MYH9 rs2239781 together explained 14.6% variation of tacrolimus C0/D. Tacrolimus 99-109 actinin alpha 4 Homo sapiens 25-30 31902946-9 2020 In CYP3A5 nonexpressers, ACTN4 rs62121818 and MYH9 rs2239781 together explained 14.6% variation of tacrolimus C0/D. Tacrolimus 99-109 myosin heavy chain 9 Homo sapiens 46-50 31902946-10 2020 MYH9 rs2239781, LAMB2 rs62119873 and age together explained 22.3% variability of tacrolimus level in CYP3A5 expressers. Tacrolimus 81-91 myosin heavy chain 9 Homo sapiens 0-4 31902946-10 2020 MYH9 rs2239781, LAMB2 rs62119873 and age together explained 22.3% variability of tacrolimus level in CYP3A5 expressers. Tacrolimus 81-91 laminin subunit beta 2 Homo sapiens 16-21 31902946-10 2020 MYH9 rs2239781, LAMB2 rs62119873 and age together explained 22.3% variability of tacrolimus level in CYP3A5 expressers. Tacrolimus 81-91 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 101-107 31902946-11 2020 CYP3A5*3 was still an important factor affecting tacrolimus concentration in patients with NS. Tacrolimus 49-59 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 31902946-12 2020 Podocyte-associated gene polymorphisms, especially ACTN4 rs62121818 and MYH9 rs2239781, were the other most important biomarkers for tacrolimus whole blood levels. Tacrolimus 133-143 actinin alpha 4 Homo sapiens 51-56 31902946-12 2020 Podocyte-associated gene polymorphisms, especially ACTN4 rs62121818 and MYH9 rs2239781, were the other most important biomarkers for tacrolimus whole blood levels. Tacrolimus 133-143 myosin heavy chain 9 Homo sapiens 72-76 31902946-13 2020 Genotyping of CYP3A5, ACTN4, and MYH9 polymorphisms may be helpful for better guiding tacrolimus dosing in pediatric patients with refractory NS. Tacrolimus 86-96 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 14-20 31902946-13 2020 Genotyping of CYP3A5, ACTN4, and MYH9 polymorphisms may be helpful for better guiding tacrolimus dosing in pediatric patients with refractory NS. Tacrolimus 86-96 myosin heavy chain 9 Homo sapiens 33-37 31902947-0 2020 CYP3A5 gene polymorphisms and their impact on dosage and trough concentration of tacrolimus among kidney transplant patients: a systematic review and meta-analysis. Tacrolimus 81-91 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 31902947-2 2020 Cytochrome P450 3A5 (CYP3A5) protein is involved in tacrolimus metabolism. Tacrolimus 52-62 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-19 31902947-2 2020 Cytochrome P450 3A5 (CYP3A5) protein is involved in tacrolimus metabolism. Tacrolimus 52-62 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 21-27 31902947-3 2020 Single nucleotide polymorphism in the CYP3A5 gene (6986A>G) results in alteration in metabolic activity of CYP3A5 protein which eventually affects the tacrolimus concentration. Tacrolimus 151-161 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 38-44 31902947-3 2020 Single nucleotide polymorphism in the CYP3A5 gene (6986A>G) results in alteration in metabolic activity of CYP3A5 protein which eventually affects the tacrolimus concentration. Tacrolimus 151-161 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 107-113 31902947-4 2020 Patients with CYP3A5 expresser genotypes (A/A *1/*1 and A/G *1/*3) metabolize tacrolimus more rapidly than CYP3A5 nonexpressers (G/G *3/*3). Tacrolimus 78-88 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 14-20 31902947-6 2020 Our results showed that the tacrolimus Co/D ratio is significantly lower in CYP3A5 expresser group as compared with nonexpresser in Asian as well as in European populations at any post-transplant period (p < 0.00001). Tacrolimus 28-38 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 76-82 32732848-9 2020 CONCLUSIONS: This single-center retrospective cohort analysis suggests that in hypersensitized kidney transplant recipients receiving tacrolimus-based immunosuppressive therapy similar clinical outcomes may be obtained using mTOR inhibitors compared to mycophenolate. Tacrolimus 134-144 mechanistic target of rapamycin kinase Homo sapiens 225-229 32848756-0 2020 The Clinical Impact of the C0/D Ratio and the CYP3A5 Genotype on Outcome in Tacrolimus Treated Kidney Transplant Recipients. Tacrolimus 76-86 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 46-52 32848756-1 2020 Tacrolimus is metabolized by CYP3A4 and CYP3A5 enzymes. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 29-35 32848756-1 2020 Tacrolimus is metabolized by CYP3A4 and CYP3A5 enzymes. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 40-46 32848756-6 2020 At first sight, the expression of CYP3A5 and a low C0/D ratio seem to be overlapping factors, both pointing towards patients in whom a higher tacrolimus dose is needed to reach the tacrolimus target concentration. Tacrolimus 142-152 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 34-40 32848756-6 2020 At first sight, the expression of CYP3A5 and a low C0/D ratio seem to be overlapping factors, both pointing towards patients in whom a higher tacrolimus dose is needed to reach the tacrolimus target concentration. Tacrolimus 181-191 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 34-40 32848756-11 2020 Steroids induce the metabolism of tacrolimus via pregnane X receptor mediated increased CYP3A4 expression, resulting in lower tacrolimus C0/D ratio in high risk patients. Tacrolimus 34-44 nuclear receptor subfamily 1 group I member 2 Homo sapiens 49-68 32848756-11 2020 Steroids induce the metabolism of tacrolimus via pregnane X receptor mediated increased CYP3A4 expression, resulting in lower tacrolimus C0/D ratio in high risk patients. Tacrolimus 34-44 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-94 32848756-11 2020 Steroids induce the metabolism of tacrolimus via pregnane X receptor mediated increased CYP3A4 expression, resulting in lower tacrolimus C0/D ratio in high risk patients. Tacrolimus 126-136 nuclear receptor subfamily 1 group I member 2 Homo sapiens 49-68 32848756-11 2020 Steroids induce the metabolism of tacrolimus via pregnane X receptor mediated increased CYP3A4 expression, resulting in lower tacrolimus C0/D ratio in high risk patients. Tacrolimus 126-136 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-94 32736525-8 2020 Matrigel tubulation assay were used to investigate the effects of FK506 on TNF-alpha-induced lymphangiogenesis. Tacrolimus 66-71 tumor necrosis factor Homo sapiens 75-84 32736525-10 2020 Flow cytometry was used to examine the effects of FK506 on LYVE-1 in precision-cut-lung-slices ex vivo and on hyaluronan uptake in vitro. Tacrolimus 50-55 lymphatic vessel endothelial hyaluronan receptor 1 Homo sapiens 59-65 32736525-11 2020 RESULTS: In vitro, FK506 downregulated telomerase reverse transcriptase expression, resulting in decreased telomerase activity and subsequent induction of p21 expression and cell senescence. Tacrolimus 19-24 H3 histone pseudogene 16 Homo sapiens 155-158 32736525-12 2020 Treatment with FK506 decreased LYVE-1 mRNA and protein levels and resulted in decreased LEC HA uptake. Tacrolimus 15-20 lymphatic vessel endothelial hyaluronan receptor 1 Homo sapiens 31-37 32736525-13 2020 Similar result showing reduction of LYVE-1 expression when treated with FK506 was observed ex vivo. Tacrolimus 72-77 lymphatic vessel endothelial hyaluronan receptor 1 Homo sapiens 36-42 32736525-15 2020 We showed that this NFAT binding site regulates LYVE-1 transcription, and mutation of this binding site blunted FK506-dependent downregulation of LYVE-1 promoter-dependent transcription. Tacrolimus 112-117 lymphatic vessel endothelial hyaluronan receptor 1 Homo sapiens 48-54 32736525-15 2020 We showed that this NFAT binding site regulates LYVE-1 transcription, and mutation of this binding site blunted FK506-dependent downregulation of LYVE-1 promoter-dependent transcription. Tacrolimus 112-117 lymphatic vessel endothelial hyaluronan receptor 1 Homo sapiens 146-152 32736525-16 2020 Finally, FK506-treated lymphatic endothelial cells show a blunted response to TNF-alpha-mediated lymphangiogenesis. Tacrolimus 9-14 tumor necrosis factor Homo sapiens 78-87 32690569-4 2020 Tacrolimus is metabolised by the cytochrome P (CYP) 450 3A enzyme system, and utilisation of CYP 3A inducers to accelerate its clearance may be used as a successful therapy to treat tacrolimus toxicity. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 93-99 32719413-2 2020 The aim of our study was to investigate the short- and long-term efficacy of anti-TNF agents [adalimumab (ADA) and infliximab (IFX)] and TAC in anti-TNF agent- and TAC-naive steroid-refractory UC patients. Tacrolimus 137-140 tumor necrosis factor Homo sapiens 149-152 32719413-2 2020 The aim of our study was to investigate the short- and long-term efficacy of anti-TNF agents [adalimumab (ADA) and infliximab (IFX)] and TAC in anti-TNF agent- and TAC-naive steroid-refractory UC patients. Tacrolimus 164-167 tumor necrosis factor Homo sapiens 82-85 32719413-5 2020 Logistic regression analysis showed the male sex and higher C-reactive protein to be independent factors for response to anti-TNF agents and TAC, respectively. Tacrolimus 141-144 C-reactive protein Homo sapiens 60-78 32674627-0 2021 Association of the IL-6 Rs1800796 SNP with Concentration/dose Ratios of Tacrolimus and Donor Liver Function after Transplantation. Tacrolimus 72-82 interleukin 6 Homo sapiens 19-23 32674627-2 2021 Here, we aimed to assess the potential influence of the IL-6 single nucleotide polymorphism (SNP) rs1800796 on the concentration/dose (C/D) ratios of tacrolimus and donor liver function in Chinese liver transplant patients. Tacrolimus 150-160 interleukin 6 Homo sapiens 56-60 32674627-5 2021 The IL-6 rs1800796 polymorphism in recipients was found to be correlated with the C/D ratios of tacrolimus at months 2 to month 6 after transplantation. Tacrolimus 96-106 interleukin 6 Homo sapiens 4-8 32674627-7 2021 In conclusion, the IL-6 rs1800796 polymorphism was associated with the C/D ratios of tacrolimus and post-transplant donor liver function. Tacrolimus 85-95 interleukin 6 Homo sapiens 19-23 32690569-4 2020 Tacrolimus is metabolised by the cytochrome P (CYP) 450 3A enzyme system, and utilisation of CYP 3A inducers to accelerate its clearance may be used as a successful therapy to treat tacrolimus toxicity. Tacrolimus 182-192 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 93-99 32661607-8 2020 Pre-exposure of RBCs to FKBP12 followed by exposure to tacrolimus significantly decreased tacrolimus distribution in RBCs in a concentration-dependent manner. Tacrolimus 90-100 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 24-30 32661607-9 2020 In addition, preincubation of tacrolimus with FKBP12 significantly reduced the rate of tacrolimus distribution in RBCs. Tacrolimus 30-40 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 46-52 32661607-9 2020 In addition, preincubation of tacrolimus with FKBP12 significantly reduced the rate of tacrolimus distribution in RBCs. Tacrolimus 87-97 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 46-52 32664235-0 2020 Tacrolimus Prevents TWEAK-Induced PLA2R Expression in Cultured Human Podocytes. Tacrolimus 0-10 TNF superfamily member 12 Homo sapiens 20-25 32664531-1 2020 Tacrolimus is a first-line calcineurin inhibitor (CNI) and an integral part of the immunosuppressive strategy in solid organ transplantation. Tacrolimus 0-10 calcineurin binding protein 1 Homo sapiens 27-48 32664235-0 2020 Tacrolimus Prevents TWEAK-Induced PLA2R Expression in Cultured Human Podocytes. Tacrolimus 0-10 phospholipase A2 receptor 1 Homo sapiens 34-39 32664235-9 2020 Interestingly, IRF4 encodes the FK506-binding protein 52 (FKBP52), a protein associated with tacrolimus. Tacrolimus 93-103 interferon regulatory factor 4 Homo sapiens 15-19 32664235-9 2020 Interestingly, IRF4 encodes the FK506-binding protein 52 (FKBP52), a protein associated with tacrolimus. Tacrolimus 93-103 FKBP prolyl isomerase 4 Homo sapiens 32-56 32664235-9 2020 Interestingly, IRF4 encodes the FK506-binding protein 52 (FKBP52), a protein associated with tacrolimus. Tacrolimus 93-103 FKBP prolyl isomerase 4 Homo sapiens 58-64 32664235-10 2020 Tacrolimus prevented the increased expression of PLA2R, NFKB1 and IRF4 induced by TWEAK in cultured podocytes. Tacrolimus 0-10 phospholipase A2 receptor 1 Homo sapiens 49-54 32664235-10 2020 Tacrolimus prevented the increased expression of PLA2R, NFKB1 and IRF4 induced by TWEAK in cultured podocytes. Tacrolimus 0-10 nuclear factor kappa B subunit 1 Homo sapiens 56-61 32664235-10 2020 Tacrolimus prevented the increased expression of PLA2R, NFKB1 and IRF4 induced by TWEAK in cultured podocytes. Tacrolimus 0-10 interferon regulatory factor 4 Homo sapiens 66-70 32664235-10 2020 Tacrolimus prevented the increased expression of PLA2R, NFKB1 and IRF4 induced by TWEAK in cultured podocytes. Tacrolimus 0-10 TNF superfamily member 12 Homo sapiens 82-87 32664235-11 2020 In conclusion, TWEAK upregulates the expression of PLA2R and of other genes linked to membranous nephropathy in podocytes, and this is prevented by tacrolimus. Tacrolimus 148-158 TNF superfamily member 12 Homo sapiens 15-20 32664235-11 2020 In conclusion, TWEAK upregulates the expression of PLA2R and of other genes linked to membranous nephropathy in podocytes, and this is prevented by tacrolimus. Tacrolimus 148-158 phospholipase A2 receptor 1 Homo sapiens 51-56 32664235-12 2020 An impact of tacrolimus on the expression of PLA2R and other genes in podocytes may underlie its efficacy in treating the disease as well as the frequent recurrence of nephrotic syndrome upon tacrolimus withdrawal. Tacrolimus 13-23 phospholipase A2 receptor 1 Homo sapiens 45-50 32664235-12 2020 An impact of tacrolimus on the expression of PLA2R and other genes in podocytes may underlie its efficacy in treating the disease as well as the frequent recurrence of nephrotic syndrome upon tacrolimus withdrawal. Tacrolimus 192-202 phospholipase A2 receptor 1 Homo sapiens 45-50 32298692-8 2020 FK506, which also forms a complex with FKBP12 but does not target mTOR, reduced platelet procoagulant responses to a similar extent as rapamycin. Tacrolimus 0-5 FKBP prolyl isomerase 1A Homo sapiens 39-45 32570960-0 2020 CYP3A5 Genotype as a Potential Pharmacodynamic Biomarker for Tacrolimus Therapy in Ulcerative Colitis in Japanese Patients. Tacrolimus 61-71 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 31888346-0 2020 Impact of Donor and Recipient CYP3A5*3 Genotype on Tacrolimus Population Pharmacokinetics in Chinese Adult Liver Transplant Recipients. Tacrolimus 51-61 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 30-36 32603360-1 2020 Fpr1 (FK506-sensitive proline rotamase 1), a protein of the FKBP12 (FK506-binding protein 12 kDa) family in Saccharomyces cerevisiae, is a primary target for the immunosuppressive agents FK506 and rapamycin. Tacrolimus 6-11 peptidylprolyl isomerase FPR1 Saccharomyces cerevisiae S288C 0-4 32603360-2 2020 Fpr1 inhibits calcineurin and TORC1 (target of rapamycin complex 1) when bound to FK506 and rapamycin, respectively. Tacrolimus 82-87 peptidylprolyl isomerase FPR1 Saccharomyces cerevisiae S288C 0-4 32580389-3 2020 This complex glucocorticoid regulation is mediated through the glucocorticoid receptor, also known as nuclear receptor subfamily 3 group C member 1 (NR3C1/GR) and related genes, like 11beta-hydroxysteroid dehydrogenases (HSD11Bs) and the FK506-binding immunophilins, FKBP5 and FKBP4. Tacrolimus 238-243 nuclear receptor subfamily 3 group C member 1 Homo sapiens 63-86 32580389-3 2020 This complex glucocorticoid regulation is mediated through the glucocorticoid receptor, also known as nuclear receptor subfamily 3 group C member 1 (NR3C1/GR) and related genes, like 11beta-hydroxysteroid dehydrogenases (HSD11Bs) and the FK506-binding immunophilins, FKBP5 and FKBP4. Tacrolimus 238-243 nuclear receptor subfamily 3 group C member 1 Homo sapiens 102-147 32580389-3 2020 This complex glucocorticoid regulation is mediated through the glucocorticoid receptor, also known as nuclear receptor subfamily 3 group C member 1 (NR3C1/GR) and related genes, like 11beta-hydroxysteroid dehydrogenases (HSD11Bs) and the FK506-binding immunophilins, FKBP5 and FKBP4. Tacrolimus 238-243 nuclear receptor subfamily 3 group C member 1 Homo sapiens 149-154 32580389-3 2020 This complex glucocorticoid regulation is mediated through the glucocorticoid receptor, also known as nuclear receptor subfamily 3 group C member 1 (NR3C1/GR) and related genes, like 11beta-hydroxysteroid dehydrogenases (HSD11Bs) and the FK506-binding immunophilins, FKBP5 and FKBP4. Tacrolimus 238-243 FKBP prolyl isomerase 5 Homo sapiens 267-272 32580389-3 2020 This complex glucocorticoid regulation is mediated through the glucocorticoid receptor, also known as nuclear receptor subfamily 3 group C member 1 (NR3C1/GR) and related genes, like 11beta-hydroxysteroid dehydrogenases (HSD11Bs) and the FK506-binding immunophilins, FKBP5 and FKBP4. Tacrolimus 238-243 FKBP prolyl isomerase 4 Homo sapiens 277-282 32578817-0 2020 Tacrolimus therapeutic efficacy in post-liver transplant patients with Cytochrome P450 3A5 (CYP3A5) genetic polymorphisms. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 71-90 32578817-0 2020 Tacrolimus therapeutic efficacy in post-liver transplant patients with Cytochrome P450 3A5 (CYP3A5) genetic polymorphisms. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 92-98 32578817-1 2020 Genetic polymorphisms of CYP3A5 have been pointed out as factors that influenciates tacrolimus immunosuppressive efficacy in post liver transplant patients. Tacrolimus 84-94 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 25-31 32578817-2 2020 This study aims to review the literature on the influence of cytochrome P450 3A5 (CYP3A5) genetic polymorphisms of tacrolimus in post-liver transplant patients. Tacrolimus 115-125 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 61-80 32578817-2 2020 This study aims to review the literature on the influence of cytochrome P450 3A5 (CYP3A5) genetic polymorphisms of tacrolimus in post-liver transplant patients. Tacrolimus 115-125 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 82-88 32578817-6 2020 Initially, the pharmacological aspects of tacrolimus were discussed, including details on its pharmacodynamics, pharmacokinetics and toxicity After that, we analyzed the studies that correlates CYP3A5 genetic polymorphisms and tacrolimus efficacy, including the ethnical specifications and the general limittions of the studies. Tacrolimus 42-52 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 194-200 32578817-7 2020 The CYP3A5 polymorphisms have pointed to alterations in the metabolism of tacrolimus according to the ethnic and populational genotype, specially the *1 and *3*3 alleles, reflecting in the need for dose adjustment and also in post liver transplant rejection. Tacrolimus 74-84 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 4-10 32060883-3 2020 Here, we aim to study the psoriasis treatment with TAC and siRNA for one of most cytokines expressed in psoriasis, the TNF-alpha. Tacrolimus 51-54 tumor necrosis factor Mus musculus 119-128 32305124-7 2020 Baseline GLP-1 levels in cyclosporine-treated renal transplant patients were higher than in both tacrolimus-treated renal transplant patients (p = 0,016) and control groups (p < 0,001). Tacrolimus 97-107 glucagon Homo sapiens 9-14 32305124-8 2020 GLP-1 levels at the 30th minute were higher in tacrolimus-treated renal transplant patients when compared to the cyclosporine-treated renal transplant patients (p = 0,024). Tacrolimus 47-57 glucagon Homo sapiens 0-5 32305124-9 2020 GLP-1 levels at the 120th minute were higher in tacrolimus-treated renal transplant patients than the control group (p = 0,024). Tacrolimus 48-58 glucagon Homo sapiens 0-5 32305124-10 2020 The areas under the curve of GLP-1 was higher in tacrolimus-treated renal transplant patients when compared to the control group (p = 0,018). Tacrolimus 49-59 glucagon Homo sapiens 29-34 32305124-12 2020 CONCLUSION: These findings showed a temporally affected incretin hormones in renal transplant patients, a preserved GLP-1 response to an oral glucose load in renal transplant patients on cyclosporine and increased GLP -1 response to an oral glucose load in those on tacrolimus. Tacrolimus 266-276 glucagon like peptide 1 receptor Homo sapiens 214-220 32422433-4 2020 Application of drugs that target either calcineurin (cyclosporine A) or FKBP12 (tacrolimus known as FK506 and sirolimus known as rapamycin) caused a decrease in TMEM16A activity. Tacrolimus 80-90 FKBP prolyl isomerase 1A Homo sapiens 72-78 32422433-4 2020 Application of drugs that target either calcineurin (cyclosporine A) or FKBP12 (tacrolimus known as FK506 and sirolimus known as rapamycin) caused a decrease in TMEM16A activity. Tacrolimus 80-90 anoctamin 1 Homo sapiens 161-168 32422433-4 2020 Application of drugs that target either calcineurin (cyclosporine A) or FKBP12 (tacrolimus known as FK506 and sirolimus known as rapamycin) caused a decrease in TMEM16A activity. Tacrolimus 100-105 FKBP prolyl isomerase 1A Homo sapiens 72-78 32422433-4 2020 Application of drugs that target either calcineurin (cyclosporine A) or FKBP12 (tacrolimus known as FK506 and sirolimus known as rapamycin) caused a decrease in TMEM16A activity. Tacrolimus 100-105 anoctamin 1 Homo sapiens 161-168 32422433-5 2020 In addition, FK506 and BAPTA-AM prevented co-immunoprecipitation between FKBP12 and TMEM16A. Tacrolimus 13-18 FKBP prolyl isomerase 1A Homo sapiens 73-79 32422433-5 2020 In addition, FK506 and BAPTA-AM prevented co-immunoprecipitation between FKBP12 and TMEM16A. Tacrolimus 13-18 anoctamin 1 Homo sapiens 84-91 32422433-7 2020 Rapamycin decreased TMEM16A activity in cells pre-treated with cyclosporine A or FK506. Tacrolimus 81-86 anoctamin 1 Homo sapiens 20-27 32078103-1 2020 BACKGROUND AND OBJECTIVES: P-glycoprotein (P-gp) has been shown previously to contribute to the intestinal absorption of verapamil, diltiazem, tacrolimus, colchicine and indinavir in situ; however, its contribution in vivo is unknown. Tacrolimus 143-153 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 27-41 32078103-1 2020 BACKGROUND AND OBJECTIVES: P-glycoprotein (P-gp) has been shown previously to contribute to the intestinal absorption of verapamil, diltiazem, tacrolimus, colchicine and indinavir in situ; however, its contribution in vivo is unknown. Tacrolimus 143-153 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 43-47 32450827-3 2020 RESULTS: Patients with the A allele of CYP3A5 treated with tacrolimus had a higher risk of acute rejection than those without the A allele, while patients carrying the homozygous GG variant for SXR A7635GG did not show any episode of acute rejection. Tacrolimus 59-69 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 39-45 32192767-0 2020 FKBP12 dimerization mutations effect FK506 binding and differentially alter calcineurin inhibition in the human pathogen Aspergillus fumigatus. Tacrolimus 37-42 FKBP prolyl isomerase 1A Homo sapiens 0-6 32192767-1 2020 The 12-kDa FK506-binding protein (FKBP12) is the target of the commonly used immunosuppressive drug FK506. Tacrolimus 11-16 FKBP prolyl isomerase 1A Homo sapiens 34-40 32192767-2 2020 The FKBP12-FK506 complex binds to calcineurin and inhibits its activity, leading to immunosuppression and preventing organ transplant rejection. Tacrolimus 11-16 FKBP prolyl isomerase 1A Homo sapiens 4-10 32192767-8 2020 Molecular dynamics and pulling simulations for each dimeric FKBP12 protein revealed a two-fold increase in dimer strength and significantly higher number of contacts for the F37M, F37L, and W60V mutations, further confirming their varying degree of impact on FK506 binding and calcineurin inhibition in vivo. Tacrolimus 259-264 FKBP prolyl isomerase 1A Homo sapiens 60-66 32499781-7 2020 Cyclosporine A, tacrolimus and steroids dose-dependently inhibited IFN-gamma secretion, and reactivity was further reduced when calcineurin inhibitors were combined with steroids. Tacrolimus 16-26 interferon gamma Homo sapiens 67-76 32369692-8 2020 RESULTS: The enhanced pro-apoptotic and anti-proliferative properties of Tacrolimus versus mTOR inhibitors were associated with increased protein kinase RNA-like endoplasmic reticulum kinase (PERK)-related ER stress, Ser15P-p53/p53 ratio and p21 protein expression that may counterbalance the risk of proliferative upregulation caused by enhanced Thr172P-Cdk4/Cdk4 activation in liver cancer cells. Tacrolimus 73-83 eukaryotic translation initiation factor 2 alpha kinase 3 Homo sapiens 138-190 32369692-8 2020 RESULTS: The enhanced pro-apoptotic and anti-proliferative properties of Tacrolimus versus mTOR inhibitors were associated with increased protein kinase RNA-like endoplasmic reticulum kinase (PERK)-related ER stress, Ser15P-p53/p53 ratio and p21 protein expression that may counterbalance the risk of proliferative upregulation caused by enhanced Thr172P-Cdk4/Cdk4 activation in liver cancer cells. Tacrolimus 73-83 eukaryotic translation initiation factor 2 alpha kinase 3 Homo sapiens 192-196 32369692-8 2020 RESULTS: The enhanced pro-apoptotic and anti-proliferative properties of Tacrolimus versus mTOR inhibitors were associated with increased protein kinase RNA-like endoplasmic reticulum kinase (PERK)-related ER stress, Ser15P-p53/p53 ratio and p21 protein expression that may counterbalance the risk of proliferative upregulation caused by enhanced Thr172P-Cdk4/Cdk4 activation in liver cancer cells. Tacrolimus 73-83 tumor protein p53 Homo sapiens 224-227 32369692-8 2020 RESULTS: The enhanced pro-apoptotic and anti-proliferative properties of Tacrolimus versus mTOR inhibitors were associated with increased protein kinase RNA-like endoplasmic reticulum kinase (PERK)-related ER stress, Ser15P-p53/p53 ratio and p21 protein expression that may counterbalance the risk of proliferative upregulation caused by enhanced Thr172P-Cdk4/Cdk4 activation in liver cancer cells. Tacrolimus 73-83 tumor protein p53 Homo sapiens 228-231 32369692-8 2020 RESULTS: The enhanced pro-apoptotic and anti-proliferative properties of Tacrolimus versus mTOR inhibitors were associated with increased protein kinase RNA-like endoplasmic reticulum kinase (PERK)-related ER stress, Ser15P-p53/p53 ratio and p21 protein expression that may counterbalance the risk of proliferative upregulation caused by enhanced Thr172P-Cdk4/Cdk4 activation in liver cancer cells. Tacrolimus 73-83 H3 histone pseudogene 16 Homo sapiens 242-245 32369692-8 2020 RESULTS: The enhanced pro-apoptotic and anti-proliferative properties of Tacrolimus versus mTOR inhibitors were associated with increased protein kinase RNA-like endoplasmic reticulum kinase (PERK)-related ER stress, Ser15P-p53/p53 ratio and p21 protein expression that may counterbalance the risk of proliferative upregulation caused by enhanced Thr172P-Cdk4/Cdk4 activation in liver cancer cells. Tacrolimus 73-83 cyclin dependent kinase 4 Homo sapiens 355-359 32369692-8 2020 RESULTS: The enhanced pro-apoptotic and anti-proliferative properties of Tacrolimus versus mTOR inhibitors were associated with increased protein kinase RNA-like endoplasmic reticulum kinase (PERK)-related ER stress, Ser15P-p53/p53 ratio and p21 protein expression that may counterbalance the risk of proliferative upregulation caused by enhanced Thr172P-Cdk4/Cdk4 activation in liver cancer cells. Tacrolimus 73-83 cyclin dependent kinase 4 Homo sapiens 360-364 32369692-10 2020 Tacrolimus and mTOR inhibitors increased the protein expression of FKBP12 and FKBP51 that appeared to play pro-survival role. Tacrolimus 0-10 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 67-73 32369692-12 2020 Tacrolimus and mTOR inhibitors decreased miR-92a-1-5p, miR-197-3p, miR-483-3p and miR-720, and increased miR-22-3p, miR-376a-3p, miR-663b, miR-886-5p, miR-1300 and miR-1303 expressions in HepG2 cells. Tacrolimus 0-10 microRNA 92a-1 Homo sapiens 41-50 32369692-12 2020 Tacrolimus and mTOR inhibitors decreased miR-92a-1-5p, miR-197-3p, miR-483-3p and miR-720, and increased miR-22-3p, miR-376a-3p, miR-663b, miR-886-5p, miR-1300 and miR-1303 expressions in HepG2 cells. Tacrolimus 0-10 microRNA 197 Homo sapiens 55-62 32369692-12 2020 Tacrolimus and mTOR inhibitors decreased miR-92a-1-5p, miR-197-3p, miR-483-3p and miR-720, and increased miR-22-3p, miR-376a-3p, miR-663b, miR-886-5p, miR-1300 and miR-1303 expressions in HepG2 cells. Tacrolimus 0-10 microRNA 223 Homo sapiens 105-114 32369692-12 2020 Tacrolimus and mTOR inhibitors decreased miR-92a-1-5p, miR-197-3p, miR-483-3p and miR-720, and increased miR-22-3p, miR-376a-3p, miR-663b, miR-886-5p, miR-1300 and miR-1303 expressions in HepG2 cells. Tacrolimus 0-10 microRNA 663b Homo sapiens 129-137 32369692-12 2020 Tacrolimus and mTOR inhibitors decreased miR-92a-1-5p, miR-197-3p, miR-483-3p and miR-720, and increased miR-22-3p, miR-376a-3p, miR-663b, miR-886-5p, miR-1300 and miR-1303 expressions in HepG2 cells. Tacrolimus 0-10 vault RNA 2-1 Homo sapiens 139-146 32369692-12 2020 Tacrolimus and mTOR inhibitors decreased miR-92a-1-5p, miR-197-3p, miR-483-3p and miR-720, and increased miR-22-3p, miR-376a-3p, miR-663b, miR-886-5p, miR-1300 and miR-1303 expressions in HepG2 cells. Tacrolimus 0-10 microRNA 1303 Homo sapiens 164-172 32369692-13 2020 CONCLUSION: The more potent pro-apoptotic and anti-proliferative properties of Tacrolimus versus mTOR inhibitors were associated with an increased activation of PERK and p53 signaling, and p21 protein expression. Tacrolimus 79-89 eukaryotic translation initiation factor 2 alpha kinase 3 Homo sapiens 161-165 32369692-13 2020 CONCLUSION: The more potent pro-apoptotic and anti-proliferative properties of Tacrolimus versus mTOR inhibitors were associated with an increased activation of PERK and p53 signaling, and p21 protein expression. Tacrolimus 79-89 tumor protein p53 Homo sapiens 170-173 32369692-13 2020 CONCLUSION: The more potent pro-apoptotic and anti-proliferative properties of Tacrolimus versus mTOR inhibitors were associated with an increased activation of PERK and p53 signaling, and p21 protein expression. Tacrolimus 79-89 H3 histone pseudogene 16 Homo sapiens 189-192 32369692-14 2020 FKBP12 and FKBP51 appeared to be the most relevant partners of Tacrolimus and mTOR inhibitors exerting a pro-survival effect in HepG2 cells. Tacrolimus 63-73 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 0-6 32269108-4 2020 Using an animal model of CIPS, we found that systemic administration of FK506 in male and female mice significantly increased the amount of alpha2delta-1-GluN1 complexes in the spinal cord and the level of alpha2delta-1-bound GluN1 proteins in spinal synaptosomes. Tacrolimus 72-77 glutamate receptor, ionotropic, NMDA1 (zeta 1) Mus musculus 154-159 32269108-4 2020 Using an animal model of CIPS, we found that systemic administration of FK506 in male and female mice significantly increased the amount of alpha2delta-1-GluN1 complexes in the spinal cord and the level of alpha2delta-1-bound GluN1 proteins in spinal synaptosomes. Tacrolimus 72-77 glutamate receptor, ionotropic, NMDA1 (zeta 1) Mus musculus 226-231 32269108-5 2020 Treatment with FK506 significantly increased the frequency of miniature excitatory postsynaptic currents (EPSCs) and the amplitudes of monosynaptic EPSCs evoked from the dorsal root and puff NMDAR currents in spinal dorsal horn neurons. Tacrolimus 15-20 glutamate receptor, ionotropic, NMDA1 (zeta 1) Mus musculus 191-196 32269108-6 2020 Inhibiting alpha2delta-1 with gabapentin or disrupting the alpha2delta-1-NMDAR interaction with alpha2delta-1Tat peptide completely reversed the effects of FK506. Tacrolimus 156-161 glutamate receptor, ionotropic, NMDA1 (zeta 1) Mus musculus 73-78 32269108-9 2020 In addition, genetically deleting GluN1 in primary sensory neurons or alpha2delta-1 similarly attenuated FK506-induced thermal and mechanical hypersensitivity. Tacrolimus 105-110 glutamate receptor, ionotropic, NMDA1 (zeta 1) Mus musculus 34-39 32570960-8 2020 The relationship between CYP3A5 genotype and blood concentration, dose, and concentration/dose (C/D) ratio of tacrolimus in 15 subjects was studied. Tacrolimus 110-120 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 25-31 32570960-9 2020 The tacrolimus dose to maintain equivalent blood concentrations was lower in CYP3A5*3/*3 than in CYP3A5*1 carriers, and the C/D ratio was significantly higher in the latter. Tacrolimus 4-14 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 77-83 32570960-9 2020 The tacrolimus dose to maintain equivalent blood concentrations was lower in CYP3A5*3/*3 than in CYP3A5*1 carriers, and the C/D ratio was significantly higher in the latter. Tacrolimus 4-14 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 97-103 32570960-10 2020 Thus, CYP3A5 polymorphism information played a role in determining the initial dose of tacrolimus. Tacrolimus 87-97 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 6-12 32570960-11 2020 Furthermore, since the effect of tacrolimus appears earlier in CYP3A5*3/*3 than in CYP3A5*1/*1 and *1/*3, it seems necessary to change the evaluation time of therapeutic effect by CYP3A5 genotype. Tacrolimus 33-43 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 63-69 32570960-11 2020 Furthermore, since the effect of tacrolimus appears earlier in CYP3A5*3/*3 than in CYP3A5*1/*1 and *1/*3, it seems necessary to change the evaluation time of therapeutic effect by CYP3A5 genotype. Tacrolimus 33-43 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 83-89 32570960-11 2020 Furthermore, since the effect of tacrolimus appears earlier in CYP3A5*3/*3 than in CYP3A5*1/*1 and *1/*3, it seems necessary to change the evaluation time of therapeutic effect by CYP3A5 genotype. Tacrolimus 33-43 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 83-89 32570960-12 2020 Additionally, the relationship between CYP3A5 genotype and C/D ratio of tacrolimus in colonic mucosa was investigated in 10 subjects. Tacrolimus 72-82 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 39-45 32570960-13 2020 Tacrolimus concentration in the mucosa was two-fold higher in CYP3A5*3/*3 than in CYP3A5*1 carriers, although no significant difference in tacrolimus-blood levels was observed. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 62-68 32570960-13 2020 Tacrolimus concentration in the mucosa was two-fold higher in CYP3A5*3/*3 than in CYP3A5*1 carriers, although no significant difference in tacrolimus-blood levels was observed. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 82-88 32570960-14 2020 Therefore, the local concentration of tacrolimus affected by CYP3A5 polymorphism might be related to its therapeutic effect. Tacrolimus 38-48 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 61-67 31622734-3 2020 Tacrolimus and rectal indomethacin have each been reported to reduce risk of PEP. Tacrolimus 0-10 progestagen associated endometrial protein Homo sapiens 77-80 31654367-4 2020 METHODS: This was a multi-center, single-arm, prospective trial with a planned interim analysis after 16 patients, in which the tacrolimus starting dose was based on bodyweight, cytochrome P450 3A5 genotype, and donor status (living vs. deceased donor). Tacrolimus 128-138 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 178-197 31654367-9 2020 Cytochrome P450 3A5 genotype, hematocrit, and creatinine influenced the tacrolimus clearance. Tacrolimus 72-82 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-19 31654367-12 2020 CONCLUSIONS: The weight-normalized starting dose of tacrolimus should be higher in patients with a lower bodyweight and in those who are cytochrome P450 3A5 expressers. Tacrolimus 52-62 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 137-156 31955224-6 2020 Based on the prediction, dual-luciferase reporter assay and miRNA transfection were used to discover the mechanism of how SNP rs15524 controls tacrolimus serum concentration through influencing CYP3A5 expression. Tacrolimus 143-153 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 194-200 31955224-7 2020 RESULTS: In this article, we found multiple SNPs on CYP3A4, CYP3A5, FKBP1A, NFATC2 genes were predicted closely related to tacrolimus serum concentration, therapeutic effect which reflected by QMG score changes or even reasonable drug dose. Tacrolimus 123-133 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 52-58 31955224-7 2020 RESULTS: In this article, we found multiple SNPs on CYP3A4, CYP3A5, FKBP1A, NFATC2 genes were predicted closely related to tacrolimus serum concentration, therapeutic effect which reflected by QMG score changes or even reasonable drug dose. Tacrolimus 123-133 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 60-66 31955224-7 2020 RESULTS: In this article, we found multiple SNPs on CYP3A4, CYP3A5, FKBP1A, NFATC2 genes were predicted closely related to tacrolimus serum concentration, therapeutic effect which reflected by QMG score changes or even reasonable drug dose. Tacrolimus 123-133 FKBP prolyl isomerase 1A Homo sapiens 68-74 31955224-7 2020 RESULTS: In this article, we found multiple SNPs on CYP3A4, CYP3A5, FKBP1A, NFATC2 genes were predicted closely related to tacrolimus serum concentration, therapeutic effect which reflected by QMG score changes or even reasonable drug dose. Tacrolimus 123-133 nuclear factor of activated T cells 2 Homo sapiens 76-82 31622734-4 2020 We investigated the incidence of PEP in patients who have undergone ERCP after liver transplantation and the effectiveness of tacrolimus and/or indomethacin in reducing risk of PEP. Tacrolimus 126-136 progestagen associated endometrial protein Homo sapiens 177-180 31622734-10 2020 We calculated adjusted odds ratios (ORs) for the association between tacrolimus and indomethacin use and risk of PEP using mixed-effects multivariable logistic regression. Tacrolimus 69-79 progestagen associated endometrial protein Homo sapiens 113-116 31622734-13 2020 A trough level of tacrolimus above 2.5 ng/mL was associated with 79% lower odds of PEP (OR, 0.21; 95% CI, 0.06-0.72; P=.01). Tacrolimus 18-28 progestagen associated endometrial protein Homo sapiens 83-86 31622734-16 2020 In patients with trough levels of tacrolimus above 2.5 ng/mL, addition of indomethacin reduced the odds of PEP by 93% compared to patients who were unexposed to indomethacin. Tacrolimus 34-44 progestagen associated endometrial protein Homo sapiens 107-110 31622734-18 2020 CONCLUSIONS: In a retrospective study of patients who underwent ERCP for biliary complications after liver transplantation, we found trough levels of tacrolimus above 2.5 ng/mL to significantly reduce risk for PEP. Tacrolimus 150-160 progestagen associated endometrial protein Homo sapiens 210-213 32151541-0 2020 Tacrolimus, a calcineurin inhibitor, promotes capsaicin-induced colonic pain in mice. Tacrolimus 0-10 calcineurin binding protein 1 Mus musculus 14-35 32151541-2 2020 Since the clinical use of calcineurin-inhibiting immunosuppressants is commonly associated with chronic diarrhea, we examined if tacrolimus, a calcineurin inhibitor, promotes TRPV1-dependent colonic hypersensitivity in mice. Tacrolimus 129-139 calcineurin binding protein 1 Mus musculus 143-164 32151541-2 2020 Since the clinical use of calcineurin-inhibiting immunosuppressants is commonly associated with chronic diarrhea, we examined if tacrolimus, a calcineurin inhibitor, promotes TRPV1-dependent colonic hypersensitivity in mice. Tacrolimus 129-139 transient receptor potential cation channel, subfamily V, member 1 Mus musculus 175-180 32151541-6 2020 Thus, tacrolimus may aggravate TRPV1-related colonic pain accompanying irritable bowel syndrome. Tacrolimus 6-16 transient receptor potential cation channel, subfamily V, member 1 Mus musculus 31-36 32213713-6 2020 We further demonstrated that immunotherapy with recombinant IL-22 treatment ameliorated the ST258 pulmonary infection in both FK506 treated WT mice and Rag2-/-Il2rg-/- mice via hepatic IL-22ra1 signaling. Tacrolimus 126-131 interleukin 22 Mus musculus 60-65 31530218-0 2020 Optimization of initial dosing scheme of tacrolimus in pediatric refractory nephrotic syndrome patients based on CYP3A5 genotype and coadministration with wuzhi-capsule. Tacrolimus 41-51 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 113-119 31530218-10 2020 The present study recommended the tacrolimus initial dosing scheme in pediatric refractory nephrotic syndrome patients based on CYP3A5 genotype and coadministration with wuzhi-capsule. Tacrolimus 34-44 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 128-134 32425928-8 2020 Interestingly, when we compared the ability of Mo-MDSC to suppress T cell proliferation, we observed that tacrolimus, but not rapamycin-treated KTR, was able to inhibit CD4+ T cell proliferation in vitro. Tacrolimus 106-116 CD4 molecule Homo sapiens 169-172 32340188-0 2020 Donor CYP3A5 Gene Polymorphism Alone Cannot Predict Tacrolimus Intrarenal Concentration in Renal Transplant Recipients. Tacrolimus 52-62 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 6-12 32340188-1 2020 CYP3A5 gene polymorphism in recipients plays an important role in tacrolimus blood pharmacokinetics after renal transplantation. Tacrolimus 66-76 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 32340188-3 2020 The aim of our study was to investigate how the tacrolimus intrarenal concentration (Ctissue) could be predicted based on donor CYP3A5 gene polymorphism in renal transplant recipients. Tacrolimus 48-58 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 128-134 32368128-0 2020 Effects of CYP3A5 Polymorphisms on Efficacy and Safety of Tacrolimus Therapy in Patients with Idiopathic Membranous Nephropathy. Tacrolimus 58-68 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 11-17 32368128-4 2020 The aim of this study was to analyze the effects of CYP3A5 gene polymorphisms on the efficacy and safety of TAC in IMN patients. Tacrolimus 108-111 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 52-58 32368128-10 2020 The significant association between the CYP3A5 phenotype and TAC metabolism was observed. Tacrolimus 61-64 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 40-46 32368128-15 2020 Conclusion: Our results demonstrated that CYP3A5 polymorphisms had important guiding roles in the treatment of IMN with tacrolimus. Tacrolimus 120-130 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 42-48 32368128-16 2020 CYP3A5 expressers required higher daily doses of TAC to achieve the target drug concentration, but with fewer side effects. Tacrolimus 49-52 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 32317681-5 2020 The ex vivo study showed that TAC-loaded NPs caused a significant suppression of the proliferation of CD4+ and CD8+ cells, which was comparable to the control formulation (Prograf). Tacrolimus 30-33 CD4 antigen Mus musculus 102-105 32363004-0 2020 Correction: Tacrolimus dose requirement based on the CYP3A5 genotype in renal transplant patients. Tacrolimus 12-22 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 53-59 32290462-11 2020 Finally, CD56bright and CD94/NK group 2 member A receptor positive (NKG2A+) Natural Killer (NK) cell subsets increased in mTORi- compared to tacrolimus-treated patients (both p < 0.001). Tacrolimus 141-151 killer cell lectin like receptor D1 Homo sapiens 24-28 32290462-11 2020 Finally, CD56bright and CD94/NK group 2 member A receptor positive (NKG2A+) Natural Killer (NK) cell subsets increased in mTORi- compared to tacrolimus-treated patients (both p < 0.001). Tacrolimus 141-151 killer cell lectin like receptor C1 Homo sapiens 68-73 32260456-3 2020 rs776746 (CYP3A5) and rs1137115 (CYP2A6) are single nucleotide polymorphisms (SNPs) that can affect exposure to tacrolimus. Tacrolimus 112-122 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 10-16 32260456-3 2020 rs776746 (CYP3A5) and rs1137115 (CYP2A6) are single nucleotide polymorphisms (SNPs) that can affect exposure to tacrolimus. Tacrolimus 112-122 cytochrome P450 family 2 subfamily A member 6 Homo sapiens 33-39 31811646-7 2020 The inhibition of calcineurin with FK506 significantly inhibited the nuclear levels of NFAT2 and NFAT4 and the inhibition of P38 MAPK with SB203580 inhibited the nuclear and cytoplasmic accumulation of NFAT1. Tacrolimus 35-40 nuclear factor of activated T-cells 3 Rattus norvegicus 97-102 31820394-1 2020 The calcineurin inhibitor tacrolimus is an effective immunosuppressant and is extensively used in solid organ transplantation. Tacrolimus 26-36 calcineurin binding protein 1 Homo sapiens 4-25 31838663-0 2020 Tacrolimus Inhibits TNF-alpha/IL-17A-Produced pro-Inflammatory Effect on Human Keratinocytes by Regulating IkappaBzeta. Tacrolimus 0-10 tumor necrosis factor Homo sapiens 20-29 31838663-0 2020 Tacrolimus Inhibits TNF-alpha/IL-17A-Produced pro-Inflammatory Effect on Human Keratinocytes by Regulating IkappaBzeta. Tacrolimus 0-10 interleukin 17A Homo sapiens 30-36 31838663-0 2020 Tacrolimus Inhibits TNF-alpha/IL-17A-Produced pro-Inflammatory Effect on Human Keratinocytes by Regulating IkappaBzeta. Tacrolimus 0-10 NFKB inhibitor zeta Homo sapiens 107-118 31838663-3 2020 This study aimed to investigate the potential regulatory effect of tacrolimus on TNF-alpha/ IL-17A-costimulated human keratinocytes in the mimic psoriatic microenvironment. Tacrolimus 67-77 tumor necrosis factor Homo sapiens 81-90 31838663-3 2020 This study aimed to investigate the potential regulatory effect of tacrolimus on TNF-alpha/ IL-17A-costimulated human keratinocytes in the mimic psoriatic microenvironment. Tacrolimus 67-77 interleukin 17A Homo sapiens 92-98 31838663-8 2020 Tacrolimus significantly inhibited TNF-alpha/IL-17A-induced IL-36gamma, CCL-20, IL-1beta, and S100-A9 expression at gene level and IL-36gamma and CCL-20 expression at protein level. Tacrolimus 0-10 tumor necrosis factor Homo sapiens 35-44 31838663-8 2020 Tacrolimus significantly inhibited TNF-alpha/IL-17A-induced IL-36gamma, CCL-20, IL-1beta, and S100-A9 expression at gene level and IL-36gamma and CCL-20 expression at protein level. Tacrolimus 0-10 interleukin 17A Homo sapiens 45-51 31838663-8 2020 Tacrolimus significantly inhibited TNF-alpha/IL-17A-induced IL-36gamma, CCL-20, IL-1beta, and S100-A9 expression at gene level and IL-36gamma and CCL-20 expression at protein level. Tacrolimus 0-10 C-C motif chemokine ligand 20 Homo sapiens 72-78 31838663-8 2020 Tacrolimus significantly inhibited TNF-alpha/IL-17A-induced IL-36gamma, CCL-20, IL-1beta, and S100-A9 expression at gene level and IL-36gamma and CCL-20 expression at protein level. Tacrolimus 0-10 interleukin 1 beta Homo sapiens 80-88 31838663-8 2020 Tacrolimus significantly inhibited TNF-alpha/IL-17A-induced IL-36gamma, CCL-20, IL-1beta, and S100-A9 expression at gene level and IL-36gamma and CCL-20 expression at protein level. Tacrolimus 0-10 C-C motif chemokine ligand 20 Homo sapiens 146-152 31838663-9 2020 We further discovered TNF-alpha/IL-17A induced significant IkappaBzeta mRNA and protein expression in NHKs, which could be inhibited by tacrolimus. Tacrolimus 136-146 tumor necrosis factor Homo sapiens 22-31 31838663-9 2020 We further discovered TNF-alpha/IL-17A induced significant IkappaBzeta mRNA and protein expression in NHKs, which could be inhibited by tacrolimus. Tacrolimus 136-146 interleukin 17A Homo sapiens 32-38 31838663-9 2020 We further discovered TNF-alpha/IL-17A induced significant IkappaBzeta mRNA and protein expression in NHKs, which could be inhibited by tacrolimus. Tacrolimus 136-146 NFKB inhibitor zeta Homo sapiens 59-70 31838663-10 2020 Tacrolimus can inhibit pro-inflammatory synergistic action of TNF-alpha/IL-17A on human keratinocytes by regulating IkappaBzeta expression. Tacrolimus 0-10 tumor necrosis factor Homo sapiens 62-71 31838663-10 2020 Tacrolimus can inhibit pro-inflammatory synergistic action of TNF-alpha/IL-17A on human keratinocytes by regulating IkappaBzeta expression. Tacrolimus 0-10 interleukin 17A Homo sapiens 72-78 31838663-10 2020 Tacrolimus can inhibit pro-inflammatory synergistic action of TNF-alpha/IL-17A on human keratinocytes by regulating IkappaBzeta expression. Tacrolimus 0-10 NFKB inhibitor zeta Homo sapiens 116-127 31721244-0 2020 A novel random forest integrative approach based on endogenous CYP3A4 phenotype for predicting tacrolimus concentrations and dosages in Chinese renal transplant patients. Tacrolimus 95-105 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 63-69 32170593-1 2020 BACKGROUND: The aim of this meta-analysis is to explore the effect of IL-2RA vs rATG on the rate of acute rejection, post-transplant infections, and graft as well as patient"s survival in standard- and high-risk renal transplant patients receiving tacrolimus-based maintenance immunotherapy. Tacrolimus 248-258 interleukin 2 receptor subunit alpha Homo sapiens 70-76 31721244-2 2020 The present study aimed to evaluate the potential of an integrative approach to predict individual tacrolimus concentrations and dosages based on endogenous CYP3A4 phenotype, CYP3A5 genotype and clinical variables. Tacrolimus 99-109 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 157-163 31721244-4 2020 RESULTS AND DISCUSSION: The results suggested that endogenous CYP3A4 phenotype was the most important determinant of tacrolimus concentrations and dose requirements. Tacrolimus 117-127 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 62-68 31721244-7 2020 WHAT IS NEW AND CONCLUSION: In summary, endogenous CYP3A4 phenotype is a critical biomarker for the determination of tacrolimus disposition. Tacrolimus 117-127 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 51-57 31721244-8 2020 This predictive RF approach based on CYP3A4 biomarker with the combination of CYP3A5*3 genotype and other clinical variables can be used for predicting tacrolimus concentrations and dosages, which may serve as a useful tool in individualized tacrolimus dosing. Tacrolimus 152-162 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 31721244-8 2020 This predictive RF approach based on CYP3A4 biomarker with the combination of CYP3A5*3 genotype and other clinical variables can be used for predicting tacrolimus concentrations and dosages, which may serve as a useful tool in individualized tacrolimus dosing. Tacrolimus 152-162 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 78-84 31721244-8 2020 This predictive RF approach based on CYP3A4 biomarker with the combination of CYP3A5*3 genotype and other clinical variables can be used for predicting tacrolimus concentrations and dosages, which may serve as a useful tool in individualized tacrolimus dosing. Tacrolimus 242-252 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 31721244-8 2020 This predictive RF approach based on CYP3A4 biomarker with the combination of CYP3A5*3 genotype and other clinical variables can be used for predicting tacrolimus concentrations and dosages, which may serve as a useful tool in individualized tacrolimus dosing. Tacrolimus 242-252 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 78-84 32467610-11 2020 Finally, we found that FK506 reversed hypoxia-induced activation of the calcineurin/NFAT signaling pathway in NP cells and an ex vivo model. Tacrolimus 23-28 nuclear factor of activated T-cells 1 Rattus norvegicus 84-88 32308133-5 2020 CYP3A5 genotype significantly impacts oral tacrolimus concentrations and response after solid organ transplantation. Tacrolimus 43-53 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 31908055-6 2020 hILC showed lower TMG binding comparing to Lin+ cells, reduced expression of CD25 (basiliximab target), and diminished calcineurin activity with undetectable calcineurin and FKBP12 (tacrolimus target). Tacrolimus 182-192 C-C motif chemokine ligand 27 Homo sapiens 0-4 31049814-1 2020 BACKGROUND: Tacrolimus, a calcineurin inhibitor, is recommended by the recent guidelines from the Kidney Disease Improving Global Outcomes Group as the first-line treatment for steroid-resistant nephrotic syndrome (SRNS), but its clinical application in China is still limited. Tacrolimus 12-22 calcineurin binding protein 1 Homo sapiens 26-47 31379240-9 2020 The SNPs in 3 genes (CYP1A2, DRD2, and PON1) were associated with risk of tacrolimus-induced nephrotoxicity. Tacrolimus 74-84 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 21-27 31379240-9 2020 The SNPs in 3 genes (CYP1A2, DRD2, and PON1) were associated with risk of tacrolimus-induced nephrotoxicity. Tacrolimus 74-84 paraoxonase 1 Homo sapiens 39-43 32296037-4 2020 In this study, we observed that tacrolimus could induce triglyceride accumulation in hepatocytes by stimulating sterol response element-binding proteins (SREBPs) and miR-33a. Tacrolimus 32-42 microRNA 33a Homo sapiens 166-173 32296037-6 2020 Tacrolimus could downregulate circFASN and result in elevated miR-33a in vivo and in vitro. Tacrolimus 0-10 microRNA 33a Homo sapiens 62-69 32296037-7 2020 Overexpression of circFASN or silencing of miR-33a decreased the promoting effects of tacrolimus on triglyceride accumulation. Tacrolimus 86-96 microRNA 33a Homo sapiens 43-50 32296037-9 2020 Our results showed that the circFASN/miR-33a regulatory system plays a distinct role in tacrolimus-induced disruption of lipid homeostasis. Tacrolimus 88-98 microRNA 33a Homo sapiens 37-44 32296037-10 2020 MiR-33a is likely a risk factor for tacrolimus-related dyslipidemia, providing a potential therapeutic target to combat tacrolimus-induced dyslipidemia after liver transplantation. Tacrolimus 36-46 microRNA 33a Homo sapiens 0-7 32296037-10 2020 MiR-33a is likely a risk factor for tacrolimus-related dyslipidemia, providing a potential therapeutic target to combat tacrolimus-induced dyslipidemia after liver transplantation. Tacrolimus 120-130 microRNA 33a Homo sapiens 0-7 32225074-0 2020 Influence of POR*28 Polymorphisms on CYP3A5*3-Associated Variations in Tacrolimus Blood Levels at an Early Stage after Liver Transplantation. Tacrolimus 71-81 cytochrome p450 oxidoreductase Homo sapiens 13-16 32225074-0 2020 Influence of POR*28 Polymorphisms on CYP3A5*3-Associated Variations in Tacrolimus Blood Levels at an Early Stage after Liver Transplantation. Tacrolimus 71-81 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 37-43 32225074-1 2020 It is well known that the CYP3A5*3 polymorphism is an important marker that correlates with the tacrolimus dose requirement after organ transplantation. Tacrolimus 96-106 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 26-32 32225074-2 2020 Recently, it has been revealed that the POR*28 polymorphism affects the pharmacokinetics of tacrolimus in renal transplant patients. Tacrolimus 92-102 cytochrome p450 oxidoreductase Homo sapiens 40-43 32225074-3 2020 In this study, we examined whether POR*28 as well as CYP3A5*3 polymorphism in Japanese recipients and donors would be another biomarker for the variation of tacrolimus blood levels in the recipients during the first month after living-donor liver transplantation. Tacrolimus 157-167 cytochrome p450 oxidoreductase Homo sapiens 35-38 32225074-3 2020 In this study, we examined whether POR*28 as well as CYP3A5*3 polymorphism in Japanese recipients and donors would be another biomarker for the variation of tacrolimus blood levels in the recipients during the first month after living-donor liver transplantation. Tacrolimus 157-167 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 53-59 32225074-8 2020 In conclusion, to our knowledge, this is the first report suggesting that the POR*28 polymorphism is another biomarker for the tacrolimus oral dosage after liver transplantation in patients carrying CYP3A5*1 rather than CYP3A5*3/*3. Tacrolimus 127-137 cytochrome p450 oxidoreductase Homo sapiens 78-81 32225074-8 2020 In conclusion, to our knowledge, this is the first report suggesting that the POR*28 polymorphism is another biomarker for the tacrolimus oral dosage after liver transplantation in patients carrying CYP3A5*1 rather than CYP3A5*3/*3. Tacrolimus 127-137 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 199-205 32210081-4 2020 We show that treatment of cultured hippocampal mouse and fetal human astrocytes with a CaN inhibitor FK506 resulted in a dynamic modulation of GLAST protein expression, being downregulated after 24-48 h, but upregulated after 7 days of continuous FK506 (200 nM) treatment. Tacrolimus 101-106 solute carrier family 1 member 3 Homo sapiens 143-148 32210081-4 2020 We show that treatment of cultured hippocampal mouse and fetal human astrocytes with a CaN inhibitor FK506 resulted in a dynamic modulation of GLAST protein expression, being downregulated after 24-48 h, but upregulated after 7 days of continuous FK506 (200 nM) treatment. Tacrolimus 247-252 solute carrier family 1 member 3 Homo sapiens 143-148 32235696-5 2020 In Nc/Nga mice, FX or TAC applied to the skin inhibited eosinophil infiltration with decreased expression of Il-33. Tacrolimus 22-25 interleukin 33 Mus musculus 109-114 32308538-10 2020 This can be explained by the increase in TAC concentration caused by CYP3A4 inhibition due to LMV and by the decrease in TAC concentration ascribed to the decrease in VRCZ concentration by CYP2C19 induction due to LMV. Tacrolimus 41-44 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-75 32308538-10 2020 This can be explained by the increase in TAC concentration caused by CYP3A4 inhibition due to LMV and by the decrease in TAC concentration ascribed to the decrease in VRCZ concentration by CYP2C19 induction due to LMV. Tacrolimus 121-124 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 189-196 31654553-5 2020 In addition, TAC caused hepatic insulin resistance and triglyceride accumulation through IRS2/AKT and SREBP1 signaling, respectively. Tacrolimus 13-16 insulin receptor substrate 2 Mus musculus 89-93 31654553-5 2020 In addition, TAC caused hepatic insulin resistance and triglyceride accumulation through IRS2/AKT and SREBP1 signaling, respectively. Tacrolimus 13-16 thymoma viral proto-oncogene 1 Mus musculus 94-97 31654553-5 2020 In addition, TAC caused hepatic insulin resistance and triglyceride accumulation through IRS2/AKT and SREBP1 signaling, respectively. Tacrolimus 13-16 sterol regulatory element binding transcription factor 1 Mus musculus 102-108 31654553-6 2020 Furthermore, we found a pivotal role of CRTC2 in TAC-induced metabolic disorders. Tacrolimus 49-52 CREB regulated transcription coactivator 2 Mus musculus 40-45 31654553-10 2020 Taken together, in addition to its impact on pancreatic cells, TAC induces "hepatogenous diabetes" via CRTC2 signaling. Tacrolimus 63-66 CREB regulated transcription coactivator 2 Mus musculus 103-108 31678537-8 2020 Rising serum tacrolimus or sirolimus levels, new acute kidney injury, and increasing platelet transfusion requirements were significant early predictors of onset in the week preceding prior VOD/SOS diagnosis. Tacrolimus 13-23 xylosyltransferase 2 Homo sapiens 194-197 31755126-0 2020 Initial dose optimization of tacrolimus for children with systemic lupus erythematosus based on the CYP3A5 polymorphism and coadministration with Wuzhi capsule. Tacrolimus 29-39 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 100-106 31755126-4 2020 RESULTS AND DISCUSSION: The results showed that weight, the CYP3A5 genotype and combined treatment with Wuzhi capsule can affect tacrolimus clearance in children with systemic lupus erythematosus. Tacrolimus 129-139 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 60-66 31755126-8 2020 WHAT IS NEW AND CONCLUSION: This study is the first study to recommend an optimal initial regimen of tacrolimus for children with systemic lupus erythematosus based on the CYP3A5 polymorphism and coadministration of Wuzhi capsule. Tacrolimus 101-111 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 172-178 31756280-6 2020 Gene screening for CYP3A5 6986 A>G and ABCB1 3435 C>T in organ transplant recipients may help in preventing DDI and facilitating tacrolimus dose adjustment. Tacrolimus 129-139 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 19-25 31756280-6 2020 Gene screening for CYP3A5 6986 A>G and ABCB1 3435 C>T in organ transplant recipients may help in preventing DDI and facilitating tacrolimus dose adjustment. Tacrolimus 129-139 ATP binding cassette subfamily B member 1 Homo sapiens 39-44 31705533-13 2020 CONCLUSION AND IMPLICATIONS: The hypertensive effects of the immunosuppressant drugs FK506 and rapamycin, while mediated by endothelial cells, do not appear to be exerted at documented cellular targets of the drugs on Ca2+ release and altered FKBP binding to IP3 and RyR. Tacrolimus 85-90 ryanodine receptor 2 Homo sapiens 267-270 32006551-5 2020 Transcription assays of calcineurin (CaN)- and mTOR (mammalian target of rapamycin)-downstream target genes confirm that BbFKBP12 is the target of both FK506 and rapamycin, associated with CaN- and mTOR-signal pathways in B. bassiana. Tacrolimus 152-157 mechanistic target of rapamycin kinase Homo sapiens 47-51 31931373-0 2020 Effects of donor-recipient combinational CYP3A5 genotypes on tacrolimus dosing in Chinese DDLT adult recipients. Tacrolimus 61-71 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 41-47 31931373-3 2020 This retrospective study was conducted to investigate the combined effects of donor-recipient CYP3A5 genotype on tacrolimus pharmacokinetics in Chinese LT adult patients. Tacrolimus 113-123 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 94-100 31931373-12 2020 CONCLUSIONS: To predict the initial dose of tacrolimus in LT patients, both donor and recipient CYP3A5 genotypes must be taken into account; during the maintenance phase of targeted blood concentration, the donor"s CYP3A5 genotype may be of prime importance, especially at three months after transplantation. Tacrolimus 44-54 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 215-221 30890073-9 2020 Next, using the calcineurin inhibitor FK506, we implicated this phosphatase in activation of the nuclear factor of activated T-cells (NFAT; a transcription factor activated through calcineurin-mediated dephosphorylation) and propose that this pathway is involved in transcriptional upregulation of the IL-4 synthesis in NMDA-treated neurons. Tacrolimus 38-43 nuclear factor of activated T-cells 5 Rattus norvegicus 134-138 30890073-9 2020 Next, using the calcineurin inhibitor FK506, we implicated this phosphatase in activation of the nuclear factor of activated T-cells (NFAT; a transcription factor activated through calcineurin-mediated dephosphorylation) and propose that this pathway is involved in transcriptional upregulation of the IL-4 synthesis in NMDA-treated neurons. Tacrolimus 38-43 interleukin 4 Rattus norvegicus 302-306 32006551-5 2020 Transcription assays of calcineurin (CaN)- and mTOR (mammalian target of rapamycin)-downstream target genes confirm that BbFKBP12 is the target of both FK506 and rapamycin, associated with CaN- and mTOR-signal pathways in B. bassiana. Tacrolimus 152-157 mechanistic target of rapamycin kinase Homo sapiens 53-82 32006551-5 2020 Transcription assays of calcineurin (CaN)- and mTOR (mammalian target of rapamycin)-downstream target genes confirm that BbFKBP12 is the target of both FK506 and rapamycin, associated with CaN- and mTOR-signal pathways in B. bassiana. Tacrolimus 152-157 mechanistic target of rapamycin kinase Homo sapiens 198-202 32067305-6 2020 Two patients with severe food allergy responded favorably to conversion from tacrolimus-based immunosuppression to MMF and corticosteroids with reduction in clinical symptoms, total IgE, specific IgE, IL-1ra, IL-4, RANTES, PDGF, MIP-1a, and TNFalpha. Tacrolimus 77-87 interleukin 1 receptor antagonist Homo sapiens 201-207 31733802-2 2020 Although dasatinib is the first-line treatment for CML, it has inhibitory activity against CYP3A4; this might increase the blood concentration of tacrolimus (administered to KT patients for immune suppression). Tacrolimus 146-156 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 91-97 32067305-6 2020 Two patients with severe food allergy responded favorably to conversion from tacrolimus-based immunosuppression to MMF and corticosteroids with reduction in clinical symptoms, total IgE, specific IgE, IL-1ra, IL-4, RANTES, PDGF, MIP-1a, and TNFalpha. Tacrolimus 77-87 interleukin 4 Homo sapiens 209-213 32067305-6 2020 Two patients with severe food allergy responded favorably to conversion from tacrolimus-based immunosuppression to MMF and corticosteroids with reduction in clinical symptoms, total IgE, specific IgE, IL-1ra, IL-4, RANTES, PDGF, MIP-1a, and TNFalpha. Tacrolimus 77-87 C-C motif chemokine ligand 5 Homo sapiens 215-221 32067305-6 2020 Two patients with severe food allergy responded favorably to conversion from tacrolimus-based immunosuppression to MMF and corticosteroids with reduction in clinical symptoms, total IgE, specific IgE, IL-1ra, IL-4, RANTES, PDGF, MIP-1a, and TNFalpha. Tacrolimus 77-87 C-C motif chemokine ligand 3 Homo sapiens 229-235 32067305-6 2020 Two patients with severe food allergy responded favorably to conversion from tacrolimus-based immunosuppression to MMF and corticosteroids with reduction in clinical symptoms, total IgE, specific IgE, IL-1ra, IL-4, RANTES, PDGF, MIP-1a, and TNFalpha. Tacrolimus 77-87 tumor necrosis factor Homo sapiens 241-249 32048900-1 2022 Background: The pathogenesis of vitiligo is complex and multifactorial, accumulating evidence of increased oxidative stress and reduction in catalase levels in vitiligo patients has been shown, hence, pseudocatalase/superoxide dismutase (PSD) gel has been used as treatment option for vitiligo.Aim: To assesses the synergic effect of PSD when combines with Tacrolimus 0.1% ointment versus Tacrolimus 0.1% alone.Method: A randomized controlled trial that included 49 children with vitiligo with limited area (10% or less). Tacrolimus 357-367 catalase Homo sapiens 141-149 32058973-8 2020 In parallel, chemical inhibition of the Cam/Calcineurin pathway by Cyclosporin A or FK506 also reduces CDTa phenotypes, potentially opening new avenues for treating CDIs. Tacrolimus 84-89 Calcineurin A1 Drosophila melanogaster 44-55 32048900-1 2022 Background: The pathogenesis of vitiligo is complex and multifactorial, accumulating evidence of increased oxidative stress and reduction in catalase levels in vitiligo patients has been shown, hence, pseudocatalase/superoxide dismutase (PSD) gel has been used as treatment option for vitiligo.Aim: To assesses the synergic effect of PSD when combines with Tacrolimus 0.1% ointment versus Tacrolimus 0.1% alone.Method: A randomized controlled trial that included 49 children with vitiligo with limited area (10% or less). Tacrolimus 389-399 catalase Homo sapiens 141-149 31807785-1 2020 FKBP53 is one of the seven multi-domain FK506-binding proteins present in Arabidopsis thaliana, and it is known to get targeted to the nucleus. Tacrolimus 40-45 FK506 BINDING PROTEIN 53 Arabidopsis thaliana 0-6 31725919-9 2020 Body weight, age, CYP3A5 genotype, cystatin-C and daily dose of tacrolimus may have significant effects on the pharmacokinetics of tacrolimus in children with glomerular disease. Tacrolimus 131-141 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 18-24 32034192-0 2020 Author Correction: Whole exome sequencing for the identification of CYP3A7 variants associated with tacrolimus concentrations in kidney transplant patients. Tacrolimus 100-110 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 68-74 31386765-2 2020 Tacrolimus (or FK506), a calcineurin inhibitor (CNI) introduced in field of transplantation in the 1990s, is the cornerstone of most immunosuppressive regimens in solid organ transplantation. Tacrolimus 0-10 calcineurin binding protein 1 Homo sapiens 25-46 31386765-2 2020 Tacrolimus (or FK506), a calcineurin inhibitor (CNI) introduced in field of transplantation in the 1990s, is the cornerstone of most immunosuppressive regimens in solid organ transplantation. Tacrolimus 15-20 calcineurin binding protein 1 Homo sapiens 25-46 31725919-9 2020 Body weight, age, CYP3A5 genotype, cystatin-C and daily dose of tacrolimus may have significant effects on the pharmacokinetics of tacrolimus in children with glomerular disease. Tacrolimus 131-141 cystatin C Homo sapiens 35-45 31732500-0 2020 Tacrolimus-Induced BMP/SMAD Signaling Associates with Metabolic Stress-Activated FOXO1 to Trigger beta-Cell Failure. Tacrolimus 0-10 bone morphogenetic protein 1 Homo sapiens 19-22 31441337-6 2020 Data Synthesis: Studies demonstrate pharmacokinetic differences between cyclosporine and tacrolimus, particularly with regard to inhibition of 2 hepatic transporters: P-glycoprotein and organic anion transporting polypeptide (OATP). Tacrolimus 89-99 ATP binding cassette subfamily B member 1 Homo sapiens 167-181 31441337-6 2020 Data Synthesis: Studies demonstrate pharmacokinetic differences between cyclosporine and tacrolimus, particularly with regard to inhibition of 2 hepatic transporters: P-glycoprotein and organic anion transporting polypeptide (OATP). Tacrolimus 89-99 solute carrier organic anion transporter family member 1A2 Homo sapiens 186-224 31441337-6 2020 Data Synthesis: Studies demonstrate pharmacokinetic differences between cyclosporine and tacrolimus, particularly with regard to inhibition of 2 hepatic transporters: P-glycoprotein and organic anion transporting polypeptide (OATP). Tacrolimus 89-99 solute carrier organic anion transporter family member 1A2 Homo sapiens 226-230 31732500-0 2020 Tacrolimus-Induced BMP/SMAD Signaling Associates with Metabolic Stress-Activated FOXO1 to Trigger beta-Cell Failure. Tacrolimus 0-10 forkhead box O1 Homo sapiens 81-86 31732500-3 2020 Here we show that tacrolimus induces loss of human beta-cell maturity and beta-cell failure through activation of the BMP/SMAD signaling pathway when administered under mild metabolic stress conditions. Tacrolimus 18-28 bone morphogenetic protein 1 Homo sapiens 118-121 31732500-4 2020 Tacrolimus-induced phospho-SMAD1/5 acts in synergy with metabolic stress-activated FOXO1 through formation of a complex. Tacrolimus 0-10 forkhead box O1 Homo sapiens 83-88 31732500-6 2020 Pharmacological inhibition of BMP signaling protects human beta-cells from tacrolimus-induced beta-cell dysfunction in vitro Furthermore, we confirm that BMP/SMAD signaling is activated in protocol pancreas allograft biopsies from recipients on tacrolimus. Tacrolimus 75-85 bone morphogenetic protein 1 Homo sapiens 30-33 31732500-6 2020 Pharmacological inhibition of BMP signaling protects human beta-cells from tacrolimus-induced beta-cell dysfunction in vitro Furthermore, we confirm that BMP/SMAD signaling is activated in protocol pancreas allograft biopsies from recipients on tacrolimus. Tacrolimus 75-85 bone morphogenetic protein 1 Homo sapiens 154-157 31732500-6 2020 Pharmacological inhibition of BMP signaling protects human beta-cells from tacrolimus-induced beta-cell dysfunction in vitro Furthermore, we confirm that BMP/SMAD signaling is activated in protocol pancreas allograft biopsies from recipients on tacrolimus. Tacrolimus 245-255 bone morphogenetic protein 1 Homo sapiens 30-33 31732500-6 2020 Pharmacological inhibition of BMP signaling protects human beta-cells from tacrolimus-induced beta-cell dysfunction in vitro Furthermore, we confirm that BMP/SMAD signaling is activated in protocol pancreas allograft biopsies from recipients on tacrolimus. Tacrolimus 245-255 bone morphogenetic protein 1 Homo sapiens 154-157 32013193-2 2020 Germline mutations in cytochrome P450 isoforms 4 and 5 genes (CYP3A4/5) and the ATP-binding cassette B1 gene (ABCB1) may contribute to interindividual tacrolimus PK variability, which may impact clinical outcomes among allogeneic hematopoietic stem cell transplantation (HSCT) patients. Tacrolimus 151-161 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 62-70 32010314-0 2020 Tacrolimus reduces atherosclerotic plaque formation in ApoE-/- mice by inhibiting NLRP3 inflammatory corpuscles. Tacrolimus 0-10 apolipoprotein E Mus musculus 55-59 32010314-0 2020 Tacrolimus reduces atherosclerotic plaque formation in ApoE-/- mice by inhibiting NLRP3 inflammatory corpuscles. Tacrolimus 0-10 NLR family, pyrin domain containing 3 Mus musculus 82-87 32010314-10 2020 The protein content of NLRP3, ASC, Casp-1, IL-1beta and IL-18 in the aorta in ApoE-/- mice was remarkably increased, and they were inhibited to some extent after tacrolimus intervention. Tacrolimus 162-172 NLR family, pyrin domain containing 3 Mus musculus 23-28 32010314-10 2020 The protein content of NLRP3, ASC, Casp-1, IL-1beta and IL-18 in the aorta in ApoE-/- mice was remarkably increased, and they were inhibited to some extent after tacrolimus intervention. Tacrolimus 162-172 caspase 1 Mus musculus 35-41 32010314-10 2020 The protein content of NLRP3, ASC, Casp-1, IL-1beta and IL-18 in the aorta in ApoE-/- mice was remarkably increased, and they were inhibited to some extent after tacrolimus intervention. Tacrolimus 162-172 interleukin 1 alpha Mus musculus 43-51 32010314-10 2020 The protein content of NLRP3, ASC, Casp-1, IL-1beta and IL-18 in the aorta in ApoE-/- mice was remarkably increased, and they were inhibited to some extent after tacrolimus intervention. Tacrolimus 162-172 interleukin 18 Mus musculus 56-61 32010314-11 2020 In conclusion, it is speculated that tacrolimus may reduce the formation of AS through inhibiting ROS in macrophages and activation of NLRP3 inflammatory corpuscles and reducing the release of IL-1beta and IL-18. Tacrolimus 37-47 NLR family, pyrin domain containing 3 Mus musculus 135-140 32010314-11 2020 In conclusion, it is speculated that tacrolimus may reduce the formation of AS through inhibiting ROS in macrophages and activation of NLRP3 inflammatory corpuscles and reducing the release of IL-1beta and IL-18. Tacrolimus 37-47 interleukin 1 alpha Mus musculus 193-201 32010314-11 2020 In conclusion, it is speculated that tacrolimus may reduce the formation of AS through inhibiting ROS in macrophages and activation of NLRP3 inflammatory corpuscles and reducing the release of IL-1beta and IL-18. Tacrolimus 37-47 interleukin 18 Mus musculus 206-211 32657689-0 2020 CYP3A5 polymorphisms and their effects on tacrolimus exposure in an ethnically diverse South African renal transplant population. Tacrolimus 42-52 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 32013193-2 2020 Germline mutations in cytochrome P450 isoforms 4 and 5 genes (CYP3A4/5) and the ATP-binding cassette B1 gene (ABCB1) may contribute to interindividual tacrolimus PK variability, which may impact clinical outcomes among allogeneic hematopoietic stem cell transplantation (HSCT) patients. Tacrolimus 151-161 ATP binding cassette subfamily B member 1 Homo sapiens 110-115 32013193-4 2020 Significant associations were detected between germline variants in CYP3A4/5 and ABCB1 and PK endpoints (e.g., median steady-state tacrolimus concentrations and time to goal tacrolimus concentration). Tacrolimus 131-141 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-76 32013193-4 2020 Significant associations were detected between germline variants in CYP3A4/5 and ABCB1 and PK endpoints (e.g., median steady-state tacrolimus concentrations and time to goal tacrolimus concentration). Tacrolimus 131-141 ATP binding cassette subfamily B member 1 Homo sapiens 81-86 32013193-4 2020 Significant associations were detected between germline variants in CYP3A4/5 and ABCB1 and PK endpoints (e.g., median steady-state tacrolimus concentrations and time to goal tacrolimus concentration). Tacrolimus 174-184 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-76 32013193-4 2020 Significant associations were detected between germline variants in CYP3A4/5 and ABCB1 and PK endpoints (e.g., median steady-state tacrolimus concentrations and time to goal tacrolimus concentration). Tacrolimus 174-184 ATP binding cassette subfamily B member 1 Homo sapiens 81-86 32013193-6 2020 Decreased age and CYP3A5*1/*1 genotype were independently associated with subtherapeutic tacrolimus trough concentrations while CYP3A5*1*3 or CYP3A5*3/*3 genotypes, myeloablative allogeneic HSCT conditioning regimen (MAC) and increased weight were independently associated with supratherapeutic tacrolimus trough concentrations. Tacrolimus 89-99 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 18-24 31941840-3 2020 Both TAC and SIR impaired insulin secretion in fasted and/or stimulated conditions. Tacrolimus 5-8 insulin Homo sapiens 26-33 31941840-4 2020 Treatment with TAC or SIR increased amyloid deposition and islet macrophages, disrupted insulin granule formation, and induced broad transcriptional dysregulation related to peptide processing, ion/calcium flux, and the extracellular matrix; however, it did not affect regulation of beta cell mass. Tacrolimus 15-18 insulin Homo sapiens 88-95 32657689-3 2020 Cytochrome P-450 3A5 (CYP3A5) is the main enzyme involved in tacrolimus metabolism, and rs776746A>G is the most frequently studied polymorphism in the CYP3A5 gene. Tacrolimus 61-71 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-20 32657689-3 2020 Cytochrome P-450 3A5 (CYP3A5) is the main enzyme involved in tacrolimus metabolism, and rs776746A>G is the most frequently studied polymorphism in the CYP3A5 gene. Tacrolimus 61-71 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 22-28 31941840-6 2020 Furthermore, cotreatment with a GLP-1 receptor agonist completely prevented TAC-induced beta cell dysfunction and partially prevented SIR-induced beta cell dysfunction. Tacrolimus 76-79 glucagon like peptide 1 receptor Homo sapiens 32-46 32657689-3 2020 Cytochrome P-450 3A5 (CYP3A5) is the main enzyme involved in tacrolimus metabolism, and rs776746A>G is the most frequently studied polymorphism in the CYP3A5 gene. Tacrolimus 61-71 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 151-157 31794606-5 2020 Intriguingly, although NFAT is activated in both DLBCL subtypes, long-term calcineurin inhibition with cyclosporin A or FK506, both clinically approved drugs, triggers potent cytotoxicity specifically in ABC DLBCL cells. Tacrolimus 120-125 ATP binding cassette subfamily B member 6 (Langereis blood group) Homo sapiens 204-207 32657689-4 2020 The rs776746A>G (i.e. CYP3A5*3) single-nucleotide polymorphism in CYP3A5 alters tacrolimus predose trough concentration (C0) and may also affect IPV, which may lead to immune- and/or drug-mediated allograft injury. Tacrolimus 80-90 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 22-28 32657689-4 2020 The rs776746A>G (i.e. CYP3A5*3) single-nucleotide polymorphism in CYP3A5 alters tacrolimus predose trough concentration (C0) and may also affect IPV, which may lead to immune- and/or drug-mediated allograft injury. Tacrolimus 80-90 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 66-72 32657689-7 2020 OBJECTIVES: To determine the frequencies and effect of CYP3A5 and adenosine triphosphate-binding cassette subfamily B member 1 (ABCB1) polymorphisms on tacrolimus C0/dose ratios in different ethnic groups attending a tertiary renal transplant clinic in SA, and other factors that may explain inter- and IPV in tacrolimus C0. Tacrolimus 152-162 ATP binding cassette subfamily B member 1 Homo sapiens 128-133 32657689-19 2020 CONCLUSIONS: Compared with global transplant populations, SA renal transplant recipients demonstrated a very high rate of CYP3A5 expression, with a significant impact on tacrolimus pharmacokinetics. Tacrolimus 170-180 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 122-128 32657689-20 2020 Genetic variation in CYP3A5 expression affects tacrolimus dosing requirements, and knowing the CYP3A5 genotype of transplant patients may allow better dose prediction compared with current standard dosing recommendations in a multi-ethnic population. Tacrolimus 47-57 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 21-27 32149187-1 2020 Tacrolimus is a reversible calcineurin inhibitor. Tacrolimus 0-10 calcineurin binding protein 1 Homo sapiens 27-48 31919468-8 2020 Consistently, AMPA receptor antagonist CNQX or calcineurin inhibitor FK506 abolished the S-SCAM overexpression-induced loss of GABAA receptors, supporting that GABAergic synapse loss by S-SCAM overexpression is due to the activity-induced dispersal of synaptic GABAA receptors. Tacrolimus 69-74 membrane associated guanylate kinase, WW and PDZ domain containing 2 Homo sapiens 89-95 31919468-8 2020 Consistently, AMPA receptor antagonist CNQX or calcineurin inhibitor FK506 abolished the S-SCAM overexpression-induced loss of GABAA receptors, supporting that GABAergic synapse loss by S-SCAM overexpression is due to the activity-induced dispersal of synaptic GABAA receptors. Tacrolimus 69-74 membrane associated guanylate kinase, WW and PDZ domain containing 2 Homo sapiens 186-192 32268334-1 2020 BACKGROUND: This study aims to assess outcomes of interleukin-2 (IL-2) receptor blocker induction therapy on allograft and patients" outcomes in standard risk recipients in the tacrolimus era, analysing data form the British Renal Transplant Registry. Tacrolimus 177-187 interleukin 2 Homo sapiens 50-63 32268334-1 2020 BACKGROUND: This study aims to assess outcomes of interleukin-2 (IL-2) receptor blocker induction therapy on allograft and patients" outcomes in standard risk recipients in the tacrolimus era, analysing data form the British Renal Transplant Registry. Tacrolimus 177-187 interleukin 2 Homo sapiens 65-69 32999170-3 2020 Because tacrolimus, which is a well-established immunosuppressant for kidney transplantation, and vonoprazan share the CYP3A4 system for metabolism, drug interactions are anticipated upon simultaneous administration. Tacrolimus 8-18 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 119-125 31413313-4 2020 The association of tacrolimus and mTOR inhibitor is supported by pre-clinical data and has been used as GVHD prophylaxis. Tacrolimus 19-29 mechanistic target of rapamycin kinase Homo sapiens 34-38 32378649-1 2020 Tacrolimus, a calcineurin inhibitor, affects bone metabolism and increases the risk of fracture due to marked bone loss. Tacrolimus 0-10 calcineurin binding protein 1 Rattus norvegicus 14-35 32640952-5 2020 The recent progress shows that the recommended strategy is to use as maintenance immunosuppressive therapy a combination of a calcineurin inhibitor (preferably tacrolimus) with an antiproliferative drug (preferably mycophenolate mofetil) with steroids that can be withdrawn early or late in low-risk children. Tacrolimus 160-170 calcineurin binding protein 1 Homo sapiens 126-147 32932253-7 2020 The immunological impact of tacrolimus was revealed by reduced percentages of Tfh, Breg, CD19+BAFF-R+ B cells, and increased percentages of Treg cells as well as down-regulated expression of IL-2, IL-4, IL-10, and IL-13 mRNA levels in PBMCs during the treatment. Tacrolimus 28-38 CD19 molecule Homo sapiens 89-93 31897105-7 2020 Evaluation of the effectiveness revealed that MMF + GC produced significantly higher overall responses (i.e. complete remission plus partial remission) and that MMF + GC (OR=2.58; 95% CI, 1.67-3.97), CTX + RTX + GC (OR=3.89; 95% CI, 1.60-9.45), CTX + LEF + GC (OR=3.05; 95% CI, 1.05-8.84) and CTX + TAC + GC (OR=6.22; 95% CI, 1.93-20.05) had significantly higher overall responses compared with those to the traditional treatment regimen (CTX + GC). Tacrolimus 299-302 cytochrome P450 family 27 subfamily A member 1 Homo sapiens 200-203 31897105-8 2020 Ranking probability based on the surface under the cumulative ranking curve indicated that CTX + TAC + GC had the highest probability (80.6%) of being the best treatment for achieving an overall response. Tacrolimus 97-100 cytochrome P450 family 27 subfamily A member 1 Homo sapiens 91-94 31914663-9 2020 Inhibition of calcineurin by FK506 results in an increase in the net phosphorylation and a consequent decrease in catalytic activity of sperm GSK3. Tacrolimus 29-34 glycogen synthase kinase 3 beta Mus musculus 142-146 31849280-0 2020 CYP3A5*3 and CYP2C8*3 variants influence exposure and clinical outcomes of tacrolimus-based therapy. Tacrolimus 75-85 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 31849280-4 2020 Main results: CYP3A5*3/*3 genotype influenced increase in TAC concentration from week 1 to month 6 post-transplantation (p < 0.05). Tacrolimus 58-61 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 14-20 31849280-6 2020 Conclusion: The CYP3A5*3 variant is associated with increased early exposure to TAC. Tacrolimus 80-83 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 16-22 31908154-0 2020 Tacrolimus-induced hypomagnesemia and hypercalciuria requires FKBP12 suggesting a role for calcineurin. Tacrolimus 0-10 FK506 binding protein 1a Mus musculus 62-68 31908154-5 2020 The CNI tacrolimus can inhibit calcineurin only when it binds with the immunophilin, FKBP12; we previously generated mice in which FKBP12 could be deleted along the nephron, to test whether calcineurin inhibition is involved, these mice are normal at baseline. Tacrolimus 8-18 FK506 binding protein 1a Mus musculus 85-91 31908154-6 2020 Here, we confirmed that tacrolimus-treated control mice developed hypomagnesemia and urinary calcium wasting, with decreased protein and mRNA abundance of key magnesium and calcium transport proteins (NCX-1 and Calbindin-D28k ). Tacrolimus 24-34 solute carrier family 8 (sodium/calcium exchanger), member 1 Mus musculus 201-206 31908154-6 2020 Here, we confirmed that tacrolimus-treated control mice developed hypomagnesemia and urinary calcium wasting, with decreased protein and mRNA abundance of key magnesium and calcium transport proteins (NCX-1 and Calbindin-D28k ). Tacrolimus 24-34 calbindin 1 Mus musculus 211-225 31908154-8 2020 In contrast, KS-FKBP12-/- mice treated with tacrolimus were completely protected from these effects. Tacrolimus 44-54 FK506 binding protein 1a Mus musculus 16-22 31683063-4 2020 We show here that both an ATP-independent protein chaperone, Spy L32P, and the FK506 binding domain of a prolyl isomerase, FKBP-25 F145A/I223P, are disordered, yet exhibit structures that are distinct from chemically denatured unfolded states in solution, and that they undergo transitions to a more structured state upon ligand binding. Tacrolimus 79-84 FKBP prolyl isomerase 3 Homo sapiens 123-130 31683063-7 2020 The protein-ligand systems studied here (the ATP-independent protein chaperone, Spy L32P, and the FK506 binding domain of a prolyl isomerase, FKBP-25 F145A/I223P) may serve as models for understanding ligand-induced disorder-to-order transitions in proteins. Tacrolimus 98-103 FKBP prolyl isomerase 3 Homo sapiens 142-149 31689461-6 2019 At the molecular level, FK506-TKM significantly inhibited infiltration of CD4+ and CD8+ T lymphocytes in colon and differentiation of CD4+ T cells into Th1 and Th17 cells in colon-draining mesenteric lymph nodes via restricting dendritic cell migration from colon. Tacrolimus 24-29 CD4 antigen Mus musculus 74-77 31689461-6 2019 At the molecular level, FK506-TKM significantly inhibited infiltration of CD4+ and CD8+ T lymphocytes in colon and differentiation of CD4+ T cells into Th1 and Th17 cells in colon-draining mesenteric lymph nodes via restricting dendritic cell migration from colon. Tacrolimus 24-29 CD4 antigen Mus musculus 134-137 31931404-0 2019 Tacrolimus is effective for neuromyelitis optica spectrum disorders with or without anti-AQP4 antibody. Tacrolimus 0-10 aquaporin 4 Homo sapiens 89-93 31931404-14 2019 CONCLUSION: Combined use of TAC with PSL clearly suppressed relapse of both anti-AQP4 antibody-positive and -negative NMOSD. Tacrolimus 28-31 aquaporin 4 Homo sapiens 81-85 31921171-3 2019 The tacrolimus TTR percentage was calculated by linear interpolation with a target range (5-10 ng/ml months 0-3, 4-8 ng/ml months 4-12). Tacrolimus 4-14 transthyretin Homo sapiens 15-18 31921171-14 2019 Conclusions: Increasing the TTR of tacrolimus in the first year was associated with improved long-term outcomes in living kidney transplants, and TTR may be a novel valuable strategy to monitor tacrolimus exposure. Tacrolimus 35-45 transthyretin Homo sapiens 28-31 31921171-14 2019 Conclusions: Increasing the TTR of tacrolimus in the first year was associated with improved long-term outcomes in living kidney transplants, and TTR may be a novel valuable strategy to monitor tacrolimus exposure. Tacrolimus 194-204 transthyretin Homo sapiens 28-31 31921171-14 2019 Conclusions: Increasing the TTR of tacrolimus in the first year was associated with improved long-term outcomes in living kidney transplants, and TTR may be a novel valuable strategy to monitor tacrolimus exposure. Tacrolimus 194-204 transthyretin Homo sapiens 146-149 31949424-0 2019 Concomitant Treatment with Etanercept and Tacrolimus Synergistically Attenuates Arthritis Progression via Inhibition of Matrix Metalloproteinase-3 Production and Osteoclastogenesis in Human TNF-alpha Transgenic Mice. Tacrolimus 42-52 tumor necrosis factor Homo sapiens 190-199 31836014-0 2019 FXR activation alleviates tacrolimus-induced post-transplant diabetes mellitus by regulating renal gluconeogenesis and glucose uptake. Tacrolimus 26-36 nuclear receptor subfamily 1, group H, member 4 Mus musculus 0-3 31836014-4 2019 The objective of this study was to explore whether FXR is involved in the development of tacrolimus-induced diabetes mellitus. Tacrolimus 89-99 nuclear receptor subfamily 1, group H, member 4 Mus musculus 51-54 32932253-7 2020 The immunological impact of tacrolimus was revealed by reduced percentages of Tfh, Breg, CD19+BAFF-R+ B cells, and increased percentages of Treg cells as well as down-regulated expression of IL-2, IL-4, IL-10, and IL-13 mRNA levels in PBMCs during the treatment. Tacrolimus 28-38 TNF receptor superfamily member 13C Homo sapiens 94-100 31836014-5 2019 METHODS: After C57BL/6J mice were treated with tacrolimus (FK506) for 3 months, the fasting blood glucose levels, body weights, renal morphological alterations, and mRNA expression levels of phosphoenolpyruvate carboxykinase (PEPCK) and glucose transporter 2 (GLUT2) among the control group, the FK506 group and the FK506 + GW4064 (a FXR agonist) group (n = 7) were measured. Tacrolimus 47-57 phosphoenolpyruvate carboxykinase 1, cytosolic Mus musculus 191-224 31836014-5 2019 METHODS: After C57BL/6J mice were treated with tacrolimus (FK506) for 3 months, the fasting blood glucose levels, body weights, renal morphological alterations, and mRNA expression levels of phosphoenolpyruvate carboxykinase (PEPCK) and glucose transporter 2 (GLUT2) among the control group, the FK506 group and the FK506 + GW4064 (a FXR agonist) group (n = 7) were measured. Tacrolimus 59-64 phosphoenolpyruvate carboxykinase 1, cytosolic Mus musculus 191-224 32932253-7 2020 The immunological impact of tacrolimus was revealed by reduced percentages of Tfh, Breg, CD19+BAFF-R+ B cells, and increased percentages of Treg cells as well as down-regulated expression of IL-2, IL-4, IL-10, and IL-13 mRNA levels in PBMCs during the treatment. Tacrolimus 28-38 interleukin 2 Homo sapiens 191-195 31836014-9 2019 RESULTS: FK506 significantly inhibited the mRNA and protein levels of FXR at 48 h and 72 h in HK-2 cells (P < 0.05). Tacrolimus 9-14 nuclear receptor subfamily 1, group H, member 4 Mus musculus 70-73 31836014-12 2019 The FXR agonist GW4064 significantly decreased the fasting blood glucose in mice challenged with FK506 for 3 months (P < 0.05), inhibited gluconeogenesis (P < 0.05) and significantly promoted glucose uptake (P < 0.05). Tacrolimus 97-102 nuclear receptor subfamily 1, group H, member 4 Mus musculus 4-7 32932253-7 2020 The immunological impact of tacrolimus was revealed by reduced percentages of Tfh, Breg, CD19+BAFF-R+ B cells, and increased percentages of Treg cells as well as down-regulated expression of IL-2, IL-4, IL-10, and IL-13 mRNA levels in PBMCs during the treatment. Tacrolimus 28-38 interleukin 4 Homo sapiens 197-201 31836014-14 2019 CONCLUSIONS: FXR activation may mitigate tacrolimus-induced diabetes mellitus by regulating gluconeogenesis as well as glucose uptake of renal cortex proximal tubule epithelial cells in a PGC1alpha/FOXO1-dependent manner, which may be a potential therapeutic strategy for the prevention and treatment of PTDM. Tacrolimus 41-51 nuclear receptor subfamily 1, group H, member 4 Mus musculus 13-16 32932253-7 2020 The immunological impact of tacrolimus was revealed by reduced percentages of Tfh, Breg, CD19+BAFF-R+ B cells, and increased percentages of Treg cells as well as down-regulated expression of IL-2, IL-4, IL-10, and IL-13 mRNA levels in PBMCs during the treatment. Tacrolimus 28-38 interleukin 10 Homo sapiens 203-208 31836014-14 2019 CONCLUSIONS: FXR activation may mitigate tacrolimus-induced diabetes mellitus by regulating gluconeogenesis as well as glucose uptake of renal cortex proximal tubule epithelial cells in a PGC1alpha/FOXO1-dependent manner, which may be a potential therapeutic strategy for the prevention and treatment of PTDM. Tacrolimus 41-51 peroxisome proliferative activated receptor, gamma, coactivator 1 alpha Mus musculus 188-197 31836014-14 2019 CONCLUSIONS: FXR activation may mitigate tacrolimus-induced diabetes mellitus by regulating gluconeogenesis as well as glucose uptake of renal cortex proximal tubule epithelial cells in a PGC1alpha/FOXO1-dependent manner, which may be a potential therapeutic strategy for the prevention and treatment of PTDM. Tacrolimus 41-51 forkhead box O1 Mus musculus 198-203 32932253-7 2020 The immunological impact of tacrolimus was revealed by reduced percentages of Tfh, Breg, CD19+BAFF-R+ B cells, and increased percentages of Treg cells as well as down-regulated expression of IL-2, IL-4, IL-10, and IL-13 mRNA levels in PBMCs during the treatment. Tacrolimus 28-38 interleukin 13 Homo sapiens 214-219 31526865-10 2019 The serum MMP-8 and MMP-9 levels of allograft+FK506 + GM6001 group were significantly lower than those of allograft+FK506 group (P < .05). Tacrolimus 46-51 matrix metallopeptidase 8 Mus musculus 10-15 32047842-0 2020 One-year Outcome of Everolimus With Standard-dose Tacrolimus Immunosuppression in De Novo ABO-incompatible Living Donor Kidney Transplantation: A Retrospective, Single-center, Propensity Score Matching Comparison With Mycophenolate in 42 Transplants. Tacrolimus 50-60 ABO, alpha 1-3-N-acetylgalactosaminyltransferase and alpha 1-3-galactosyltransferase Homo sapiens 90-93 31696965-11 2019 Notably, inactivation of the Cul3-Klhl18 ligase and calcineurin inhibitors FK506 and cyclosporine A that are known immunosuppressant drugs repressed light-induced photoreceptor damage, suggesting potential therapeutic targets. Tacrolimus 75-80 cullin 3 Mus musculus 29-33 31696965-11 2019 Notably, inactivation of the Cul3-Klhl18 ligase and calcineurin inhibitors FK506 and cyclosporine A that are known immunosuppressant drugs repressed light-induced photoreceptor damage, suggesting potential therapeutic targets. Tacrolimus 75-80 kelch-like 18 Mus musculus 34-40 31152486-0 2019 Inhibition of the mTOR pathway: A new mechanism of beta cell toxicity induced by tacrolimus. Tacrolimus 81-91 mechanistic target of rapamycin kinase Rattus norvegicus 18-22 31152486-2 2019 Tacrolimus (TAC) and rapamycin (Rapa) both bind to FK506-binding protein 12 (FKBP12). Tacrolimus 0-10 FKBP prolyl isomerase 1A Rattus norvegicus 51-75 31152486-2 2019 Tacrolimus (TAC) and rapamycin (Rapa) both bind to FK506-binding protein 12 (FKBP12). Tacrolimus 0-10 FKBP prolyl isomerase 1A Rattus norvegicus 77-83 31152486-2 2019 Tacrolimus (TAC) and rapamycin (Rapa) both bind to FK506-binding protein 12 (FKBP12). Tacrolimus 12-15 FKBP prolyl isomerase 1A Rattus norvegicus 51-75 31152486-2 2019 Tacrolimus (TAC) and rapamycin (Rapa) both bind to FK506-binding protein 12 (FKBP12). Tacrolimus 12-15 FKBP prolyl isomerase 1A Rattus norvegicus 77-83 31152486-4 2019 Because of this similarity, we hypothesized that TAC can also inhibit the mTOR signalling, constituting a possible mechanism of beta cell toxicity. Tacrolimus 49-52 mechanistic target of rapamycin kinase Rattus norvegicus 74-78 31152486-6 2019 TAC and Rapa inhibited the mTOR pathway as reflected by lower levels of phospho-mTOR, phospo-p70S6K, and phospo-S6. Tacrolimus 0-3 mechanistic target of rapamycin kinase Rattus norvegicus 27-31 31152486-6 2019 TAC and Rapa inhibited the mTOR pathway as reflected by lower levels of phospho-mTOR, phospo-p70S6K, and phospo-S6. Tacrolimus 0-3 mechanistic target of rapamycin kinase Rattus norvegicus 80-84 31152486-6 2019 TAC and Rapa inhibited the mTOR pathway as reflected by lower levels of phospho-mTOR, phospo-p70S6K, and phospo-S6. Tacrolimus 0-3 ribosomal protein S6 kinase B1 Rattus norvegicus 93-99 31152486-10 2019 In silico docking and immunoprecipitation experiments confirmed that TAC can form a stable noncovalent interaction with FKBP12-mTOR. Tacrolimus 69-72 FKBP prolyl isomerase 1A Rattus norvegicus 120-126 31152486-10 2019 In silico docking and immunoprecipitation experiments confirmed that TAC can form a stable noncovalent interaction with FKBP12-mTOR. Tacrolimus 69-72 mechanistic target of rapamycin kinase Rattus norvegicus 127-131 31152486-11 2019 Thus, the mTOR inhibition may be a mechanism contributing to the diabetogenic effect of TAC. Tacrolimus 88-91 mechanistic target of rapamycin kinase Rattus norvegicus 10-14 31152598-0 2019 Prolonged-Release Tacrolimus Is Less Susceptible to Interaction With the Strong CYP3A Inhibitor Voriconazole in Healthy Volunteers. Tacrolimus 18-28 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 80-85 31087280-0 2019 The Effects of CYP3A5 Genetic Polymorphisms on Serum Tacrolimus Dose-Adjusted Concentrations and Long-Term Prognosis in Chinese Heart Transplantation Recipients. Tacrolimus 53-63 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 15-21 31087280-2 2019 We aim to investigate the effects of cytochrome P450 (CYP) 3A5 (rs776746) single nucleotide polymorphisms (SNPs) on serum tacrolimus concentrations/doses (C/Ds, ng/mL per mg/kg) and long-term prognosis in Chinese heart transplant recipients. Tacrolimus 122-132 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 37-62 31087280-8 2019 RESULTS: In 55 heart transplant recipients (43 males and 12 females), CYP3A5 non-expressors (CYP3A5*3/*3, n = 40) had significantly higher tacrolimus C/Ds than expressors (CYP3A5*1/*3, n = 15) at all time points (P < 0.001). Tacrolimus 139-149 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 70-76 31087280-8 2019 RESULTS: In 55 heart transplant recipients (43 males and 12 females), CYP3A5 non-expressors (CYP3A5*3/*3, n = 40) had significantly higher tacrolimus C/Ds than expressors (CYP3A5*1/*3, n = 15) at all time points (P < 0.001). Tacrolimus 139-149 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 93-99 31087280-8 2019 RESULTS: In 55 heart transplant recipients (43 males and 12 females), CYP3A5 non-expressors (CYP3A5*3/*3, n = 40) had significantly higher tacrolimus C/Ds than expressors (CYP3A5*1/*3, n = 15) at all time points (P < 0.001). Tacrolimus 139-149 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 93-99 31087280-12 2019 CONCLUSIONS: CYP3A5 SNPs affect tacrolimus pharmacokinetics in Chinese heart transplant recipients, and non-expressors have higher tacrolimus C/Ds. Tacrolimus 32-42 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 13-19 31087280-12 2019 CONCLUSIONS: CYP3A5 SNPs affect tacrolimus pharmacokinetics in Chinese heart transplant recipients, and non-expressors have higher tacrolimus C/Ds. Tacrolimus 131-141 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 13-19 31638188-0 2019 Tacrolimus increases the expression level of the chemokine receptor CXCR2 to promote renal fibrosis progression. Tacrolimus 0-10 C-X-C motif chemokine receptor 2 Homo sapiens 68-73 31638188-7 2019 The present results demonstrated that compared with the normal control group, the tacrolimus nephrotoxicity group exhibited severe renal fibrosis (P<0.05), upregulated vimentin (P<0.01), downregulated E-cadherin (P<0.05) and upregulated alpha-SMA (P<0.01). Tacrolimus 82-92 vimentin Homo sapiens 171-179 31638188-7 2019 The present results demonstrated that compared with the normal control group, the tacrolimus nephrotoxicity group exhibited severe renal fibrosis (P<0.05), upregulated vimentin (P<0.01), downregulated E-cadherin (P<0.05) and upregulated alpha-SMA (P<0.01). Tacrolimus 82-92 cadherin 1 Homo sapiens 207-217 31638188-9 2019 Moreover, KEGG pathway enrichment analysis identified that tacrolimus increased the expression levels of chemokine (C-X-C) motif ligand (CXCL)1, CXCL2 and CXCL3 and the chemokine receptor C-X-C chemokine receptor type 2 (CXCR2). Tacrolimus 59-69 C-X-C motif chemokine ligand 1 Homo sapiens 116-143 31638188-9 2019 Moreover, KEGG pathway enrichment analysis identified that tacrolimus increased the expression levels of chemokine (C-X-C) motif ligand (CXCL)1, CXCL2 and CXCL3 and the chemokine receptor C-X-C chemokine receptor type 2 (CXCR2). Tacrolimus 59-69 C-X-C motif chemokine ligand 2 Homo sapiens 145-150 31638188-9 2019 Moreover, KEGG pathway enrichment analysis identified that tacrolimus increased the expression levels of chemokine (C-X-C) motif ligand (CXCL)1, CXCL2 and CXCL3 and the chemokine receptor C-X-C chemokine receptor type 2 (CXCR2). Tacrolimus 59-69 C-X-C motif chemokine ligand 3 Homo sapiens 155-160 31638188-9 2019 Moreover, KEGG pathway enrichment analysis identified that tacrolimus increased the expression levels of chemokine (C-X-C) motif ligand (CXCL)1, CXCL2 and CXCL3 and the chemokine receptor C-X-C chemokine receptor type 2 (CXCR2). Tacrolimus 59-69 C-X-C motif chemokine receptor 2 Homo sapiens 221-226 31638188-10 2019 Collectively, the present study suggested that tacrolimus increases the level of chemokine receptor CXCR2 to promote renal fibrosis progression, which is one of the potential mechanisms underlying tacrolimus-induced nephrotoxicity. Tacrolimus 47-57 C-X-C motif chemokine receptor 2 Homo sapiens 100-105 31638188-10 2019 Collectively, the present study suggested that tacrolimus increases the level of chemokine receptor CXCR2 to promote renal fibrosis progression, which is one of the potential mechanisms underlying tacrolimus-induced nephrotoxicity. Tacrolimus 197-207 C-X-C motif chemokine receptor 2 Homo sapiens 100-105 31514576-0 2019 Comparison of Tacrolimus Starting Doses Based on CYP3A5 Phenotype or Genotype in Kidney Transplant Recipients. Tacrolimus 14-24 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 49-55 31514576-1 2019 BACKGROUND: Selection of expected phenotypes (ie, expressers/non-expressers) is currently used in CYP3A5*3 genotype-based tacrolimus dosing. Tacrolimus 122-132 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 98-104 31514576-8 2019 Based on these results, new tacrolimus starting doses were set at 0.10, 0.20, and 0.30 mg/kg/d for CYP3A5*3/*3, CYP3A5*1/*3, and CYP3A5*1/*1 genotypes, respectively. Tacrolimus 28-38 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 99-105 31514576-8 2019 Based on these results, new tacrolimus starting doses were set at 0.10, 0.20, and 0.30 mg/kg/d for CYP3A5*3/*3, CYP3A5*1/*3, and CYP3A5*1/*1 genotypes, respectively. Tacrolimus 28-38 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 112-118 31514576-8 2019 Based on these results, new tacrolimus starting doses were set at 0.10, 0.20, and 0.30 mg/kg/d for CYP3A5*3/*3, CYP3A5*1/*3, and CYP3A5*1/*1 genotypes, respectively. Tacrolimus 28-38 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 112-118 31514576-9 2019 Tacrolimus overexposure was reduced in the CYP3A5*3/*3 group (63.6% vs 40%, P = .0038). Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 43-49 31514576-12 2019 Our results indicate that the best tacrolimus exposure was obtained for doses of 0.10, 0.20, and 0.20 mg/kg/d for CYP3A5*3/3, CYP3A5*1/*3, and CYP3A5*1/*1, respectively. Tacrolimus 35-45 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 114-120 31514576-12 2019 Our results indicate that the best tacrolimus exposure was obtained for doses of 0.10, 0.20, and 0.20 mg/kg/d for CYP3A5*3/3, CYP3A5*1/*3, and CYP3A5*1/*1, respectively. Tacrolimus 35-45 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 126-132 31514576-12 2019 Our results indicate that the best tacrolimus exposure was obtained for doses of 0.10, 0.20, and 0.20 mg/kg/d for CYP3A5*3/3, CYP3A5*1/*3, and CYP3A5*1/*1, respectively. Tacrolimus 35-45 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 126-132 31733794-7 2019 Therapeutic concentrations of TAC and SRL reduced the percentage of pd1+ and icos+ Tfh cells compared to controls. Tacrolimus 30-33 patr class I histocompatibility antigen, A-126 alpha chain-like Sus scrofa 68-71 31733794-8 2019 In addition, T cells grown in the presence of TAC or SRL expressed less IL-21 and provided less B-cell help. Tacrolimus 46-49 interleukin 21 Homo sapiens 72-77 31526865-10 2019 The serum MMP-8 and MMP-9 levels of allograft+FK506 + GM6001 group were significantly lower than those of allograft+FK506 group (P < .05). Tacrolimus 46-51 matrix metallopeptidase 9 Mus musculus 20-25 31526865-11 2019 MMP-8 and MMP-9 protein expression in the grafts of allograft+FK506 + GM6001 group were lower than those of allograft+FK506 group verified by immunohistochemical staining and western blotting. Tacrolimus 62-67 matrix metallopeptidase 8 Mus musculus 0-5 31526865-11 2019 MMP-8 and MMP-9 protein expression in the grafts of allograft+FK506 + GM6001 group were lower than those of allograft+FK506 group verified by immunohistochemical staining and western blotting. Tacrolimus 62-67 matrix metallopeptidase 9 Mus musculus 10-15 31526865-12 2019 CONCLUSION: FK506 combined with GM6001 could alleviate tracheal obliteration in mouse heterotopic tracheal transplantation model, due to its inhibitory effect on MMPs. Tacrolimus 12-17 matrix metallopeptidase 8 Mus musculus 162-166 31271885-2 2019 Sirolimus is a mammalian target of rapamycin inhibitor that has proven effective in GVHD prophylaxis in combination with a calcineurin inhibitor, such as tacrolimus. Tacrolimus 154-164 mechanistic target of rapamycin kinase Homo sapiens 15-44 32782938-3 2020 Tacrolimus is topically active, water soluble, and has minimal systemic toxicity when administered rectally; we therefore tested a simple tap water-based enema formulation. Tacrolimus 0-10 nuclear RNA export factor 1 Homo sapiens 138-141 31882422-5 2019 The effects of TSLP-DCs and treatments with FK506, an NFATc1 inhibitor, on naive T cell differentiation were monitored by measuring the interleukin (IL)-4, IL-13, and interferon-gamma (IFN-gamma) expression levels. Tacrolimus 44-49 nuclear factor of activated T cells 1 Homo sapiens 54-60 31710427-0 2019 Effect of CYP3A5 and ABCB1 Gene Polymorphisms on Tacrolimus Blood Concentration in Renal Transplant Recipients. Tacrolimus 49-59 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 10-16 31600833-17 2019 Addition of bFGF related decapeptide solution to Tacrolimus gave better results than Tacrolimus alone therapy. Tacrolimus 49-59 fibroblast growth factor 2 Homo sapiens 12-16 31600833-17 2019 Addition of bFGF related decapeptide solution to Tacrolimus gave better results than Tacrolimus alone therapy. Tacrolimus 85-95 fibroblast growth factor 2 Homo sapiens 12-16 31710427-0 2019 Effect of CYP3A5 and ABCB1 Gene Polymorphisms on Tacrolimus Blood Concentration in Renal Transplant Recipients. Tacrolimus 49-59 ATP binding cassette subfamily B member 1 Homo sapiens 21-26 31710427-3 2019 CYP3A5 and MDR1 single-nucleotide polymorphisms (SNPs) are the most effective polymorphisms that play an significant role in the pharmacokinetics of Tac. Tacrolimus 149-152 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 31710427-3 2019 CYP3A5 and MDR1 single-nucleotide polymorphisms (SNPs) are the most effective polymorphisms that play an significant role in the pharmacokinetics of Tac. Tacrolimus 149-152 ATP binding cassette subfamily B member 1 Homo sapiens 11-15 31710427-14 2019 CONCLUSIONS: CYP3A5 but not MDR1 genetic polymorphisms affected the Tac pharmacokinetics and dose requirements in renal transplant recipients. Tacrolimus 68-71 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 13-19 31468631-4 2019 Tacrolimus, a calcineurin inhibitor, restored the high- and low-pressure baroreflex control of RSNA following cisplatin-induced renal injury. Tacrolimus 0-10 calcineurin binding protein 1 Rattus norvegicus 14-35 31401678-0 2019 CYP3A5 and CYP3A7 genetic polymorphisms affect tacrolimus concentration in pediatric patients with nephrotic range proteinuria. Tacrolimus 47-57 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 31401678-0 2019 CYP3A5 and CYP3A7 genetic polymorphisms affect tacrolimus concentration in pediatric patients with nephrotic range proteinuria. Tacrolimus 47-57 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 11-17 31401678-1 2019 PURPOSE: The purpose of this study was to investigate the potential impact of CYP3A4, CYP3A5, and CYP3A7 polymorphisms on the concentration and efficacy of tacrolimus in a cohort of pediatric patients with nephrotic range proteinuria. Tacrolimus 156-166 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 78-84 31401678-1 2019 PURPOSE: The purpose of this study was to investigate the potential impact of CYP3A4, CYP3A5, and CYP3A7 polymorphisms on the concentration and efficacy of tacrolimus in a cohort of pediatric patients with nephrotic range proteinuria. Tacrolimus 156-166 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 86-92 31401678-1 2019 PURPOSE: The purpose of this study was to investigate the potential impact of CYP3A4, CYP3A5, and CYP3A7 polymorphisms on the concentration and efficacy of tacrolimus in a cohort of pediatric patients with nephrotic range proteinuria. Tacrolimus 156-166 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 98-104 31401678-4 2019 RESULTS: The tacrolimus concentration in patients without CYP3A5*3 A allele was 94% higher than those with A allele (90.7 vs 54.2, P = 0.00006). Tacrolimus 13-23 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 58-64 31401678-5 2019 The CYP3A7 rs2257401 was also associated with the concentration of tacrolimus. Tacrolimus 67-77 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 4-10 31401678-7 2019 In addition, there were significant differences in tacrolimus concentration among CYP3A7 rs10211 G carriers and non-carriers; the latter had an almost twofold C0 of the former (101.8 vs 59.6, P = 0.0004). Tacrolimus 51-61 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 82-88 31401678-8 2019 CONCLUSIONS: Our study demonstrated the associations between CYP3A5*3, CYP3A7 rs2257401 and rs10211, and tacrolimus concentration in pediatric patients with nephrotic range proteinuria. Tacrolimus 105-115 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 61-67 31401678-8 2019 CONCLUSIONS: Our study demonstrated the associations between CYP3A5*3, CYP3A7 rs2257401 and rs10211, and tacrolimus concentration in pediatric patients with nephrotic range proteinuria. Tacrolimus 105-115 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 71-77 31401678-9 2019 Children with CYP3A5*3 A, CYP3A7 rs2257401 C, and rs10211 G alleles might need a higher dose of tacrolimus. Tacrolimus 96-106 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 14-20 31401678-9 2019 Children with CYP3A5*3 A, CYP3A7 rs2257401 C, and rs10211 G alleles might need a higher dose of tacrolimus. Tacrolimus 96-106 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 26-32 31469511-7 2019 In an in vitro model of tacrolimus-mediated fibrogenesis by tubular cells, we found that tacrolimus treatment significantly induced mRNA and protein expression of CB1 concomitantly to col3a1 and col4a3 up regulation. Tacrolimus 24-34 cannabinoid receptor 1 Homo sapiens 163-166 31385180-1 2019 PURPOSE: In large observational studies of adult kidney transplant recipients (KTRs) where older adults (65 years old and older) were not well represented, the mammalian target of rapamycin inhibitors (mTOR inhibitors) has poorer outcomes than the standard tacrolimus-mycophenolate-steroids (TAC-MPA-S) regimen. Tacrolimus 257-267 mechanistic target of rapamycin kinase Homo sapiens 202-206 30587068-0 2019 Effects of MDR1 1236C > T-2677G > T-3435C > T polymorphisms on the intracellular accumulation of tacrolimus, cyclosporine A, sirolimus and everolimus. Tacrolimus 106-116 ATP-binding cassette, sub-family B (MDR/TAP), member 1 Sus scrofa 11-15 30587068-9 2019 MDR1 overexpression increased the resistance of LLC-PK1 cells to tacrolimus, cyclosporine A, sirolimus and everolimus. Tacrolimus 65-75 ATP-binding cassette, sub-family B (MDR/TAP), member 1 Sus scrofa 0-4 30587068-15 2019 These findings indicate that wild-type MDR1 exports tacrolimus and sirolimus more efficiency than the MDR1T-T-T, MDR1C-T-T, MDR1C-G-T variant protein. Tacrolimus 52-62 ATP-binding cassette, sub-family B (MDR/TAP), member 1 Sus scrofa 39-43 31442451-5 2019 FK506-mediated inhibition of the calcineurin-NFAT pathway in the HL-1 cells selectively inhibited the stimulatory effect of the conditioned medium derived from ET-1-pre-stimulated endothelial cells on cardiomyocyte fetal gene expression. Tacrolimus 0-5 endothelin 1 Mus musculus 160-164 30953600-6 2019 CYP3A5*3 (rs776746) was associated with higher dose-normalized tacrolimus troughs in all groups but occurred at different allele frequencies and had differing effect sizes. Tacrolimus 63-73 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 31537789-0 2019 Harnessing calcineurin-FK506-FKBP12 crystal structures from invasive fungal pathogens to develop antifungal agents. Tacrolimus 23-28 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 29-35 31362893-6 2019 In this study, we administered tacrolimus to barttin hypomorphic (Bsndneo/neo) mice, a murine model of type 4 BS that exhibits polyuria, hypokalemia, and metabolic alkalosis. Tacrolimus 31-41 barttin CLCNK type accessory beta subunit Mus musculus 45-52 31362893-8 2019 Furthermore, after treatment with tacrolimus, Bsndneo/neo mice increased levels of phosphorylated NCC and NKCC2. Tacrolimus 34-44 solute carrier family 12, member 1 Mus musculus 106-111 31880588-0 2019 Association Between CYP3A5 Genetic Polymorphisms with Tacrolimus Dose Requirement and Allograft Outcomes in Iranian Kidney Transplant Recipients. Tacrolimus 54-64 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 20-26 31880588-2 2019 This study assessed the relationship between CYP3A5/3A4 polymorphisms and tacrolimus dose requirement as well as 6-month transplant outcomes in Iranian kidney transplant recipients. Tacrolimus 74-84 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 45-55 31880588-5 2019 RESULTS: The daily tacrolimus dose was significantly higher and tacrolimus dose adjusted trough levels (C/D ratio) was significantly lower in CYP3A5 expressers compared with non-expressers (P < .05). Tacrolimus 19-29 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 142-148 31880588-5 2019 RESULTS: The daily tacrolimus dose was significantly higher and tacrolimus dose adjusted trough levels (C/D ratio) was significantly lower in CYP3A5 expressers compared with non-expressers (P < .05). Tacrolimus 64-74 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 142-148 31880588-7 2019 CONCLUSION: CYP3A5 genetic polymorphism is significantly associated with required tacrolimus dose. Tacrolimus 82-92 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 12-18 31880588-8 2019 After achieving desired tacrolimus blood level, although some transplant outcomes such as the incidence of clinically suggested acute rejection and time to first rejection were different between CYP3A5 expressers and non-expressers, however, other clinical outcomes did not differ between groups. Tacrolimus 24-34 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 195-201 31770256-7 2019 Moreover, the CYP3A5 genotyping should be considered when WZC is used to increase the blood concentration of FK506. Tacrolimus 109-114 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 14-20 31661769-1 2019 Previous studies demonstrated that the 52-kDa FK506-binding protein (FKBP52) proline-rich loop is functionally relevant in the regulation of steroid hormone receptor activity. Tacrolimus 46-51 FKBP prolyl isomerase 4 Homo sapiens 69-75 31488544-3 2019 Although AIPL1 and PDE6 are known to interact via the FK506-binding protein domain of AIPL1, the contribution of the tetratricopeptide repeat (TPR) domain of AIPL1 to its chaperone function is poorly understood. Tacrolimus 54-59 aryl hydrocarbon receptor interacting protein like 1 Homo sapiens 86-91 31488544-3 2019 Although AIPL1 and PDE6 are known to interact via the FK506-binding protein domain of AIPL1, the contribution of the tetratricopeptide repeat (TPR) domain of AIPL1 to its chaperone function is poorly understood. Tacrolimus 54-59 aryl hydrocarbon receptor interacting protein like 1 Homo sapiens 86-91 31581670-0 2019 A Low Tacrolimus Concentration/Dose Ratio Increases the Risk for the Development of Acute Calcineurin Inhibitor-Induced Nephrotoxicity. Tacrolimus 6-16 calcineurin binding protein 1 Homo sapiens 90-111 31581670-5 2019 A low C/D ratio (C/D ratio < 1.05 ng/mLx1/mg) was linked with higher C2 tacrolimus blood concentrations (19.2 +- 8.7 microg/L vs. 12.2 +- 5.2 microg/L respectively; p = 0.001) and higher degrees of nephrotoxicity despite comparable trough levels (6.3 +- 2.4 microg/L vs. 6.6 +- 2.2 microg/L respectively; p = 0.669). Tacrolimus 72-85 solute carrier family 22 (organic cation transporter), member 1 Mus musculus 40-44 31581670-7 2019 In renal tubular epithelial cells exposed to tacrolimus according to a fast metabolism pharmacokinetic profile it led to reduced viability and increased Fn14 expression. Tacrolimus 45-55 TNF receptor superfamily member 12A Homo sapiens 153-157 31588879-0 2019 Impact of CYP3A4/5 and ABCB1 polymorphisms on tacrolimus exposure and response in pediatric primary nephrotic syndrome. Tacrolimus 46-56 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 10-18 31588879-0 2019 Impact of CYP3A4/5 and ABCB1 polymorphisms on tacrolimus exposure and response in pediatric primary nephrotic syndrome. Tacrolimus 46-56 ATP binding cassette subfamily B member 1 Homo sapiens 23-28 31588879-1 2019 Aim: To evaluate the impact of CYP3A4*1G, CYP3A5*3 and ABCB1-C3435T polymorphisms on tacrolimus concentrations, efficacy and tolerance in pediatric primary nephrotic syndrome. Tacrolimus 85-95 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-37 31588879-6 2019 Conclusion: The genotypes of CYP3A4*1G and CYP3A5*3 rather than ABCB1-C3435T potentially predicted tacrolimus exposure and clinical response in pediatric primary nephrotic syndrome. Tacrolimus 99-109 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 29-35 31588879-6 2019 Conclusion: The genotypes of CYP3A4*1G and CYP3A5*3 rather than ABCB1-C3435T potentially predicted tacrolimus exposure and clinical response in pediatric primary nephrotic syndrome. Tacrolimus 99-109 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 43-49 31447189-2 2019 The aim of this study is to analyze the role of mTOR inhibitor add-on in tacrolimus-based kidney transplant recipients. Tacrolimus 73-83 mechanistic target of rapamycin kinase Homo sapiens 48-52 31447189-11 2019 CONCLUSIONS: In our preliminary result, mTOR inhibitor add-on in patients with tacrolimus-based regimen revealed less post-KT UC occurrence. Tacrolimus 79-89 mechanistic target of rapamycin kinase Homo sapiens 40-44 31922058-0 2020 Melding Pharmacogenomic Effect of MDR1 and CYP3A5 Gene Polymorphism on Tacrolimus Dosing in Renal Transplant Recipients in Northern India. Tacrolimus 71-81 ATP binding cassette subfamily B member 1 Homo sapiens 34-38 31922058-0 2020 Melding Pharmacogenomic Effect of MDR1 and CYP3A5 Gene Polymorphism on Tacrolimus Dosing in Renal Transplant Recipients in Northern India. Tacrolimus 71-81 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 43-49 31922058-8 2020 We analyzed the blending effect of mutant SNPs of the MDR gene and CYP3A5 for optimized TAC levels. Tacrolimus 88-91 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 67-73 31922058-9 2020 Results: Among CYP3A5 genotypic variants, the dose-adjusted TAC level was significantly lower, and the TAC dose required to achieve the target level was significantly higher, in CYP3A5*1*1 (expressor) than that of CYP3A5*1*3 and CYP3A5*3*3. Tacrolimus 60-63 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 15-21 31922058-9 2020 Results: Among CYP3A5 genotypic variants, the dose-adjusted TAC level was significantly lower, and the TAC dose required to achieve the target level was significantly higher, in CYP3A5*1*1 (expressor) than that of CYP3A5*1*3 and CYP3A5*3*3. Tacrolimus 60-63 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 178-184 31922058-9 2020 Results: Among CYP3A5 genotypic variants, the dose-adjusted TAC level was significantly lower, and the TAC dose required to achieve the target level was significantly higher, in CYP3A5*1*1 (expressor) than that of CYP3A5*1*3 and CYP3A5*3*3. Tacrolimus 60-63 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 178-184 31922058-9 2020 Results: Among CYP3A5 genotypic variants, the dose-adjusted TAC level was significantly lower, and the TAC dose required to achieve the target level was significantly higher, in CYP3A5*1*1 (expressor) than that of CYP3A5*1*3 and CYP3A5*3*3. Tacrolimus 60-63 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 178-184 31922058-9 2020 Results: Among CYP3A5 genotypic variants, the dose-adjusted TAC level was significantly lower, and the TAC dose required to achieve the target level was significantly higher, in CYP3A5*1*1 (expressor) than that of CYP3A5*1*3 and CYP3A5*3*3. Tacrolimus 103-106 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 15-21 31922058-9 2020 Results: Among CYP3A5 genotypic variants, the dose-adjusted TAC level was significantly lower, and the TAC dose required to achieve the target level was significantly higher, in CYP3A5*1*1 (expressor) than that of CYP3A5*1*3 and CYP3A5*3*3. Tacrolimus 103-106 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 178-184 31922058-9 2020 Results: Among CYP3A5 genotypic variants, the dose-adjusted TAC level was significantly lower, and the TAC dose required to achieve the target level was significantly higher, in CYP3A5*1*1 (expressor) than that of CYP3A5*1*3 and CYP3A5*3*3. Tacrolimus 103-106 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 178-184 31922058-9 2020 Results: Among CYP3A5 genotypic variants, the dose-adjusted TAC level was significantly lower, and the TAC dose required to achieve the target level was significantly higher, in CYP3A5*1*1 (expressor) than that of CYP3A5*1*3 and CYP3A5*3*3. Tacrolimus 103-106 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 178-184 31922058-10 2020 Of the MDR1 gene SNPs, only the G2677T/A homozygous mutant was significantly associated with TAC level, and it was strongly correlated with P-gp expression.The daily TAC dose requirement was highest with a combination of CYP3A5*1*1 and homozygous mutant TT+AA genotype of G2677T/A, and was lowest with CYP3A5*3*3 and wild-type GG of the G2677T/A genotype. Tacrolimus 166-169 ATP binding cassette subfamily B member 1 Homo sapiens 7-11 31922058-10 2020 Of the MDR1 gene SNPs, only the G2677T/A homozygous mutant was significantly associated with TAC level, and it was strongly correlated with P-gp expression.The daily TAC dose requirement was highest with a combination of CYP3A5*1*1 and homozygous mutant TT+AA genotype of G2677T/A, and was lowest with CYP3A5*3*3 and wild-type GG of the G2677T/A genotype. Tacrolimus 166-169 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 221-227 31922058-10 2020 Of the MDR1 gene SNPs, only the G2677T/A homozygous mutant was significantly associated with TAC level, and it was strongly correlated with P-gp expression.The daily TAC dose requirement was highest with a combination of CYP3A5*1*1 and homozygous mutant TT+AA genotype of G2677T/A, and was lowest with CYP3A5*3*3 and wild-type GG of the G2677T/A genotype. Tacrolimus 166-169 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 302-308 31922058-11 2020 Conclusion: Both CYP gene and MDR1 gene polymorphism affect TAC dose requirements, and there is a need to look for both in an individual to achieve the target trough concentration. Tacrolimus 60-63 peptidylprolyl isomerase G Homo sapiens 17-20 31922058-11 2020 Conclusion: Both CYP gene and MDR1 gene polymorphism affect TAC dose requirements, and there is a need to look for both in an individual to achieve the target trough concentration. Tacrolimus 60-63 ATP binding cassette subfamily B member 1 Homo sapiens 30-34 31616470-0 2019 The Impact of CYP3A4*22 on Tacrolimus Pharmacokinetics and Outcome in Clinical Practice at a Single Kidney Transplant Center. Tacrolimus 27-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-20 31616470-1 2019 Background: Although there is evidence that the CYP3A4*22 variant should be considered in tacrolimus dosing in renal transplantation, its impact beyond tacrolimus dose requirements remains controversial. Tacrolimus 90-100 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 48-54 31616470-12 2019 Conclusion: At our transplantation center, both CYP3A5*3 and, to a lesser extent, CYP3A4*22 affect tacrolimus pharmacokinetics early after onset of therapy with consequences for steady-state treatment in routine clinical practice. Tacrolimus 99-109 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 48-54 31616470-12 2019 Conclusion: At our transplantation center, both CYP3A5*3 and, to a lesser extent, CYP3A4*22 affect tacrolimus pharmacokinetics early after onset of therapy with consequences for steady-state treatment in routine clinical practice. Tacrolimus 99-109 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 82-88 31583120-0 2019 The splicing FK506-binding protein-51 isoform plays a role in glioblastoma resistance through programmed cell death ligand-1 expression regulation. Tacrolimus 13-18 CD274 antigen Mus musculus 94-124 31469511-7 2019 In an in vitro model of tacrolimus-mediated fibrogenesis by tubular cells, we found that tacrolimus treatment significantly induced mRNA and protein expression of CB1 concomitantly to col3a1 and col4a3 up regulation. Tacrolimus 24-34 collagen type III alpha 1 chain Homo sapiens 184-190 31469511-7 2019 In an in vitro model of tacrolimus-mediated fibrogenesis by tubular cells, we found that tacrolimus treatment significantly induced mRNA and protein expression of CB1 concomitantly to col3a1 and col4a3 up regulation. Tacrolimus 24-34 collagen type IV alpha 3 chain Homo sapiens 195-201 31469511-7 2019 In an in vitro model of tacrolimus-mediated fibrogenesis by tubular cells, we found that tacrolimus treatment significantly induced mRNA and protein expression of CB1 concomitantly to col3a1 and col4a3 up regulation. Tacrolimus 89-99 cannabinoid receptor 1 Homo sapiens 163-166 31469511-7 2019 In an in vitro model of tacrolimus-mediated fibrogenesis by tubular cells, we found that tacrolimus treatment significantly induced mRNA and protein expression of CB1 concomitantly to col3a1 and col4a3 up regulation. Tacrolimus 89-99 collagen type III alpha 1 chain Homo sapiens 184-190 31469511-7 2019 In an in vitro model of tacrolimus-mediated fibrogenesis by tubular cells, we found that tacrolimus treatment significantly induced mRNA and protein expression of CB1 concomitantly to col3a1 and col4a3 up regulation. Tacrolimus 89-99 collagen type IV alpha 3 chain Homo sapiens 195-201 31471736-0 2019 Successful Treatment of PAPA Syndrome with Dual Adalimumab and Tacrolimus Therapy. Tacrolimus 63-73 pappalysin 1 Homo sapiens 24-28 31483851-0 2019 Retraction: Novel Single Nucleotide Polymorphisms in Interleukin 6 Affect Tacrolimus Metabolism in Liver Transplant Patients. Tacrolimus 74-84 interleukin 6 Homo sapiens 53-66 31572289-11 2019 Besides, FK506 also significantly reduced the levels of factors involved in inflammatory response such as vascular cell adhesion molecule-1 (VCAM-1), intercellular adhesion molecule-1 (ICAM-1), tumor necrosis factor-alpha (TNF-alpha), and Protein Kinase C delta (PKCdelta) that rise after epilepsy. Tacrolimus 9-14 vascular cell adhesion molecule 1 Rattus norvegicus 106-139 31572289-11 2019 Besides, FK506 also significantly reduced the levels of factors involved in inflammatory response such as vascular cell adhesion molecule-1 (VCAM-1), intercellular adhesion molecule-1 (ICAM-1), tumor necrosis factor-alpha (TNF-alpha), and Protein Kinase C delta (PKCdelta) that rise after epilepsy. Tacrolimus 9-14 vascular cell adhesion molecule 1 Rattus norvegicus 141-147 31572289-11 2019 Besides, FK506 also significantly reduced the levels of factors involved in inflammatory response such as vascular cell adhesion molecule-1 (VCAM-1), intercellular adhesion molecule-1 (ICAM-1), tumor necrosis factor-alpha (TNF-alpha), and Protein Kinase C delta (PKCdelta) that rise after epilepsy. Tacrolimus 9-14 intercellular adhesion molecule 1 Rattus norvegicus 150-183 31572289-11 2019 Besides, FK506 also significantly reduced the levels of factors involved in inflammatory response such as vascular cell adhesion molecule-1 (VCAM-1), intercellular adhesion molecule-1 (ICAM-1), tumor necrosis factor-alpha (TNF-alpha), and Protein Kinase C delta (PKCdelta) that rise after epilepsy. Tacrolimus 9-14 intercellular adhesion molecule 1 Rattus norvegicus 185-191 31572289-11 2019 Besides, FK506 also significantly reduced the levels of factors involved in inflammatory response such as vascular cell adhesion molecule-1 (VCAM-1), intercellular adhesion molecule-1 (ICAM-1), tumor necrosis factor-alpha (TNF-alpha), and Protein Kinase C delta (PKCdelta) that rise after epilepsy. Tacrolimus 9-14 tumor necrosis factor Rattus norvegicus 194-221 31572289-11 2019 Besides, FK506 also significantly reduced the levels of factors involved in inflammatory response such as vascular cell adhesion molecule-1 (VCAM-1), intercellular adhesion molecule-1 (ICAM-1), tumor necrosis factor-alpha (TNF-alpha), and Protein Kinase C delta (PKCdelta) that rise after epilepsy. Tacrolimus 9-14 tumor necrosis factor Rattus norvegicus 223-232 31572289-11 2019 Besides, FK506 also significantly reduced the levels of factors involved in inflammatory response such as vascular cell adhesion molecule-1 (VCAM-1), intercellular adhesion molecule-1 (ICAM-1), tumor necrosis factor-alpha (TNF-alpha), and Protein Kinase C delta (PKCdelta) that rise after epilepsy. Tacrolimus 9-14 protein kinase C, delta Rattus norvegicus 239-261 31572289-11 2019 Besides, FK506 also significantly reduced the levels of factors involved in inflammatory response such as vascular cell adhesion molecule-1 (VCAM-1), intercellular adhesion molecule-1 (ICAM-1), tumor necrosis factor-alpha (TNF-alpha), and Protein Kinase C delta (PKCdelta) that rise after epilepsy. Tacrolimus 9-14 protein kinase C, delta Rattus norvegicus 263-271 31490997-8 2019 Using FKBP51 as a model system, we show that two amino acids lining the FK506-binding site are essential for binding Glmn and that the FKBP51-Glmn interaction is blocked by FKBP ligands. Tacrolimus 72-77 glomulin, FKBP associated protein Homo sapiens 117-121 31490997-8 2019 Using FKBP51 as a model system, we show that two amino acids lining the FK506-binding site are essential for binding Glmn and that the FKBP51-Glmn interaction is blocked by FKBP ligands. Tacrolimus 72-77 glomulin, FKBP associated protein Homo sapiens 142-146 31077425-10 2019 CYP3A5*1/*1 patients who have high risks of DGF should be closely monitored because of an increased risk of DGF and reduced glomerular filtration rate with high tacrolimus doses. Tacrolimus 161-171 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 30597187-0 2019 Sirolimus vs mycophenolate moftile in Tacrolimus based therapy following induction with Antithymocyte globulin promotes regulatory T cell expansion and inhibits RORgammat and T-bet expression in kidney transplantation. Tacrolimus 38-48 T-box transcription factor 21 Homo sapiens 175-180 31219197-4 2019 At 3 months post-transplant modelling revealed an association between tacrolimus Css and recipient CASP1 rs580523 genotype (P = 0.005), accounting for 52% Css variance. Tacrolimus 70-80 caspase 1 Homo sapiens 99-104 31219197-6 2019 As this is the first report of CASP1 genetic variability influencing tacrolimus Css , further validation in larger cohorts is required. Tacrolimus 69-79 caspase 1 Homo sapiens 31-36 30597187-8 2019 Patients who received Tac/MMF had significantly higher CD4+ CD25+ FOXP3+ Treg cells compared to patients who received Tac/SRL. Tacrolimus 22-25 CD4 molecule Homo sapiens 55-58 30597187-8 2019 Patients who received Tac/MMF had significantly higher CD4+ CD25+ FOXP3+ Treg cells compared to patients who received Tac/SRL. Tacrolimus 22-25 forkhead box P3 Homo sapiens 66-71 30597187-10 2019 FOXP3 mRNA levels in the patients who received Tac/MMF were increased 4 months after transplantation and the expression was significantly higher than patients who received Tac/SRL. Tacrolimus 47-50 forkhead box P3 Homo sapiens 0-5 31531197-0 2019 One-step Heck Reaction Generates Nonimmunosuppressive FK506 Analogs for Pharmacological BMP Activation. Tacrolimus 54-59 bone morphogenetic protein 1 Homo sapiens 88-91 31102573-11 2019 In conclusion, donor CYP3A5 genotype, time after transplant, and ALT values are associated with tacrolimus disposition between 1 month and 2 years after transplant. Tacrolimus 96-106 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 21-27 31402251-0 2019 Insulin Resistance in Nonobese Renal Allograft Recipients on Maintenance Doses of Cyclosporine or Tacrolimus. Tacrolimus 98-108 insulin Homo sapiens 0-7 31454358-0 2019 Retraction: Association of MDR1 Gene SNPs and Haplotypes with the Tacrolimus Dose Requirements in Han Chinese Liver Transplant Recipients. Tacrolimus 66-76 ATP binding cassette subfamily B member 1 Homo sapiens 27-31 31321978-2 2019 Seven new FK506 analogues modified at both the FK506-binding protein 12- and the calcineurin-binding regions were biosynthesized. Tacrolimus 10-15 FKBP prolyl isomerase 1A Homo sapiens 47-71 31321978-7 2019 In humans, FK506 binds to FK506-binding protein (FKBP) 12, and the resulting FKBP12-FK506 complex interacts with a Ca2+-calmodulin-dependent phosphatase, calcineurin (CaN). Tacrolimus 11-16 FKBP prolyl isomerase 1A Homo sapiens 26-57 31321978-7 2019 In humans, FK506 binds to FK506-binding protein (FKBP) 12, and the resulting FKBP12-FK506 complex interacts with a Ca2+-calmodulin-dependent phosphatase, calcineurin (CaN). Tacrolimus 11-16 FKBP prolyl isomerase 1A Homo sapiens 77-83 31321978-7 2019 In humans, FK506 binds to FK506-binding protein (FKBP) 12, and the resulting FKBP12-FK506 complex interacts with a Ca2+-calmodulin-dependent phosphatase, calcineurin (CaN). Tacrolimus 26-31 FKBP prolyl isomerase 1A Homo sapiens 77-83 31321978-8 2019 Inactivation of CaN by forming the FKBP12-FK506-CaN ternary complex prevents the activation of nuclear factor of activated T cells (NF-AT), inhibiting the production of interleukin-2 and subsequent T-cell proliferation. Tacrolimus 42-47 FKBP prolyl isomerase 1A Homo sapiens 35-41 31321978-8 2019 Inactivation of CaN by forming the FKBP12-FK506-CaN ternary complex prevents the activation of nuclear factor of activated T cells (NF-AT), inhibiting the production of interleukin-2 and subsequent T-cell proliferation. Tacrolimus 42-47 interleukin 2 Homo sapiens 169-182 31321978-10 2019 Therefore, the synthesis of FK506 analogues that can discriminate human FKBP12/CaN from its fungal counterparts may separate antifungal activity from the immunosuppressive activity, thereby allowing the development of a novel antifungal agent. Tacrolimus 28-33 FKBP prolyl isomerase 1A Homo sapiens 72-78 31531197-1 2019 FKBP12 ligands such as FK506 have been shown to activate the BMP signaling pathway and facilitate tissue regeneration. Tacrolimus 23-28 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 0-6 31531197-1 2019 FKBP12 ligands such as FK506 have been shown to activate the BMP signaling pathway and facilitate tissue regeneration. Tacrolimus 23-28 bone morphogenetic protein 1 Homo sapiens 61-64 31409869-0 2019 Model based development of tacrolimus dosing algorithm considering CYP3A5 genotypes and mycophenolate mofetil drug interaction in stable kidney transplant recipients. Tacrolimus 27-37 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 67-73 31190414-3 2019 Tac is metabolized in the liver and intestine by the cytochrome P450 3A (CYP3A) isoforms CYP3A4 and CYP3A5. Tacrolimus 0-3 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-71 31400753-0 2019 Ginseng increases Klotho expression by FoxO3-mediated manganese superoxide dismutase in a mouse model of tacrolimus-induced renal injury. Tacrolimus 105-115 klotho Mus musculus 18-24 31400753-0 2019 Ginseng increases Klotho expression by FoxO3-mediated manganese superoxide dismutase in a mouse model of tacrolimus-induced renal injury. Tacrolimus 105-115 forkhead box O3 Mus musculus 39-44 31400753-3 2019 Although tacrolimus treatment reduced Klotho level in the serum and kidney, ginseng treatment was found to reverse the levels. Tacrolimus 9-19 klotho Mus musculus 38-44 31400753-5 2019 Effect of ginseng on Klotho-induced manganese superoxide dismutase signaling pathway during tacrolimus treatment in mice revealed that ginseng suppressed phosphatidylinositol 3-kinase/serine-threonine kinase Akt-mediated phosphorylation of forkhead box protein O3a and promoted the binding of forkhead box protein O3a to manganese superoxide dismutase promoter. Tacrolimus 92-102 klotho Mus musculus 21-27 31400753-7 2019 These findings together suggested that ginseng attenuated tacrolimus-induced oxidative stress via signaling between Klotho and the phosphatidylinositol 3-kinase/serine-threonine kinase Akt/forkhead box protein O3a-related antioxidant pathway. Tacrolimus 58-68 klotho Mus musculus 116-122 31490380-0 2019 Tacrolimus-induced diabetic ketoacidosis with subsequent rapid recovery of endogenous insulin secretion after cessation of tacrolimus: A case report with review of literature. Tacrolimus 0-10 insulin Homo sapiens 86-93 31490380-1 2019 RATIONALE: Immunosuppressive agents such as tacrolimus (TAC) and cyclosporin might cause glycemic disorders by suppressing insulin production. Tacrolimus 44-54 insulin Homo sapiens 123-130 31190414-3 2019 Tac is metabolized in the liver and intestine by the cytochrome P450 3A (CYP3A) isoforms CYP3A4 and CYP3A5. Tacrolimus 0-3 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 73-78 31190414-3 2019 Tac is metabolized in the liver and intestine by the cytochrome P450 3A (CYP3A) isoforms CYP3A4 and CYP3A5. Tacrolimus 0-3 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-95 31190414-3 2019 Tac is metabolized in the liver and intestine by the cytochrome P450 3A (CYP3A) isoforms CYP3A4 and CYP3A5. Tacrolimus 0-3 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 100-106 31087501-0 2019 A Minimal Physiologically-Based Pharmacokinetic Model for Tacrolimus in Living-Donor Liver Transplantation: Perspectives Related to Liver Regeneration and the cytochrome P450 3A5 (CYP3A5) Genotype. Tacrolimus 58-68 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 180-186 31087501-1 2019 In adult patients after living-donor liver transplantation, postoperative days and the cytochrome P450 3A5 (CYP3A5) genotype are known to affect tacrolimus pharmacokinetics. Tacrolimus 145-155 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 87-106 31087501-1 2019 In adult patients after living-donor liver transplantation, postoperative days and the cytochrome P450 3A5 (CYP3A5) genotype are known to affect tacrolimus pharmacokinetics. Tacrolimus 145-155 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 108-114 31087501-2 2019 In this study, we constructed a physiologically-based pharmacokinetic model adapted to the clinical data and evaluated the contribution of liver regeneration as well as hepatic and intestine CYP3A5 genotypes on tacrolimus pharmacokinetics. Tacrolimus 211-221 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 191-197 31087501-5 2019 In conclusion, the constructed physiologically-based pharmacokinetic model clarified that the oral clearance of tacrolimus was affected by the CYP3A5 genotypes in both the liver and intestine to the same extent. Tacrolimus 112-122 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 143-149 30883749-1 2019 Tacrolimus (TAC) acts as an inhibitor of calcineurin, which inhibits the production of interleukin-2. Tacrolimus 0-10 interleukin 2 Homo sapiens 87-100 30471066-3 2019 Although cytochrome P450 (CYP) 3A5 and multi-drug resistance 1 (MDR1) polymorphisms influence tacrolimus concentrations, it is unknown if these impact on conversion. Tacrolimus 94-104 ATP binding cassette subfamily B member 1 Homo sapiens 39-62 30471066-3 2019 Although cytochrome P450 (CYP) 3A5 and multi-drug resistance 1 (MDR1) polymorphisms influence tacrolimus concentrations, it is unknown if these impact on conversion. Tacrolimus 94-104 ATP binding cassette subfamily B member 1 Homo sapiens 64-68 30471066-9 2019 A decrease in tacrolimus exposure (median 21%) was only evident among CYP3A5 expressors [227 (172-366) vs. 180 (104-347) ng h/mL, p = 0.014, n = 18], not among non-expressors [215 (197-290) vs. 217 (129-281) ng h/mL, p = 0.263, n = 8]. Tacrolimus 14-24 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 70-76 30471066-12 2019 CONCLUSION: The high prevalence of CYP3A5 polymorphism among Asians may lead to a significant reduction in tacrolimus exposure with 1:1 dose conversion of Prograf to Advagraf . Tacrolimus 107-117 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 35-41 30883749-1 2019 Tacrolimus (TAC) acts as an inhibitor of calcineurin, which inhibits the production of interleukin-2. Tacrolimus 12-15 interleukin 2 Homo sapiens 87-100 31201087-13 2019 There was an inverse relationship between FLT3 expression and tacrolimus levels (-0.029 and -0.176, respectively) in Caucasians and AAs. Tacrolimus 62-72 fms related receptor tyrosine kinase 3 Homo sapiens 42-46 31124575-0 2019 CYP3A5 genotype affects time to therapeutic tacrolimus level in pediatric kidney transplant recipients. Tacrolimus 44-54 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 31201731-0 2019 Influence of Tacrolimus on Depressive-Like Behavior in Diabetic Rats Through Brain-Derived Neurotrophic Factor Regulation in the Hippocampus. Tacrolimus 13-23 brain-derived neurotrophic factor Rattus norvegicus 77-110 31201731-2 2019 The aim of the present study was to investigate the influence of tacrolimus on brain-derived neurotrophic factor (BDNF), the critical protein for maintenance of neuronal functions, in the hippocampus in a diabetic condition. Tacrolimus 65-75 brain-derived neurotrophic factor Rattus norvegicus 79-112 31201731-2 2019 The aim of the present study was to investigate the influence of tacrolimus on brain-derived neurotrophic factor (BDNF), the critical protein for maintenance of neuronal functions, in the hippocampus in a diabetic condition. Tacrolimus 65-75 brain-derived neurotrophic factor Rattus norvegicus 114-118 31201731-6 2019 There was a significant decrease of BDNF expression in the DG and CA3 region in tacrolimus-treated and diabetic rats compared with that of the control group injected with vehicle only. Tacrolimus 80-90 brain-derived neurotrophic factor Rattus norvegicus 36-40 31201731-6 2019 There was a significant decrease of BDNF expression in the DG and CA3 region in tacrolimus-treated and diabetic rats compared with that of the control group injected with vehicle only. Tacrolimus 80-90 carbonic anhydrase 3 Rattus norvegicus 66-69 31201731-8 2019 Tacrolimus treatment in diabetic rats further decreased the BDNF expression level in the DG and CA3 region. Tacrolimus 0-10 brain-derived neurotrophic factor Rattus norvegicus 60-64 31201731-8 2019 Tacrolimus treatment in diabetic rats further decreased the BDNF expression level in the DG and CA3 region. Tacrolimus 0-10 carbonic anhydrase 3 Rattus norvegicus 96-99 31201731-9 2019 Interestingly, mossy fiber sprouting, demonstrated by prominent punctate immunolabeling of BDNF with synaptoporin, was observed in the diabetic group treated with tacrolimus, which localized at the stratum oriens of the CA3 region. Tacrolimus 163-173 brain-derived neurotrophic factor Rattus norvegicus 91-95 31201731-9 2019 Interestingly, mossy fiber sprouting, demonstrated by prominent punctate immunolabeling of BDNF with synaptoporin, was observed in the diabetic group treated with tacrolimus, which localized at the stratum oriens of the CA3 region. Tacrolimus 163-173 carbonic anhydrase 3 Rattus norvegicus 220-223 31201731-10 2019 These data suggest that tacrolimus treatment or a diabetic condition decreases BDNF expression in the hippocampus, and that tacrolimus treatment in the diabetic condition further injures the CA3 region of the hippocampus. Tacrolimus 24-34 brain-derived neurotrophic factor Rattus norvegicus 79-83 31201731-10 2019 These data suggest that tacrolimus treatment or a diabetic condition decreases BDNF expression in the hippocampus, and that tacrolimus treatment in the diabetic condition further injures the CA3 region of the hippocampus. Tacrolimus 124-134 carbonic anhydrase 3 Rattus norvegicus 191-194 31201731-11 2019 In addition to BDNF expression, decreased locomotor activity and evident depressive behavior were observed in tacrolimus-treated diabetic rats. Tacrolimus 110-120 brain-derived neurotrophic factor Rattus norvegicus 15-19 31230376-1 2019 INTRODUCTION: One factor impacting tacrolimus interpatient variability is the presence of CYP3A5 polymorphisms. Tacrolimus 35-45 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 90-96 31467711-3 2019 In this study, we investigated the effective dose and injection time of FK506 as an immunophilin ligand for providing a suitable effect on cells of CA2, CA3, and dentate gyrus of the hippocampus. Tacrolimus 72-77 carbonic anhydrase 2 Rattus norvegicus 148-151 31467711-3 2019 In this study, we investigated the effective dose and injection time of FK506 as an immunophilin ligand for providing a suitable effect on cells of CA2, CA3, and dentate gyrus of the hippocampus. Tacrolimus 72-77 carbonic anhydrase 3 Rattus norvegicus 153-156 30831086-9 2019 Compared with the epilepsy group, the levels of NO, NOS (including nNOS and iNOS), and MDA were obviously decreased by FK506 (P < 0.05). Tacrolimus 119-124 nitric oxide synthase 1 Rattus norvegicus 67-71 30831086-9 2019 Compared with the epilepsy group, the levels of NO, NOS (including nNOS and iNOS), and MDA were obviously decreased by FK506 (P < 0.05). Tacrolimus 119-124 nitric oxide synthase 2 Rattus norvegicus 76-80 30831086-11 2019 Besides, compared with the epilepsy group, FK506 significantly increased the AIF level in the mitochondrial, but decreased that in the nuclear fractions, respectively (P < 0.05). Tacrolimus 43-48 apoptosis inducing factor, mitochondria associated 1 Rattus norvegicus 77-80 31015081-1 2019 We present a case of a 65-year-old African American male, immunosuppressed on Tacrolimus, who initially presented with cerebellar ataxia and rapidly developed Progressive Encephalomyelitis with Rigidity and Myoclonus (PERM) with positive anti-glutamic acid decarboxylase (GAD65) antibodies, no underlying malignancy, and normal neuroimaging. Tacrolimus 78-88 glutamate decarboxylase 1 Homo sapiens 238-270 31015081-1 2019 We present a case of a 65-year-old African American male, immunosuppressed on Tacrolimus, who initially presented with cerebellar ataxia and rapidly developed Progressive Encephalomyelitis with Rigidity and Myoclonus (PERM) with positive anti-glutamic acid decarboxylase (GAD65) antibodies, no underlying malignancy, and normal neuroimaging. Tacrolimus 78-88 glutamate decarboxylase 2 Homo sapiens 272-277 30887101-6 2019 A knockout of the D-lactate dehydrogenase gene, combined with the overexpression of tryptophane synthase and aspartate 1-decarboxylase genes, led to a 29.8% enhancement of tacrolimus production compared to the parent strain. Tacrolimus 172-182 lactate dehydrogenase D Homo sapiens 18-41 30887101-6 2019 A knockout of the D-lactate dehydrogenase gene, combined with the overexpression of tryptophane synthase and aspartate 1-decarboxylase genes, led to a 29.8% enhancement of tacrolimus production compared to the parent strain. Tacrolimus 172-182 glutamate decarboxylase like 1 Homo sapiens 109-134 31077643-11 2019 The patients with the homozygous CYP3A5*3 had the higher blood tacrolimus concentration, while CYP3A5*3 allele was not associated with the serum levels of 4beta-OHC and 25-OHD. Tacrolimus 63-73 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 33-39 31124575-2 2019 Tacrolimus (TAC) dose requirements are significantly impacted by genetic variation in CYP3A5 polymorphisms, however the impact that genotype has on clinical outcomes in the pediatric kidney transplant population remains unclear. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 86-92 31087207-0 2019 Axonal Protection by Tacrolimus with Inhibition of NFATc1 in TNF-Induced Optic Nerve Degeneration. Tacrolimus 21-31 tumor necrosis factor Homo sapiens 61-64 31423060-0 2019 Influence of CYP3A5 and ABCB1 Polymorphism on Tacrolimus Drug Dosing in South Indian Renal Allograft Recipients. Tacrolimus 46-56 ATP binding cassette subfamily B member 1 Homo sapiens 24-29 31423060-1 2019 Introduction: Tacrolimus blood levels are influenced by polymorphisms involving Cytochrome 3A subfamily (CYP3A5) and P-Glycoprotein (ABCB-1) genes. Tacrolimus 14-24 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 105-111 31423060-1 2019 Introduction: Tacrolimus blood levels are influenced by polymorphisms involving Cytochrome 3A subfamily (CYP3A5) and P-Glycoprotein (ABCB-1) genes. Tacrolimus 14-24 ATP binding cassette subfamily B member 1 Homo sapiens 117-131 31423060-1 2019 Introduction: Tacrolimus blood levels are influenced by polymorphisms involving Cytochrome 3A subfamily (CYP3A5) and P-Glycoprotein (ABCB-1) genes. Tacrolimus 14-24 ATP binding cassette subfamily B member 1 Homo sapiens 133-139 31423060-4 2019 Methods: An analysis of CYP3A5, ABCB1 genotype done in 101 renal transplant recipients by polymerase chain reaction was correlated with blood tacrolimus trough levels (CLIA method), weight, concentration/dose (L/D) ratio, incidence of biopsy proven early acute rejections, and tacrolimus toxicity. Tacrolimus 142-152 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 24-30 31423060-4 2019 Methods: An analysis of CYP3A5, ABCB1 genotype done in 101 renal transplant recipients by polymerase chain reaction was correlated with blood tacrolimus trough levels (CLIA method), weight, concentration/dose (L/D) ratio, incidence of biopsy proven early acute rejections, and tacrolimus toxicity. Tacrolimus 142-152 ATP binding cassette subfamily B member 1 Homo sapiens 32-37 31423060-4 2019 Methods: An analysis of CYP3A5, ABCB1 genotype done in 101 renal transplant recipients by polymerase chain reaction was correlated with blood tacrolimus trough levels (CLIA method), weight, concentration/dose (L/D) ratio, incidence of biopsy proven early acute rejections, and tacrolimus toxicity. Tacrolimus 277-287 ATP binding cassette subfamily B member 1 Homo sapiens 32-37 31423060-8 2019 Incidence of early acute rejections (30% vs. 9.76%; P 0.016) and tacrolimus-related toxicity (14.6% vs. 5%; P 0.039) were significantly higher in CYP3A5 expressers and nonexpressers, respectively. Tacrolimus 65-75 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 146-152 31423060-11 2019 Conclusions: CYP3A5 polymorphisms correlated with tacrolimus dose requirements and blood levels, incidence of early acute rejection, and tacrolimus nephrotoxicity. Tacrolimus 50-60 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 13-19 31423060-11 2019 Conclusions: CYP3A5 polymorphisms correlated with tacrolimus dose requirements and blood levels, incidence of early acute rejection, and tacrolimus nephrotoxicity. Tacrolimus 137-147 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 13-19 31423060-12 2019 CYP3A5 polymorphism analysis prior to renal transplant will aid more precise early tacrolimus dose calculation to balance between rejection and toxicity. Tacrolimus 83-93 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 31087207-7 2019 A significant increase in TNF protein level was observed in optic nerve 14 days after TNF injection and this increase was prevented by tacrolimus. Tacrolimus 135-145 tumor necrosis factor Homo sapiens 26-29 31087207-7 2019 A significant increase in TNF protein level was observed in optic nerve 14 days after TNF injection and this increase was prevented by tacrolimus. Tacrolimus 135-145 tumor necrosis factor Homo sapiens 86-89 30124124-0 2019 Tacrolimus for the treatment of immune-related adverse effects refractory to systemic steroids and anti-tumor necrosis factor alpha therapy. Tacrolimus 0-10 tumor necrosis factor Homo sapiens 104-131 31087207-10 2019 Treatment of tacrolimus significantly ameliorated the TNF-mediated axonal loss. Tacrolimus 13-23 tumor necrosis factor Homo sapiens 54-57 31087207-11 2019 These results suggest that tacrolimus is neuroprotective against axon loss in TNF-induced optic neuropathy and that the effect arises from suppression of the CaN/NFATc1 pathway. Tacrolimus 27-37 tumor necrosis factor Homo sapiens 78-81 30124124-7 2019 Presented here are three patient cases supporting the use of the calcinuerin inhibitor tacrolimus to treat immune-related adverse effects refractory to corticosteroids and anti-tumor necrosis factor alpha. Tacrolimus 87-97 tumor necrosis factor Homo sapiens 177-204 31087207-11 2019 These results suggest that tacrolimus is neuroprotective against axon loss in TNF-induced optic neuropathy and that the effect arises from suppression of the CaN/NFATc1 pathway. Tacrolimus 27-37 nuclear factor of activated T cells 1 Homo sapiens 162-168 31261624-15 2019 In conclusion, GLP-1R could be implemented for recipients while closely monitoring their tacrolimus levels and any potential side effects. Tacrolimus 89-99 glucagon like peptide 1 receptor Homo sapiens 15-21 30058048-0 2019 Drug-metabolizing enzymes CYP3A as a link between tacrolimus and vitamin D in renal transplant recipients: is it relevant in clinical practice? Tacrolimus 50-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 26-31 30058048-1 2019 CYP3A enzymes are involved in the metabolism of calcineurin inhibitor tacrolimus as well as vitamin D. Tacrolimus 70-80 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-5 30058048-2 2019 In this review, we summarize the clinical aspects of CYP3A-mediated metabolism of tacrolimus and vitamin D with emphasis on the influence of single-nucleotide polymorphisms on tacrolimus disposition. Tacrolimus 82-92 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-58 30058048-2 2019 In this review, we summarize the clinical aspects of CYP3A-mediated metabolism of tacrolimus and vitamin D with emphasis on the influence of single-nucleotide polymorphisms on tacrolimus disposition. Tacrolimus 176-186 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-58 31005256-6 2019 Inhibition of calcineurin with cyclosporine A, FK506 down-regulates the levels of NFATc3 nuclear translocation and proinflammatory cytokines expression. Tacrolimus 47-52 nuclear factor of activated T cells 3 Homo sapiens 82-88 31242630-2 2019 The urinary neutrophil gelatinase-associated lipocalin (NGAL) level has been linked to tacrolimus-induced AKI in patients starting tacrolimus treatment the morning after liver transplantation. Tacrolimus 87-97 lipocalin 2 Homo sapiens 12-54 31242630-2 2019 The urinary neutrophil gelatinase-associated lipocalin (NGAL) level has been linked to tacrolimus-induced AKI in patients starting tacrolimus treatment the morning after liver transplantation. Tacrolimus 87-97 lipocalin 2 Homo sapiens 56-60 31242630-2 2019 The urinary neutrophil gelatinase-associated lipocalin (NGAL) level has been linked to tacrolimus-induced AKI in patients starting tacrolimus treatment the morning after liver transplantation. Tacrolimus 131-141 lipocalin 2 Homo sapiens 12-54 31242630-2 2019 The urinary neutrophil gelatinase-associated lipocalin (NGAL) level has been linked to tacrolimus-induced AKI in patients starting tacrolimus treatment the morning after liver transplantation. Tacrolimus 131-141 lipocalin 2 Homo sapiens 56-60 31242630-6 2019 HE4 levels after tacrolimus administration were significantly higher in patients who developed AKI (n = 6) than in those who did not (n = 20), whereas NGAL, MCP-1, and L-FABP levels did not differ significantly before or after tacrolimus administration. Tacrolimus 17-27 WAP four-disulfide core domain 2 Homo sapiens 0-3 31181889-2 2019 We have utilized a gene delivery vector containing inducible caspase 9 (iCasp9) gene, which is a synthetic analogue based on the mammalian caspase 9 and fused to a human FK506 binding protein that allows its conditional dimerization to a synthetic, small molecule [chemical inducer of dimerization, AP20187] and results in target cell apoptosis. Tacrolimus 170-175 caspase 9 Homo sapiens 61-70 31200653-11 2019 CL treatment decreased apoptotic cell death (decreased TUNEL-positive cells and reduced expression of active caspase-3) in TAC-treated kidney. Tacrolimus 123-126 caspase 3 Homo sapiens 109-118 30565852-3 2019 Herein we show that recipient C3aR1 deficiency or pharmacological C3aR1 blockade synergizes with tacrolimus to significantly prolong allograft survival versus tacrolimus-treated controls (median survival time 21 vs. 14 days, P < .05). Tacrolimus 159-169 complement component 3a receptor 1 Mus musculus 30-35 30565852-3 2019 Herein we show that recipient C3aR1 deficiency or pharmacological C3aR1 blockade synergizes with tacrolimus to significantly prolong allograft survival versus tacrolimus-treated controls (median survival time 21 vs. 14 days, P < .05). Tacrolimus 159-169 complement component 3a receptor 1 Mus musculus 66-71 31355232-11 2019 Besides, the expression levels of Runx2 and Osterix were up-regulated, and that of PPAR-gamma and C/EBP-alpha were down-regulated in diabetic rats after FK506 treatment. Tacrolimus 153-158 RUNX family transcription factor 2 Rattus norvegicus 34-39 31355232-11 2019 Besides, the expression levels of Runx2 and Osterix were up-regulated, and that of PPAR-gamma and C/EBP-alpha were down-regulated in diabetic rats after FK506 treatment. Tacrolimus 153-158 Sp7 transcription factor Rattus norvegicus 44-51 31355232-11 2019 Besides, the expression levels of Runx2 and Osterix were up-regulated, and that of PPAR-gamma and C/EBP-alpha were down-regulated in diabetic rats after FK506 treatment. Tacrolimus 153-158 peroxisome proliferator-activated receptor gamma Rattus norvegicus 83-93 31355232-11 2019 Besides, the expression levels of Runx2 and Osterix were up-regulated, and that of PPAR-gamma and C/EBP-alpha were down-regulated in diabetic rats after FK506 treatment. Tacrolimus 153-158 CCAAT/enhancer binding protein alpha Rattus norvegicus 98-109 31355232-12 2019 In addition, the nuclear translocation of beta-catenin protein levels were increased in diabetic rats after the treatment of FK506. Tacrolimus 125-130 catenin beta 1 Rattus norvegicus 42-54 30729267-0 2019 IL-2 gene polymorphisms affect tacrolimus response in myasthenia gravis. Tacrolimus 31-41 interleukin 2 Homo sapiens 0-4 30729267-2 2019 However, there are no published studies examining the influence of the IL-2 gene polymorphisms on the response of myasthenia gravis (MG) patients to tacrolimus (Tac). Tacrolimus 149-159 interleukin 2 Homo sapiens 71-75 30729267-3 2019 The goal of this study was to investigate the relationship between the polymorphisms of IL-2 and Tac response in MG patients. Tacrolimus 97-100 interleukin 2 Homo sapiens 88-92 30729267-10 2019 CONCLUSION: Myasthenia gravis patients with the rs2069762 variant, rs2069762 G/T and G/G genotype, and TAGG haplotype for IL-2 tended to respond poorly to Tac treatment. Tacrolimus 155-158 interleukin 2 Homo sapiens 122-126 29025381-5 2019 Simultaneously, the patient had very low absolute total lymphocyte count of 70 cells/muL during which he received supratherapeutic tacrolimus at whole blood trough levels and mycophenolate mofetil. Tacrolimus 131-141 tripartite motif containing 37 Homo sapiens 85-88 30877873-7 2019 Both DHMEQ and tacrolimus suppress DNCB-induced increase of serum total IgE and attenuate expression of inflammatory factors IL-4, IL-6, IL-13, IL-1beta and interferon (IFN)-gamma in the disrupted ear tissues. Tacrolimus 15-25 interleukin 4 Mus musculus 125-129 30633591-5 2019 Results: It is found that percentages of CD3+, CD3+CD4+ and CD3+CD8+ T cells in FK506 group are lowered compared to the control group but they are elevated in FK506 + MMF group. Tacrolimus 80-85 CD4 molecule Homo sapiens 51-54 30633591-5 2019 Results: It is found that percentages of CD3+, CD3+CD4+ and CD3+CD8+ T cells in FK506 group are lowered compared to the control group but they are elevated in FK506 + MMF group. Tacrolimus 80-85 CD8a molecule Homo sapiens 64-67 30633591-5 2019 Results: It is found that percentages of CD3+, CD3+CD4+ and CD3+CD8+ T cells in FK506 group are lowered compared to the control group but they are elevated in FK506 + MMF group. Tacrolimus 159-164 CD8a molecule Homo sapiens 64-67 30633591-6 2019 Amount of CD4+CD25+CD127low/-Treg cells in CD3+ CD4+T cells in FK506 + MMF group was higher than that in FK506 group and control group. Tacrolimus 63-68 CD4 molecule Homo sapiens 10-13 30633591-6 2019 Amount of CD4+CD25+CD127low/-Treg cells in CD3+ CD4+T cells in FK506 + MMF group was higher than that in FK506 group and control group. Tacrolimus 63-68 CD4 molecule Homo sapiens 48-51 30633591-6 2019 Amount of CD4+CD25+CD127low/-Treg cells in CD3+ CD4+T cells in FK506 + MMF group was higher than that in FK506 group and control group. Tacrolimus 105-110 CD4 molecule Homo sapiens 10-13 30633591-6 2019 Amount of CD4+CD25+CD127low/-Treg cells in CD3+ CD4+T cells in FK506 + MMF group was higher than that in FK506 group and control group. Tacrolimus 105-110 CD4 molecule Homo sapiens 48-51 30633591-7 2019 The expressions of co-inhibitory receptors (CTLA-4, PD-1, Tim-3, LAG-3 and TIGIT) on Tregs in FK506 + MMF group were significant higher than those in the FK506 group and control group. Tacrolimus 94-99 cytotoxic T-lymphocyte associated protein 4 Homo sapiens 44-50 30633591-7 2019 The expressions of co-inhibitory receptors (CTLA-4, PD-1, Tim-3, LAG-3 and TIGIT) on Tregs in FK506 + MMF group were significant higher than those in the FK506 group and control group. Tacrolimus 94-99 programmed cell death 1 Homo sapiens 52-56 30633591-7 2019 The expressions of co-inhibitory receptors (CTLA-4, PD-1, Tim-3, LAG-3 and TIGIT) on Tregs in FK506 + MMF group were significant higher than those in the FK506 group and control group. Tacrolimus 94-99 hepatitis A virus cellular receptor 2 Homo sapiens 58-63 30633591-7 2019 The expressions of co-inhibitory receptors (CTLA-4, PD-1, Tim-3, LAG-3 and TIGIT) on Tregs in FK506 + MMF group were significant higher than those in the FK506 group and control group. Tacrolimus 94-99 lymphocyte activating 3 Homo sapiens 65-70 30633591-7 2019 The expressions of co-inhibitory receptors (CTLA-4, PD-1, Tim-3, LAG-3 and TIGIT) on Tregs in FK506 + MMF group were significant higher than those in the FK506 group and control group. Tacrolimus 94-99 T cell immunoreceptor with Ig and ITIM domains Homo sapiens 75-80 30633591-8 2019 The levels of the relative cytokines (TGF-beta and IL-10) in FK506 group are down-regulated compared to the control group. Tacrolimus 61-66 transforming growth factor beta 1 Homo sapiens 38-46 30633591-8 2019 The levels of the relative cytokines (TGF-beta and IL-10) in FK506 group are down-regulated compared to the control group. Tacrolimus 61-66 interleukin 10 Homo sapiens 51-56 30877873-7 2019 Both DHMEQ and tacrolimus suppress DNCB-induced increase of serum total IgE and attenuate expression of inflammatory factors IL-4, IL-6, IL-13, IL-1beta and interferon (IFN)-gamma in the disrupted ear tissues. Tacrolimus 15-25 interleukin 6 Mus musculus 131-135 30849430-2 2019 Tacrolimus and micelles are probed for the first time by this high spatial resolution technique by element-selective excitation in the C 1s- and O 1s-regimes. Tacrolimus 0-10 complement component 1, s subcomponent 1 Mus musculus 135-146 30877873-7 2019 Both DHMEQ and tacrolimus suppress DNCB-induced increase of serum total IgE and attenuate expression of inflammatory factors IL-4, IL-6, IL-13, IL-1beta and interferon (IFN)-gamma in the disrupted ear tissues. Tacrolimus 15-25 interleukin 13 Mus musculus 137-142 30877873-7 2019 Both DHMEQ and tacrolimus suppress DNCB-induced increase of serum total IgE and attenuate expression of inflammatory factors IL-4, IL-6, IL-13, IL-1beta and interferon (IFN)-gamma in the disrupted ear tissues. Tacrolimus 15-25 interleukin 1 alpha Mus musculus 144-152 30877873-7 2019 Both DHMEQ and tacrolimus suppress DNCB-induced increase of serum total IgE and attenuate expression of inflammatory factors IL-4, IL-6, IL-13, IL-1beta and interferon (IFN)-gamma in the disrupted ear tissues. Tacrolimus 15-25 interferon gamma Mus musculus 157-179 30222017-6 2019 For other body locations, a TCI, either pimecrolimus 1% cream, tacrolimus 0.03% ointment in children or 0.1% ointment in adults, should be applied twice daily until clearance. Tacrolimus 63-73 latexin Homo sapiens 28-31 30861159-4 2019 In wild-type CYP3A4 rs2242480 (TT) carriers, patients who took calcium channel blockers had lower tacrolimus stable doses than those without the concomitant medications (P < 1 x 10-4 ). Tacrolimus 98-108 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 13-19 30861159-6 2019 Similarly, the tacrolimus stable doses in wild-type CYP3A5 rs776746 carriers who had hypertension were higher than those without hypertension (P = 4.10 x 10-3 ). Tacrolimus 15-25 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 52-58 30861159-8 2019 Our finding suggested that wild-type CYP3A4 rs2242480 (TT) carriers should be more cautious to take tacrolimus when they are coadministrated with calcium channel blockers, and CYP3A5 rs776746 (AA) carriers may need higher tacrolimus dosage when they are in combination with hypertension. Tacrolimus 100-110 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 30861159-8 2019 Our finding suggested that wild-type CYP3A4 rs2242480 (TT) carriers should be more cautious to take tacrolimus when they are coadministrated with calcium channel blockers, and CYP3A5 rs776746 (AA) carriers may need higher tacrolimus dosage when they are in combination with hypertension. Tacrolimus 222-232 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 30861159-8 2019 Our finding suggested that wild-type CYP3A4 rs2242480 (TT) carriers should be more cautious to take tacrolimus when they are coadministrated with calcium channel blockers, and CYP3A5 rs776746 (AA) carriers may need higher tacrolimus dosage when they are in combination with hypertension. Tacrolimus 222-232 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 176-182 31261526-5 2019 The most commonly reported genotype was CYP3A53/3, which was strongly associated with cyclosporine A (CsA) and tacrolimus (FK506). Tacrolimus 111-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 40-49 31261526-5 2019 The most commonly reported genotype was CYP3A53/3, which was strongly associated with cyclosporine A (CsA) and tacrolimus (FK506). Tacrolimus 123-128 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 40-49 31003147-0 2019 Recipient ABCB1, donor and recipient CYP3A5 genotypes influence tacrolimus pharmacokinetics in liver transplant cases. Tacrolimus 64-74 ATP binding cassette subfamily B member 1 Homo sapiens 10-15 31003147-0 2019 Recipient ABCB1, donor and recipient CYP3A5 genotypes influence tacrolimus pharmacokinetics in liver transplant cases. Tacrolimus 64-74 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 37-43 31003147-2 2019 METHODS: Meta-analysis was carried out to evaluate how donor/recipient CYP3A5 (n = 678) and recipient ABCB1 (n = 318) genotypes influence tacrolimus pharmacokinetics till one-month of transplantation. Tacrolimus 138-148 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 71-77 31003147-2 2019 METHODS: Meta-analysis was carried out to evaluate how donor/recipient CYP3A5 (n = 678) and recipient ABCB1 (n = 318) genotypes influence tacrolimus pharmacokinetics till one-month of transplantation. Tacrolimus 138-148 ATP binding cassette subfamily B member 1 Homo sapiens 102-107 31003147-7 2019 CONCLUSIONS: The donor and recipient CYP3A5*3 polymorphism influences tacrolimus pharmacokinetics in the first month post-transplantation, whereas the association with recipient ABCB1 3435 C > T is inconclusive. Tacrolimus 70-80 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 37-43 31003147-7 2019 CONCLUSIONS: The donor and recipient CYP3A5*3 polymorphism influences tacrolimus pharmacokinetics in the first month post-transplantation, whereas the association with recipient ABCB1 3435 C > T is inconclusive. Tacrolimus 70-80 ATP binding cassette subfamily B member 1 Homo sapiens 178-183 31045868-12 2019 The association between CYP3A5 genotype and tacrolimus dose requirement is consistent (Grading A I). Tacrolimus 44-54 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 24-30 31045868-16 2019 Population PK models including CYP3A5 and CYP3A4 genotypes will be considered to guide initial tacrolimus dosing. Tacrolimus 95-105 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 31-37 31045868-16 2019 Population PK models including CYP3A5 and CYP3A4 genotypes will be considered to guide initial tacrolimus dosing. Tacrolimus 95-105 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 42-48 31214251-9 2019 In addition, we found that CYP3A5, which is known to affect the metabolism of tacrolimus, only influenced tacrolimus pharmacokinetics in the SP. Tacrolimus 78-88 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 27-33 31214251-9 2019 In addition, we found that CYP3A5, which is known to affect the metabolism of tacrolimus, only influenced tacrolimus pharmacokinetics in the SP. Tacrolimus 106-116 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 27-33 30827938-5 2019 Further study showed that both FK506 and FKVP activate BMP signaling in multiple cell types through FKBP12 antagonism. Tacrolimus 31-36 bone morphogenetic protein 1 Homo sapiens 55-58 30827938-5 2019 Further study showed that both FK506 and FKVP activate BMP signaling in multiple cell types through FKBP12 antagonism. Tacrolimus 31-36 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 100-106 31096684-0 2019 Impact of CYP3A5, POR, and CYP2C19 Polymorphisms on Trough Concentration to Dose Ratio of Tacrolimus in Allogeneic Hematopoietic Stem Cell Transplantation. Tacrolimus 90-100 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 10-16 31100260-3 2019 (2019) utilize FKBP12 ligand to demonstrate that wound healing effects of FK506 occur via activation of the BMP (bone morphogenic protein) signaling pathway. Tacrolimus 74-79 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 15-21 31100260-3 2019 (2019) utilize FKBP12 ligand to demonstrate that wound healing effects of FK506 occur via activation of the BMP (bone morphogenic protein) signaling pathway. Tacrolimus 74-79 bone morphogenetic protein 1 Homo sapiens 108-111 31100260-3 2019 (2019) utilize FKBP12 ligand to demonstrate that wound healing effects of FK506 occur via activation of the BMP (bone morphogenic protein) signaling pathway. Tacrolimus 74-79 bone morphogenetic protein 1 Homo sapiens 113-137 30659828-11 2019 Treatment with Mdivi-1 and FK506 upregulated the phosphorylation of Drp1, inhibited Drp1 translocation to mitochondria, and alleviated mitochondrial fragmentation after HIR. Tacrolimus 27-32 dynamin 1-like Mus musculus 68-72 30659828-11 2019 Treatment with Mdivi-1 and FK506 upregulated the phosphorylation of Drp1, inhibited Drp1 translocation to mitochondria, and alleviated mitochondrial fragmentation after HIR. Tacrolimus 27-32 dynamin 1-like Mus musculus 84-88 30659828-12 2019 What"s more, Mdivi-1 and FK506 restrained cytochrome c release and cleaved caspase-3 expression, ameliorated hippocampal neurons apoptosis, and decreased serum S100beta/NSE concentrations as well. Tacrolimus 25-30 caspase 3 Mus musculus 75-84 30659828-12 2019 What"s more, Mdivi-1 and FK506 restrained cytochrome c release and cleaved caspase-3 expression, ameliorated hippocampal neurons apoptosis, and decreased serum S100beta/NSE concentrations as well. Tacrolimus 25-30 S100 calcium binding protein A1 Mus musculus 160-168 30659828-12 2019 What"s more, Mdivi-1 and FK506 restrained cytochrome c release and cleaved caspase-3 expression, ameliorated hippocampal neurons apoptosis, and decreased serum S100beta/NSE concentrations as well. Tacrolimus 25-30 enolase 2, gamma neuronal Mus musculus 169-172 31096684-0 2019 Impact of CYP3A5, POR, and CYP2C19 Polymorphisms on Trough Concentration to Dose Ratio of Tacrolimus in Allogeneic Hematopoietic Stem Cell Transplantation. Tacrolimus 90-100 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 27-34 31096684-2 2019 Here, we investigated the influence of genotypes of CYP3A5, CYP2C19, and POR on the concentration/dose (C/D) ratio of tacrolimus and episodes of acute graft-versus-host disease (GVHD) in Japanese recipients of allogeneic hematopoietic stem cell transplantation (HSCT). Tacrolimus 118-128 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 52-58 31096684-2 2019 Here, we investigated the influence of genotypes of CYP3A5, CYP2C19, and POR on the concentration/dose (C/D) ratio of tacrolimus and episodes of acute graft-versus-host disease (GVHD) in Japanese recipients of allogeneic hematopoietic stem cell transplantation (HSCT). Tacrolimus 118-128 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 60-67 31096684-2 2019 Here, we investigated the influence of genotypes of CYP3A5, CYP2C19, and POR on the concentration/dose (C/D) ratio of tacrolimus and episodes of acute graft-versus-host disease (GVHD) in Japanese recipients of allogeneic hematopoietic stem cell transplantation (HSCT). Tacrolimus 118-128 cytochrome p450 oxidoreductase Homo sapiens 73-76 31096684-4 2019 During continuous intravenous infusion, HSCT recipients carrying the CYP3A5*1 allele, particularly those with at least one POR*28 allele, had a significantly lower tacrolimus C/D ratio throughout all three post-HSCT weeks compared to that in recipients with POR*1/*1 (p < 0.05). Tacrolimus 164-174 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 69-75 30928512-6 2019 Compared with 0.05% tacrolimus eye drops, the in vivo immunofluorescence analysis indicated the tacrolimus loaded mPEG-b-PLGA micelles remarkably inhibit the immune rejection after corneal allograft, with the lower expression levels of nuclear factor of activated T cells (NFAT), cluster of differentiation 4 (CD4) and cluster of differentiation 8 (CD8). Tacrolimus 96-106 nuclear factor of activated T-cells 5 Rattus norvegicus 273-277 30928512-6 2019 Compared with 0.05% tacrolimus eye drops, the in vivo immunofluorescence analysis indicated the tacrolimus loaded mPEG-b-PLGA micelles remarkably inhibit the immune rejection after corneal allograft, with the lower expression levels of nuclear factor of activated T cells (NFAT), cluster of differentiation 4 (CD4) and cluster of differentiation 8 (CD8). Tacrolimus 96-106 Cd4 molecule Rattus norvegicus 280-308 30928512-6 2019 Compared with 0.05% tacrolimus eye drops, the in vivo immunofluorescence analysis indicated the tacrolimus loaded mPEG-b-PLGA micelles remarkably inhibit the immune rejection after corneal allograft, with the lower expression levels of nuclear factor of activated T cells (NFAT), cluster of differentiation 4 (CD4) and cluster of differentiation 8 (CD8). Tacrolimus 96-106 Cd4 molecule Rattus norvegicus 310-313 31086126-0 2019 Pharmacokinetic Profile of Prolonged-Release Tacrolimus When Administered via Nasogastric Tube in De Novo Liver Transplantation: A Sub-Study of the DIAMOND Trial. Tacrolimus 45-55 tubulin epsilon 1 Homo sapiens 90-94 31086126-1 2019 BACKGROUND For patients unable to swallow during the immediate post-transplant period, immunosuppressant therapy may be initiated by administering prolonged-release tacrolimus as a suspension via a nasogastric tube. Tacrolimus 165-175 tubulin epsilon 1 Homo sapiens 210-214 31086126-6 2019 The overall mean daily dose of prolonged-release tacrolimus administered via nasogastric tube was higher on Day 1 (0.179 mg/kg) vs. Day 3 (0.140 mg/kg). Tacrolimus 49-59 tubulin epsilon 1 Homo sapiens 89-93 30589990-3 2019 A study in renal transplanted patients disclosed association of CYP3A5*6 and CYP3A5*7 with tacrolimus dosing, which led to addition of these variants to CYP3A5*3 in the CPIC tacrolimus guideline. Tacrolimus 91-101 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 64-70 30589990-3 2019 A study in renal transplanted patients disclosed association of CYP3A5*6 and CYP3A5*7 with tacrolimus dosing, which led to addition of these variants to CYP3A5*3 in the CPIC tacrolimus guideline. Tacrolimus 91-101 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 77-83 30589990-3 2019 A study in renal transplanted patients disclosed association of CYP3A5*6 and CYP3A5*7 with tacrolimus dosing, which led to addition of these variants to CYP3A5*3 in the CPIC tacrolimus guideline. Tacrolimus 91-101 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 77-83 30589990-3 2019 A study in renal transplanted patients disclosed association of CYP3A5*6 and CYP3A5*7 with tacrolimus dosing, which led to addition of these variants to CYP3A5*3 in the CPIC tacrolimus guideline. Tacrolimus 174-184 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 64-70 30589990-3 2019 A study in renal transplanted patients disclosed association of CYP3A5*6 and CYP3A5*7 with tacrolimus dosing, which led to addition of these variants to CYP3A5*3 in the CPIC tacrolimus guideline. Tacrolimus 174-184 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 77-83 30589990-3 2019 A study in renal transplanted patients disclosed association of CYP3A5*6 and CYP3A5*7 with tacrolimus dosing, which led to addition of these variants to CYP3A5*3 in the CPIC tacrolimus guideline. Tacrolimus 174-184 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 77-83 30387123-5 2019 Mechanically, inhibition of Ca 2+ -calcineurin-NFATc1 signaling by FK506 or 11R-VIVIT abrogated the TRPV4 overexpression-induced osteoclast differentiation and autophagy induction. Tacrolimus 67-72 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 47-53 30387123-5 2019 Mechanically, inhibition of Ca 2+ -calcineurin-NFATc1 signaling by FK506 or 11R-VIVIT abrogated the TRPV4 overexpression-induced osteoclast differentiation and autophagy induction. Tacrolimus 67-72 transient receptor potential cation channel, subfamily V, member 4 Mus musculus 100-105 30753461-5 2019 We further showed that treatment with FK506 (tacrolimus) possibly inhibits the increase in IL-8 levels in RA patients with anti-RANKL Ab, and in vitro assay confirmed that FK506 suppressed IL-8 production in pre-OCLs. Tacrolimus 38-43 C-X-C motif chemokine ligand 8 Homo sapiens 91-95 30753461-5 2019 We further showed that treatment with FK506 (tacrolimus) possibly inhibits the increase in IL-8 levels in RA patients with anti-RANKL Ab, and in vitro assay confirmed that FK506 suppressed IL-8 production in pre-OCLs. Tacrolimus 38-43 TNF superfamily member 11 Homo sapiens 128-133 30753461-5 2019 We further showed that treatment with FK506 (tacrolimus) possibly inhibits the increase in IL-8 levels in RA patients with anti-RANKL Ab, and in vitro assay confirmed that FK506 suppressed IL-8 production in pre-OCLs. Tacrolimus 38-43 C-X-C motif chemokine ligand 8 Homo sapiens 189-193 30753461-5 2019 We further showed that treatment with FK506 (tacrolimus) possibly inhibits the increase in IL-8 levels in RA patients with anti-RANKL Ab, and in vitro assay confirmed that FK506 suppressed IL-8 production in pre-OCLs. Tacrolimus 45-55 C-X-C motif chemokine ligand 8 Homo sapiens 91-95 30753461-5 2019 We further showed that treatment with FK506 (tacrolimus) possibly inhibits the increase in IL-8 levels in RA patients with anti-RANKL Ab, and in vitro assay confirmed that FK506 suppressed IL-8 production in pre-OCLs. Tacrolimus 45-55 TNF superfamily member 11 Homo sapiens 128-133 30753461-5 2019 We further showed that treatment with FK506 (tacrolimus) possibly inhibits the increase in IL-8 levels in RA patients with anti-RANKL Ab, and in vitro assay confirmed that FK506 suppressed IL-8 production in pre-OCLs. Tacrolimus 45-55 C-X-C motif chemokine ligand 8 Homo sapiens 189-193 30753461-5 2019 We further showed that treatment with FK506 (tacrolimus) possibly inhibits the increase in IL-8 levels in RA patients with anti-RANKL Ab, and in vitro assay confirmed that FK506 suppressed IL-8 production in pre-OCLs. Tacrolimus 172-177 C-X-C motif chemokine ligand 8 Homo sapiens 91-95 30753461-5 2019 We further showed that treatment with FK506 (tacrolimus) possibly inhibits the increase in IL-8 levels in RA patients with anti-RANKL Ab, and in vitro assay confirmed that FK506 suppressed IL-8 production in pre-OCLs. Tacrolimus 172-177 TNF superfamily member 11 Homo sapiens 128-133 30753461-5 2019 We further showed that treatment with FK506 (tacrolimus) possibly inhibits the increase in IL-8 levels in RA patients with anti-RANKL Ab, and in vitro assay confirmed that FK506 suppressed IL-8 production in pre-OCLs. Tacrolimus 172-177 C-X-C motif chemokine ligand 8 Homo sapiens 189-193 31024070-7 2019 Consistent with the human fertility studies, this investigation reveals a beneficial systemic use of tacrolimus (0.1 mg/kg) in promoting early pregnancy in individuals with PCOS and suggests the need for further research into the selective inhibition of IL17A as a plausibly alternative immunotherapeutic approach in the clinical management of infertile individuals with PCOS. Tacrolimus 101-111 interleukin 17A Homo sapiens 254-259 31096684-4 2019 During continuous intravenous infusion, HSCT recipients carrying the CYP3A5*1 allele, particularly those with at least one POR*28 allele, had a significantly lower tacrolimus C/D ratio throughout all three post-HSCT weeks compared to that in recipients with POR*1/*1 (p < 0.05). Tacrolimus 164-174 cytochrome p450 oxidoreductase Homo sapiens 123-126 31096684-5 2019 The CYP3A5*3/*3 genotype and the concomitant use of voriconazole were independent predictors of an increased tacrolimus C/D ratio during the switch from continuous intravenous infusion to oral administration (p < 0.05). Tacrolimus 109-119 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 4-10 31096684-8 2019 Our results suggest that CYP3A5, POR, and CYP2C19 polymorphisms are useful biomarkers for individualized dosage adjustment of tacrolimus in HSCT recipients. Tacrolimus 126-136 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 25-31 31096684-8 2019 Our results suggest that CYP3A5, POR, and CYP2C19 polymorphisms are useful biomarkers for individualized dosage adjustment of tacrolimus in HSCT recipients. Tacrolimus 126-136 cytochrome p450 oxidoreductase Homo sapiens 33-36 31096684-8 2019 Our results suggest that CYP3A5, POR, and CYP2C19 polymorphisms are useful biomarkers for individualized dosage adjustment of tacrolimus in HSCT recipients. Tacrolimus 126-136 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 42-49 30983820-3 2019 The performance of the calcineurin inhibitor tacrolimus in this clinical setting is insufficiently elucidated. Tacrolimus 45-55 calcineurin binding protein 1 Homo sapiens 23-44 30983820-19 2019 In all, tacrolimus therapy appears to be a viable option for short-term treatment of steroid-refractory acute severe ulcerative colitis besides ciclosporin and anti-tumor necrosis factor alpha treatment. Tacrolimus 8-18 tumor necrosis factor Homo sapiens 165-192 30597277-0 2019 Effect of CYP3A4, CYP3A5, and ABCB1 Polymorphisms on Intravenous Tacrolimus Exposure and Adverse Events in Adult Allogeneic Stem Cell Transplant Patients. Tacrolimus 65-75 ATP binding cassette subfamily B member 1 Homo sapiens 30-35 30324847-9 2019 Notably, Cd treatment increased the activity of PPP3/calcineurin, and pharmacological inhibition of PPP3/calcineurin with FK506 suppressed AKT dephosphorylation and TFE3 activity. Tacrolimus 122-127 AKT serine/threonine kinase 1 Homo sapiens 139-142 30324847-9 2019 Notably, Cd treatment increased the activity of PPP3/calcineurin, and pharmacological inhibition of PPP3/calcineurin with FK506 suppressed AKT dephosphorylation and TFE3 activity. Tacrolimus 122-127 transcription factor binding to IGHM enhancer 3 Homo sapiens 165-169 30597277-10 2019 ABCB1 C2677T was significantly associated with concentrations >15ng/mL (odds ratio, 6.2; 95% confidence interval, 1.8 to 23.6; P = .004) and tacrolimus-related toxicities (odds ratio, 7.5; 95% confidence interval, 1.6 to 55.2; P = .02). Tacrolimus 144-154 ATP binding cassette subfamily B member 1 Homo sapiens 0-5 30597277-12 2019 tacrolimus exposure, whereas ABCB1 C2677T also impacts tacrolimus-related toxicities in stem cell transplants. Tacrolimus 55-65 ATP binding cassette subfamily B member 1 Homo sapiens 29-34 30707421-4 2019 It has been well established that calcineurin, highly conserved from yeast to mammals, is necessary for invasive fungal disease and is inhibited when in complex with FK506/FKBP12. Tacrolimus 166-171 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 172-178 30707421-3 2019 One potential antifungal drug, FK506, establishes a ternary complex between the phosphatase, calcineurin, and the 12-kDa peptidyl-prolyl isomerase FK506-binding protein, FKBP12. Tacrolimus 31-36 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 170-176 30707421-7 2019 Here we report the backbone and sidechain NMR assignments of recombinant FKBP12 proteins from the pathogenic fungi Mucor circinelloides and Aspergillus fumigatus in the apo form and compare these to the backbone assignments of the FK506 bound form. Tacrolimus 231-236 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 73-79 30707421-8 2019 In addition, we report the backbone assignments of the apo and FK506 bound forms of the Homo sapiens FKBP12 protein for evaluation against the fungal forms. Tacrolimus 63-68 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 101-107 30707421-9 2019 These data are the first steps towards defining, at a residue specific level, the impacts of FK506 binding to fungal and mammalian FKBP12 proteins. Tacrolimus 93-98 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 131-137 30713033-10 2019 RESULTS: In rats pre-treated with FK506, the levels of transaminases, TNF-alpha and IL-1beta were reduced significantly and also liver damage was dramatically mitigated compared to those without FK506 pre-treatment. Tacrolimus 34-39 tumor necrosis factor Rattus norvegicus 70-79 30879170-2 2019 Human FKBP12 is a prototype of this family and it is involved in many diseases due to its interaction with the immunosuppressive drugs FK506 and rapamycin. Tacrolimus 135-140 FKBP prolyl isomerase 1A pseudogene 1 Homo sapiens 6-12 30713033-10 2019 RESULTS: In rats pre-treated with FK506, the levels of transaminases, TNF-alpha and IL-1beta were reduced significantly and also liver damage was dramatically mitigated compared to those without FK506 pre-treatment. Tacrolimus 34-39 interleukin 1 beta Rattus norvegicus 84-92 30713033-11 2019 Moreover, the expression of HO-1 at the level of both transcription and translation increased clearly and the activation of the HIF-1alpha was found in FK506 pre-treated livers. Tacrolimus 152-157 heme oxygenase 1 Rattus norvegicus 28-32 30713033-11 2019 Moreover, the expression of HO-1 at the level of both transcription and translation increased clearly and the activation of the HIF-1alpha was found in FK506 pre-treated livers. Tacrolimus 152-157 hypoxia inducible factor 1 subunit alpha Rattus norvegicus 128-138 30713033-12 2019 Moreover, NFAT3 protein transportation to the nucleus was reduced and Bax protein expression was decreased, but the expression of Bcl-2 protein was markedly increased after FK506 pre-treatment. Tacrolimus 173-178 BCL2, apoptosis regulator Rattus norvegicus 130-135 30713033-13 2019 CONCLUSION: FK506 pre-treatment could lessen hepatic ischemia-reperfusion injury through up-regulating the expression of HIF-1alpha and HO-1, and inhibiting nuclear translocation of NFAT3 in liver tissues. Tacrolimus 12-17 hypoxia inducible factor 1 subunit alpha Rattus norvegicus 121-131 30713033-13 2019 CONCLUSION: FK506 pre-treatment could lessen hepatic ischemia-reperfusion injury through up-regulating the expression of HIF-1alpha and HO-1, and inhibiting nuclear translocation of NFAT3 in liver tissues. Tacrolimus 12-17 heme oxygenase 1 Rattus norvegicus 136-140 30983501-0 2019 Impact of CYP3A5 phenotype on tacrolimus concentrations after sublingual and oral administration in lung transplant. Tacrolimus 30-40 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 10-16 30294901-3 2019 The immunophilin FKBP12 binding ligand FK506 is well known as an immunosuppressive agent by inhibiting the calcineurin expression. Tacrolimus 39-44 FK506 binding protein 1a Mus musculus 4-23 30294901-4 2019 In this study, we synthesized a series of modified compounds based on the FKBP12 binding moiety to as same as the binding structure of rapamycin and FK506 particularly. Tacrolimus 149-154 FK506 binding protein 1a Mus musculus 74-80 30704156-0 2019 Individualized treatment based on CYP3A5 single-nucleotide polymorphisms with tacrolimus in ulcerative colitis. Tacrolimus 78-88 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 34-40 30704156-1 2019 BACKGROUND/AIMS: The pharmacokinetics of tacrolimus (TAC) is known to be largely influenced by single-nucleotide polymorphisms (SNPs) in CYP3A5. Tacrolimus 41-51 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 137-143 30251118-10 2019 As calcineurin may dephosphorylate Drp1, we determined the effect of a calcineurin inhibitor, FK506, which prevented leptin-induced hypertrophy as well as mitochondrial fission and mitochondrial dysfunction. Tacrolimus 94-99 leptin Homo sapiens 117-123 30983501-6 2019 Conclusion: This study suggests personalized dosing strategies for tacrolimus likely need to consider characteristics beyond CYP3A5 genotype. Tacrolimus 67-77 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 125-131 30260738-5 2019 Recently, it was shown that tacrolimus increased ALK-1 signaling and had beneficial effects in selected end-stage PAH patients. Tacrolimus 28-38 activin A receptor like type 1 Homo sapiens 49-54 30979494-7 2019 CONCLUSION: Wild-type MDR1 gene product P-glycoprotein expressed in the intestine reduces drug absorption from the gastrointestinal tract and may have contributed to low blood levels of tacrolimus in this patient when tacrolimus was orally administered. Tacrolimus 186-196 ATP binding cassette subfamily B member 1 Homo sapiens 22-26 30592973-20 2019 On TLR-day an association of renal function and Tac concentration with TLR4ex was clear only in the tacrolimus population. Tacrolimus 100-110 toll like receptor 4 Homo sapiens 71-75 30592973-25 2019 Evaluation of the averaged TLR4ex can be used to assess the efficacy of immunosuppression in the treatment with tacrolimus and to estimate the likelihood of deterioration in renal function. Tacrolimus 112-122 toll like receptor 4 Homo sapiens 27-31 30979494-7 2019 CONCLUSION: Wild-type MDR1 gene product P-glycoprotein expressed in the intestine reduces drug absorption from the gastrointestinal tract and may have contributed to low blood levels of tacrolimus in this patient when tacrolimus was orally administered. Tacrolimus 186-196 ATP binding cassette subfamily B member 1 Homo sapiens 40-54 30979494-7 2019 CONCLUSION: Wild-type MDR1 gene product P-glycoprotein expressed in the intestine reduces drug absorption from the gastrointestinal tract and may have contributed to low blood levels of tacrolimus in this patient when tacrolimus was orally administered. Tacrolimus 218-228 ATP binding cassette subfamily B member 1 Homo sapiens 22-26 30979494-7 2019 CONCLUSION: Wild-type MDR1 gene product P-glycoprotein expressed in the intestine reduces drug absorption from the gastrointestinal tract and may have contributed to low blood levels of tacrolimus in this patient when tacrolimus was orally administered. Tacrolimus 218-228 ATP binding cassette subfamily B member 1 Homo sapiens 40-54 30983748-0 2019 Loss of Subpodocytic Space Predicts Poor Response to Tacrolimus in Steroid-Resistant Calcineurin Inhibitor-Naive Adult-Onset Primary Focal Segmental Glomerulosclerosis. Tacrolimus 53-63 calcineurin binding protein 1 Homo sapiens 85-106 30260084-5 2019 Tacrolimus clearances were 26, 18.8 and 12.3 L/h, for patients with genetic polymorphisms CYP3A5*1*1, *1*3 and *3*3, respectively. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 90-96 30983748-8 2019 The tacrolimus-resistant patients were of older age, had a longer duration of illness, and a lower eGFR as compared to tacrolimus responsive cases. Tacrolimus 4-14 epidermal growth factor receptor Homo sapiens 99-103 30371942-1 2019 Tacrolimus, a calcineurin inhibitor, is a common immunosuppressant prescribed after organ transplantation and has notable inter- and intrapatient pharmacokinetic variability. Tacrolimus 0-10 calcineurin binding protein 1 Homo sapiens 14-35 30371942-8 2019 The CYP3A5 genotype, as a covariate, consistently impacted tacrolimus clearance, and dosing adjustments were required to achieve similar drug exposure among patients. Tacrolimus 59-69 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 4-10 30472069-0 2019 Tacrolimus inhibits Th1 and Th17 responses in MuSK-antibody positive myasthenia gravis patients. Tacrolimus 0-10 muscle associated receptor tyrosine kinase Homo sapiens 46-50 30457174-6 2019 Treatment with calcineurin inhibitor cyclosporin A (CsA) or FK506 suppressed cell proliferation and induced apoptotic cell death in both MYCN-amplified and MYCN-non-amplified NB cell lines. Tacrolimus 60-65 MYCN proto-oncogene, bHLH transcription factor Homo sapiens 137-141 30457174-6 2019 Treatment with calcineurin inhibitor cyclosporin A (CsA) or FK506 suppressed cell proliferation and induced apoptotic cell death in both MYCN-amplified and MYCN-non-amplified NB cell lines. Tacrolimus 60-65 MYCN proto-oncogene, bHLH transcription factor Homo sapiens 156-160 30946720-5 2019 Some studies suggest that post-transplant immunosuppression with tacrolimus is linked to an increased occurrence of IgE-mediated sensitization and manifestation of allergic disease. Tacrolimus 65-75 immunoglobulin heavy constant epsilon Homo sapiens 116-119 30879580-13 2019 CONCLUSION: Rituximab and switching tacrolimus to cyclosporine, in conjunction with plasmapheresis, appeared to be effective and safe in children with recurrent FSGS. Tacrolimus 36-46 actinin alpha 4 Homo sapiens 161-165 30907352-0 2019 [Clinical effect of tacrolimus combined with glucocorticoid in the treatment of IgA nephropathy in children]. Tacrolimus 20-30 IGAN1 Homo sapiens 80-95 30931336-14 2019 Furthermore, they could demonstrate that treatment with the immunosuppressive drug tacrolimus resulted in decreased CMV-specific IFN-gamma and of IL-21 production. Tacrolimus 83-93 interferon gamma Homo sapiens 129-138 30931336-14 2019 Furthermore, they could demonstrate that treatment with the immunosuppressive drug tacrolimus resulted in decreased CMV-specific IFN-gamma and of IL-21 production. Tacrolimus 83-93 interleukin 21 Homo sapiens 146-151 30997048-1 2019 We report the initiation of CFTR modulator lumacaftor/ivacaftor combination (LUM/IVA) in two adolescents with cystic fibrosis who were treated with antifungal azoles (AZO) and tacrolimus (TCS) for liver transplantation. Tacrolimus 176-186 CF transmembrane conductance regulator Homo sapiens 28-32 30997048-1 2019 We report the initiation of CFTR modulator lumacaftor/ivacaftor combination (LUM/IVA) in two adolescents with cystic fibrosis who were treated with antifungal azoles (AZO) and tacrolimus (TCS) for liver transplantation. Tacrolimus 176-186 lumican Homo sapiens 77-80 30997048-1 2019 We report the initiation of CFTR modulator lumacaftor/ivacaftor combination (LUM/IVA) in two adolescents with cystic fibrosis who were treated with antifungal azoles (AZO) and tacrolimus (TCS) for liver transplantation. Tacrolimus 188-191 CF transmembrane conductance regulator Homo sapiens 28-32 30997048-1 2019 We report the initiation of CFTR modulator lumacaftor/ivacaftor combination (LUM/IVA) in two adolescents with cystic fibrosis who were treated with antifungal azoles (AZO) and tacrolimus (TCS) for liver transplantation. Tacrolimus 188-191 lumican Homo sapiens 77-80 30545944-0 2019 The Immunosuppressant Macrolide Tacrolimus Activates Cold-Sensing TRPM8 Channels. Tacrolimus 32-42 transient receptor potential cation channel subfamily M member 8 Homo sapiens 66-71 30545944-2 2019 We found that TRPM8 is a pharmacological target of tacrolimus (FK506), a macrolide immunosuppressant with several clinical uses, including the treatment of organ rejection following transplants, treatment of atopic dermatitis, and dry eye disease. Tacrolimus 51-61 transient receptor potential cation channel subfamily M member 8 Homo sapiens 14-19 30545944-2 2019 We found that TRPM8 is a pharmacological target of tacrolimus (FK506), a macrolide immunosuppressant with several clinical uses, including the treatment of organ rejection following transplants, treatment of atopic dermatitis, and dry eye disease. Tacrolimus 63-68 transient receptor potential cation channel subfamily M member 8 Homo sapiens 14-19 30545944-4 2019 Tacrolimus activates TRPM8 channels in different species, including humans, and sensitizes their response to cold temperature by inducing a leftward shift in the voltage-dependent activation curve. Tacrolimus 0-10 transient receptor potential cation channel subfamily M member 8 Homo sapiens 21-26 30545944-5 2019 The effects of tacrolimus on purified TRPM8 in lipid bilayers demonstrates conclusively that it has a direct gating effect. Tacrolimus 15-25 transient receptor potential cation channel subfamily M member 8 Homo sapiens 38-43 30545944-7 2019 Menthol (TRPM8-Y745H)- and icilin (TRPM8-N799A)-insensitive mutants were also activated by tacrolimus, suggesting a different binding site. Tacrolimus 91-101 transient receptor potential cation channel subfamily M member 8 Homo sapiens 9-14 30545944-7 2019 Menthol (TRPM8-Y745H)- and icilin (TRPM8-N799A)-insensitive mutants were also activated by tacrolimus, suggesting a different binding site. Tacrolimus 91-101 transient receptor potential cation channel subfamily M member 8 Homo sapiens 35-40 30545944-8 2019 In cultured mouse DRG neurons, tacrolimus evokes an increase in intracellular calcium almost exclusively in cold-sensitive neurons, and these responses were drastically blunted in Trpm8 KO mice or after the application of TRPM8 antagonists. Tacrolimus 31-41 transient receptor potential cation channel, subfamily M, member 8 Mus musculus 180-185 30545944-8 2019 In cultured mouse DRG neurons, tacrolimus evokes an increase in intracellular calcium almost exclusively in cold-sensitive neurons, and these responses were drastically blunted in Trpm8 KO mice or after the application of TRPM8 antagonists. Tacrolimus 31-41 transient receptor potential cation channel, subfamily M, member 8 Mus musculus 222-227 30545944-10 2019 Together, our results identify TRPM8 channels in sensory neurons as molecular targets of the immunosuppressant tacrolimus. Tacrolimus 111-121 transient receptor potential cation channel, subfamily M, member 8 Mus musculus 31-36 30545944-11 2019 The actions of tacrolimus on TRPM8 resemble those of menthol but likely involve interactions with other channel residues.SIGNIFICANCE STATEMENT TRPM8 is a polymodal TRP channel involved in cold temperature sensing, thermoregulation, and cold pain. Tacrolimus 15-25 transient receptor potential cation channel, subfamily M, member 8 Mus musculus 29-34 30545944-11 2019 The actions of tacrolimus on TRPM8 resemble those of menthol but likely involve interactions with other channel residues.SIGNIFICANCE STATEMENT TRPM8 is a polymodal TRP channel involved in cold temperature sensing, thermoregulation, and cold pain. Tacrolimus 15-25 transient receptor potential cation channel, subfamily M, member 8 Mus musculus 144-149 30545944-13 2019 We report the direct agonist effect of tacrolimus, a potent natural immunosuppressant with multiple clinical applications, on TRPM8 activity. Tacrolimus 39-49 transient receptor potential cation channel, subfamily M, member 8 Mus musculus 126-131 30478741-0 2019 FK506 (tacrolimus) causes pain sensation through the activation of transient receptor potential ankyrin 1 (TRPA1) channels. Tacrolimus 0-5 transient receptor potential cation channel subfamily A member 1 Homo sapiens 67-105 30478741-0 2019 FK506 (tacrolimus) causes pain sensation through the activation of transient receptor potential ankyrin 1 (TRPA1) channels. Tacrolimus 0-5 transient receptor potential cation channel subfamily A member 1 Homo sapiens 107-112 30478741-0 2019 FK506 (tacrolimus) causes pain sensation through the activation of transient receptor potential ankyrin 1 (TRPA1) channels. Tacrolimus 7-17 transient receptor potential cation channel subfamily A member 1 Homo sapiens 67-105 30478741-0 2019 FK506 (tacrolimus) causes pain sensation through the activation of transient receptor potential ankyrin 1 (TRPA1) channels. Tacrolimus 7-17 transient receptor potential cation channel subfamily A member 1 Homo sapiens 107-112 30478741-3 2019 In this study, we found that FK506 activates transient receptor potential ankyrin 1 (TRPA1) channels. Tacrolimus 29-34 transient receptor potential cation channel subfamily A member 1 Homo sapiens 45-83 30478741-3 2019 In this study, we found that FK506 activates transient receptor potential ankyrin 1 (TRPA1) channels. Tacrolimus 29-34 transient receptor potential cation channel subfamily A member 1 Homo sapiens 85-90 30478741-4 2019 In Ca2+-imaging experiments, increases in intracellular Ca2+ concentrations ([Ca2+]i) by FK506 were observed in HEK293T cells expressing hTRPA1 or hTRPM8. Tacrolimus 89-94 transient receptor potential cation channel subfamily A member 1 Homo sapiens 137-143 30478741-4 2019 In Ca2+-imaging experiments, increases in intracellular Ca2+ concentrations ([Ca2+]i) by FK506 were observed in HEK293T cells expressing hTRPA1 or hTRPM8. Tacrolimus 89-94 transient receptor potential cation channel subfamily M member 8 Homo sapiens 147-153 30478741-5 2019 FK506-induced currents were observed in HEK293T cells expressing hTRPA1 or mTRPA1, but less or not at all in cells expressing hTRPV1 or hTRPM8 using a patch-clamp technique. Tacrolimus 0-5 transient receptor potential cation channel subfamily A member 1 Homo sapiens 65-71 30478741-5 2019 FK506-induced currents were observed in HEK293T cells expressing hTRPA1 or mTRPA1, but less or not at all in cells expressing hTRPV1 or hTRPM8 using a patch-clamp technique. Tacrolimus 0-5 transient receptor potential cation channel, subfamily A, member 1 Mus musculus 75-81 30478741-6 2019 FK506 also evoked single-channel opening of hTRPA1 in an inside-out configuration. Tacrolimus 0-5 transient receptor potential cation channel subfamily A member 1 Homo sapiens 44-50 30478741-7 2019 FK506-induced [Ca2+]i increases were also observed in TRPA1-expressing mouse primary sensory neurons. Tacrolimus 0-5 transient receptor potential cation channel, subfamily A, member 1 Mus musculus 54-59 30478741-8 2019 Furthermore, injection of FK506 evoked licking or biting behaviors and these behaviors were almost abolished in TRPA1 knockout mice. Tacrolimus 26-31 transient receptor potential cation channel, subfamily A, member 1 Mus musculus 112-117 30478741-9 2019 These results indicate that FK506 might cause pain sensations through TRPA1 activation. Tacrolimus 28-33 transient receptor potential cation channel subfamily A member 1 Homo sapiens 70-75 30457174-8 2019 c-Myc, MYCN, and beta-catenin were downregulated at the mRNA and protein levels in CsA or FK506-treated NB cells. Tacrolimus 90-95 MYC proto-oncogene, bHLH transcription factor Homo sapiens 0-5 30457174-8 2019 c-Myc, MYCN, and beta-catenin were downregulated at the mRNA and protein levels in CsA or FK506-treated NB cells. Tacrolimus 90-95 MYCN proto-oncogene, bHLH transcription factor Homo sapiens 7-11 30457174-8 2019 c-Myc, MYCN, and beta-catenin were downregulated at the mRNA and protein levels in CsA or FK506-treated NB cells. Tacrolimus 90-95 catenin beta 1 Homo sapiens 17-29 30532015-1 2019 Rapamycin and FK506 are macrocyclic natural products with an extraordinary mode of action, in which they form binary complexes with FK506-binding protein (FKBP) through a shared FKBP-binding domain before forming ternary complexes with their respective targets, mechanistic target of rapamycin (mTOR) and calcineurin, respectively. Tacrolimus 14-19 mechanistic target of rapamycin kinase Homo sapiens 295-299 30794705-0 2019 Correction: Alteration of urinary neutrophil gelatinase-associated lipocalin as a predictor of tacrolimus-induced chronic renal allograft fibrosis in tacrolimus dose adjustments following kidney transplantation. Tacrolimus 95-105 lipocalin 2 Homo sapiens 34-76 30794705-0 2019 Correction: Alteration of urinary neutrophil gelatinase-associated lipocalin as a predictor of tacrolimus-induced chronic renal allograft fibrosis in tacrolimus dose adjustments following kidney transplantation. Tacrolimus 150-160 lipocalin 2 Homo sapiens 34-76 30718414-10 2019 In vivo, tacrolimus increases levels of KLHL3S433-P, resulting in increased levels of WNK4, phosphorylated SPAK, and NCC. Tacrolimus 9-19 WNK lysine deficient protein kinase 4 Homo sapiens 86-90 30718414-10 2019 In vivo, tacrolimus increases levels of KLHL3S433-P, resulting in increased levels of WNK4, phosphorylated SPAK, and NCC. Tacrolimus 9-19 serine/threonine kinase 39 Homo sapiens 107-111 30718414-11 2019 Moreover, tacrolimus attenuates KLHL3-mediated WNK4 ubiquitylation and degradation, while this effect is absent in KLHL3 with S433A substitution. Tacrolimus 10-20 kelch like family member 3 Homo sapiens 32-37 30718414-11 2019 Moreover, tacrolimus attenuates KLHL3-mediated WNK4 ubiquitylation and degradation, while this effect is absent in KLHL3 with S433A substitution. Tacrolimus 10-20 WNK lysine deficient protein kinase 4 Homo sapiens 47-51 30718414-12 2019 Additionally, increased extracellular K+ induced calcineurin-dependent dephosphorylation of KLHL3S433-P These findings demonstrate that KLHL3S433-P is a calcineurin substrate and implicate increased KLHL3 phosphorylation in tacrolimus-induced pathologies. Tacrolimus 224-234 kelch like family member 3 Homo sapiens 92-97 30719576-6 2019 The CL/F of tacrolimus in Wuzhi tablets co-administration and CYP3A5 non-expresser groups were 19.3% and 19.1% lower than that of the non-Wuzhi tablets and CYP3A5 expresser groups, respectively. Tacrolimus 12-22 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 62-68 30719576-8 2019 Monte Carlo simulation showed that the nephrotic syndrome patients that were CYP3A5 non-expressers or co-administered Wuzhi tablets received 50% or 33.3% lower dose of tacrolimus to reach the target concentration. Tacrolimus 168-178 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 77-83 30719576-9 2019 In contrast, the NR1I2 rs227707 TT genotype carriers were administered a 33.3% higher dose of tacrolimus than the NR1I2 rs227707 CC/CT genotype carriers. Tacrolimus 94-104 nuclear receptor subfamily 1 group I member 2 Homo sapiens 17-22 30307767-0 2019 Effect of Klotho on autophagy clearance in tacrolimus-induced renal injury. Tacrolimus 43-53 klotho Mus musculus 10-16 30307767-1 2019 Recently, we showed that tacrolimus-induced renal injury was closely associated with impairment of autophagy clearance, and Klotho deficiency aggravated tacrolimus-induced renal injury. Tacrolimus 153-163 klotho Mus musculus 124-130 30307767-2 2019 In this study, we evaluated the effect of Klotho treatment on autophagy clearance in tacrolimus-induced renal injury. Tacrolimus 85-95 klotho Mus musculus 42-48 30307767-3 2019 We evaluated the effect of Klotho on tacrolimus-induced renal injury in an experimental mouse model and in vitro by treatment with tacrolimus and/or recombinant mouse Klotho. Tacrolimus 37-47 klotho Mus musculus 27-33 30307767-4 2019 In vivo and in vitro studies showed that tacrolimus treatment impaired lysosomal acidification and decreased cathepsin B activity, expression of lysosome-associated membrane protein 2, and expression of transcription factor EB (TFEB), a master regulator for lysosomal biogenesis. Tacrolimus 41-51 cathepsin B Mus musculus 109-120 30307767-4 2019 In vivo and in vitro studies showed that tacrolimus treatment impaired lysosomal acidification and decreased cathepsin B activity, expression of lysosome-associated membrane protein 2, and expression of transcription factor EB (TFEB), a master regulator for lysosomal biogenesis. Tacrolimus 41-51 transcription factor EB Mus musculus 203-226 30307767-4 2019 In vivo and in vitro studies showed that tacrolimus treatment impaired lysosomal acidification and decreased cathepsin B activity, expression of lysosome-associated membrane protein 2, and expression of transcription factor EB (TFEB), a master regulator for lysosomal biogenesis. Tacrolimus 41-51 transcription factor EB Mus musculus 228-232 30307767-8 2019 Collectively, our data suggest that Klotho improves autophagy clearance via activation of lysosomal function in tacrolimus-induced nephrotoxicity.-Lim, S. W., Shin, Y. J., Luo, K., Quan, Y., Ko, E. J., Chung, B. H., Yang, C. W. Effect of Klotho on autophagy clearance in tacrolimus-induced renal injury. Tacrolimus 112-122 klotho Mus musculus 36-42 30307767-8 2019 Collectively, our data suggest that Klotho improves autophagy clearance via activation of lysosomal function in tacrolimus-induced nephrotoxicity.-Lim, S. W., Shin, Y. J., Luo, K., Quan, Y., Ko, E. J., Chung, B. H., Yang, C. W. Effect of Klotho on autophagy clearance in tacrolimus-induced renal injury. Tacrolimus 271-281 klotho Mus musculus 36-42 30472069-3 2019 Tacrolimus, an immunosuppressant used in AChR-MG and transplantation patients, inhibits T cell responses through interference with IL-2 transcription. Tacrolimus 0-10 interleukin 2 Homo sapiens 131-135 30472069-6 2019 We determined that tacrolimus profoundly suppressed CD4 and CD8 T cell proliferation and significantly suppressed Th1 and Th17 responses, as demonstrated by a reduced frequency of IFN-gamma, IL-2, and IL-17 producing CD4 T cells and reduced frequencies of IFN-gamma and IL-2 producing CD8 T cells. Tacrolimus 19-29 CD4 molecule Homo sapiens 52-55 30472069-6 2019 We determined that tacrolimus profoundly suppressed CD4 and CD8 T cell proliferation and significantly suppressed Th1 and Th17 responses, as demonstrated by a reduced frequency of IFN-gamma, IL-2, and IL-17 producing CD4 T cells and reduced frequencies of IFN-gamma and IL-2 producing CD8 T cells. Tacrolimus 19-29 CD8a molecule Homo sapiens 60-63 30472069-6 2019 We determined that tacrolimus profoundly suppressed CD4 and CD8 T cell proliferation and significantly suppressed Th1 and Th17 responses, as demonstrated by a reduced frequency of IFN-gamma, IL-2, and IL-17 producing CD4 T cells and reduced frequencies of IFN-gamma and IL-2 producing CD8 T cells. Tacrolimus 19-29 interferon gamma Homo sapiens 180-189 30472069-6 2019 We determined that tacrolimus profoundly suppressed CD4 and CD8 T cell proliferation and significantly suppressed Th1 and Th17 responses, as demonstrated by a reduced frequency of IFN-gamma, IL-2, and IL-17 producing CD4 T cells and reduced frequencies of IFN-gamma and IL-2 producing CD8 T cells. Tacrolimus 19-29 interleukin 2 Homo sapiens 191-195 30472069-6 2019 We determined that tacrolimus profoundly suppressed CD4 and CD8 T cell proliferation and significantly suppressed Th1 and Th17 responses, as demonstrated by a reduced frequency of IFN-gamma, IL-2, and IL-17 producing CD4 T cells and reduced frequencies of IFN-gamma and IL-2 producing CD8 T cells. Tacrolimus 19-29 interleukin 17A Homo sapiens 201-206 30472069-6 2019 We determined that tacrolimus profoundly suppressed CD4 and CD8 T cell proliferation and significantly suppressed Th1 and Th17 responses, as demonstrated by a reduced frequency of IFN-gamma, IL-2, and IL-17 producing CD4 T cells and reduced frequencies of IFN-gamma and IL-2 producing CD8 T cells. Tacrolimus 19-29 CD4 molecule Homo sapiens 217-220 30472069-6 2019 We determined that tacrolimus profoundly suppressed CD4 and CD8 T cell proliferation and significantly suppressed Th1 and Th17 responses, as demonstrated by a reduced frequency of IFN-gamma, IL-2, and IL-17 producing CD4 T cells and reduced frequencies of IFN-gamma and IL-2 producing CD8 T cells. Tacrolimus 19-29 interferon gamma Homo sapiens 256-265 30472069-6 2019 We determined that tacrolimus profoundly suppressed CD4 and CD8 T cell proliferation and significantly suppressed Th1 and Th17 responses, as demonstrated by a reduced frequency of IFN-gamma, IL-2, and IL-17 producing CD4 T cells and reduced frequencies of IFN-gamma and IL-2 producing CD8 T cells. Tacrolimus 19-29 interleukin 2 Homo sapiens 270-274 30472069-6 2019 We determined that tacrolimus profoundly suppressed CD4 and CD8 T cell proliferation and significantly suppressed Th1 and Th17 responses, as demonstrated by a reduced frequency of IFN-gamma, IL-2, and IL-17 producing CD4 T cells and reduced frequencies of IFN-gamma and IL-2 producing CD8 T cells. Tacrolimus 19-29 CD8a molecule Homo sapiens 285-288 30472069-7 2019 Tacrolimus also inhibits pathogenic Th17 cells coproducing IL-17 and IFN-gamma. Tacrolimus 0-10 interleukin 17A Homo sapiens 59-64 30472069-7 2019 Tacrolimus also inhibits pathogenic Th17 cells coproducing IL-17 and IFN-gamma. Tacrolimus 0-10 interferon gamma Homo sapiens 69-78 30323313-0 2019 Impact of single nucleotide polymorphisms on P450 oxidoreductase and peroxisome proliferator-activated receptor alpha on tacrolimus pharmacokinetics in renal transplant recipients. Tacrolimus 121-131 peroxisome proliferator activated receptor alpha Homo sapiens 69-117 30446894-1 2019 Background Dosage quantities of tacrolimus (TAC) vary according to cytochrome P450 3A5 (CYP3A5) genotype. Tacrolimus 32-42 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 67-86 30446894-1 2019 Background Dosage quantities of tacrolimus (TAC) vary according to cytochrome P450 3A5 (CYP3A5) genotype. Tacrolimus 32-42 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 88-94 30323313-2 2019 We aimed to investigate the impact of single nucleotide polymorphisms (SNPs) in the POR and PPARA genes on the pharmacokinetics of tacrolimus (TAC) in renal transplant recipients. Tacrolimus 131-141 cytochrome p450 oxidoreductase Homo sapiens 84-87 30323313-2 2019 We aimed to investigate the impact of single nucleotide polymorphisms (SNPs) in the POR and PPARA genes on the pharmacokinetics of tacrolimus (TAC) in renal transplant recipients. Tacrolimus 131-141 peroxisome proliferator activated receptor alpha Homo sapiens 92-97 30643171-7 2019 Moreover, Tacrolimus reduced TLR5 expression in bladder macrophages during UTI. Tacrolimus 10-20 toll-like receptor 5 Mus musculus 29-33 30520827-0 2019 Switching Immunosuppression From Cyclosporine to Tacrolimus in Kidney Transplant Recipients Based on CYP3A5 Genotyping. Tacrolimus 49-59 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 101-107 31384453-0 2019 Implication of interleukin-2 receptor antibody induction therapy in standard risk renal transplant in the tacrolimus era: a meta-analysis. Tacrolimus 106-116 interleukin 2 Homo sapiens 15-28 31384453-3 2019 The aim of our study and meta-analysis is to explore the effect of IL-2 induction therapy on the rate of rejection and patient and graft survival in standard-risk renal transplant patients with tacrolimus-based maintenance immunotherapy. Tacrolimus 194-204 interleukin 2 Homo sapiens 67-71 30295407-1 2019 INTRODUCTION: Isavuconazole, a triazole antifungal, is an inhibitor of cytochrome P450 3A4, which also metabolizes tacrolimus and sirolimus. Tacrolimus 115-125 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 71-90 30643171-8 2019 This immunosuppressive state can be explained by the upregulation of TLR-signaling negative regulators (A20, ATF3, IRAK-M and SOCS1) and parallel downregulation of TLR5 as observed in Tacrolimus treated granulocytes and macrophages. Tacrolimus 184-194 toll-like receptor 5 Mus musculus 164-168 30521345-11 2019 A model drug, tacrolimus, was encapsulated in MNP (T-RNP) and significantly suppressed the progression of RA in mice. Tacrolimus 14-24 modifier of Niemann Pick type C1 Mus musculus 46-49 30476735-0 2019 Downregulation of TRPC6 expression is a critical molecular event during FK506 treatment for overactive bladder. Tacrolimus 72-77 transient receptor potential cation channel, subfamily C, member 6 Rattus norvegicus 18-23 31061321-0 2019 Effect of Serum Parathyroid Hormone on Tacrolimus Therapy in Kidney Transplant Patients: A Possible Biomarker for a Tacrolimus Dosage Schedule. Tacrolimus 39-49 parathyroid hormone Homo sapiens 16-35 31061321-0 2019 Effect of Serum Parathyroid Hormone on Tacrolimus Therapy in Kidney Transplant Patients: A Possible Biomarker for a Tacrolimus Dosage Schedule. Tacrolimus 116-126 parathyroid hormone Homo sapiens 16-35 31061321-3 2019 This retrospective observational study assessed the relationship between serum iPTH levels and the blood concentration or dosage of tacrolimus, a CYP3A substrate, after oral administration in kidney transplant patients. Tacrolimus 132-142 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 146-151 30476735-11 2019 FK506 inhibited NFAT translocation to the nucleus and disrupted the interaction of TRPC6 with FKBP12. Tacrolimus 0-5 nuclear factor of activated T-cells 5 Rattus norvegicus 16-20 29989304-1 2019 The magnitude of interaction between the CYP3A4 substrate tacrolimus and various CYP3A4 inhibitors is highly unpredictable. Tacrolimus 58-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 41-47 29989304-1 2019 The magnitude of interaction between the CYP3A4 substrate tacrolimus and various CYP3A4 inhibitors is highly unpredictable. Tacrolimus 58-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 81-87 29989304-2 2019 We investigated whether an individual"s baseline in vivo CYP3A4 activity, assessed using the oral midazolam (MDZ) probe, could be used to predict the magnitude of drug-drug interaction between tacrolimus and the potent CYP3A4 inhibitor itraconazole. Tacrolimus 193-203 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 57-63 29989304-2 2019 We investigated whether an individual"s baseline in vivo CYP3A4 activity, assessed using the oral midazolam (MDZ) probe, could be used to predict the magnitude of drug-drug interaction between tacrolimus and the potent CYP3A4 inhibitor itraconazole. Tacrolimus 193-203 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 219-225 30551354-7 2019 Meanwhile TMP could regulate the Interleukin 10 (IL-10) and FK506 could restrain the Interleukin 2 (IL-2). Tacrolimus 60-65 interleukin 2 Homo sapiens 85-98 30551354-7 2019 Meanwhile TMP could regulate the Interleukin 10 (IL-10) and FK506 could restrain the Interleukin 2 (IL-2). Tacrolimus 60-65 interleukin 2 Homo sapiens 100-104 30713247-8 2019 3) Rheumatoid arthritis patients with a genetic mutation of ATP-binding cassette subfamily B member 1 (ABCB1) had high plasma concentrations of tacrolimus and its 13-O-demethylate. Tacrolimus 144-154 ATP binding cassette subfamily B member 1 Homo sapiens 60-101 30713247-8 2019 3) Rheumatoid arthritis patients with a genetic mutation of ATP-binding cassette subfamily B member 1 (ABCB1) had high plasma concentrations of tacrolimus and its 13-O-demethylate. Tacrolimus 144-154 ATP binding cassette subfamily B member 1 Homo sapiens 103-108 30713247-9 2019 The ABCB1 genetic mutation and associated high plasma concentration of tacrolimus decreased kidney function. Tacrolimus 71-81 ATP binding cassette subfamily B member 1 Homo sapiens 4-9 30476735-11 2019 FK506 inhibited NFAT translocation to the nucleus and disrupted the interaction of TRPC6 with FKBP12. Tacrolimus 0-5 transient receptor potential cation channel, subfamily C, member 6 Rattus norvegicus 83-88 30476735-9 2019 TRPC6 elevation in OAB rats was inhibited by FK506, and this inhibition coincided with improvements in urodynamic indices. Tacrolimus 45-50 transient receptor potential cation channel, subfamily C, member 6 Rattus norvegicus 0-5 31244435-0 2019 Association of Genetic Variants in CYP3A4, CYP3A5, CYP2C8, and CYP2C19 with Tacrolimus Pharmacokinetics in Renal Transplant Recipients. Tacrolimus 76-86 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 35-41 30476735-11 2019 FK506 inhibited NFAT translocation to the nucleus and disrupted the interaction of TRPC6 with FKBP12. Tacrolimus 0-5 FKBP prolyl isomerase 1A Rattus norvegicus 94-100 31244435-0 2019 Association of Genetic Variants in CYP3A4, CYP3A5, CYP2C8, and CYP2C19 with Tacrolimus Pharmacokinetics in Renal Transplant Recipients. Tacrolimus 76-86 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 43-49 31244435-0 2019 Association of Genetic Variants in CYP3A4, CYP3A5, CYP2C8, and CYP2C19 with Tacrolimus Pharmacokinetics in Renal Transplant Recipients. Tacrolimus 76-86 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 51-57 31244435-0 2019 Association of Genetic Variants in CYP3A4, CYP3A5, CYP2C8, and CYP2C19 with Tacrolimus Pharmacokinetics in Renal Transplant Recipients. Tacrolimus 76-86 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 63-70 30251062-3 2019 The CYP3A5 (rs776746; CYP3A5*3) genotype was determined after monitoring and analysing tacrolimus blood concentrations. Tacrolimus 87-97 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 4-10 30415182-1 2019 Calcineurin-inhibitor induced pain syndrome (CIPS) is a condition characterized by lower extremity pain in patients receiving tacrolimus or cyclosporine therapy following organ transplantation. Tacrolimus 126-136 calcineurin binding protein 1 Homo sapiens 0-21 30251062-3 2019 The CYP3A5 (rs776746; CYP3A5*3) genotype was determined after monitoring and analysing tacrolimus blood concentrations. Tacrolimus 87-97 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 22-28 30251062-7 2019 Significant correlations were observed between C0 and area under the concentration-time curve (AUC0-12) of tacrolimus after the discontinuation of clotrimazole in the CYP3A5 expresser and non-expresser groups, respectively (R2 = 0.49 and 0.42, all P < 0.05), but not before the discontinuation of clotrimazole. Tacrolimus 107-117 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 167-173 30251062-8 2019 CONCLUSION: The effects of clotrimazole on tacrolimus pharmacokinetics in the CYP3A5 expresser patients were significantly greater than those in the CYP3A5 non-expresser patients. Tacrolimus 43-53 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 78-84 30251062-10 2019 Careful dose adjustment of tacrolimus based on CYP3A5 genotypes may be beneficial for the patients with heart transplants who are concomitantly treated with clotrimazole. Tacrolimus 27-37 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 47-53 30296431-9 2019 CONCLUSIONS: Younger age at the time of diagnosis with PBC or at liver transplantation, tacrolimus use, and biochemical markers of cholestasis after liver transplantation are associated with PBC recurrence. Tacrolimus 88-98 dihydrolipoamide S-acetyltransferase Homo sapiens 191-194 31497276-2 2019 Objective: To evaluate M235T and T174M polymorphisms of angiotensinogen gene along with some demographic and clinical factors including age; sex; body mass index (BMI); model for end-stage liver disease (MELD) score; prednisolone, mycophenolate mofetil and tacrolimus dose; and serum level in NODAT among liver recipients. Tacrolimus 257-267 angiotensinogen Homo sapiens 56-71 30318624-0 2018 Once-daily vs twice-daily tacrolimus for de novo living kidney transplantation patients including ABO/HLA compatible and incompatible: A randomized trial. Tacrolimus 26-36 ABO, alpha 1-3-N-acetylgalactosaminyltransferase and alpha 1-3-galactosyltransferase Homo sapiens 98-101 30648591-11 2019 KBrO3 increased the protein levels of these signals and the specific inhibitor, such as cyclosporine A and tacrolimus, attenuated the signaling in H9c2 cells at concentrations sufficient to inhibit calcineurin in addition to the reduction of mRNA levels of UBE3A, similar to ANP or BNP. Tacrolimus 107-117 ubiquitin protein ligase E3A Rattus norvegicus 257-262 30648591-11 2019 KBrO3 increased the protein levels of these signals and the specific inhibitor, such as cyclosporine A and tacrolimus, attenuated the signaling in H9c2 cells at concentrations sufficient to inhibit calcineurin in addition to the reduction of mRNA levels of UBE3A, similar to ANP or BNP. Tacrolimus 107-117 natriuretic peptide B Rattus norvegicus 282-285 29479631-1 2019 The calcineurin inhibitor tacrolimus, cornerstone of most immunosuppressive regimens, is a drug with a narrow therapeutic window: underexposure can lead to allograft rejection and overexposure can result in an increased incidence of infections, toxicity and malignancies. Tacrolimus 26-36 calcineurin binding protein 1 Homo sapiens 4-25 29479631-2 2019 Tacrolimus is metabolised in the liver and intestine by the cytochrome P450 3A (CYP3A) isoforms CYP3A4 and CYP3A5. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 60-78 29479631-2 2019 Tacrolimus is metabolised in the liver and intestine by the cytochrome P450 3A (CYP3A) isoforms CYP3A4 and CYP3A5. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 80-85 29479631-2 2019 Tacrolimus is metabolised in the liver and intestine by the cytochrome P450 3A (CYP3A) isoforms CYP3A4 and CYP3A5. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 96-102 29479631-2 2019 Tacrolimus is metabolised in the liver and intestine by the cytochrome P450 3A (CYP3A) isoforms CYP3A4 and CYP3A5. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 107-113 30489455-1 2019 BACKGROUND: CYP3A4/5 and P-glycoprotein (P-gp, ABCB1) affect tacrolimus (TAC) exposure in T cells and kidney cells. Tacrolimus 61-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 12-20 30489455-1 2019 BACKGROUND: CYP3A4/5 and P-glycoprotein (P-gp, ABCB1) affect tacrolimus (TAC) exposure in T cells and kidney cells. Tacrolimus 61-71 ATP binding cassette subfamily B member 1 Homo sapiens 25-39 30489455-1 2019 BACKGROUND: CYP3A4/5 and P-glycoprotein (P-gp, ABCB1) affect tacrolimus (TAC) exposure in T cells and kidney cells. Tacrolimus 61-71 ATP binding cassette subfamily B member 1 Homo sapiens 41-45 30489455-1 2019 BACKGROUND: CYP3A4/5 and P-glycoprotein (P-gp, ABCB1) affect tacrolimus (TAC) exposure in T cells and kidney cells. Tacrolimus 61-71 ATP binding cassette subfamily B member 1 Homo sapiens 47-52 30489455-1 2019 BACKGROUND: CYP3A4/5 and P-glycoprotein (P-gp, ABCB1) affect tacrolimus (TAC) exposure in T cells and kidney cells. Tacrolimus 73-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 12-20 30489455-1 2019 BACKGROUND: CYP3A4/5 and P-glycoprotein (P-gp, ABCB1) affect tacrolimus (TAC) exposure in T cells and kidney cells. Tacrolimus 73-76 ATP binding cassette subfamily B member 1 Homo sapiens 25-39 30489455-1 2019 BACKGROUND: CYP3A4/5 and P-glycoprotein (P-gp, ABCB1) affect tacrolimus (TAC) exposure in T cells and kidney cells. Tacrolimus 73-76 ATP binding cassette subfamily B member 1 Homo sapiens 41-45 30489455-1 2019 BACKGROUND: CYP3A4/5 and P-glycoprotein (P-gp, ABCB1) affect tacrolimus (TAC) exposure in T cells and kidney cells. Tacrolimus 73-76 ATP binding cassette subfamily B member 1 Homo sapiens 47-52 30537010-0 2019 TLR9 rs352139 Genetic Variant Promotes Tacrolimus Elimination in Chinese Liver Transplant Patients During the Early Posttransplantation Period. Tacrolimus 39-49 toll like receptor 9 Homo sapiens 0-4 30537010-9 2019 RESULTS: Tacrolimus dose-adjusted trough blood concentrations (C/D) ratios were significantly lower for donor TLR9 rs352139 AG/GG carriers than AA carriers at weeks 1, 2, and 3 after LT. Tacrolimus 9-19 toll like receptor 9 Homo sapiens 110-114 30537010-10 2019 In multivariate analysis, donor and recipient CYP3A5 rs776746 and donor TLR9 rs352139 were independent predictors of tacrolimus C/D ratios in the early period after transplantation in both cohorts. Tacrolimus 117-127 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 46-52 30537010-10 2019 In multivariate analysis, donor and recipient CYP3A5 rs776746 and donor TLR9 rs352139 were independent predictors of tacrolimus C/D ratios in the early period after transplantation in both cohorts. Tacrolimus 117-127 toll like receptor 9 Homo sapiens 72-76 30537010-13 2019 In addition, we demonstrated that the TLR9 rs352139 genetic variant promotes tacrolimus metabolism of liver cells via upregulation of CYP3A5, which is dependent on the repression of NF-kappaB/pregnane X receptor (PXR) signaling. Tacrolimus 77-87 toll like receptor 9 Homo sapiens 38-42 30537010-13 2019 In addition, we demonstrated that the TLR9 rs352139 genetic variant promotes tacrolimus metabolism of liver cells via upregulation of CYP3A5, which is dependent on the repression of NF-kappaB/pregnane X receptor (PXR) signaling. Tacrolimus 77-87 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 134-140 30537010-13 2019 In addition, we demonstrated that the TLR9 rs352139 genetic variant promotes tacrolimus metabolism of liver cells via upregulation of CYP3A5, which is dependent on the repression of NF-kappaB/pregnane X receptor (PXR) signaling. Tacrolimus 77-87 nuclear receptor subfamily 1 group I member 2 Homo sapiens 182-211 30537010-13 2019 In addition, we demonstrated that the TLR9 rs352139 genetic variant promotes tacrolimus metabolism of liver cells via upregulation of CYP3A5, which is dependent on the repression of NF-kappaB/pregnane X receptor (PXR) signaling. Tacrolimus 77-87 nuclear receptor subfamily 1 group I member 2 Homo sapiens 213-216 30537010-14 2019 CONCLUSIONS: Donor TLR9 rs352139 genetic variant facilitated tacrolimus elimination during the early stage after LT in Chinese patients, which might be related to the upregulation of CYP3A5 enzyme via the NF-kB/PXR signaling pathway. Tacrolimus 61-71 toll like receptor 9 Homo sapiens 19-23 30537010-14 2019 CONCLUSIONS: Donor TLR9 rs352139 genetic variant facilitated tacrolimus elimination during the early stage after LT in Chinese patients, which might be related to the upregulation of CYP3A5 enzyme via the NF-kB/PXR signaling pathway. Tacrolimus 61-71 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 183-189 30537010-14 2019 CONCLUSIONS: Donor TLR9 rs352139 genetic variant facilitated tacrolimus elimination during the early stage after LT in Chinese patients, which might be related to the upregulation of CYP3A5 enzyme via the NF-kB/PXR signaling pathway. Tacrolimus 61-71 nuclear receptor subfamily 1 group I member 2 Homo sapiens 211-214 30730287-7 2019 Tacrolimus apparent clearance was significantly reduced in CYP3A5 nonexpressers (CYP3A5*3/*3), concomitant with azole antifungal drugs and Wuzhi capsule (WZ). Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 59-65 30730287-7 2019 Tacrolimus apparent clearance was significantly reduced in CYP3A5 nonexpressers (CYP3A5*3/*3), concomitant with azole antifungal drugs and Wuzhi capsule (WZ). Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 81-87 30293884-7 2019 At week 24, peripheral blood CD4+CD25+high T cells with tacrolimus decreased significantly (P<0.01), but increased significantly without tacrolimus (P<0.01). Tacrolimus 56-66 CD4 molecule Homo sapiens 29-32 30293884-7 2019 At week 24, peripheral blood CD4+CD25+high T cells with tacrolimus decreased significantly (P<0.01), but increased significantly without tacrolimus (P<0.01). Tacrolimus 56-66 interferon stimulated exonuclease gene 20 Homo sapiens 33-37 30293884-9 2019 Interferon (IFN)-gamma concentrations in peripheral blood also diminished significantly with tacrolimus (P<0.01). Tacrolimus 93-103 interferon gamma Homo sapiens 0-22 31255354-0 2019 Impact of CYP3A5 Genetic Polymorphism on Intrapatient Variability of Tacrolimus Exposure in Chinese Kidney Transplant Recipients. Tacrolimus 69-79 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 10-16 31582605-9 2019 A physiologically based pharmacokinetic model adapted to tacrolimus pharmacokinetic data in patients who underwent living-donor liver transplantation was constructed, and clarified that oral clearance of this drug was affected by CYP3A5 genotypes in both the liver and intestine to the same extent. Tacrolimus 57-67 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 230-236 30584253-0 2018 Whole exome sequencing for the identification of CYP3A7 variants associated with tacrolimus concentrations in kidney transplant patients. Tacrolimus 81-91 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 49-55 30584253-10 2018 The combined set LMM showed that only CYP3A7 rs2257401 was associated with tacrolimus C0/D after adjusting for patient age, albumin, and creatinine. Tacrolimus 75-85 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 38-44 30584253-11 2018 The CYP3A7 rs2257401 genotype variant showed a significant difference on the tacrolimus C0/D in those expressing CYP3A5, showing its own effect. Tacrolimus 77-87 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 4-10 30584253-11 2018 The CYP3A7 rs2257401 genotype variant showed a significant difference on the tacrolimus C0/D in those expressing CYP3A5, showing its own effect. Tacrolimus 77-87 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 113-119 30584253-12 2018 The results suggest that CYP3A7 rs2257401 may serve as a significant genetic marker for tacrolimus pharmacokinetics in kidney transplantation. Tacrolimus 88-98 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 25-31 30348662-0 2019 FK506 Resistance of Saccharomyces cerevisiae Pdr5 and Candida albicans Cdr1 Involves Mutations in the Transmembrane Domains and Extracellular Loops. Tacrolimus 0-5 ATP-binding cassette multidrug transporter PDR5 Saccharomyces cerevisiae S288C 45-49 30348662-3 2019 Thus, to obtain further insights we searched for FK506-resistant mutants of Saccharomyces cerevisiae cells overexpressing either the endogenous multidrug efflux pump Pdr5 or its Candida albicans orthologue, Cdr1. Tacrolimus 49-54 ATP-binding cassette multidrug transporter PDR5 Saccharomyces cerevisiae S288C 166-170 30348662-4 2019 A simple but powerful screen gave 69 FK506-resistant mutants with, between them, 72 mutations in either Pdr5 or Cdr1. Tacrolimus 37-42 ATP-binding cassette multidrug transporter PDR5 Saccharomyces cerevisiae S288C 104-108 30348662-7 2019 We propose that FK506 inhibits Pdr5 and Cdr1 drug efflux by slowing transporter opening and/or substrate release, and that FK506 resistance of Pdr5/Cdr1 drug efflux is achieved by modifying critical intramolecular contact points that, when mutated, enable the cotransport of FK506 with other pump substrates. Tacrolimus 16-21 ATP-binding cassette multidrug transporter PDR5 Saccharomyces cerevisiae S288C 31-35 30348662-7 2019 We propose that FK506 inhibits Pdr5 and Cdr1 drug efflux by slowing transporter opening and/or substrate release, and that FK506 resistance of Pdr5/Cdr1 drug efflux is achieved by modifying critical intramolecular contact points that, when mutated, enable the cotransport of FK506 with other pump substrates. Tacrolimus 123-128 ATP-binding cassette multidrug transporter PDR5 Saccharomyces cerevisiae S288C 143-147 30348662-7 2019 We propose that FK506 inhibits Pdr5 and Cdr1 drug efflux by slowing transporter opening and/or substrate release, and that FK506 resistance of Pdr5/Cdr1 drug efflux is achieved by modifying critical intramolecular contact points that, when mutated, enable the cotransport of FK506 with other pump substrates. Tacrolimus 123-128 ATP-binding cassette multidrug transporter PDR5 Saccharomyces cerevisiae S288C 143-147 30576367-0 2018 Alteration of urinary neutrophil gelatinase-associated lipocalin as a predictor of tacrolimus-induced chronic renal allograft fibrosis in tacrolimus dose adjustments following kidney transplantation. Tacrolimus 83-93 lipocalin 2 Homo sapiens 22-64 30576367-0 2018 Alteration of urinary neutrophil gelatinase-associated lipocalin as a predictor of tacrolimus-induced chronic renal allograft fibrosis in tacrolimus dose adjustments following kidney transplantation. Tacrolimus 138-148 lipocalin 2 Homo sapiens 22-64 30459239-9 2018 Further analysis showed that addition of LY294002 and FK-506 partly attenuated these protective effects of OP-1 against NP cell apoptosis and activation of the PI3K/Akt/mTOR pathway in a hyperosmotic culture. Tacrolimus 54-60 AKT serine/threonine kinase 1 Rattus norvegicus 165-168 30459239-9 2018 Further analysis showed that addition of LY294002 and FK-506 partly attenuated these protective effects of OP-1 against NP cell apoptosis and activation of the PI3K/Akt/mTOR pathway in a hyperosmotic culture. Tacrolimus 54-60 mechanistic target of rapamycin kinase Rattus norvegicus 169-173 29689130-5 2018 Genotyping the donor for the ABCB1 c.1199 G>A (exon 11, rs2229109) allele may be of interest before prescribing tacrolimus to the recipient, although this polymorphism is rather rare and its effect may be limited to certain mechanisms of graft loss. Tacrolimus 115-125 ATP binding cassette subfamily B member 1 Homo sapiens 29-34 30524720-2 2018 The aim of this study is to compare the carotid intima-media thickness (cIMT) between de novo tacrolimus/mycophenolate and tacrolimus/sirolimus at low doses. Tacrolimus 123-133 CIMT Homo sapiens 72-76 30524720-9 2018 Conclusions: The use of sirolimus plus tacrolimus de novo in kidney transplantation is associated with a reduction in cIMT after 12 months, a decrease more significant than seen with the combination of mycophenolate plus tacrolimus. Tacrolimus 39-49 CIMT Homo sapiens 118-122 31483188-8 2019 Taken together, we have shown that JAK3 inhibitor could be used in replacement of tacrolimus in a highly translatable NHP islet transplantation model and these results suggest that JAK3 inhibitor will be potentially incorporated in human allogeneic islet transplantation. Tacrolimus 82-92 Janus kinase 3 Homo sapiens 35-39 30524720-2 2018 The aim of this study is to compare the carotid intima-media thickness (cIMT) between de novo tacrolimus/mycophenolate and tacrolimus/sirolimus at low doses. Tacrolimus 94-104 CIMT Homo sapiens 72-76 30318624-1 2018 Tacrolimus (TAC) is available as a twice-daily capsule (TAC-BID), once-daily capsule (TAC-QD), and once-daily tablet. Tacrolimus 0-10 BH3 interacting domain death agonist Homo sapiens 60-63 30498175-1 2018 AIM: The current study will attempt to throw light on the role of desmoglein 1 and desmoglein 3 in the pathogenesis of erosive lichen planus and their response to topical application of tacrolimus. Tacrolimus 186-196 desmoglein 1 Homo sapiens 66-78 29691732-0 2018 Impact of the CYP3A5*1 Allele on the Pharmacokinetics of Tacrolimus in Japanese Heart Transplant Patients. Tacrolimus 57-67 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 14-20 29691732-2 2018 A common variant of the cytochrome P450 (CYP) 3A5 gene, CYP3A5*3, affects blood concentrations of tacrolimus. Tacrolimus 98-108 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 24-49 29691732-2 2018 A common variant of the cytochrome P450 (CYP) 3A5 gene, CYP3A5*3, affects blood concentrations of tacrolimus. Tacrolimus 98-108 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 56-62 29691732-4 2018 We retrospectively examined the impact of the CYP3A5 genotype on tacrolimus pharmacokinetics at the early stage of heart transplantation. Tacrolimus 65-75 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 46-52 29691732-11 2018 These results demonstrate the importance of the CYP3A5 genotype in tacrolimus dose optimization based on therapeutic drug monitoring after heart transplantation. Tacrolimus 67-77 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 48-54 30288799-10 2018 CONCLUSION: Topical calcineurin inhibitors are a suitable therapy for AD, and selection of the specific TCI should be based on factors which differentiate tacrolimus from pimecrolimus. Tacrolimus 155-165 latexin Homo sapiens 104-107 30442353-8 2018 The association of T/C and C/C genotypes in the SNP rs11706052 (IMPDH2) with the occurrence of rejection episodes considering only patients who received immunosuppressive drug MMF associated with cyclosporine or tacrolimus and corticoids, demonstrated association with a protection against rejection 15.6-fold. Tacrolimus 212-222 inosine monophosphate dehydrogenase 2 Homo sapiens 64-70 30577195-1 2018 BACKGROUND: The purpose of this study is to explore the association of CYP3A5, ABCB1, and CYP2C8 polymorphisms with the risk of developing early kidney impairment in Chinese liver transplant recipients receiving tacrolimus. Tacrolimus 212-222 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 71-77 30577195-11 2018 CONCLUSIONS: CYP2C8*3 and CYP3A5*3 appear to be predictive of risk of tacrolimus-induced early renal impairment. Tacrolimus 70-80 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 13-19 30577195-11 2018 CONCLUSIONS: CYP2C8*3 and CYP3A5*3 appear to be predictive of risk of tacrolimus-induced early renal impairment. Tacrolimus 70-80 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 26-32 30341186-9 2018 Analysis of the effects of FK506 and methylprednisolone, common immunosuppressive agents following organ transplantation, suggested a link between these immunosuppressive drugs and impaired macrophage migration via the Cx43/iNOS/Src/FAK pathway. Tacrolimus 27-32 gap junction protein, alpha 1 Mus musculus 219-223 30341186-9 2018 Analysis of the effects of FK506 and methylprednisolone, common immunosuppressive agents following organ transplantation, suggested a link between these immunosuppressive drugs and impaired macrophage migration via the Cx43/iNOS/Src/FAK pathway. Tacrolimus 27-32 nitric oxide synthase 2, inducible Mus musculus 224-228 30341186-9 2018 Analysis of the effects of FK506 and methylprednisolone, common immunosuppressive agents following organ transplantation, suggested a link between these immunosuppressive drugs and impaired macrophage migration via the Cx43/iNOS/Src/FAK pathway. Tacrolimus 27-32 Rous sarcoma oncogene Mus musculus 229-232 30341186-9 2018 Analysis of the effects of FK506 and methylprednisolone, common immunosuppressive agents following organ transplantation, suggested a link between these immunosuppressive drugs and impaired macrophage migration via the Cx43/iNOS/Src/FAK pathway. Tacrolimus 27-32 PTK2 protein tyrosine kinase 2 Mus musculus 233-236 30166405-1 2018 CYP3A5 genotype is a major determinant of tacrolimus clearance, and has been shown to affect systemic tacrolimus metabolite/parent ratios in healthy volunteers, which may have implications for efficacy and toxicity. Tacrolimus 42-52 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 30166405-1 2018 CYP3A5 genotype is a major determinant of tacrolimus clearance, and has been shown to affect systemic tacrolimus metabolite/parent ratios in healthy volunteers, which may have implications for efficacy and toxicity. Tacrolimus 102-112 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 30166405-2 2018 In a cohort of 50 renal transplant recipients who underwent quantification of CYP3A4 activity using the oral midazolam drug probe, we confirmed that CYP3A5 genotype is the single most important determinant of tacrolimus metabolite/parent ratio [CYP3A5 expressors displayed 2.7- and 2-fold higher relative exposure to 13-desmethyltacrolimus (DMT) and 31-DMT, respectively; P < 0.001]. Tacrolimus 209-219 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 78-84 30166405-2 2018 In a cohort of 50 renal transplant recipients who underwent quantification of CYP3A4 activity using the oral midazolam drug probe, we confirmed that CYP3A5 genotype is the single most important determinant of tacrolimus metabolite/parent ratio [CYP3A5 expressors displayed 2.7- and 2-fold higher relative exposure to 13-desmethyltacrolimus (DMT) and 31-DMT, respectively; P < 0.001]. Tacrolimus 209-219 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 149-155 30166405-2 2018 In a cohort of 50 renal transplant recipients who underwent quantification of CYP3A4 activity using the oral midazolam drug probe, we confirmed that CYP3A5 genotype is the single most important determinant of tacrolimus metabolite/parent ratio [CYP3A5 expressors displayed 2.7- and 2-fold higher relative exposure to 13-desmethyltacrolimus (DMT) and 31-DMT, respectively; P < 0.001]. Tacrolimus 209-219 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 245-251 30166405-4 2018 Additional analyses in 16 healthy volunteers showed that dual pharmacological inhibition of CYP3A4 and P-glycoprotein using itraconazole resulted in increased tacrolimus metabolite/parent ratios (+65%, +112%, and 25% for 13-, 15-, and 31-DMT, respectively; P < 0.01). Tacrolimus 159-169 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 92-98 30166405-4 2018 Additional analyses in 16 healthy volunteers showed that dual pharmacological inhibition of CYP3A4 and P-glycoprotein using itraconazole resulted in increased tacrolimus metabolite/parent ratios (+65%, +112%, and 25% for 13-, 15-, and 31-DMT, respectively; P < 0.01). Tacrolimus 159-169 ATP binding cassette subfamily B member 1 Homo sapiens 103-117 30019212-0 2018 Evaluating tacrolimus pharmacokinetic models in adult renal transplant recipients with different CYP3A5 genotypes. Tacrolimus 11-21 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 97-103 30178515-1 2018 BACKGROUND: Tacrolimus pharmacokinetics are influenced by age and CYP3A5 genotype with CYP3A5 expressors (CYP3A5*1/*1 or *1/*3) being fast metabolizers. Tacrolimus 12-22 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 66-72 30178515-1 2018 BACKGROUND: Tacrolimus pharmacokinetics are influenced by age and CYP3A5 genotype with CYP3A5 expressors (CYP3A5*1/*1 or *1/*3) being fast metabolizers. Tacrolimus 12-22 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 87-93 30178515-1 2018 BACKGROUND: Tacrolimus pharmacokinetics are influenced by age and CYP3A5 genotype with CYP3A5 expressors (CYP3A5*1/*1 or *1/*3) being fast metabolizers. Tacrolimus 12-22 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 87-93 30178515-3 2018 OBJECTIVE: To determine whether age and CYP3A5 genotype-guided starting dose of tacrolimus result in earlier attainment of therapeutic drug concentrations. Tacrolimus 80-90 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 40-46 30178515-11 2018 CONCLUSIONS: CYP3A5 genotype-guided dosing stratified by age resulted in earlier attainment of therapeutic tacrolimus concentrations and fewer out-of-range concentrations. Tacrolimus 107-117 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 13-19 30401377-2 2018 METHODS: From October 2005 to November 2016, 61 LDLT patients administered tacrolimus, who could be genotyped for CYP3A5*3 and *1, were chosen from the electronic record database. Tacrolimus 75-85 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 114-120 30181374-2 2018 In mammals, FK506 inhibits the calcineurin-nuclear factor of activated T cells (NFAT) pathway to prevent T-cell proliferation by forming a ternary complex with its binding protein, FKBP12, and calcineurin. Tacrolimus 12-17 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 181-187 30388516-10 2018 Moreover, knockdown of PPP3R1 in Jurkat T cell line enhanced the immunosuppressive effect of tacrolimus. Tacrolimus 93-103 protein phosphatase 3 regulatory subunit B, alpha Homo sapiens 23-29 30388516-12 2018 The functional polymorphism might alter PPP3R1 expression via modulating the interaction of miR-582-5p with PPP3R1, which further affected the immunosuppressive effect of tacrolimus. Tacrolimus 171-181 protein phosphatase 3 regulatory subunit B, alpha Homo sapiens 40-46 30388516-12 2018 The functional polymorphism might alter PPP3R1 expression via modulating the interaction of miR-582-5p with PPP3R1, which further affected the immunosuppressive effect of tacrolimus. Tacrolimus 171-181 microRNA 582 Homo sapiens 92-99 30388516-12 2018 The functional polymorphism might alter PPP3R1 expression via modulating the interaction of miR-582-5p with PPP3R1, which further affected the immunosuppressive effect of tacrolimus. Tacrolimus 171-181 protein phosphatase 3 regulatory subunit B, alpha Homo sapiens 108-114 30222497-9 2018 The proportion of terminal deoxynucleotidyl transferase-mediated nick end labeling-positive cells and mRNA levels of inflammatory cytokines were higher in tacrolimus-treated corneas, compared with controls. Tacrolimus 155-165 deoxynucleotidyltransferase, terminal Mus musculus 18-55 30483129-11 2018 Moreover, the present study reveals that combination of radicicol, VER-155008, cyclosporine A, and FK506, which are specific pharmacological inhibitors of Hsp90, Hsp70, Cyps, and FKBPs, respectively, resulted in a stronger inhibition of intoxication of cells with C2 toxin compared to application of the single inhibitors. Tacrolimus 99-104 heat shock protein 90 alpha family class A member 1 Homo sapiens 155-160 30483129-11 2018 Moreover, the present study reveals that combination of radicicol, VER-155008, cyclosporine A, and FK506, which are specific pharmacological inhibitors of Hsp90, Hsp70, Cyps, and FKBPs, respectively, resulted in a stronger inhibition of intoxication of cells with C2 toxin compared to application of the single inhibitors. Tacrolimus 99-104 heat shock protein family A (Hsp70) member 4 Homo sapiens 162-167 30498355-0 2018 CYP3A5 genotype-based model to predict tacrolimus dosage in the early postoperative period after living donor liver transplantation. Tacrolimus 39-49 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 29989311-9 2018 Multivariate analysis showed that high tacrolimus trough level variability was associated with >8-fold increased risk for any rejection beyond the first year post-HTx (P = .011). Tacrolimus 39-49 Zic family member 3 Homo sapiens 166-169 30132043-6 2018 Pharmacologic inhibition of mTOR signaling using rapamycin (20 nM), FK506 (5 nM), or 4EGI-1 (1 microM), and siRNA knockdown of mTOR, or the mTOR complex binding proteins, raptor or rictor, blocked PCB 95-induced dendritic growth. Tacrolimus 68-73 mechanistic target of rapamycin kinase Rattus norvegicus 28-32 29708622-0 2018 Evaluation of tacrolimus-related CYP3A5 genotyping in China: Results from the First External Quality Assessment Exercise. Tacrolimus 14-24 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 33-39 30498175-1 2018 AIM: The current study will attempt to throw light on the role of desmoglein 1 and desmoglein 3 in the pathogenesis of erosive lichen planus and their response to topical application of tacrolimus. Tacrolimus 186-196 desmoglein 3 Homo sapiens 83-95 30498175-11 2018 Also, there is a significant decrease in the level of anti-Dsgl and anti-Dsg3 autoantibodies with topical tacrolimus 0.1% ointment. Tacrolimus 106-116 desmoglein 3 Homo sapiens 73-77 30498175-12 2018 CLINICAL SIGNIFICANCE: Monitoring the serum level of antibodies against keratinocyte cadherins Dsg 1 and Dsg 3 can be used to evaluate the effect of topical application of tacrolimus on Erosive Oral lichen planus. Tacrolimus 172-182 desmoglein 1 Homo sapiens 95-100 30498175-12 2018 CLINICAL SIGNIFICANCE: Monitoring the serum level of antibodies against keratinocyte cadherins Dsg 1 and Dsg 3 can be used to evaluate the effect of topical application of tacrolimus on Erosive Oral lichen planus. Tacrolimus 172-182 desmoglein 3 Homo sapiens 105-110 29878980-0 2018 Impact of POR and CYP3A5 Polymorphisms on Trough Concentration to Dose Ratio of Tacrolimus in the Early Post-operative Period Following Kidney Transplantation. Tacrolimus 80-90 cytochrome p450 oxidoreductase Homo sapiens 10-13 29878980-0 2018 Impact of POR and CYP3A5 Polymorphisms on Trough Concentration to Dose Ratio of Tacrolimus in the Early Post-operative Period Following Kidney Transplantation. Tacrolimus 80-90 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 18-24 29878980-3 2018 The significant impact of CYP3A5*3 polymorphisms on tacrolimus exposure has been reported. Tacrolimus 52-62 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 26-32 29878980-4 2018 Conflicting results of the additional influence of POR*28 polymorphisms on tacrolimus pharmacokinetic interindividual variability have been observed among different populations. Tacrolimus 75-85 cytochrome p450 oxidoreductase Homo sapiens 51-54 29878980-5 2018 The objective of this study was to explore the interaction between POR*28 and CYP3A5*3 polymorphisms and their main effects on tacrolimus trough concentration to dose ratios on day 7 after kidney transplantation. Tacrolimus 127-137 cytochrome p450 oxidoreductase Homo sapiens 67-70 29878980-5 2018 The objective of this study was to explore the interaction between POR*28 and CYP3A5*3 polymorphisms and their main effects on tacrolimus trough concentration to dose ratios on day 7 after kidney transplantation. Tacrolimus 127-137 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 78-84 29878980-20 2018 CONCLUSIONS: After adjusting for the influences of hemoglobin, age, and prednisolone dose, significant impacts of the CYP3A5 and POR polymorphisms on tacrolimus exposure were found. Tacrolimus 150-160 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 118-124 29878980-20 2018 CONCLUSIONS: After adjusting for the influences of hemoglobin, age, and prednisolone dose, significant impacts of the CYP3A5 and POR polymorphisms on tacrolimus exposure were found. Tacrolimus 150-160 cytochrome p450 oxidoreductase Homo sapiens 129-132 30316389-1 2018 BACKGROUND: Inhibition of calcineurin inhibitor (CNI) metabolism with diltiazem reduces the dose of tacrolimus required to achieve its therapeutic blood concentration in kidney transplant recipients (KTRs). Tacrolimus 100-110 calcineurin binding protein 1 Homo sapiens 26-47 30208561-0 2018 FK506 Attenuates the MRP1-Mediated Chemoresistant Phenotype in Glioblastoma Stem-Like Cells. Tacrolimus 0-5 ATP binding cassette subfamily C member 1 Homo sapiens 21-25 29708622-2 2018 The cytochrome P450 3A5 (CYP3A5) has been proved to be associated with tacrolimus dose requirement. Tacrolimus 71-81 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 4-23 29708622-2 2018 The cytochrome P450 3A5 (CYP3A5) has been proved to be associated with tacrolimus dose requirement. Tacrolimus 71-81 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 25-31 29708622-3 2018 Molecular detection for CYP3A5 genotyping is demanded for the optimization of treatments of tacrolimus. Tacrolimus 92-102 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 24-30 30254425-6 2018 Furthermore, both tacrolimus and anti-VEGF significantly decreased the VEGF-A expression on Days 7 and 14, with no significant difference between the two groups. Tacrolimus 18-28 vascular endothelial growth factor A Rattus norvegicus 71-77 30254425-8 2018 Additionally, the expression of IL-1beta, IL-6, monocyte chemotactic protein-1, macrophage inflammatory protein-1alpha and TGF-beta were significantly decreased by tacrolimus. Tacrolimus 164-174 interleukin 1 beta Rattus norvegicus 32-40 30254425-8 2018 Additionally, the expression of IL-1beta, IL-6, monocyte chemotactic protein-1, macrophage inflammatory protein-1alpha and TGF-beta were significantly decreased by tacrolimus. Tacrolimus 164-174 interleukin 6 Rattus norvegicus 42-46 30254425-8 2018 Additionally, the expression of IL-1beta, IL-6, monocyte chemotactic protein-1, macrophage inflammatory protein-1alpha and TGF-beta were significantly decreased by tacrolimus. Tacrolimus 164-174 C-C motif chemokine ligand 2 Rattus norvegicus 48-78 30254425-8 2018 Additionally, the expression of IL-1beta, IL-6, monocyte chemotactic protein-1, macrophage inflammatory protein-1alpha and TGF-beta were significantly decreased by tacrolimus. Tacrolimus 164-174 C-C motif chemokine ligand 3 Rattus norvegicus 80-118 30254425-8 2018 Additionally, the expression of IL-1beta, IL-6, monocyte chemotactic protein-1, macrophage inflammatory protein-1alpha and TGF-beta were significantly decreased by tacrolimus. Tacrolimus 164-174 transforming growth factor, beta 1 Rattus norvegicus 123-131 30208561-3 2018 Tacrolimus (FK506) has been identified as an MRP1 regulator in differentiated glioblastoma (GBM) cells (non-GSCs); however, the effect of FK506 on GSCs is currently unknown. Tacrolimus 0-10 ATP binding cassette subfamily C member 1 Homo sapiens 45-49 30208561-3 2018 Tacrolimus (FK506) has been identified as an MRP1 regulator in differentiated glioblastoma (GBM) cells (non-GSCs); however, the effect of FK506 on GSCs is currently unknown. Tacrolimus 12-17 ATP binding cassette subfamily C member 1 Homo sapiens 45-49 30208561-4 2018 The objective of the following research is to evaluate the effect of FK506 on the MRP1-related chemo-resistant phenotype of GSCs. Tacrolimus 69-74 ATP binding cassette subfamily C member 1 Homo sapiens 82-86 30208561-12 2018 In vivo, the FK506/Vincristine treatment decreased the tumor size as well as ki67, Glial Fibrillary Acidic Protein (GFAP), and nestin expression. Tacrolimus 13-18 glial fibrillary acidic protein Homo sapiens 83-114 30208561-12 2018 In vivo, the FK506/Vincristine treatment decreased the tumor size as well as ki67, Glial Fibrillary Acidic Protein (GFAP), and nestin expression. Tacrolimus 13-18 glial fibrillary acidic protein Homo sapiens 116-120 30208561-13 2018 We conclude that FK506 confers a chemo-sensitive phenotype to MRP1-drug substrate in GSCs. Tacrolimus 17-22 ATP binding cassette subfamily C member 1 Homo sapiens 62-66 29603629-0 2018 CYP3A5*3 and ABCB1 61A>G Significantly Influence Dose-adjusted Trough Blood Tacrolimus Concentrations in the First Three Months Post-Kidney Transplantation. Tacrolimus 79-89 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 29790290-0 2018 Tacrolimus prevents von Willebrand factor secretion by allostimulated human glomerular endothelium. Tacrolimus 0-10 von Willebrand factor Homo sapiens 20-41 29790290-5 2018 Therefore, we hypothesized that tacrolimus would prevent alloantibody-induced glomerular lesions, in part via inhibition of vWF secretion from endothelial cells. Tacrolimus 32-42 von Willebrand factor Homo sapiens 124-127 29790290-7 2018 We observed that tacrolimus treatment decreased vWF secretion after stimulation with both classes of anti-HLA antibodies and decreased platelet adhesion on allostimulated endothelial cells in a microfluidic chamber. Tacrolimus 17-27 von Willebrand factor Homo sapiens 48-51 29790290-8 2018 In kidney recipients, tacrolimus trough levels were negatively associated with vWF blood levels. Tacrolimus 22-32 von Willebrand factor Homo sapiens 79-82 29603629-0 2018 CYP3A5*3 and ABCB1 61A>G Significantly Influence Dose-adjusted Trough Blood Tacrolimus Concentrations in the First Three Months Post-Kidney Transplantation. Tacrolimus 79-89 ATP binding cassette subfamily B member 1 Homo sapiens 13-18 29330784-12 2018 A multivariate analysis of variance revealed that the tacrolimus concentration in oral fluids is related to the tacrolimus concentration in whole blood and tacrolimus plasma-binding proteins including albumin and cholesterol. Tacrolimus 54-64 albumin Homo sapiens 201-208 29330784-12 2018 A multivariate analysis of variance revealed that the tacrolimus concentration in oral fluids is related to the tacrolimus concentration in whole blood and tacrolimus plasma-binding proteins including albumin and cholesterol. Tacrolimus 112-122 albumin Homo sapiens 201-208 29330784-12 2018 A multivariate analysis of variance revealed that the tacrolimus concentration in oral fluids is related to the tacrolimus concentration in whole blood and tacrolimus plasma-binding proteins including albumin and cholesterol. Tacrolimus 112-122 albumin Homo sapiens 201-208 30031280-12 2018 TQ and tacrolimus also significantly attenuated mRNA expression levels of IL-4, IL-5 and IFN-gamma (p < 0.001). Tacrolimus 7-17 interleukin 4 Mus musculus 74-78 29989311-1 2018 Tacrolimus, the major immunosuppressant after heart transplant (HTx) therapy, is a narrow therapeutic index drug. Tacrolimus 0-10 Zic family member 3 Homo sapiens 64-67 29775201-1 2018 Tacrolimus exhibits inter-patient pharmacokinetic variability attributed to CYP3A5 isoenzymes and the efflux transporter, P-glycoprotein. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 76-82 29775201-1 2018 Tacrolimus exhibits inter-patient pharmacokinetic variability attributed to CYP3A5 isoenzymes and the efflux transporter, P-glycoprotein. Tacrolimus 0-10 ATP binding cassette subfamily B member 1 Homo sapiens 122-136 29775201-3 2018 An established guideline provides tacrolimus genotype dosing recommendations based on CYP3A5*1(W/T) and loss of protein function variants: CYP3A5*3 (rs776746), CYP3A5*6 (rs10264272), CYP3A5*7 (rs41303343) and may provide more comprehensive race-adjusted dosing recommendations. Tacrolimus 34-44 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 86-92 29775201-3 2018 An established guideline provides tacrolimus genotype dosing recommendations based on CYP3A5*1(W/T) and loss of protein function variants: CYP3A5*3 (rs776746), CYP3A5*6 (rs10264272), CYP3A5*7 (rs41303343) and may provide more comprehensive race-adjusted dosing recommendations. Tacrolimus 34-44 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 139-145 29775201-3 2018 An established guideline provides tacrolimus genotype dosing recommendations based on CYP3A5*1(W/T) and loss of protein function variants: CYP3A5*3 (rs776746), CYP3A5*6 (rs10264272), CYP3A5*7 (rs41303343) and may provide more comprehensive race-adjusted dosing recommendations. Tacrolimus 34-44 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 139-145 29775201-3 2018 An established guideline provides tacrolimus genotype dosing recommendations based on CYP3A5*1(W/T) and loss of protein function variants: CYP3A5*3 (rs776746), CYP3A5*6 (rs10264272), CYP3A5*7 (rs41303343) and may provide more comprehensive race-adjusted dosing recommendations. Tacrolimus 34-44 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 139-145 29775201-11 2018 The CYP3A5*3*6*7 metabolic composite was significantly associated with tacrolimus clearance (P value < .05), which was faster in extensive (mean: 45.0 L/hr) and intermediate (29.5 L/hr) metabolizers than poor metabolizers (19.8 L/hr). Tacrolimus 71-81 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 4-10 29775201-12 2018 Simulations support CYP3A5*3*6*7 genotype-based tacrolimus dosing to enhance general race-adjusted regimens, with dose increases of 1.5-fold and 2-fold, respectively, in intermediate and extensive metabolizers for comparable exposures to poor metabolizers. Tacrolimus 48-58 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 20-26 29775201-13 2018 This model offers a novel approach to determine tacrolimus dosing adjustments that maintain comparable therapeutic exposure between black and white recipients with different CYP3A5 genotypes. Tacrolimus 48-58 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 174-180 30031280-12 2018 TQ and tacrolimus also significantly attenuated mRNA expression levels of IL-4, IL-5 and IFN-gamma (p < 0.001). Tacrolimus 7-17 interleukin 5 Mus musculus 80-84 30031280-12 2018 TQ and tacrolimus also significantly attenuated mRNA expression levels of IL-4, IL-5 and IFN-gamma (p < 0.001). Tacrolimus 7-17 interferon gamma Mus musculus 89-98 29733390-11 2018 Independently, the PXR G7635G SNP is related to this increase, proving the role of PXR in tacrolimus metabolism. Tacrolimus 90-100 nuclear receptor subfamily 1 group I member 2 Homo sapiens 19-22 29733390-0 2018 Increase in tacrolimus exposure after steroid tapering is influenced by CYP3A5 and pregnane X receptor genetic polymorphisms in renal transplant recipients. Tacrolimus 12-22 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 72-78 29733390-11 2018 Independently, the PXR G7635G SNP is related to this increase, proving the role of PXR in tacrolimus metabolism. Tacrolimus 90-100 nuclear receptor subfamily 1 group I member 2 Homo sapiens 83-86 29733390-0 2018 Increase in tacrolimus exposure after steroid tapering is influenced by CYP3A5 and pregnane X receptor genetic polymorphisms in renal transplant recipients. Tacrolimus 12-22 nuclear receptor subfamily 1 group I member 2 Homo sapiens 83-102 29535109-14 2018 CYP3A5 polymorphism had a significant impact on tacrolimus concentration. Tacrolimus 48-58 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 29733390-1 2018 Background: Tacrolimus, a drug for prevention of rejection after kidney transplantation, has a narrow therapeutic window and is metabolized by the cytochrome P540 3A (CYP3A) system. Tacrolimus 12-22 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 147-165 29733390-1 2018 Background: Tacrolimus, a drug for prevention of rejection after kidney transplantation, has a narrow therapeutic window and is metabolized by the cytochrome P540 3A (CYP3A) system. Tacrolimus 12-22 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 167-172 29733390-5 2018 Methods: In a cohort of renal transplant recipients, the influence of CYP3A5 and PXR SNPs (A7635G, C8055T and C25385T) on the dose-normalized Tacrolimus trough concentration (DnC0) and their potential interaction with each other after steroid taper were analysed by linear regression. Tacrolimus 142-152 nuclear receptor subfamily 1 group I member 2 Homo sapiens 81-84 30092051-3 2018 Tacrolimus (0.2 mg/kg daily) was administered from day 1 to day 30 (TAC1) or from day 7 to day 30 (TAC7), respectively. Tacrolimus 0-10 tachykinin, precursor 1 Rattus norvegicus 68-72 29855074-0 2018 Effect of CYP3A5*1 expression on tacrolimus required dose after liver transplantation: A systematic review and meta-analysis. Tacrolimus 33-43 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 10-16 29855074-1 2018 We systematically collected eligible data to measure the effect of CYP3A5*1 expression on personalized tacrolimus therapy. Tacrolimus 103-113 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 67-73 29855074-2 2018 Six databases were searched for studies on adult liver transplant recipients and donors of liver graft which reported tacrolimus dose requirement, trough blood concentration, and/or concentration/dose (C/D) ratio in expressers and nonexpressers of CYP3A5*1. Tacrolimus 118-128 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 248-254 29855074-8 2018 CYP3A5*1 expression in recipients increased tacrolimus required dose by 0.023 at first, 0.022 at third, and 0.012 mg/kg/day at sixth month. Tacrolimus 44-54 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 29855074-10 2018 Considering CYP3A5*1 polymorphism can be helpful in individualization of tacrolimus efficient dose prior to administration, and it can remove initial high-risk lag time (over/underdose period before reaching target blood level) at first few days post-transplantation. Tacrolimus 73-83 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 12-18 29920787-2 2018 Single nucleotide polymorphisms (SNPs) in genes important to tacrolimus bioavailability and clearance (ABCB1, CYP3A4, and CYP3A5) are associated with differences in tacrolimus pharmacokinetics. Tacrolimus 61-71 ATP binding cassette subfamily B member 1 Homo sapiens 103-108 29920787-2 2018 Single nucleotide polymorphisms (SNPs) in genes important to tacrolimus bioavailability and clearance (ABCB1, CYP3A4, and CYP3A5) are associated with differences in tacrolimus pharmacokinetics. Tacrolimus 61-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 110-116 29920787-2 2018 Single nucleotide polymorphisms (SNPs) in genes important to tacrolimus bioavailability and clearance (ABCB1, CYP3A4, and CYP3A5) are associated with differences in tacrolimus pharmacokinetics. Tacrolimus 61-71 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 122-128 29920787-2 2018 Single nucleotide polymorphisms (SNPs) in genes important to tacrolimus bioavailability and clearance (ABCB1, CYP3A4, and CYP3A5) are associated with differences in tacrolimus pharmacokinetics. Tacrolimus 165-175 ATP binding cassette subfamily B member 1 Homo sapiens 103-108 29920787-2 2018 Single nucleotide polymorphisms (SNPs) in genes important to tacrolimus bioavailability and clearance (ABCB1, CYP3A4, and CYP3A5) are associated with differences in tacrolimus pharmacokinetics. Tacrolimus 165-175 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 110-116 29920787-2 2018 Single nucleotide polymorphisms (SNPs) in genes important to tacrolimus bioavailability and clearance (ABCB1, CYP3A4, and CYP3A5) are associated with differences in tacrolimus pharmacokinetics. Tacrolimus 165-175 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 122-128 29920787-6 2018 Compared with CYP3A poor metabolizers (PM), time to therapeutic tacrolimus trough was increased by 5.1 +- 1.6 days for CYP3A extensive metabolizers (EM, P < 0.001). Tacrolimus 64-74 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 119-124 30116308-0 2018 Analysis of FK506-mediated functional recovery and neuroprotection in a rat model of spinal cord injury indicates that EGF is modulated in astrocytes. Tacrolimus 12-17 epidermal growth factor like 1 Rattus norvegicus 119-122 30116308-9 2018 Furthermore, FK506 upregulated EGF expression of astrocytes both in vivo and in vitro. Tacrolimus 13-18 epidermal growth factor like 1 Rattus norvegicus 31-34 30116308-11 2018 Furthermore, addition of anti-EGF neutralizing antibodies could interrupt the promotion of neurite outgrowth by FK506-CM. Tacrolimus 112-117 epidermal growth factor like 1 Rattus norvegicus 30-33 30116308-12 2018 The present study indicates that astrocytes have an important role as mediators of FK506-improved spinal cord function recovery, and this partially clarifies the role of cell-cell interaction through modulating EGF in this process. Tacrolimus 83-88 epidermal growth factor like 1 Rattus norvegicus 211-214 29380240-2 2018 Previously, we have shown that the calcineurin inhibiting drugs tacrolimus and cyclosporin A reduce adipocyte and myocyte glucose uptakes by reducing the amount of glucose transporter type 4 (GLUT4) at the cell surface, due to an increased internalization rate. Tacrolimus 64-74 solute carrier family 2 member 4 Homo sapiens 164-190 29380240-2 2018 Previously, we have shown that the calcineurin inhibiting drugs tacrolimus and cyclosporin A reduce adipocyte and myocyte glucose uptakes by reducing the amount of glucose transporter type 4 (GLUT4) at the cell surface, due to an increased internalization rate. Tacrolimus 64-74 solute carrier family 2 member 4 Homo sapiens 192-197 29380240-5 2018 Short- and long-term treatments with tacrolimus, cyclosporin A or another CNI deltamethrin (herbicide) decreased basal and insulin-dependent glucose uptake in adipocytes, without any additive effects observed when added together. Tacrolimus 37-47 insulin Homo sapiens 123-130 30040022-0 2018 Tacrolimus population pharmacokinetic models according to CYP3A5/CYP3A4/POR genotypes in Chinese Han renal transplant patients. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 58-64 30040022-0 2018 Tacrolimus population pharmacokinetic models according to CYP3A5/CYP3A4/POR genotypes in Chinese Han renal transplant patients. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 65-71 30040022-0 2018 Tacrolimus population pharmacokinetic models according to CYP3A5/CYP3A4/POR genotypes in Chinese Han renal transplant patients. Tacrolimus 0-10 cytochrome p450 oxidoreductase Homo sapiens 72-75 30040022-7 2018 CONCLUSION: Our final model confirmed that CYP3A5*3 plays a more significant role in tacrolimus PK and could affect the blood concentrations and CL/F (clearance rate/bioavailbility). Tacrolimus 85-95 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 43-49 29621122-11 2018 CONCLUSIONS: Tacrolimus C0 values, its variability, and CYP3A5 polymorphisms were identified as risk factors of AR and tacrolimus ADR. Tacrolimus 119-129 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 56-62 30228949-7 2018 While both rapamycin and the calcineurin inhibitor tacrolimus elongated the survival of OVA-expressing skin grafts, and inhibited short-term antigen-specific CD8+ T cell responses, rapamycin but not tacrolimus permitted the statistically significant infiltration of CD8+ effector memory T cells into UV-induced SCC lesions. Tacrolimus 51-61 CD8a molecule Homo sapiens 158-161 30228949-7 2018 While both rapamycin and the calcineurin inhibitor tacrolimus elongated the survival of OVA-expressing skin grafts, and inhibited short-term antigen-specific CD8+ T cell responses, rapamycin but not tacrolimus permitted the statistically significant infiltration of CD8+ effector memory T cells into UV-induced SCC lesions. Tacrolimus 51-61 CD8a molecule Homo sapiens 266-269 30036394-7 2018 In vitro experiments revealed that 50 ng/ml tacrolimus affected NFATc1 amplification by 58% (mean; p = 0.02). Tacrolimus 44-54 nuclear factor of activated T cells 1 Homo sapiens 64-70 29664738-4 2018 We further report that ARNT expression itself is controlled by the FKBP12/YY1 transcriptional repressor complex and that disruption of such FKBP12/YY1 complexes by picomolar FK506 at subimmunosuppressive doses increases ARNT expression, subsequently leading to homodimeric ARNT-induced ALK3 transcription. Tacrolimus 174-179 aryl hydrocarbon receptor nuclear translocator Homo sapiens 23-27 29664738-4 2018 We further report that ARNT expression itself is controlled by the FKBP12/YY1 transcriptional repressor complex and that disruption of such FKBP12/YY1 complexes by picomolar FK506 at subimmunosuppressive doses increases ARNT expression, subsequently leading to homodimeric ARNT-induced ALK3 transcription. Tacrolimus 174-179 FKBP prolyl isomerase 1A pseudogene 3 Homo sapiens 140-146 29664738-4 2018 We further report that ARNT expression itself is controlled by the FKBP12/YY1 transcriptional repressor complex and that disruption of such FKBP12/YY1 complexes by picomolar FK506 at subimmunosuppressive doses increases ARNT expression, subsequently leading to homodimeric ARNT-induced ALK3 transcription. Tacrolimus 174-179 YY1 transcription factor Homo sapiens 147-150 29664738-4 2018 We further report that ARNT expression itself is controlled by the FKBP12/YY1 transcriptional repressor complex and that disruption of such FKBP12/YY1 complexes by picomolar FK506 at subimmunosuppressive doses increases ARNT expression, subsequently leading to homodimeric ARNT-induced ALK3 transcription. Tacrolimus 174-179 aryl hydrocarbon receptor nuclear translocator Homo sapiens 220-224 29664738-4 2018 We further report that ARNT expression itself is controlled by the FKBP12/YY1 transcriptional repressor complex and that disruption of such FKBP12/YY1 complexes by picomolar FK506 at subimmunosuppressive doses increases ARNT expression, subsequently leading to homodimeric ARNT-induced ALK3 transcription. Tacrolimus 174-179 aryl hydrocarbon receptor nuclear translocator Homo sapiens 220-224 29664738-4 2018 We further report that ARNT expression itself is controlled by the FKBP12/YY1 transcriptional repressor complex and that disruption of such FKBP12/YY1 complexes by picomolar FK506 at subimmunosuppressive doses increases ARNT expression, subsequently leading to homodimeric ARNT-induced ALK3 transcription. Tacrolimus 174-179 bone morphogenetic protein receptor type 1A Homo sapiens 286-290 29266762-1 2018 Calcineurin inhibitor toxicity (CNT) is a frequent occurrence in transplanted renal grafts and autochthone kidneys from patients undergoing long-term treatment with calcineurin inhibitors, notably cyclosporin A (CsA) and tacrolimus. Tacrolimus 221-231 calcineurin binding protein 1 Mus musculus 0-21 29316256-5 2018 Tacrolimus treatment significantly altered the relative abundance of Allobaculum, Bacteroides, and Lactobacillus and CD4+ CD25hi FoxP3+ regulatory T cells in the colonic mucosa and the circulation. Tacrolimus 0-10 CD4 antigen Mus musculus 117-120 29316256-5 2018 Tacrolimus treatment significantly altered the relative abundance of Allobaculum, Bacteroides, and Lactobacillus and CD4+ CD25hi FoxP3+ regulatory T cells in the colonic mucosa and the circulation. Tacrolimus 0-10 interleukin 2 receptor, alpha chain Mus musculus 122-126 29316256-5 2018 Tacrolimus treatment significantly altered the relative abundance of Allobaculum, Bacteroides, and Lactobacillus and CD4+ CD25hi FoxP3+ regulatory T cells in the colonic mucosa and the circulation. Tacrolimus 0-10 forkhead box P3 Mus musculus 129-134 29502069-4 2018 RESULTS: Patients with AC and OVA-sensitised WT mice exhibited increased levels of Gal-3 in the conjunctiva compared with control, an effect reverted by the action of Dex and TC therapy. Tacrolimus 175-177 lectin, galactose binding, soluble 3 Mus musculus 83-88 29804850-7 2018 RESULTS: The histologically proven rejection grade in group AT was significantly lower than that in group T. The serum levels of hepatocyte growth factor and the expression of cMet in group AT accompanied by low CD40 expression were also significantly higher than those of the lung grafts of group T. CONCLUSIONS: These results suggest that co-administration of ADMSCs with tacrolimus is a beneficial therapeutic approach in lung transplantation. Tacrolimus 374-384 MET proto-oncogene, receptor tyrosine kinase Rattus norvegicus 176-180 29920880-0 2018 Effect of CYP3A5*1 expression on tacrolimus required dose for transplant pediatrics: A systematic review and meta-analysis. Tacrolimus 33-43 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 10-16 30036394-0 2018 Analysis of NFATc1 amplification in T cells for pharmacodynamic monitoring of tacrolimus in kidney transplant recipients. Tacrolimus 78-88 nuclear factor of activated T cells 1 Homo sapiens 12-18 30036394-2 2018 Here, we tested whether measuring NFATc1 amplification, a member of the calcineurin pathway, is suitable for TDM of tacrolimus. Tacrolimus 116-126 nuclear factor of activated T cells 1 Homo sapiens 34-40 30036394-3 2018 MATERIALS AND METHODS: NFATc1 amplification was monitored in T cells of kidney transplant recipients who received either tacrolimus- (n = 11) or belatacept-based (n = 10) therapy. Tacrolimus 121-131 nuclear factor of activated T cells 1 Homo sapiens 23-29 30036394-5 2018 RESULTS: At day 30 after transplantation, in tacrolimus-treated patients, NFATc1 amplification was inhibited in CD4+ T cells expressing the co-stimulation receptor CD28 (mean inhibition 37%; p = 0.01) and in CD8+CD28+ T cells (29% inhibition; p = 0.02), while this was not observed in CD8+CD28- T cells or belatacept-treated patients. Tacrolimus 45-55 nuclear factor of activated T cells 1 Homo sapiens 74-80 30036394-5 2018 RESULTS: At day 30 after transplantation, in tacrolimus-treated patients, NFATc1 amplification was inhibited in CD4+ T cells expressing the co-stimulation receptor CD28 (mean inhibition 37%; p = 0.01) and in CD8+CD28+ T cells (29% inhibition; p = 0.02), while this was not observed in CD8+CD28- T cells or belatacept-treated patients. Tacrolimus 45-55 CD28 molecule Homo sapiens 164-168 30036394-5 2018 RESULTS: At day 30 after transplantation, in tacrolimus-treated patients, NFATc1 amplification was inhibited in CD4+ T cells expressing the co-stimulation receptor CD28 (mean inhibition 37%; p = 0.01) and in CD8+CD28+ T cells (29% inhibition; p = 0.02), while this was not observed in CD8+CD28- T cells or belatacept-treated patients. Tacrolimus 45-55 CD28 molecule Homo sapiens 212-216 30036394-5 2018 RESULTS: At day 30 after transplantation, in tacrolimus-treated patients, NFATc1 amplification was inhibited in CD4+ T cells expressing the co-stimulation receptor CD28 (mean inhibition 37%; p = 0.01) and in CD8+CD28+ T cells (29% inhibition; p = 0.02), while this was not observed in CD8+CD28- T cells or belatacept-treated patients. Tacrolimus 45-55 CD28 molecule Homo sapiens 212-216 30036394-6 2018 Tacrolimus pre-dose concentrations of these patients correlated inversely with NFATc1 amplification in CD28+ T cells (rs = -0.46; p < 0.01). Tacrolimus 0-10 nuclear factor of activated T cells 1 Homo sapiens 79-85 30036394-6 2018 Tacrolimus pre-dose concentrations of these patients correlated inversely with NFATc1 amplification in CD28+ T cells (rs = -0.46; p < 0.01). Tacrolimus 0-10 CD28 molecule Homo sapiens 103-107 30036394-8 2018 CONCLUSION: In conclusion, measuring NFATc1 amplification is a direct tool for monitoring biological effects of tacrolimus on T cells in whole blood samples of kidney transplant recipients. Tacrolimus 112-122 nuclear factor of activated T cells 1 Homo sapiens 37-43 29991328-1 2018 AIM: To investigate the association between donor CYP3A5 and ABCB1 polymorphisms and tacrolimus (Tac)-induced nephrotoxicity and renal function in kidney transplant recipients. Tacrolimus 85-95 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 50-56 29991328-1 2018 AIM: To investigate the association between donor CYP3A5 and ABCB1 polymorphisms and tacrolimus (Tac)-induced nephrotoxicity and renal function in kidney transplant recipients. Tacrolimus 85-95 ATP binding cassette subfamily B member 1 Homo sapiens 61-66 29757603-5 2018 Pin1 activity, and synapse and dendritic spine numbers are rescued by FK506, a highly specific and United States Food and Drug Administration approved CN inhibitor. Tacrolimus 70-75 peptidylprolyl cis/trans isomerase, NIMA-interacting 1 Homo sapiens 0-4 29757603-7 2018 As such, we suggest prospective clinical trials to determine if systemic FK506 can normalize CN activity in the brain, preserve Pin1 function and support synaptic health in early AD. Tacrolimus 73-78 peptidylprolyl cis/trans isomerase, NIMA-interacting 1 Homo sapiens 128-132 29804290-0 2018 Tacrolimus Elimination in Four Patients With a CYP3A5*3/*3 CYP3A4*22/*22 Genotype Combination. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 47-53 29804290-0 2018 Tacrolimus Elimination in Four Patients With a CYP3A5*3/*3 CYP3A4*22/*22 Genotype Combination. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 59-65 29804290-1 2018 Cytochrome P450 3A5 (CYP3A5) and cytochrome P450 3A4 (CYP3A4) are the predominate enzymes responsible for tacrolimus metabolism. Tacrolimus 106-116 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-19 29804290-1 2018 Cytochrome P450 3A5 (CYP3A5) and cytochrome P450 3A4 (CYP3A4) are the predominate enzymes responsible for tacrolimus metabolism. Tacrolimus 106-116 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 21-27 29804290-1 2018 Cytochrome P450 3A5 (CYP3A5) and cytochrome P450 3A4 (CYP3A4) are the predominate enzymes responsible for tacrolimus metabolism. Tacrolimus 106-116 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 33-52 29804290-1 2018 Cytochrome P450 3A5 (CYP3A5) and cytochrome P450 3A4 (CYP3A4) are the predominate enzymes responsible for tacrolimus metabolism. Tacrolimus 106-116 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 54-60 29804290-2 2018 The presence of CYP3A4 and CYP3A5 genetic variants significantly affects tacrolimus clearance and dose requirements. Tacrolimus 73-83 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 16-22 29804290-2 2018 The presence of CYP3A4 and CYP3A5 genetic variants significantly affects tacrolimus clearance and dose requirements. Tacrolimus 73-83 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 27-33 30264877-12 2018 CONCLUSION: Costimulatory blockade-based and anti-CD20 antibody/tacrolimus-based immunosuppressive therapies seem to be comparably safe with steroid therapy in nonhuman primates receiving corneal xenotransplantation, as they did not reactivate Rhesus Cytomegalovirus and maintained manageable systemic status. Tacrolimus 64-74 keratin 20 Homo sapiens 50-54 29920880-1 2018 This systematic review was designed to find out optimal tacrolimus dose in pediatrics according to their CYP3A5*1 genotype by performing meta-analysis. Tacrolimus 56-66 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 105-111 29920880-5 2018 Analysis of tacrolimus required dose, blood concentration, and C/D ratio in 14 time points post-transplantation resulted in significant differences between expressers and non-expressers of CYP3A5*1. Tacrolimus 12-22 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 189-195 29594315-2 2018 We previously reported that MITA correctly reflected the change in mRNA of human whole-blood cells treated with dexamethasone, cyclosporine, FK506, or several other immunosuppressive drugs. Tacrolimus 141-146 stimulator of interferon response cGAMP interactor 1 Mus musculus 28-32 29894515-8 2018 The administration of the beta2-GPI DNA vaccine mixed with FK506 reduced the blood IgG anti-beta2-GPI antibody titers and suppressed APS manifestations in mice. Tacrolimus 59-64 apolipoprotein H Mus musculus 26-35 29894515-8 2018 The administration of the beta2-GPI DNA vaccine mixed with FK506 reduced the blood IgG anti-beta2-GPI antibody titers and suppressed APS manifestations in mice. Tacrolimus 59-64 apolipoprotein H Mus musculus 92-101 29666890-0 2018 Manipulating the expression of SARP family regulator BulZ and its target gene product to increase tacrolimus production. Tacrolimus 98-108 ankyrin repeat domain 42 Homo sapiens 31-35 29666890-2 2018 In this study, we identified that BulZ, a Streptomyces antibiotic regulatory protein (SARP) family regulator, acted as a positive regulator for spore differentiation and tacrolimus production. Tacrolimus 170-180 ankyrin repeat domain 42 Homo sapiens 42-84 29666890-2 2018 In this study, we identified that BulZ, a Streptomyces antibiotic regulatory protein (SARP) family regulator, acted as a positive regulator for spore differentiation and tacrolimus production. Tacrolimus 170-180 ankyrin repeat domain 42 Homo sapiens 86-90 30003047-0 2018 Immunosuppressant drug tacrolimus induced mitochondrial nephrotoxicity, modified PCNA and Bcl-2 expression attenuated by Ocimum basilicum L. in CD1 mice. Tacrolimus 23-33 proliferating cell nuclear antigen Mus musculus 81-85 30003047-0 2018 Immunosuppressant drug tacrolimus induced mitochondrial nephrotoxicity, modified PCNA and Bcl-2 expression attenuated by Ocimum basilicum L. in CD1 mice. Tacrolimus 23-33 CD1 antigen complex Mus musculus 144-147 29676018-0 2018 Conversion from tacrolimus-mycophenolate mofetil to tacrolimus-mTOR immunosuppression after kidney-pancreas transplantation reduces the incidence of both BK and CMV viremia. Tacrolimus 16-26 mechanistic target of rapamycin kinase Homo sapiens 63-67 30078783-6 2018 IL-18 was a potential CYP3A expression modulator and was capable of affecting tacrolimus pharmacokinetics. Tacrolimus 78-88 interleukin 18 Homo sapiens 0-5 29757021-1 2018 INTRODUCTION: Cornerstone immunosuppressive therapy currently relies on immediate-release tacrolimus, a calcineurin inhibitor (CNI) that is potentially nephrotoxic and is more diabetogenic than cyclosporine A. Tacrolimus 90-100 calcineurin binding protein 1 Homo sapiens 104-125 29757021-7 2018 Other studies report that Advagraf -treated patients receiving a mTOR-inhibitor agent (sirolimus or everolimus) instead of MMF: this was associated with good allograft outcome, and might also prevent late-onset cytomegalovirus infection. Tacrolimus 26-34 mechanistic target of rapamycin kinase Homo sapiens 65-69 29676018-0 2018 Conversion from tacrolimus-mycophenolate mofetil to tacrolimus-mTOR immunosuppression after kidney-pancreas transplantation reduces the incidence of both BK and CMV viremia. Tacrolimus 52-62 mechanistic target of rapamycin kinase Homo sapiens 63-67 29676018-1 2018 BACKGROUND: We sought to determine whether conversion from tacrolimus/mycophenolate mofetil (TAC-MMF) into tacrolimus/mTOR inhibitor (TAC-mTOR) immunosuppression would reduce the incidences of BK and CMV viremia after kidney/pancreas (KP) transplantation. Tacrolimus 107-117 mechanistic target of rapamycin kinase Homo sapiens 138-142 29676018-2 2018 METHODS: In this single-center review, the TAC-mTOR cohort (n = 39) was converted at 1 month post-transplant to an mTOR inhibitor and reduced-dose tacrolimus. Tacrolimus 147-157 mechanistic target of rapamycin kinase Homo sapiens 47-51 29446493-9 2018 The results indicate that allo-MSC are inherently immunogenic when delivered intramuscularly to healthy and ischemic mouse hind limb, but induce an IgG1-skewed humoral response that is suppressed by tacrolimus. Tacrolimus 199-209 immunoglobulin heavy constant gamma 1 (G1m marker) Mus musculus 148-152 29879072-14 2018 Since previous studies indicate a role of Th1 inflammation in TAFRO syndrome pathogenesis, tacrolimus may, therefore, be effective in treating TAFRO syndrome. Tacrolimus 91-101 negative elongation factor complex member C/D Homo sapiens 42-45 29454984-6 2018 Interferon (IFN)-gamma and IL-2 content in the serum were lower after operation (P < .05) in the AdOX40Ig and FK506 groups. Tacrolimus 113-118 interferon gamma Rattus norvegicus 0-22 29454984-6 2018 Interferon (IFN)-gamma and IL-2 content in the serum were lower after operation (P < .05) in the AdOX40Ig and FK506 groups. Tacrolimus 113-118 interleukin 2 Rattus norvegicus 27-31 29454984-7 2018 On the contrary, IL-4 and IL-10 content in the serum was higher after operation (P < 0.05) in the AdOX40Ig and FK506 groups. Tacrolimus 114-119 interleukin 4 Rattus norvegicus 17-21 29454984-7 2018 On the contrary, IL-4 and IL-10 content in the serum was higher after operation (P < 0.05) in the AdOX40Ig and FK506 groups. Tacrolimus 114-119 interleukin 10 Rattus norvegicus 26-31 29851248-3 2018 Endothelial dysfunction induced by tacrolimus is related to both increased nicotinamide adenine dinucleotide phosphate (NADPH) oxidase (NOX2) and uncoupled endothelial nitric oxide synthase (eNOS)-driven superoxide production and Rho-kinase-mediated eNOS inhibition. Tacrolimus 35-45 cytochrome b-245, beta polypeptide Mus musculus 136-140 29851248-3 2018 Endothelial dysfunction induced by tacrolimus is related to both increased nicotinamide adenine dinucleotide phosphate (NADPH) oxidase (NOX2) and uncoupled endothelial nitric oxide synthase (eNOS)-driven superoxide production and Rho-kinase-mediated eNOS inhibition. Tacrolimus 35-45 nitric oxide synthase 3, endothelial cell Mus musculus 156-189 29851248-3 2018 Endothelial dysfunction induced by tacrolimus is related to both increased nicotinamide adenine dinucleotide phosphate (NADPH) oxidase (NOX2) and uncoupled endothelial nitric oxide synthase (eNOS)-driven superoxide production and Rho-kinase-mediated eNOS inhibition. Tacrolimus 35-45 Rho-associated coiled-coil containing protein kinase 2 Mus musculus 230-240 29546446-0 2018 CYP3A4 and GCK genetic polymorphisms are the risk factors of tacrolimus-induced new-onset diabetes after transplantation in renal transplant recipients. Tacrolimus 61-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 29546446-0 2018 CYP3A4 and GCK genetic polymorphisms are the risk factors of tacrolimus-induced new-onset diabetes after transplantation in renal transplant recipients. Tacrolimus 61-71 glucokinase Homo sapiens 11-14 29546446-1 2018 PURPOSE: We intend to investigate the association between tacrolimus-induced new-onset diabetes after transplantation (NODAT) and polymorphisms of CYP3A4, CYP3A5, ATP-binding cassette transporter sub-family C member 8 (ABCC8), and glucokinase (GCK) in renal transplant recipients. Tacrolimus 58-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 147-153 29546446-1 2018 PURPOSE: We intend to investigate the association between tacrolimus-induced new-onset diabetes after transplantation (NODAT) and polymorphisms of CYP3A4, CYP3A5, ATP-binding cassette transporter sub-family C member 8 (ABCC8), and glucokinase (GCK) in renal transplant recipients. Tacrolimus 58-68 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 155-161 29546446-1 2018 PURPOSE: We intend to investigate the association between tacrolimus-induced new-onset diabetes after transplantation (NODAT) and polymorphisms of CYP3A4, CYP3A5, ATP-binding cassette transporter sub-family C member 8 (ABCC8), and glucokinase (GCK) in renal transplant recipients. Tacrolimus 58-68 ATP binding cassette subfamily C member 8 Homo sapiens 163-217 29546446-1 2018 PURPOSE: We intend to investigate the association between tacrolimus-induced new-onset diabetes after transplantation (NODAT) and polymorphisms of CYP3A4, CYP3A5, ATP-binding cassette transporter sub-family C member 8 (ABCC8), and glucokinase (GCK) in renal transplant recipients. Tacrolimus 58-68 ATP binding cassette subfamily C member 8 Homo sapiens 219-224 29546446-1 2018 PURPOSE: We intend to investigate the association between tacrolimus-induced new-onset diabetes after transplantation (NODAT) and polymorphisms of CYP3A4, CYP3A5, ATP-binding cassette transporter sub-family C member 8 (ABCC8), and glucokinase (GCK) in renal transplant recipients. Tacrolimus 58-68 glucokinase Homo sapiens 231-242 29546446-1 2018 PURPOSE: We intend to investigate the association between tacrolimus-induced new-onset diabetes after transplantation (NODAT) and polymorphisms of CYP3A4, CYP3A5, ATP-binding cassette transporter sub-family C member 8 (ABCC8), and glucokinase (GCK) in renal transplant recipients. Tacrolimus 58-68 glucokinase Homo sapiens 244-247 29546446-10 2018 CONCLUSIONS: The polymorphisms of CYP3A4 *18B and GCK G-30A were related to NODAT induced by tacrolimus. Tacrolimus 93-103 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-40 29546446-10 2018 CONCLUSIONS: The polymorphisms of CYP3A4 *18B and GCK G-30A were related to NODAT induced by tacrolimus. Tacrolimus 93-103 glucokinase Homo sapiens 50-53 29904381-0 2018 The Calcineurin Inhibitor Tacrolimus Specifically Suppresses Human T Follicular Helper Cells. Tacrolimus 26-36 calcineurin binding protein 1 Homo sapiens 4-25 29904381-8 2018 Results: The calcineurin inhibitor (CNIs) tacrolimus specifically suppresses both LN Tfh cells and circulating Tfh cells, but not their regulatory counterparts or other CD4 T cell subsets. Tacrolimus 42-52 calcineurin binding protein 1 Homo sapiens 13-34 29942927-5 2018 NCX1 inhibition by small interfering RNA or small molecules activates the calcineurin/nuclear factor of activated T cells (NFAT) pathway and inhibits apoptosis induced by the immunosuppressors cyclosporine A (CsA) and tacrolimus in insulin-producing cell. Tacrolimus 218-228 solute carrier family 8 (sodium/calcium exchanger), member 1 Mus musculus 0-4 29160300-0 2018 Genome-wide association study identifies the common variants in CYP3A4 and CYP3A5 responsible for variation in tacrolimus trough concentration in Caucasian kidney transplant recipients. Tacrolimus 111-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 64-70 29160300-0 2018 Genome-wide association study identifies the common variants in CYP3A4 and CYP3A5 responsible for variation in tacrolimus trough concentration in Caucasian kidney transplant recipients. Tacrolimus 111-121 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 75-81 29160300-1 2018 The immunosuppressant tacrolimus (TAC) is metabolized by both cytochrome P450 3A4 (CYP3A4) and CYP3A5 enzymes. Tacrolimus 22-32 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 62-81 29160300-1 2018 The immunosuppressant tacrolimus (TAC) is metabolized by both cytochrome P450 3A4 (CYP3A4) and CYP3A5 enzymes. Tacrolimus 22-32 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 83-89 29160300-1 2018 The immunosuppressant tacrolimus (TAC) is metabolized by both cytochrome P450 3A4 (CYP3A4) and CYP3A5 enzymes. Tacrolimus 22-32 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 95-101 29550576-10 2018 The clinical impact of CYP3A5 genetic differences may be small under the current immunosuppressive regimen consisting of mycophenolate mofetil, steroids, basiliximab, and lower target trough levels of tacrolimus with suitable TDM in a low immunological risk population. Tacrolimus 201-211 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 23-29 29863266-9 2018 The detection of SOD and ROS showed that ox-LDL could induce the cell oxidative stress injury, whereas tacrolimus could inhibit such an effect. Tacrolimus 103-113 superoxide dismutase 1 Homo sapiens 17-20 29550576-8 2018 Despite therapeutic drug monitoring (TDM), trough levels of tacrolimus were lower in carriers with the CYP3A5*1 allele (expressers) than in those with the CTP3A5*3/*3 genotype (non-expressers) throughout the 1-year post-transplantation period. Tacrolimus 60-70 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 103-109 29488613-0 2018 Association of the PPARgamma/PI3K/Akt pathway with the cardioprotective effects of tacrolimus in myocardial ischemic/reperfusion injury. Tacrolimus 83-93 peroxisome proliferator-activated receptor gamma Rattus norvegicus 19-28 29718866-2 2018 The current study aimed to assess the efficacy and safety of tacrolimus in the treatment of cases of refractory IgAN.In this retrospective observational study, 34 primary IgAN patients with refractory proteinuria received tacrolimus for at least 12 months. Tacrolimus 61-71 IGAN1 Homo sapiens 112-116 29718866-9 2018 Crescent formation in biopsy specimens was seen more often in nonresponder patients.Tacrolimus was safe and effective at lowering proteinuria in refractory IgAN patients. Tacrolimus 84-94 IGAN1 Homo sapiens 156-160 29488613-0 2018 Association of the PPARgamma/PI3K/Akt pathway with the cardioprotective effects of tacrolimus in myocardial ischemic/reperfusion injury. Tacrolimus 83-93 AKT serine/threonine kinase 1 Rattus norvegicus 34-37 29488613-8 2018 The phosphorylation of PPARgamma and Akt was significantly activated by tacrolimus, whereas inhibitors of PPARgamma/PI3K/Akt significantly abolished the effects of tacrolimus (P<0.05). Tacrolimus 72-82 peroxisome proliferator-activated receptor gamma Rattus norvegicus 23-32 29488613-8 2018 The phosphorylation of PPARgamma and Akt was significantly activated by tacrolimus, whereas inhibitors of PPARgamma/PI3K/Akt significantly abolished the effects of tacrolimus (P<0.05). Tacrolimus 72-82 AKT serine/threonine kinase 1 Rattus norvegicus 37-40 29488613-8 2018 The phosphorylation of PPARgamma and Akt was significantly activated by tacrolimus, whereas inhibitors of PPARgamma/PI3K/Akt significantly abolished the effects of tacrolimus (P<0.05). Tacrolimus 164-174 peroxisome proliferator-activated receptor gamma Rattus norvegicus 23-32 29488613-8 2018 The phosphorylation of PPARgamma and Akt was significantly activated by tacrolimus, whereas inhibitors of PPARgamma/PI3K/Akt significantly abolished the effects of tacrolimus (P<0.05). Tacrolimus 164-174 peroxisome proliferator-activated receptor gamma Rattus norvegicus 106-115 29488613-8 2018 The phosphorylation of PPARgamma and Akt was significantly activated by tacrolimus, whereas inhibitors of PPARgamma/PI3K/Akt significantly abolished the effects of tacrolimus (P<0.05). Tacrolimus 164-174 AKT serine/threonine kinase 1 Rattus norvegicus 121-124 29488613-9 2018 Together, these results suggest that tacrolimus may protect rats from MIRI through activation of the PPARgamma/PI3K/Akt pathway. Tacrolimus 37-47 peroxisome proliferator-activated receptor gamma Rattus norvegicus 101-110 29488613-9 2018 Together, these results suggest that tacrolimus may protect rats from MIRI through activation of the PPARgamma/PI3K/Akt pathway. Tacrolimus 37-47 AKT serine/threonine kinase 1 Rattus norvegicus 116-119 29731088-2 2018 Tacrolimus (Tac)-induced apoptosis was characterized by nuclear fragmentation and caspase-3 activation. Tacrolimus 0-10 caspase 3 Homo sapiens 82-91 29731088-2 2018 Tacrolimus (Tac)-induced apoptosis was characterized by nuclear fragmentation and caspase-3 activation. Tacrolimus 0-3 caspase 3 Homo sapiens 82-91 29731062-4 2018 OBJECTIVE: The aim of this study was to identify the proportion of CYP3A5 gene polymorphism in Myanmar kidney transplant recipients and to determine the impact of CYP3A5 gene polymorphisms on tacrolimus level in CYP3A5 expressors and nonexpressors. Tacrolimus 192-202 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 163-169 29731062-4 2018 OBJECTIVE: The aim of this study was to identify the proportion of CYP3A5 gene polymorphism in Myanmar kidney transplant recipients and to determine the impact of CYP3A5 gene polymorphisms on tacrolimus level in CYP3A5 expressors and nonexpressors. Tacrolimus 192-202 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 163-169 29731088-8 2018 Interestingly, we found that 1 nmol/L Tac treatment induced activation of caspase-12 protease as well as the catalytic activity of caspase-3 but not catalytic activation of caspase-6, -8, and -9 proteases in Jurkat cells. Tacrolimus 38-41 caspase 3 Homo sapiens 131-140 29731062-8 2018 The tacrolimus concentration/dose ratio in the CYP3A5 expressor group was lower than in the CYP3A5 nonexpressor group (1.49 +- 0.69 vs 3.49 +- 3.08 [P = .003] at 1 month; and 1.54 +- 0.9 vs 7.88 +- 8.25 [P = .0001] at 3 months). Tacrolimus 4-14 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 47-53 29731062-10 2018 CYP3A5 genetic polymorphism is one of the important factors in determining daily requirements for tacrolimus and in adjusting tacrolimus trough concentrations. Tacrolimus 98-108 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 29731062-10 2018 CYP3A5 genetic polymorphism is one of the important factors in determining daily requirements for tacrolimus and in adjusting tacrolimus trough concentrations. Tacrolimus 126-136 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 29621269-1 2018 The objective of the current study was to explore the role of ABCB1 and CYP3A5 genetic polymorphisms in predicting the bioavailability of tacrolimus and the risk for post-transplant diabetes. Tacrolimus 138-148 ATP binding cassette subfamily B member 1 Homo sapiens 62-67 29621269-1 2018 The objective of the current study was to explore the role of ABCB1 and CYP3A5 genetic polymorphisms in predicting the bioavailability of tacrolimus and the risk for post-transplant diabetes. Tacrolimus 138-148 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 72-78 29621269-5 2018 ABCB1 1236 C>T and 2677G>T/A showed inverse association while CYP3A5*3 showed a positive association with the bioavailability of tacrolimus. Tacrolimus 135-145 ATP binding cassette subfamily B member 1 Homo sapiens 0-5 29621269-5 2018 ABCB1 1236 C>T and 2677G>T/A showed inverse association while CYP3A5*3 showed a positive association with the bioavailability of tacrolimus. Tacrolimus 135-145 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 68-74 29362864-3 2018 Treatment of CD-1 mice with Tacrolimus (1 mg/kg/d for 28 days) resulted in kidney injury and was associated with alteration of a gene expression signature associated with cellular stress, fibrosis and inflammation. Tacrolimus 28-38 CD1 antigen complex Mus musculus 13-17 29615122-0 2018 Effect of CYP3 A4, CYP3 A5 and ABCB1 gene polymorphisms on the clinical efficacy of tacrolimus in the treatment of nephrotic syndrome. Tacrolimus 84-94 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 10-17 29615122-0 2018 Effect of CYP3 A4, CYP3 A5 and ABCB1 gene polymorphisms on the clinical efficacy of tacrolimus in the treatment of nephrotic syndrome. Tacrolimus 84-94 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 19-26 29615122-0 2018 Effect of CYP3 A4, CYP3 A5 and ABCB1 gene polymorphisms on the clinical efficacy of tacrolimus in the treatment of nephrotic syndrome. Tacrolimus 84-94 ATP binding cassette subfamily B member 1 Homo sapiens 31-36 29362864-4 2018 Tacrolimus also affected renal miRNA expression, including miRNAs previously involved in fibrotic and inflammatory processes as "fibromirs" such as miR-21-5p, miR-199a-5p and miR-214-3p. Tacrolimus 0-10 microRNA 215 Mus musculus 148-157 29362864-5 2018 In agreement with in vivo data, Renal Proximal Tubular Epithelial cells exposed to Tacrolimus (25 and 50 microM) showed upregulation of miR-21-5p and the concomitant induction of epithelial phenotypic changes, inflammation and oxidative stress. Tacrolimus 83-93 microRNA 215 Mus musculus 136-145 29454235-0 2018 Donor and recipient P450 gene polymorphisms influence individual pharmacological effects of tacrolimus in Chinese liver transplantation patients. Tacrolimus 92-102 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 20-24 28833755-7 2018 In vitro, tacrolimus inhibited receptor activator of nuclear factor-kappaB ligand-mediated osteoclast formation augmented by interleukin-1beta, thapsigargin, or both. Tacrolimus 10-20 interleukin 1 beta Mus musculus 125-142 28833755-8 2018 Furthermore, tacrolimus inhibited glucose-regulated protein (GRP78), protein kinase R-like endoplasmic reticulum kinase, inositol-requiring enzyme 1 (IRE 1), and activating transcription factor 6 (ATF6) augmented by interleukin-1beta, thapsigargin, or both. Tacrolimus 13-23 heat shock protein 5 Mus musculus 61-66 28833755-8 2018 Furthermore, tacrolimus inhibited glucose-regulated protein (GRP78), protein kinase R-like endoplasmic reticulum kinase, inositol-requiring enzyme 1 (IRE 1), and activating transcription factor 6 (ATF6) augmented by interleukin-1beta, thapsigargin, or both. Tacrolimus 13-23 endoplasmic reticulum (ER) to nucleus signalling 2 Mus musculus 121-148 28833755-8 2018 Furthermore, tacrolimus inhibited glucose-regulated protein (GRP78), protein kinase R-like endoplasmic reticulum kinase, inositol-requiring enzyme 1 (IRE 1), and activating transcription factor 6 (ATF6) augmented by interleukin-1beta, thapsigargin, or both. Tacrolimus 13-23 endoplasmic reticulum (ER) to nucleus signalling 2 Mus musculus 150-155 28833755-8 2018 Furthermore, tacrolimus inhibited glucose-regulated protein (GRP78), protein kinase R-like endoplasmic reticulum kinase, inositol-requiring enzyme 1 (IRE 1), and activating transcription factor 6 (ATF6) augmented by interleukin-1beta, thapsigargin, or both. Tacrolimus 13-23 activating transcription factor 6 Mus musculus 162-195 28833755-8 2018 Furthermore, tacrolimus inhibited glucose-regulated protein (GRP78), protein kinase R-like endoplasmic reticulum kinase, inositol-requiring enzyme 1 (IRE 1), and activating transcription factor 6 (ATF6) augmented by interleukin-1beta, thapsigargin, or both. Tacrolimus 13-23 activating transcription factor 6 Mus musculus 197-201 28833755-8 2018 Furthermore, tacrolimus inhibited glucose-regulated protein (GRP78), protein kinase R-like endoplasmic reticulum kinase, inositol-requiring enzyme 1 (IRE 1), and activating transcription factor 6 (ATF6) augmented by interleukin-1beta, thapsigargin, or both. Tacrolimus 13-23 interleukin 1 beta Mus musculus 216-233 28681225-10 2018 Cytochrome P450 3A5 expressers and recipients who received a kidney from a deceased donor had a significantly higher tacrolimus clearance. Tacrolimus 117-127 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-19 28681225-15 2018 CONCLUSION: During the first 6 weeks after transplantation, the tacrolimus weight-normalized starting dose should be higher in pediatric kidney transplant recipients with a lower bodyweight, those who express the cytochrome P450 3A5 genotype, and those who receive a kidney from a deceased donor. Tacrolimus 64-74 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 213-232 29454235-1 2018 The immunosuppressant drug tacrolimus (Tac) used for the prevention of immunological rejection is a metabolic substrate of cytochrome P450 enzymes. Tacrolimus 27-37 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 134-138 29629825-0 2018 CYP3A pharmacogenetic association with tacrolimus pharmacokinetics differs based on route of drug administration. Tacrolimus 39-49 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-5 28891077-0 2018 A comparison of the effects of CYP3A5 polymorphism on tacrolimus blood concentrations measured by 4 immunoassay methods in renal transplant patients. Tacrolimus 54-64 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 31-37 28891077-2 2018 The aim of this study was to investigate differences in the effects of CYP3A5 polymorphism on tacrolimus concentrations obtained by four immunoassay methods in renal transplant patients. Tacrolimus 94-104 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 71-77 28891077-11 2018 Because patients with the CYP3A5*1 allele identified using LTIA may show higher blood concentrations of tacrolimus at lower target concentrations, for example 3.0 ng/mL, compared with other immunoassay methods, there is a need for sufficient consideration of the interpretation of values measured by LTIA. Tacrolimus 104-114 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 26-32 28941036-0 2018 Association of donor small ubiquitin-like modifier 4 rs237025 genetic variant with tacrolimus elimination in the early period after liver transplantation. Tacrolimus 83-93 small ubiquitin like modifier 4 Homo sapiens 21-52 28941036-2 2018 In this study, we aimed to investigate the association of donor and recipient small ubiquitin-like modifier 4 (SUMO4) rs237025 polymorphisms with tacrolimus elimination and the potential mechanism. Tacrolimus 146-156 small ubiquitin like modifier 4 Homo sapiens 78-109 28941036-2 2018 In this study, we aimed to investigate the association of donor and recipient small ubiquitin-like modifier 4 (SUMO4) rs237025 polymorphisms with tacrolimus elimination and the potential mechanism. Tacrolimus 146-156 small ubiquitin like modifier 4 Homo sapiens 111-116 28941036-7 2018 RESULTS: Tacrolimus C/D ratios was significantly lower for donor SUMO4 rs237025 AA carriers than AG/GG carriers at weeks 1, 2, 3. Tacrolimus 9-19 small ubiquitin like modifier 4 Homo sapiens 65-70 28941036-8 2018 In multivariate analysis, donor and recipient CYP3A5 rs776747, donor SUMO4 rs237025 and total bilirubin were independent predictors of tacrolimus C/D ratios in the early post-transplantation period both in Cohort A and Cohort B. Tacrolimus 135-145 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 46-52 28941036-8 2018 In multivariate analysis, donor and recipient CYP3A5 rs776747, donor SUMO4 rs237025 and total bilirubin were independent predictors of tacrolimus C/D ratios in the early post-transplantation period both in Cohort A and Cohort B. Tacrolimus 135-145 small ubiquitin like modifier 4 Homo sapiens 69-74 28941036-9 2018 When combined donor CYP3A5 rs776746 and donor SUMO4 rs237025 genotypes, tacrolimus C/D ratios was highly significant at all investigated time points within the four groups. Tacrolimus 72-82 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 20-26 28941036-9 2018 When combined donor CYP3A5 rs776746 and donor SUMO4 rs237025 genotypes, tacrolimus C/D ratios was highly significant at all investigated time points within the four groups. Tacrolimus 72-82 small ubiquitin like modifier 4 Homo sapiens 46-51 29629825-2 2018 CYP3A5 genotype is an established predictor of oral tacrolimus dose requirements, and clinical guideline recommendations exist for CYP3A5-guided dose selection. Tacrolimus 52-62 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 29629825-3 2018 However, the association between CYP3A5 and nonoral tacrolimus administration is currently poorly understood, and differs from the oral tacrolimus relationship. Tacrolimus 52-62 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 33-39 29629825-4 2018 In addition to CYP3A5, other pharmacogenes associated with CYP3A activity, including CYP3A4, CYP3A7 and POR have also been identified as predictors of tacrolimus exposure. Tacrolimus 151-161 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 15-21 29629825-4 2018 In addition to CYP3A5, other pharmacogenes associated with CYP3A activity, including CYP3A4, CYP3A7 and POR have also been identified as predictors of tacrolimus exposure. Tacrolimus 151-161 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 15-20 29629825-4 2018 In addition to CYP3A5, other pharmacogenes associated with CYP3A activity, including CYP3A4, CYP3A7 and POR have also been identified as predictors of tacrolimus exposure. Tacrolimus 151-161 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 85-91 29629825-4 2018 In addition to CYP3A5, other pharmacogenes associated with CYP3A activity, including CYP3A4, CYP3A7 and POR have also been identified as predictors of tacrolimus exposure. Tacrolimus 151-161 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 93-99 29629825-4 2018 In addition to CYP3A5, other pharmacogenes associated with CYP3A activity, including CYP3A4, CYP3A7 and POR have also been identified as predictors of tacrolimus exposure. Tacrolimus 151-161 cytochrome p450 oxidoreductase Homo sapiens 104-107 29274751-6 2018 NCX2 or NCX3 heterozygotes displayed impaired maintenance of hippocampal LTP, a phenotype that in NCX2+/- mice was correlated with elevated calcineurin activity and rescued by treatment with the calcineurin (CaN) inhibitor FK506. Tacrolimus 223-228 solute carrier family 8 (sodium/calcium exchanger), member 2 Mus musculus 0-4 29547545-0 2018 Prediction of Tacrolimus Exposure by CYP3A5 Genotype and Exposure of Co-Administered Everolimus in Japanese Renal Transplant Recipients. Tacrolimus 14-24 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 37-43 29547545-1 2018 While tacrolimus and everolimus have common metabolic pathways through CYP3A4/5, tacrolimus is metabolized solely by CYP3A4 in recipients with the CYP3A5*3/*3. Tacrolimus 6-16 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 71-77 29547545-1 2018 While tacrolimus and everolimus have common metabolic pathways through CYP3A4/5, tacrolimus is metabolized solely by CYP3A4 in recipients with the CYP3A5*3/*3. Tacrolimus 81-91 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 117-123 29547545-1 2018 While tacrolimus and everolimus have common metabolic pathways through CYP3A4/5, tacrolimus is metabolized solely by CYP3A4 in recipients with the CYP3A5*3/*3. Tacrolimus 81-91 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 147-153 29547545-2 2018 The purpose of this study was to evaluate how the area under the blood concentration-time curves (AUC) of tacrolimus could be predicted based on CYP3A5 genotype and the AUC of everolimus in renal transplant patients taking both drugs. Tacrolimus 106-116 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 145-151 29547545-4 2018 Significant correlations between the AUC/D of tacrolimus and everolimus were found for patients with the CYP3A5*1 allele or CYP3A5*3/*3 at both one month and one year. Tacrolimus 46-56 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 105-111 29547545-4 2018 Significant correlations between the AUC/D of tacrolimus and everolimus were found for patients with the CYP3A5*1 allele or CYP3A5*3/*3 at both one month and one year. Tacrolimus 46-56 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 124-130 29547545-6 2018 A good correlation between single doses of tacrolimus and everolimus was found for CYP3A5*3/*3 patients at 1 year after transplantation (r = 0.794, p < 0.001). Tacrolimus 43-53 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 83-89 29547545-7 2018 The variability of the AUC0-24/D of tacrolimus for each CYP3A5 genotype could be predicted based on the AUC0-12/D of everolimus. Tacrolimus 36-46 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 56-62 29547545-8 2018 Clinicians may be able to comprehensively carry out the dose adjustments of tacrolimus and everolimus based on relationship with AUCs of both drugs in each CYP3A5 genotype. Tacrolimus 76-86 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 156-162 29274751-6 2018 NCX2 or NCX3 heterozygotes displayed impaired maintenance of hippocampal LTP, a phenotype that in NCX2+/- mice was correlated with elevated calcineurin activity and rescued by treatment with the calcineurin (CaN) inhibitor FK506. Tacrolimus 223-228 solute carrier family 8 (sodium/calcium exchanger), member 3 Mus musculus 8-12 29559812-7 2018 The IRR (95% confidence interval [CI]) for lymphoma, tacrolimus versus TCSs, was 3.74 (1.00-14.06) in children and 1.27 (0.94-1.71) in adults. Tacrolimus 53-63 insulin receptor related receptor Homo sapiens 4-7 29412644-0 2018 Conformational Entropy of FK506 Binding to FKBP12 Determined by Nuclear Magnetic Resonance Relaxation and Molecular Dynamics Simulations. Tacrolimus 26-31 FKBP prolyl isomerase 1A Homo sapiens 43-49 29412644-3 2018 Here we report backbone and methyl-axis order parameters of the apo and FK506-bound forms of FKBP12, based on 15N and 2H NMR relaxation. Tacrolimus 72-77 FKBP prolyl isomerase 1A Homo sapiens 93-99 29412644-4 2018 Binding of FK506 to FKBP12 results in localized changes in order parameters, notably for the backbone of residues E54 and I56 and the side chains of I56, I90, and I91, all positioned in the binding site. Tacrolimus 11-16 FKBP prolyl isomerase 1A Homo sapiens 20-26 29162334-1 2018 BACKGROUND: Differences in tacrolimus dosing across ancestries is partly attributable to polymorphisms in CYP3A5 genes that encode tacrolimus-metabolizing cytochrome P450 3A5 enzymes. Tacrolimus 27-37 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 106-112 29563827-0 2018 CYP3A5 polymorphisms in renal transplant recipients: influence on tacrolimus treatment. Tacrolimus 66-76 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 29563827-3 2018 Genetic polymorphism in CYP3A5 enzyme expression contributes to differences in tacrolimus bioavailability between individuals. Tacrolimus 79-89 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 24-30 29563827-4 2018 Individuals carrying one or more copies of the wild-type allele *1 express CYP3A5, which increases tacrolimus clearance. Tacrolimus 99-109 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 75-81 29563827-5 2018 CYP3A5 expressers require 1.5 to 2-fold higher tacrolimus doses compared to usual dosing to achieve therapeutic blood concentrations. Tacrolimus 47-57 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 29563827-8 2018 Differences between CYP3A5 genotypes in tacrolimus disposition have not translated into differences in clinical outcomes, such as acute rejection and graft survival. Tacrolimus 40-50 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 20-26 29563827-10 2018 CYP3A5 genotype may predict differences in absorption of extended-release and immediate-release oral formulations of tacrolimus. Tacrolimus 117-127 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 29563827-11 2018 Two studies found that CYP3A5 expressers require higher doses of tacrolimus in the extended-release formulation compared to immediate release. Tacrolimus 65-75 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 23-29 29563827-12 2018 CYP3A5 genotype plays a role in determining the impact of interacting drugs, such as fluconazole, on tacrolimus pharmacokinetics. Tacrolimus 101-111 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 29563827-13 2018 Evidence conflicts regarding the impact of CYP3A5 genotype on risk of nephrotoxicity associated with tacrolimus. Tacrolimus 101-111 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 43-49 29162334-1 2018 BACKGROUND: Differences in tacrolimus dosing across ancestries is partly attributable to polymorphisms in CYP3A5 genes that encode tacrolimus-metabolizing cytochrome P450 3A5 enzymes. Tacrolimus 131-141 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 106-112 29162334-2 2018 The CYP3A5*1 allele, preponderant in African Americans, is associated with rapid metabolism, subtherapeutic concentrations, and higher dose requirements for tacrolimus, all contributing to worse outcomes. Tacrolimus 157-167 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 4-10 28945011-1 2018 Schisantherin A and schisandrin A, the most abundant active ingredients of Wuzhi capsule, are known to inhibit tacrolimus metabolism by inhibiting CYP3A4/5. Tacrolimus 111-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 147-153 29218605-10 2018 But FK506 increased the mRNA levels of IL12 and inhibited the expression of ICAM-1 mRNAs and had no effects on the IFN-gammaRalpha, MDC, and SOCS1 mRNA in HaCaT cells stimulated with TNF-alpha and IFN-gamma. Tacrolimus 4-9 intercellular adhesion molecule 1 Homo sapiens 76-82 29314738-9 2018 CONCLUSION: Adding tacrolimus onto anti-TNF therapy is a promising therapeutic option with sustained benefit for refractory RA patients despite treatment with anti-TNF therapy combined with methotrexate. Tacrolimus 19-29 tumor necrosis factor Homo sapiens 164-167 29131377-1 2018 FKBP12, known as FK506 binding protein, binds to immunosuppressive drug FK506, which must be taken by patients who received organ transplant. Tacrolimus 17-22 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 0-6 29131377-5 2018 Inhibiting FKBP12 by FK506 significantly increased the rate of 1-cell and fragmented embryos, greatly reduced the rate of 2-cell embryos during in vitro fertilization. Tacrolimus 21-26 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 11-17 29131377-7 2018 QPCR demonstrated that Fbxo43 and P27kip, which are related to the release of MII oocyte arrest, and calcium channel partner protein Orai1 were downregulated, while Cdc2 and Ca2+ sensor at ER, stromal interaction molecule 1 (Stim1) were upregulated for a short time after adding FK506. Tacrolimus 279-284 ORAI calcium release-activated calcium modulator 1 Homo sapiens 133-138 29469606-0 2018 Detection of a rare CYP3A4 variant in a transplant patient characterized by a tacrolimus poor metabolizer phenotype. Tacrolimus 78-88 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 20-26 29162334-12 2018 With IR-Tac, tacrolimus Cmax was 33% higher in CYP3A5 expressers compared with nonexpressers (P=0.04): With LCPT, this difference was 11% (P=0.4). Tacrolimus 13-23 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 47-53 29495430-4 2018 We assessed the amount of tacrolimus and its metabolites, M-1 and M-3, that would be ingested by the breastfed neonates. Tacrolimus 26-36 myoregulin Homo sapiens 58-69 29495430-10 2018 Low concentrations of tacrolimus and its metabolites, M-1 and M-3, in colostrum show that neonates will ingest trace amounts of the drug. Tacrolimus 22-32 myoregulin Homo sapiens 54-65 29520229-0 2018 Tacrolimus Reverses UVB Irradiation-Induced Epidermal Langerhans Cell Reduction by Inhibiting TNF-alpha Secretion in Keratinocytes via Regulation of NF-kappaB/p65. Tacrolimus 0-10 tumor necrosis factor Homo sapiens 94-103 29520229-0 2018 Tacrolimus Reverses UVB Irradiation-Induced Epidermal Langerhans Cell Reduction by Inhibiting TNF-alpha Secretion in Keratinocytes via Regulation of NF-kappaB/p65. Tacrolimus 0-10 nuclear factor kappa B subunit 1 Homo sapiens 149-158 29520229-0 2018 Tacrolimus Reverses UVB Irradiation-Induced Epidermal Langerhans Cell Reduction by Inhibiting TNF-alpha Secretion in Keratinocytes via Regulation of NF-kappaB/p65. Tacrolimus 0-10 RELA proto-oncogene, NF-kB subunit Homo sapiens 159-162 29520229-10 2018 Results: Topical tacrolimus significantly reversed high-dose UVB irradiation-induced epidermal LC reduction and CD1a+ cell increment in culture medium. Tacrolimus 17-27 CD1a molecule Homo sapiens 112-116 29520229-11 2018 Tacrolimus significantly inhibited UVB irradiation-induced tumor necrosis factor-alpha (TNF-alpha) and nuclear factor kappa B (NF-kappaB)/p65 mRNA and protein expression in HaCaT cells. Tacrolimus 0-10 tumor necrosis factor Homo sapiens 59-86 29520229-11 2018 Tacrolimus significantly inhibited UVB irradiation-induced tumor necrosis factor-alpha (TNF-alpha) and nuclear factor kappa B (NF-kappaB)/p65 mRNA and protein expression in HaCaT cells. Tacrolimus 0-10 tumor necrosis factor Homo sapiens 88-97 29520229-11 2018 Tacrolimus significantly inhibited UVB irradiation-induced tumor necrosis factor-alpha (TNF-alpha) and nuclear factor kappa B (NF-kappaB)/p65 mRNA and protein expression in HaCaT cells. Tacrolimus 0-10 nuclear factor kappa B subunit 1 Homo sapiens 103-125 29520229-11 2018 Tacrolimus significantly inhibited UVB irradiation-induced tumor necrosis factor-alpha (TNF-alpha) and nuclear factor kappa B (NF-kappaB)/p65 mRNA and protein expression in HaCaT cells. Tacrolimus 0-10 nuclear factor kappa B subunit 1 Homo sapiens 127-136 29520229-11 2018 Tacrolimus significantly inhibited UVB irradiation-induced tumor necrosis factor-alpha (TNF-alpha) and nuclear factor kappa B (NF-kappaB)/p65 mRNA and protein expression in HaCaT cells. Tacrolimus 0-10 RELA proto-oncogene, NF-kB subunit Homo sapiens 138-141 29520229-12 2018 Tacrolimus also significantly inhibited high-dose UVB irradiation-induced TNF-alpha expression in cultured tissues. Tacrolimus 0-10 tumor necrosis factor Homo sapiens 74-83 29520229-14 2018 Conclusion: Topical tacrolimus 0.03% could reverse UVB irradiation-induced epidermal LC reduction by inhibiting TNF-alpha secretion in keratinocytes via regulation of NF-kappaB/p65. Tacrolimus 20-30 tumor necrosis factor Homo sapiens 112-121 29520229-14 2018 Conclusion: Topical tacrolimus 0.03% could reverse UVB irradiation-induced epidermal LC reduction by inhibiting TNF-alpha secretion in keratinocytes via regulation of NF-kappaB/p65. Tacrolimus 20-30 nuclear factor kappa B subunit 1 Homo sapiens 167-176 29520229-14 2018 Conclusion: Topical tacrolimus 0.03% could reverse UVB irradiation-induced epidermal LC reduction by inhibiting TNF-alpha secretion in keratinocytes via regulation of NF-kappaB/p65. Tacrolimus 20-30 RELA proto-oncogene, NF-kB subunit Homo sapiens 177-180 29527316-2 2018 We aimed to describe the utility of tacrolimus to prevent colectomy during second-line vedolizumab initiation after corticosteroid and anti-TNF treatment failure in paediatric severe colitis. Tacrolimus 36-46 tumor necrosis factor Homo sapiens 140-143 29527316-10 2018 Conclusion: We report real-world data on the outcome of tacrolimus around vedolizumab initiation in paediatric UC or CD after corticosteroid and anti-TNF therapy treatment failure. Tacrolimus 56-66 tumor necrosis factor Homo sapiens 150-153 29422055-7 2018 However, Fk506-treated mice displayed a decrease in GFAP levels in the ARC. Tacrolimus 9-14 glial fibrillary acidic protein Mus musculus 52-56 29283464-6 2018 Changes in release of TGF-beta were sensitive to the calcineurin (CaN) inhibitor FK506. Tacrolimus 81-86 transforming growth factor alpha Mus musculus 22-30 29553465-18 2018 Myeloperoxidase and malondialdehyde levels were significantly correlated between the EGb761 and FK506 groups, even at lower levels in the EGb761 group (p<0.001). Tacrolimus 96-101 myeloperoxidase Rattus norvegicus 0-15 29375315-8 2017 In addition, FK506 treatment down-regulated the expression level of GFAP, a specific marker of astrocytes. Tacrolimus 13-18 glial fibrillary acidic protein Rattus norvegicus 68-72 29102373-6 2018 Specifically, combination therapy inhibited TLR7 expression in the kidneys of mice with lupus nephritis; combination of tacrolimus and mycophenolate mofetil led to better stabilization of the podocyte actin cytoskeleton through the reciprocal regulation of RhoA and Rac1 activities. Tacrolimus 120-130 ras homolog family member A Mus musculus 257-261 29102373-6 2018 Specifically, combination therapy inhibited TLR7 expression in the kidneys of mice with lupus nephritis; combination of tacrolimus and mycophenolate mofetil led to better stabilization of the podocyte actin cytoskeleton through the reciprocal regulation of RhoA and Rac1 activities. Tacrolimus 120-130 Rac family small GTPase 1 Mus musculus 266-270 28974433-11 2018 The higher level of circulating Tfh cells in tacrolimus group might be related to STAT3 signaling. Tacrolimus 45-55 signal transducer and activator of transcription 3 Sus scrofa 82-87 29128286-0 2018 TRPA1 channel participates in tacrolimus-induced pruritus in a chronic contact hypersensitivity murine model. Tacrolimus 30-40 transient receptor potential cation channel, subfamily A, member 1 Mus musculus 0-5 29288897-9 2018 The NFAT signaling inhibitor, FK-506, eliminated the effect of TRPC6 on HK-2 cells. Tacrolimus 30-36 transient receptor potential cation channel subfamily C member 6 Homo sapiens 63-68 29256966-0 2018 Influence of donor liver CYP3A4*20 loss-of-function genotype on tacrolimus pharmacokinetics in transplanted patients. Tacrolimus 64-74 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 25-31 29256966-2 2018 Here, we report the effect of the CYP3A4*20 frameshift allele in two Spanish liver transplant patients treated with tacrolimus. Tacrolimus 116-126 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-40 29256966-10 2018 CONCLUSION: This first description of CYP3A4*20 null genotype in liver-transplanted patients, supports the relevance of CYP3A genotyping in tacrolimus therapy. Tacrolimus 140-150 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-44 29256966-10 2018 CONCLUSION: This first description of CYP3A4*20 null genotype in liver-transplanted patients, supports the relevance of CYP3A genotyping in tacrolimus therapy. Tacrolimus 140-150 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-43 29594146-0 2018 Early Conversion from Tacrolimus to Belatacept in a Highly Sensitized Renal Allograft Recipient with Calcineurin Inhibitor-Induced de novo Post-Transplant Hemolytic Uremic Syndrome. Tacrolimus 22-32 calcineurin binding protein 1 Homo sapiens 101-122 28689771-0 2018 Immunosuppression with tacrolimus improved implantation and rescued expression of uterine progesterone receptor and its co-regulators FKBP52 and PIASy at nidation in the obese and diabetic mice: Comparative studies with metformin. Tacrolimus 23-33 progesterone receptor Mus musculus 90-111 28689771-0 2018 Immunosuppression with tacrolimus improved implantation and rescued expression of uterine progesterone receptor and its co-regulators FKBP52 and PIASy at nidation in the obese and diabetic mice: Comparative studies with metformin. Tacrolimus 23-33 FK506 binding protein 4 Mus musculus 134-140 28689771-0 2018 Immunosuppression with tacrolimus improved implantation and rescued expression of uterine progesterone receptor and its co-regulators FKBP52 and PIASy at nidation in the obese and diabetic mice: Comparative studies with metformin. Tacrolimus 23-33 protein inhibitor of activated STAT 4 Mus musculus 145-150 28689771-3 2018 Immunosuppression with tacrolimus improved pregnancy outcomes in obese and diabetic mice and repeated IF in women with elevated Th1/Th2 blood cell ratios. Tacrolimus 23-33 negative elongation factor complex member C/D Homo sapiens 128-131 28689771-8 2018 Therapeutic interventions with tacrolimus or metformin normalized the expression of decidual IFNgamma, PGR and FKBP52, increased co-localization of protein inhibitor of activated STATy (PIASy) to PGR and resulted in the upregulation of uterine IL11and LIF. Tacrolimus 31-41 interferon gamma Mus musculus 93-101 28689771-8 2018 Therapeutic interventions with tacrolimus or metformin normalized the expression of decidual IFNgamma, PGR and FKBP52, increased co-localization of protein inhibitor of activated STATy (PIASy) to PGR and resulted in the upregulation of uterine IL11and LIF. Tacrolimus 31-41 progesterone receptor Mus musculus 103-106 28689771-8 2018 Therapeutic interventions with tacrolimus or metformin normalized the expression of decidual IFNgamma, PGR and FKBP52, increased co-localization of protein inhibitor of activated STATy (PIASy) to PGR and resulted in the upregulation of uterine IL11and LIF. Tacrolimus 31-41 FK506 binding protein 4 Mus musculus 111-117 28689771-8 2018 Therapeutic interventions with tacrolimus or metformin normalized the expression of decidual IFNgamma, PGR and FKBP52, increased co-localization of protein inhibitor of activated STATy (PIASy) to PGR and resulted in the upregulation of uterine IL11and LIF. Tacrolimus 31-41 protein inhibitor of activated STAT 4 Mus musculus 186-191 28689771-8 2018 Therapeutic interventions with tacrolimus or metformin normalized the expression of decidual IFNgamma, PGR and FKBP52, increased co-localization of protein inhibitor of activated STATy (PIASy) to PGR and resulted in the upregulation of uterine IL11and LIF. Tacrolimus 31-41 progesterone receptor Mus musculus 196-199 28689771-8 2018 Therapeutic interventions with tacrolimus or metformin normalized the expression of decidual IFNgamma, PGR and FKBP52, increased co-localization of protein inhibitor of activated STATy (PIASy) to PGR and resulted in the upregulation of uterine IL11and LIF. Tacrolimus 31-41 interleukin 11 Mus musculus 244-248 28689771-8 2018 Therapeutic interventions with tacrolimus or metformin normalized the expression of decidual IFNgamma, PGR and FKBP52, increased co-localization of protein inhibitor of activated STATy (PIASy) to PGR and resulted in the upregulation of uterine IL11and LIF. Tacrolimus 31-41 leukemia inhibitory factor Mus musculus 252-255 29801578-4 2018 For calcineurin inhibitors like cyclosporine and in particular tacrolimus however, cytochrome P450 3A4 and 3A5 variants were found to significantly affect the pharmacokinetics. Tacrolimus 63-73 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 83-102 29539600-1 2018 BACKGROUND: Tacrolimus is mainly metabolized by cytochrome P450 3A5 (CYP3A5), which is expressed in the liver. Tacrolimus 12-22 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 48-67 29178680-8 2018 The accumulation of eosinophils and Th2 cells in the skin was suppressed by both dexamethasone and FK506, indicating an essential role of Th2 cells in eosinophil recruitment. Tacrolimus 99-104 heart and neural crest derivatives expressed 2 Mus musculus 36-39 29178680-8 2018 The accumulation of eosinophils and Th2 cells in the skin was suppressed by both dexamethasone and FK506, indicating an essential role of Th2 cells in eosinophil recruitment. Tacrolimus 99-104 heart and neural crest derivatives expressed 2 Mus musculus 138-141 29539600-1 2018 BACKGROUND: Tacrolimus is mainly metabolized by cytochrome P450 3A5 (CYP3A5), which is expressed in the liver. Tacrolimus 12-22 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 69-75 29539600-2 2018 However, CYP3A5 is also expressed in the kidney tissue and may contribute to local tacrolimus clearance in the kidney allograft. Tacrolimus 83-93 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 9-15 29055041-0 2018 The possible clinical impact of risperidone on P-glycoprotein-mediated transport of tacrolimus: A case report and in vitro study. Tacrolimus 84-94 ATP binding cassette subfamily B member 1 Homo sapiens 47-61 28617417-2 2018 FKBP14 is an ER-resident protein belonging to the family of FK506-binding peptidyl-prolyl cis-trans isomerases (PPIases); it catalyzes the folding of type III collagen and interacts with type III, type VI, and type X collagens. Tacrolimus 60-65 FKBP prolyl isomerase 14 Homo sapiens 0-6 29298646-1 2018 BACKGROUND: The calcineurin inhibitor tacrolimus (Tac) is an integral part of the standard immunosuppressive regimen after renal transplantation (RTx). Tacrolimus 38-48 calcineurin binding protein 1 Homo sapiens 16-37 30156148-9 2018 Notably, the CYP3A7-CYP3A4 switch taking place during the very early life will affect tacrolimus metabolism. Tacrolimus 86-96 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 13-26 30156148-11 2018 The guideline has recommended that the tacrolimus dosage should be adjusted according to the CYP3A5 genotype. Tacrolimus 39-49 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 93-99 30156148-12 2018 Additionally, genetic CYP3A4 variation (e.g., CYP3A4*22) is also associated with interindividual variability of exposure level to tacrolimus. Tacrolimus 130-140 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 22-28 30156148-12 2018 Additionally, genetic CYP3A4 variation (e.g., CYP3A4*22) is also associated with interindividual variability of exposure level to tacrolimus. Tacrolimus 130-140 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 46-52 29393157-0 2018 Tacrolimus Dose Optimization Strategy for Refractory Ulcerative Colitis Based on the Cytochrome P450 3A5 Polymorphism Prediction Using Trough Concentration after 24 Hours. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 85-104 29393157-2 2018 Cytochrome P450 (CYP) 3A5 polymorphism affects tacrolimus blood concentrations. Tacrolimus 47-57 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-25 29393157-7 2018 In the CYP3A5 non-expressers, the dose of tacrolimus (mg/kg) was lower and dose-adjusted trough levels (ng/mL per mg/kg) were higher compared with those in expressers. Tacrolimus 42-52 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 7-13 29393157-12 2018 Key Message: The trough concentration 24 h after the first tacrolimus administration appears to be a useful predictor of -CYP3A5 polymorphism. Tacrolimus 59-69 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 122-128 29055041-3 2018 It was hypothesized that cytochrome P450 (CYP)3A inhibition of the small intestine by voriconazole and P-glycoprotein (P-gp) inhibition of the small intestine by risperidone exerted a synergistic effect on the bioavailability of tacrolimus. Tacrolimus 229-239 ATP binding cassette subfamily B member 1 Homo sapiens 103-117 29055041-3 2018 It was hypothesized that cytochrome P450 (CYP)3A inhibition of the small intestine by voriconazole and P-glycoprotein (P-gp) inhibition of the small intestine by risperidone exerted a synergistic effect on the bioavailability of tacrolimus. Tacrolimus 229-239 ATP binding cassette subfamily B member 1 Homo sapiens 119-123 29055041-4 2018 The aim of the present study was to evaluate the effect of risperidone on the P-gp-mediated transport of tacrolimus. Tacrolimus 105-115 ATP binding cassette subfamily B member 1 Homo sapiens 78-82 29161757-6 2018 Tacrolimus total daily dose at first therapeutic level was significantly higher in CYP3A5*1 expressers (12 mg/day) compared to nonexpressers (8 mg/day; P < .001). Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 83-89 29161757-9 2018 The findings from this retrospective study suggest that AAs with CYP3A5*1 expression require 50% more tacrolimus and have an increased incidence of DGF and acute rejection. Tacrolimus 102-112 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 65-71 30251601-0 2018 Influence of CYP3A and ABCB1 Single Nucleotide Polymorphisms on the Pharmacokinetics/Pharmacodynamics of Tacrolimus in Pediatric Patients. Tacrolimus 105-115 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 13-18 30251601-0 2018 Influence of CYP3A and ABCB1 Single Nucleotide Polymorphisms on the Pharmacokinetics/Pharmacodynamics of Tacrolimus in Pediatric Patients. Tacrolimus 105-115 ATP binding cassette subfamily B member 1 Homo sapiens 23-28 30251601-4 2018 This article focuses on the effects of ABCB1 and CYP3A SNPs on tacrolimus in children who are undergoing organ transplantations. Tacrolimus 63-73 ATP binding cassette subfamily B member 1 Homo sapiens 39-44 30251601-4 2018 This article focuses on the effects of ABCB1 and CYP3A SNPs on tacrolimus in children who are undergoing organ transplantations. Tacrolimus 63-73 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 49-54 30251601-9 2018 However, although the amount of literature is limited, it does show a link between ABCB1 SNPs and tacrolimus pharmacodynamics. Tacrolimus 98-108 ATP binding cassette subfamily B member 1 Homo sapiens 83-88 30251601-10 2018 In addition, the literature shows a strong link between CYP3A5 SNP and pharmacokinetics of tacrolimus, but there is no direct evidence that CYP3A5 SNP has the same effect on the pharmacodynamics of tacrolimus. Tacrolimus 91-101 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 56-62 30251601-11 2018 CONCLUSION: More standardized clinical trials are needed to assess the relationship between CYP3A5 SNP and tacrolimus pharmacodynamics in children, particularly in terms of acute rejection and nephrotoxicity. Tacrolimus 107-117 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 92-98 28522399-7 2017 Sacran solutions and 0.1%Tacrolimus reduced disease severity, suppressed histological changes and decreased the serum Th-1 (IFN-gamma, TNF-alpha, IL-2) and Th-2 (IL-4, IL-6, IL-10) cytokines in allergic mice (vs. controls). Tacrolimus 25-35 negative elongation factor complex member C/D, Th1l Mus musculus 118-122 28094348-0 2018 Weight of ABCB1 and POR genes on oral tacrolimus exposure in CYP3A5 nonexpressor pediatric patients with stable kidney transplant. Tacrolimus 38-48 ATP binding cassette subfamily B member 1 Homo sapiens 10-15 28094348-0 2018 Weight of ABCB1 and POR genes on oral tacrolimus exposure in CYP3A5 nonexpressor pediatric patients with stable kidney transplant. Tacrolimus 38-48 cytochrome p450 oxidoreductase Homo sapiens 20-23 28094348-0 2018 Weight of ABCB1 and POR genes on oral tacrolimus exposure in CYP3A5 nonexpressor pediatric patients with stable kidney transplant. Tacrolimus 38-48 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 61-67 29375701-8 2018 In conclusion, the clearance of tacrolimus in patients with autoimmune diseases was affected by the CYP3A5 genotype, as previously reported in organ transplant patients. Tacrolimus 32-42 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 100-106 29348725-0 2018 Protective effect of ginsenoside Rb1 against tacrolimus-induced apoptosis in renal proximal tubular LLC-PK1 cells. Tacrolimus 45-55 RB transcriptional corepressor 1 Sus scrofa 33-36 29348725-1 2018 Background: The aim of the present study was to evaluate the potential protective effects of six ginsenosides (Rb1, Rb2, Rc, Rd, Rg1, and Rg3) isolated from Panax ginseng against tacrolimus (FK506)-induced apoptosis in renal proximal tubular LLC-PK1 cells. Tacrolimus 179-189 RB transcriptional corepressor 1 Sus scrofa 111-114 29348725-1 2018 Background: The aim of the present study was to evaluate the potential protective effects of six ginsenosides (Rb1, Rb2, Rc, Rd, Rg1, and Rg3) isolated from Panax ginseng against tacrolimus (FK506)-induced apoptosis in renal proximal tubular LLC-PK1 cells. Tacrolimus 191-196 RB transcriptional corepressor 1 Sus scrofa 111-114 29348725-5 2018 Results: Reduction in cell viability by 60muM FK506 was ameliorated significantly by cotreatment with ginsenosides Rg1 and Rb1. Tacrolimus 46-51 RB transcriptional corepressor 1 Sus scrofa 123-126 29348725-6 2018 The phosphorylation of p38, extracellular signal-regulated kinases, and KIM-1, and cleavage of caspase-3, increased markedly in LLC-PK1 cells treated with FK506 and significantly decreased after cotreatment with ginsenoside Rb1. Tacrolimus 155-160 caspase 3 Sus scrofa 95-104 29348725-6 2018 The phosphorylation of p38, extracellular signal-regulated kinases, and KIM-1, and cleavage of caspase-3, increased markedly in LLC-PK1 cells treated with FK506 and significantly decreased after cotreatment with ginsenoside Rb1. Tacrolimus 155-160 RB transcriptional corepressor 1 Sus scrofa 224-227 29348725-8 2018 Conclusion: The antiapoptotic effects of ginsenoside Rb1 on FK506-induced apoptosis were mediated by the inhibition of mitogen-activated protein kinases and caspase activation. Tacrolimus 60-65 RB transcriptional corepressor 1 Sus scrofa 53-56 30531101-6 2018 By contrast, NCX2+/- mice was correlated with elevated calcineurin (CaN) activity and rescued by treatment with the calcineurin inhibitor FK506. Tacrolimus 138-143 solute carrier family 8 (sodium/calcium exchanger), member 2 Mus musculus 13-17 29199543-4 2018 NR1I2 and NR1I3 genetic polymorphisms can affect the pharmacokinetics and therapeutic response to many drugs, such as irinotecan, tacrolimus and atazanavir. Tacrolimus 130-140 nuclear receptor subfamily 1 group I member 2 Homo sapiens 0-5 29199543-4 2018 NR1I2 and NR1I3 genetic polymorphisms can affect the pharmacokinetics and therapeutic response to many drugs, such as irinotecan, tacrolimus and atazanavir. Tacrolimus 130-140 nuclear receptor subfamily 1 group I member 3 Homo sapiens 10-15 29023988-3 2018 However, the structural conservation of the FK1 domains between FKBP51 and FKBP52 make it difficult to obtain satisfactory selectivity in FK506-based drug design. Tacrolimus 138-143 FKBP prolyl isomerase 4 Homo sapiens 75-81 29229832-3 2017 Calcineurin can be inhibited with Tacrolimus through the recruitment and inhibition of the 12-kDa cis-trans proline isomerase FK506-binding protein (FKBP12). Tacrolimus 34-44 FKBP prolyl isomerase 1A Rattus norvegicus 149-155 29229832-7 2017 Using a rat model of PD, partial elimination of the functional interaction between FKBP12 and calcineurin, with low doses of the Food and Drug Administration (FDA)-approved compound Tacrolimus, blocks calcineurin"s activity toward those proteins and protects against the toxic hallmarks of alpha-syn pathology. Tacrolimus 182-192 FKBP prolyl isomerase 1A Rattus norvegicus 83-89 28973643-0 2017 Tacrolimus rescues the signaling and gene expression signature of endothelial ALK1 loss-of-function and improves HHT vascular pathology. Tacrolimus 0-10 activin A receptor, type II-like 1 Mus musculus 78-82 28973643-4 2017 By screening the NIH clinical collections of FDA-approved drugs, we identified tacrolimus (FK-506) as the most potent activator of ALK1 signaling in BMP9-challenged C2C12 reporter cells. Tacrolimus 79-89 activin A receptor, type II-like 1 Mus musculus 131-135 28973643-4 2017 By screening the NIH clinical collections of FDA-approved drugs, we identified tacrolimus (FK-506) as the most potent activator of ALK1 signaling in BMP9-challenged C2C12 reporter cells. Tacrolimus 79-89 growth differentiation factor 2 Mus musculus 149-153 28973643-4 2017 By screening the NIH clinical collections of FDA-approved drugs, we identified tacrolimus (FK-506) as the most potent activator of ALK1 signaling in BMP9-challenged C2C12 reporter cells. Tacrolimus 91-97 activin A receptor, type II-like 1 Mus musculus 131-135 28973643-4 2017 By screening the NIH clinical collections of FDA-approved drugs, we identified tacrolimus (FK-506) as the most potent activator of ALK1 signaling in BMP9-challenged C2C12 reporter cells. Tacrolimus 91-97 growth differentiation factor 2 Mus musculus 149-153 28973643-5 2017 In HUVECs, tacrolimus activated Smad1/5/8 and opposed the pro-angiogenic gene expression signature associated with ALK1 loss-of-function, by notably reducing Dll4 expression. Tacrolimus 11-21 SMAD family member 1 Mus musculus 32-39 28973643-5 2017 In HUVECs, tacrolimus activated Smad1/5/8 and opposed the pro-angiogenic gene expression signature associated with ALK1 loss-of-function, by notably reducing Dll4 expression. Tacrolimus 11-21 activin A receptor, type II-like 1 Mus musculus 115-119 28973643-5 2017 In HUVECs, tacrolimus activated Smad1/5/8 and opposed the pro-angiogenic gene expression signature associated with ALK1 loss-of-function, by notably reducing Dll4 expression. Tacrolimus 11-21 delta like canonical Notch ligand 4 Mus musculus 158-162 28973643-6 2017 In these cells, tacrolimus also inhibited Akt and p38 stimulation by vascular endothelial growth factor, a major driver of angiogenesis. Tacrolimus 16-26 mitogen-activated protein kinase 14 Mus musculus 50-53 28973643-7 2017 In the BMP9/10-immunodepleted postnatal retina-a mouse model of HHT vascular pathology-tacrolimus activated endothelial Smad1/5/8 and prevented the Dll4 overexpression and hypervascularization associated with this model. Tacrolimus 87-97 growth differentiation factor 2 Mus musculus 7-11 28973643-7 2017 In the BMP9/10-immunodepleted postnatal retina-a mouse model of HHT vascular pathology-tacrolimus activated endothelial Smad1/5/8 and prevented the Dll4 overexpression and hypervascularization associated with this model. Tacrolimus 87-97 SMAD family member 1 Mus musculus 120-127 28973643-7 2017 In the BMP9/10-immunodepleted postnatal retina-a mouse model of HHT vascular pathology-tacrolimus activated endothelial Smad1/5/8 and prevented the Dll4 overexpression and hypervascularization associated with this model. Tacrolimus 87-97 delta like canonical Notch ligand 4 Mus musculus 148-152 28973643-8 2017 Finally, tacrolimus stimulated Smad1/5/8 signaling in C2C12 cells expressing BMP9-unresponsive ALK1 HHT mutants and in HHT patient blood outgrowth ECs. Tacrolimus 9-19 SMAD family member 1 Mus musculus 31-38 28973643-8 2017 Finally, tacrolimus stimulated Smad1/5/8 signaling in C2C12 cells expressing BMP9-unresponsive ALK1 HHT mutants and in HHT patient blood outgrowth ECs. Tacrolimus 9-19 growth differentiation factor 2 Mus musculus 77-81 28973643-8 2017 Finally, tacrolimus stimulated Smad1/5/8 signaling in C2C12 cells expressing BMP9-unresponsive ALK1 HHT mutants and in HHT patient blood outgrowth ECs. Tacrolimus 9-19 activin A receptor, type II-like 1 Mus musculus 95-99 28437851-5 2017 Predictors of tacrolimus clearance were CYP3A5 genotype, midazolam clearance, hematocrit, weight, and age (R2 = 0.61). Tacrolimus 14-24 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 40-46 28522399-7 2017 Sacran solutions and 0.1%Tacrolimus reduced disease severity, suppressed histological changes and decreased the serum Th-1 (IFN-gamma, TNF-alpha, IL-2) and Th-2 (IL-4, IL-6, IL-10) cytokines in allergic mice (vs. controls). Tacrolimus 25-35 interferon gamma Mus musculus 124-133 28522399-7 2017 Sacran solutions and 0.1%Tacrolimus reduced disease severity, suppressed histological changes and decreased the serum Th-1 (IFN-gamma, TNF-alpha, IL-2) and Th-2 (IL-4, IL-6, IL-10) cytokines in allergic mice (vs. controls). Tacrolimus 25-35 tumor necrosis factor Mus musculus 135-144 28522399-7 2017 Sacran solutions and 0.1%Tacrolimus reduced disease severity, suppressed histological changes and decreased the serum Th-1 (IFN-gamma, TNF-alpha, IL-2) and Th-2 (IL-4, IL-6, IL-10) cytokines in allergic mice (vs. controls). Tacrolimus 25-35 interleukin 2 Mus musculus 146-150 28522399-7 2017 Sacran solutions and 0.1%Tacrolimus reduced disease severity, suppressed histological changes and decreased the serum Th-1 (IFN-gamma, TNF-alpha, IL-2) and Th-2 (IL-4, IL-6, IL-10) cytokines in allergic mice (vs. controls). Tacrolimus 25-35 heart and neural crest derivatives expressed 2 Mus musculus 156-160 28522399-7 2017 Sacran solutions and 0.1%Tacrolimus reduced disease severity, suppressed histological changes and decreased the serum Th-1 (IFN-gamma, TNF-alpha, IL-2) and Th-2 (IL-4, IL-6, IL-10) cytokines in allergic mice (vs. controls). Tacrolimus 25-35 interleukin 4 Mus musculus 162-166 28522399-7 2017 Sacran solutions and 0.1%Tacrolimus reduced disease severity, suppressed histological changes and decreased the serum Th-1 (IFN-gamma, TNF-alpha, IL-2) and Th-2 (IL-4, IL-6, IL-10) cytokines in allergic mice (vs. controls). Tacrolimus 25-35 interleukin 6 Mus musculus 168-172 28522399-7 2017 Sacran solutions and 0.1%Tacrolimus reduced disease severity, suppressed histological changes and decreased the serum Th-1 (IFN-gamma, TNF-alpha, IL-2) and Th-2 (IL-4, IL-6, IL-10) cytokines in allergic mice (vs. controls). Tacrolimus 25-35 interleukin 10 Mus musculus 174-179 28885495-0 2017 Isoglycyrrhizinate Magnesium Enhances Hepatoprotective Effect of FK506 on Ischemia-Reperfusion Injury Through HMGB1 Inhibition in a Rat Model of Liver Transplantation. Tacrolimus 65-70 high mobility group box 1 Rattus norvegicus 110-115 27378609-0 2017 Effect of ABCB1 diplotype on tacrolimus disposition in renal recipients depends on CYP3A5 and CYP3A4 genotype. Tacrolimus 29-39 ATP binding cassette subfamily B member 1 Homo sapiens 10-15 27378609-0 2017 Effect of ABCB1 diplotype on tacrolimus disposition in renal recipients depends on CYP3A5 and CYP3A4 genotype. Tacrolimus 29-39 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 83-89 27378609-0 2017 Effect of ABCB1 diplotype on tacrolimus disposition in renal recipients depends on CYP3A5 and CYP3A4 genotype. Tacrolimus 29-39 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 94-100 28885495-10 2017 However, autophagy induced by FK506 also lead to high-mobility group box (HMGB) 1 release from nuclei, resulting in hepatocyte injury through triggering of p38 phosphorylation and chemokine release. Tacrolimus 30-35 mitogen activated protein kinase 14 Rattus norvegicus 156-159 28885495-12 2017 CONCLUSIONS: Iso could inhibit release of HMGB1 by FK506 and enhance the hepatoprotective effect of FK506 in rat LT. Tacrolimus 51-56 high mobility group box 1 Rattus norvegicus 42-47 28965948-9 2017 To further study the mechanism of FK506 protection effect, we discovered it could increase autophagy via inhibit mTOR pathway. Tacrolimus 34-39 mechanistic target of rapamycin kinase Mus musculus 113-117 28965948-10 2017 CONCLUSION: FK506 protect heart function after MI as it improved myocardial cells autophagy process via inhibiting mTOR pathway. Tacrolimus 12-17 mechanistic target of rapamycin kinase Mus musculus 115-119 29155873-1 2017 BACKGROUND: The immunosuppressive drug tacrolimus has the short-term effect of reducing proteinuria in patients with immunoglobulin A nephropathy (IgAN). Tacrolimus 39-49 IGAN1 Homo sapiens 147-151 29155873-17 2017 The use of tacrolimus for a short period of time for patients with IgAN temporarily reduces proteinuria, but the data showed no long-term efficacy regarding proteinuria reduction and improvement of renal function. Tacrolimus 11-21 IGAN1 Homo sapiens 67-71 28864813-4 2017 Sequestration of FKBP12 by rapamycin or tacrolimus activates hepcidin both in vitro and in murine hepatocytes. Tacrolimus 40-50 hepcidin antimicrobial peptide Mus musculus 61-69 28864813-5 2017 Acute tacrolimus treatment transiently increases hepcidin in wild-type mice. Tacrolimus 6-16 hepcidin antimicrobial peptide Mus musculus 49-57 28603840-1 2017 AIMS: The CYP3A metric 4beta-hydroxycholesterol (4betaOHC) has been shown to correlate with tacrolimus steady-state apparent oral clearance (CL/F). Tacrolimus 92-102 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 10-15 28603840-8 2017 In a linear mixed model for the 14-day period, determinants of tacrolimus C0 were CYP3A5 genotype, haematocrit, age and weight (overall R2 = 0.179). Tacrolimus 63-73 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 82-88 28864749-5 2017 Subsequently, 32 patients were enrolled in a prospective, randomized, controlled study and randomly assigned to receive tacrolimus by CYP3A5 genotype plus Wuzhi tablet co-administration guided dosing (study group) or standard dosing (control group). Tacrolimus 120-130 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 134-140 28346662-3 2017 Here, we report three cases of anti-MDA5 antibody-associated DM with RP-ILD in which the patients were treated with combined-modality therapy, including high-dose prednisolone, tacrolimus, intravenous cyclophosphamide and intravenous immunoglobulin (IVIG). Tacrolimus 177-187 interferon induced with helicase C domain 1 Homo sapiens 36-40 28864749-8 2017 Our results show that CYP3A5 genotype plus Wuzhi tablet co-administration guided tacrolimus dosing is a promising therapy for CYP3A5 expressers in the early post-transplant stage, while further study with a larger sample size is required to prove these findings. Tacrolimus 81-91 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 126-132 28761977-9 2017 Calcineurin inhibitors ciclosporin A (CsA) and tacrolimus (FK-506) decreased Fgf23 gene expression and FGF23 protein production. Tacrolimus 47-57 fibroblast growth factor 23 Rattus norvegicus 77-82 28945481-0 2017 Long-Term Influence of CYP3A5, CYP3A4, ABCB1, and NR1I2 Polymorphisms on Tacrolimus Concentration in Chinese Renal Transplant Recipients. Tacrolimus 73-83 nuclear receptor subfamily 1 group I member 2 Homo sapiens 50-55 28945481-7 2017 RESULTS: The alleles CYP3A5*3 and CYP3A4*18B were significantly associated with dose-adjusted tacrolimus blood trough concentrations and had a strong time-genotype interaction with tacrolimus pharmacokinetics. Tacrolimus 94-104 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 21-27 28945481-7 2017 RESULTS: The alleles CYP3A5*3 and CYP3A4*18B were significantly associated with dose-adjusted tacrolimus blood trough concentrations and had a strong time-genotype interaction with tacrolimus pharmacokinetics. Tacrolimus 94-104 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-40 28945481-7 2017 RESULTS: The alleles CYP3A5*3 and CYP3A4*18B were significantly associated with dose-adjusted tacrolimus blood trough concentrations and had a strong time-genotype interaction with tacrolimus pharmacokinetics. Tacrolimus 181-191 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 21-27 28945481-7 2017 RESULTS: The alleles CYP3A5*3 and CYP3A4*18B were significantly associated with dose-adjusted tacrolimus blood trough concentrations and had a strong time-genotype interaction with tacrolimus pharmacokinetics. Tacrolimus 181-191 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-40 28945481-10 2017 Thus, genotyping of the CYP3A4 and CYP3A5 genes should be considered with respect to determining tacrolimus dose regimens during the post-transplantation period. Tacrolimus 97-107 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 24-30 28945481-10 2017 Thus, genotyping of the CYP3A4 and CYP3A5 genes should be considered with respect to determining tacrolimus dose regimens during the post-transplantation period. Tacrolimus 97-107 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 35-41 28901449-0 2017 FK506 suppresses hypoxia-induced inflammation and protects tight junction function via the CaN-NFATc1 signaling pathway in retinal microvascular epithelial cells. Tacrolimus 0-5 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 95-101 28901449-1 2017 The present study aimed to identify whether FK506 suppresses hypoxia-induced inflammation and protects tight junction function via the calcineurin-nuclear factor of activated T-cells 1 (CaN-NFATc1) signaling pathway in mouse retinal microvascular endothelial cells (mRMECs). Tacrolimus 44-49 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 190-196 28901449-6 2017 The TEER value was decreased following hypoxia, but increased following treatment with FK506 (1 and 10 microM) for 24 and 48 h. The protein expression of ZO-1 was also increased following FK506 treatment for 24 h at 1 and 10 microM. Tacrolimus 87-92 tight junction protein 1 Mus musculus 154-158 28901449-6 2017 The TEER value was decreased following hypoxia, but increased following treatment with FK506 (1 and 10 microM) for 24 and 48 h. The protein expression of ZO-1 was also increased following FK506 treatment for 24 h at 1 and 10 microM. Tacrolimus 188-193 tight junction protein 1 Mus musculus 154-158 28901449-9 2017 Following treatment with FK506, the level of total NFATc1 was downregulated and the level of phosphorylated NFATc1 was upregulated. Tacrolimus 25-30 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 51-57 28901449-9 2017 Following treatment with FK506, the level of total NFATc1 was downregulated and the level of phosphorylated NFATc1 was upregulated. Tacrolimus 25-30 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 108-114 28901449-10 2017 Taken together, FK506 suppressed injury to the tight junctions and downregulated the expression of inflammatory cytokines in hypoxia-induced mRMECs via the CaN-NFATc1 signaling pathway. Tacrolimus 16-21 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 160-166 28761977-9 2017 Calcineurin inhibitors ciclosporin A (CsA) and tacrolimus (FK-506) decreased Fgf23 gene expression and FGF23 protein production. Tacrolimus 47-57 fibroblast growth factor 23 Rattus norvegicus 103-108 28761977-9 2017 Calcineurin inhibitors ciclosporin A (CsA) and tacrolimus (FK-506) decreased Fgf23 gene expression and FGF23 protein production. Tacrolimus 59-65 fibroblast growth factor 23 Rattus norvegicus 77-82 28761977-9 2017 Calcineurin inhibitors ciclosporin A (CsA) and tacrolimus (FK-506) decreased Fgf23 gene expression and FGF23 protein production. Tacrolimus 59-65 fibroblast growth factor 23 Rattus norvegicus 103-108 29149986-2 2017 The aim of this work was to study the effects of cyclosporine (CsA), tacrolimus (FK-506), and rapamycin (RAPA) on the release of three local factors directly implicated in bone-remodeling regulation and apoptosis of human osteoblasts: interleukin (IL)-6, osteoprotegerin, and receptor activator of nuclear factor kappabeta (RANKL). Tacrolimus 69-79 TNF receptor superfamily member 11b Homo sapiens 255-270 29149986-2 2017 The aim of this work was to study the effects of cyclosporine (CsA), tacrolimus (FK-506), and rapamycin (RAPA) on the release of three local factors directly implicated in bone-remodeling regulation and apoptosis of human osteoblasts: interleukin (IL)-6, osteoprotegerin, and receptor activator of nuclear factor kappabeta (RANKL). Tacrolimus 69-79 TNF superfamily member 11 Homo sapiens 324-329 29149986-2 2017 The aim of this work was to study the effects of cyclosporine (CsA), tacrolimus (FK-506), and rapamycin (RAPA) on the release of three local factors directly implicated in bone-remodeling regulation and apoptosis of human osteoblasts: interleukin (IL)-6, osteoprotegerin, and receptor activator of nuclear factor kappabeta (RANKL). Tacrolimus 81-87 TNF receptor superfamily member 11b Homo sapiens 255-270 29149986-2 2017 The aim of this work was to study the effects of cyclosporine (CsA), tacrolimus (FK-506), and rapamycin (RAPA) on the release of three local factors directly implicated in bone-remodeling regulation and apoptosis of human osteoblasts: interleukin (IL)-6, osteoprotegerin, and receptor activator of nuclear factor kappabeta (RANKL). Tacrolimus 81-87 TNF superfamily member 11 Homo sapiens 324-329 29149986-8 2017 MAIN FINDINGS: A significant increase in IL-6 (mRNA and released protein) was observed in the presence of FK-506 and RAPA. Tacrolimus 106-112 interleukin 6 Homo sapiens 41-45 29090089-8 2017 Moreover, we identified synergistic effects of sirtinol and FK506 on prolonging allograft survival, and sirtinol synergizes with FK506 to promote Foxp3 expression. Tacrolimus 129-134 forkhead box P3 Mus musculus 146-151 29151414-12 2017 The fewer tacrolimus daily dosage, the lower APACHE II score and levels of PCT and BNP, the more effective promotion of PaO2/FiO2 after NIV treatment, and the better curative effect is suggested. Tacrolimus 10-20 natriuretic peptide B Homo sapiens 83-86 29090089-9 2017 CONCLUSION: Sirtinol, a Sirt1 inhibitor, may be a promising immunosuppressive drug to prevent the rejection reaction in combination with FK506. Tacrolimus 137-142 sirtuin 1 Mus musculus 24-29 29079741-1 2017 FK506 binding protein of 51 kDa (FKBP51) is a heat shock protein 90 (Hsp90) co-chaperone involved in the regulation of steroid hormone receptors activity. Tacrolimus 0-5 heat shock protein 90 alpha family class A member 1 Homo sapiens 46-67 29079741-1 2017 FK506 binding protein of 51 kDa (FKBP51) is a heat shock protein 90 (Hsp90) co-chaperone involved in the regulation of steroid hormone receptors activity. Tacrolimus 0-5 heat shock protein 90 alpha family class A member 1 Homo sapiens 69-74 29073235-10 2017 Finally, the calcineurin inhibitor FK506 and Cyclosporin A reversed the effect of SFKs inhibition on NFAT1. Tacrolimus 35-40 nuclear factor of activated T cells 2 Homo sapiens 101-106 29083842-0 2017 Retraction: Inhibition of Arachidonic Acid Release by Cytosolic Phospholipase A2 Is Involved in the Antiapoptotic Effect of FK506 and Cyclosporin A on Astrocytes Exposed to Simulated Ischemia In Vitro Tacrolimus 124-129 phospholipase A2 group IVA Homo sapiens 54-80 29045960-1 2017 OBJECTIVE: Tacrolimus prolonged-release(PR) formulation is a new once-daily formulation of the calcineurin inhibitor tacrolimus, which is currently used in adult liver or kidney transplant patients,and is also gradually widely used in children with nephrotic syndrome.The present study was undertaken to preliminarily investigate the pharmacokinetic characteristics of tacrolimus PR in pediatric nephrotic syndrome recipients. Tacrolimus 11-21 calcineurin binding protein 1 Homo sapiens 95-116 29045960-1 2017 OBJECTIVE: Tacrolimus prolonged-release(PR) formulation is a new once-daily formulation of the calcineurin inhibitor tacrolimus, which is currently used in adult liver or kidney transplant patients,and is also gradually widely used in children with nephrotic syndrome.The present study was undertaken to preliminarily investigate the pharmacokinetic characteristics of tacrolimus PR in pediatric nephrotic syndrome recipients. Tacrolimus 117-127 calcineurin binding protein 1 Homo sapiens 95-116 29018183-7 2017 The calcineurin inhibitor, tacrolimus, was introduced on the fifth postoperative day. Tacrolimus 27-37 calcineurin binding protein 1 Homo sapiens 4-25 28851804-0 2017 Association of FK506 binding proteins with RyR channels - effect of CLIC2 binding on sub-conductance opening and FKBP binding. Tacrolimus 15-20 ryanodine receptor 2 Homo sapiens 43-46 28851804-0 2017 Association of FK506 binding proteins with RyR channels - effect of CLIC2 binding on sub-conductance opening and FKBP binding. Tacrolimus 15-20 chloride intracellular channel 2 Homo sapiens 68-73 28851804-2 2017 Beneficially low RyR activity and maximum conductance opening may be stabilised when RyRs bind to FK506 binding proteins (FKBPs) and destabilised by FKBP dissociation, with submaximal opening during RyR hyperactivity associated with myopathies and neurological disorders. Tacrolimus 98-103 ryanodine receptor 2 Homo sapiens 85-88 28851804-8 2017 There are significant FKBP and RyR isoform-specific actions of CLIC2, rapamycin and FK506 on FKBP-RyR association. Tacrolimus 84-89 ryanodine receptor 2 Homo sapiens 31-34 28851804-8 2017 There are significant FKBP and RyR isoform-specific actions of CLIC2, rapamycin and FK506 on FKBP-RyR association. Tacrolimus 84-89 ryanodine receptor 2 Homo sapiens 98-101 28271256-0 2017 Impact of the CYP3A5 genotype on the distributions of dose-adjusted trough concentrations and incidence of rejection in Japanese renal transplant recipients receiving different tacrolimus formulations. Tacrolimus 177-187 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 14-20 28982713-0 2017 Publisher"s Note: Association of FK506 binding proteins with RyR channels - effect of CLIC2 binding on sub-conductance opening and FKBP binding. Tacrolimus 33-38 ryanodine receptor 2 Homo sapiens 61-64 28982713-0 2017 Publisher"s Note: Association of FK506 binding proteins with RyR channels - effect of CLIC2 binding on sub-conductance opening and FKBP binding. Tacrolimus 33-38 chloride intracellular channel 2 Homo sapiens 86-91 28271256-4 2017 RESULTS: Recipients with at least one CYP3A5*1 wild-type allele (EMs) and recipients with homozygous expression of the variant allele CYP3A5*3 (PMs) were significantly identified using the tacrolimus C 0h/D cut-off values of 2.77 and 0.85 ng/mL/mg, respectively, and discrimination rates of 75.3 and 85.4%, respectively, for Tac-BID and Tac-QD groups. Tacrolimus 189-199 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 134-140 28271256-5 2017 The %CV of the tacrolimus C 0h/D in CYP3A5 EMs taking Tac-QD was significantly lower than that in those taking Tac-BID (20.4 versus 23.3%, P = 0.003). Tacrolimus 15-25 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 36-42 28640392-5 2017 A histopathological analysis showed that both cyclosporin A and tacrolimus exacerbated the NOD1-mediated coronary arteritis in a dose-dependent manner. Tacrolimus 64-74 nucleotide-binding oligomerization domain containing 1 Mus musculus 91-95 28271256-7 2017 CONCLUSIONS: The tacrolimus C 0h/D values with definite cut-offs for CYP3A5 genotypes were specifically identified in Japanese renal transplant recipients taking Tac-QD. Tacrolimus 17-27 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 69-75 28893866-2 2017 Activation of bone morphogenetic protein receptor 2 (BMPR2) signalling by FK506 (tacrolimus) reverses occlusive vasculopathy in rodent PAH models. Tacrolimus 74-79 bone morphogenetic protein receptor type 2 Homo sapiens 14-51 28710230-7 2017 FK506 and GSK3 inhibition showed the opposite effect regarding the NFATc3 localization of iCSCs. Tacrolimus 0-5 nuclear factor of activated T cells 3 Homo sapiens 67-73 28849081-6 2017 The results of the present study demonstrated that lercanidipine and FK506 inhibited Ang II-induced cardiomyocyte hypertrophy, as evidenced by decreases in fetal gene (atrial natriuretic peptide and brain natriuretic peptide) expression levels and cell surface area. Tacrolimus 69-74 angiotensinogen Rattus norvegicus 85-91 28849081-6 2017 The results of the present study demonstrated that lercanidipine and FK506 inhibited Ang II-induced cardiomyocyte hypertrophy, as evidenced by decreases in fetal gene (atrial natriuretic peptide and brain natriuretic peptide) expression levels and cell surface area. Tacrolimus 69-74 natriuretic peptide B Rattus norvegicus 199-224 28777242-1 2017 OBJECTIVES: Several genetic factors were identified to be responsible for interidividual variability in tacrolimus (TAC) pharmacokinetics, with the predominant role of CYP3A5 and CYP3A4 polymorphisms. Tacrolimus 104-114 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 168-174 28777242-1 2017 OBJECTIVES: Several genetic factors were identified to be responsible for interidividual variability in tacrolimus (TAC) pharmacokinetics, with the predominant role of CYP3A5 and CYP3A4 polymorphisms. Tacrolimus 104-114 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 179-185 28640063-0 2017 Pharmacodynamic Monitoring of Tacrolimus-Based Immunosuppression in CD14+ Monocytes After Kidney Transplantation. Tacrolimus 30-40 CD14 molecule Homo sapiens 68-72 28722255-3 2017 All of these agents are inhibitors of cytochrome P450 3A4, which plays a key role in metabolizing immunosuppressant drugs such as cyclosporine, tacrolimus, and sirolimus. Tacrolimus 144-154 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-57 28540692-0 2017 Effects of CYP3A5 polymorphisms on tacrolimus pharmacokinetics in pediatric kidney transplantation: a systematic review and meta-analysis of observational studies. Tacrolimus 35-45 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 11-17 28540692-1 2017 BACKGROUND: CYP3A5 genetic polymorphisms have been reported to be strongly associated with the tacrolimus pharmacokinetics in adult kidney transplantation. Tacrolimus 95-105 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 12-18 28540692-2 2017 However, there is no published meta-analysis in the influence of CYP3A5 variants on the requirements of the tacrolimus dose in pediatric renal-transplant recipients (RTRs). Tacrolimus 108-118 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 65-71 28540692-3 2017 We wished to determine the effects of CYP3A5 polymorphisms on tacrolimus pharmacokinetics in pediatric RTRs. Tacrolimus 62-72 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 38-44 28540692-7 2017 A significant difference was observed in the mean trough concentration/dose of tacrolimus between recipients carrying CYP3A5* 3/*3 variants (referred to as "non-expressers") and those carrying CYP3A5*1 (referred to as "expressers") [standard mean difference (SMD)=-1.09, 95% confidence interval (CI): -1.92 to -0.25, P=0.011]. Tacrolimus 79-89 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 118-124 28540692-9 2017 CONCLUSION: Our meta-analysis identified a positive correlation between CYP3A5 genotypes and tacrolimus pharmacokinetics in pediatric RTRs. Tacrolimus 93-103 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 72-78 28893866-2 2017 Activation of bone morphogenetic protein receptor 2 (BMPR2) signalling by FK506 (tacrolimus) reverses occlusive vasculopathy in rodent PAH models. Tacrolimus 74-79 bone morphogenetic protein receptor type 2 Homo sapiens 53-58 28893866-2 2017 Activation of bone morphogenetic protein receptor 2 (BMPR2) signalling by FK506 (tacrolimus) reverses occlusive vasculopathy in rodent PAH models. Tacrolimus 81-91 bone morphogenetic protein receptor type 2 Homo sapiens 14-51 28893866-2 2017 Activation of bone morphogenetic protein receptor 2 (BMPR2) signalling by FK506 (tacrolimus) reverses occlusive vasculopathy in rodent PAH models. Tacrolimus 81-91 bone morphogenetic protein receptor type 2 Homo sapiens 53-58 28893866-5 2017 PAH patients had significantly lower BMPR2 expression in peripheral blood mononuclear cells versus healthy controls (n=13; p=0.005), which improved after FK506 treatment. Tacrolimus 154-159 bone morphogenetic protein receptor type 2 Homo sapiens 37-42 28893866-6 2017 While we observed that some patients responded with a pronounced increase in BMPR2 expression as well as improvement in 6-min walk distance, and serological and echocardiographic parameters of heart failure, these changes were not significant.Low-level FK506 is well tolerated and increases BMPR2 in subsets of PAH patients. Tacrolimus 253-258 bone morphogenetic protein receptor type 2 Homo sapiens 77-82 28893866-6 2017 While we observed that some patients responded with a pronounced increase in BMPR2 expression as well as improvement in 6-min walk distance, and serological and echocardiographic parameters of heart failure, these changes were not significant.Low-level FK506 is well tolerated and increases BMPR2 in subsets of PAH patients. Tacrolimus 253-258 bone morphogenetic protein receptor type 2 Homo sapiens 291-296 28224698-9 2017 In conclusion, CYP3A5 genotype and several clinical variables were identified as modulators of the tacrolimus-azole interaction, but these did not permit accurate predictions in individual patients. Tacrolimus 99-109 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 15-21 28466977-4 2017 The study patients received daily dose of tacrolimus 1-3 mg based on initial Th1/Th2 cell ratio. Tacrolimus 42-52 negative elongation factor complex member C/D Homo sapiens 77-80 28466977-8 2017 CONCLUSION: We confirm our previous report that Th1/Th2 ratio can predict ART outcomes in patients with RIF and immunosuppressant treatment with tacrolimus, and peripheral blood Th1 cell levels were negatively correlated with pregnancy outcome. Tacrolimus 145-155 negative elongation factor complex member C/D Homo sapiens 48-51 28508247-2 2017 Based mainly on the results of short-term studies, the calcineurin inhibitor tacrolimus prevails over the mammalian target of rapamycin (mTOR) inhibitors. Tacrolimus 77-87 calcineurin binding protein 1 Homo sapiens 55-76 28669722-0 2017 Tacrolimus induces fibroblasts apoptosis and reduces epidural fibrosis by regulating miR-429 and its target of RhoE. Tacrolimus 0-10 microRNA 429 Rattus norvegicus 85-92 28669722-0 2017 Tacrolimus induces fibroblasts apoptosis and reduces epidural fibrosis by regulating miR-429 and its target of RhoE. Tacrolimus 0-10 mitogen-activated protein kinase kinase kinase 11 Rattus norvegicus 111-115 28669722-6 2017 The expression of miR-429 in fibroblasts treated with FK506 was determined by RT-qPCR. Tacrolimus 54-59 microRNA 429 Rattus norvegicus 18-25 28669722-11 2017 The results revealed FK506 induces fibroblast apoptosis and significantly downregulates miR-429 expression in fibroblasts. Tacrolimus 21-26 microRNA 429 Rattus norvegicus 88-95 28669722-14 2017 The rat model demonstrated miR-429 inhibition promotes fibroblast apoptosis and epidural fibrosis, which is consistent with the results of FK506 treatment. Tacrolimus 139-144 microRNA 429 Rattus norvegicus 27-34 28669722-15 2017 Our study demonstrates that FK506 induces fibroblast apoptosis and reduces epidural fibrosis by regulating miR-429 expression and its target of RhoE. Tacrolimus 28-33 microRNA 429 Rattus norvegicus 107-114 28669722-15 2017 Our study demonstrates that FK506 induces fibroblast apoptosis and reduces epidural fibrosis by regulating miR-429 expression and its target of RhoE. Tacrolimus 28-33 mitogen-activated protein kinase kinase kinase 11 Rattus norvegicus 144-148 28633129-4 2017 On the concentration level of 2-5mug/ml tacrolimus plus 10ng/ml PDGF-BB, combination of drugs could effectively promote ECs proliferation and migration, and meanwhile inhibit VSMCs proliferation and migration, and the inhibition of p-mTOR"s expression within VSMCs played an important role in this differentiated effect. Tacrolimus 40-50 mechanistic target of rapamycin kinase Homo sapiens 234-238 28137823-14 2017 CONCLUSION: Topical tacrolimus is effective in reducing the photophobia in patients with APS-1-associated keratitis, but showed no effects on the severity of keratitis. Tacrolimus 20-30 autoimmune regulator Homo sapiens 89-94 28624888-1 2017 PURPOSE: The study aims to evaluate the impact of recipients" and donors" polymorphisms in multidrug resistance-associated protein 2 (MRP2) gene ABCC2 -24C>T and 1249G>A on disposition of mycophenolic acid (MPA) and their interaction with cyclosporine (CsA) (compared to tacrolimus, TAC) in stable de novo adult renal transplant patients of Croatian origin. Tacrolimus 277-287 ATP binding cassette subfamily C member 2 Homo sapiens 91-132 28624888-1 2017 PURPOSE: The study aims to evaluate the impact of recipients" and donors" polymorphisms in multidrug resistance-associated protein 2 (MRP2) gene ABCC2 -24C>T and 1249G>A on disposition of mycophenolic acid (MPA) and their interaction with cyclosporine (CsA) (compared to tacrolimus, TAC) in stable de novo adult renal transplant patients of Croatian origin. Tacrolimus 277-287 ATP binding cassette subfamily C member 2 Homo sapiens 134-138 28624888-1 2017 PURPOSE: The study aims to evaluate the impact of recipients" and donors" polymorphisms in multidrug resistance-associated protein 2 (MRP2) gene ABCC2 -24C>T and 1249G>A on disposition of mycophenolic acid (MPA) and their interaction with cyclosporine (CsA) (compared to tacrolimus, TAC) in stable de novo adult renal transplant patients of Croatian origin. Tacrolimus 277-287 ATP binding cassette subfamily C member 2 Homo sapiens 145-150 28135009-4 2017 We aimed to investigate the influence of both CYP3A5 and ABCB1 polymorphisms on the efficacy of tacrolimus in ulcerative colitis treatment under the tight dose-adjusting strategy. Tacrolimus 96-106 ATP binding cassette subfamily B member 1 Homo sapiens 57-62 28720321-1 2017 AIMS: Tacrolimus (Tac) inhibits insulin secretion in a Tac-trough blood level dependent way early post-transplant in renal transplant recipients (Rtx). Tacrolimus 6-16 insulin Homo sapiens 32-39 28605053-0 2017 Prevalence of CYP3A5 Genomic Variances and Their Impact on Tacrolimus Dosing Requirements among Kidney Transplant Recipients in Eastern North Carolina. Tacrolimus 59-69 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 14-20 28704257-0 2017 The combination of CYP3A4*22 and CYP3A5*3 single-nucleotide polymorphisms determines tacrolimus dose requirement after kidney transplantation. Tacrolimus 85-95 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 19-25 28704257-0 2017 The combination of CYP3A4*22 and CYP3A5*3 single-nucleotide polymorphisms determines tacrolimus dose requirement after kidney transplantation. Tacrolimus 85-95 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 33-39 28214069-4 2017 Immunosuppressive agents, such as calcineurin inhibitors (tacrolimus, cyclosporine) are substrates of cytochromes P450 3A4 and P-gp. Tacrolimus 58-68 ATP binding cassette subfamily B member 1 Homo sapiens 127-131 28605053-1 2017 To assess the prevalence of CYP3A5 genomic variances and their impact on tacrolimus (TAC) dosing requirements among kidney transplant recipients in eastern North Carolina, we conducted a single-center retrospective cohort study at a large tertiary care medical center. Tacrolimus 73-83 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 28-34 28901186-10 2017 The percentage of CD4+/CD25+/Foxp3+ regulatory T cells were significantly increased in the rADSC-IR-FK506 group as compared to controls. Tacrolimus 100-105 forkhead box P3 Homo sapiens 29-34 28771227-0 2017 Klotho enhances FoxO3-mediated manganese superoxide dismutase expression by negatively regulating PI3K/AKT pathway during tacrolimus-induced oxidative stress. Tacrolimus 122-132 klotho Homo sapiens 0-6 28771227-0 2017 Klotho enhances FoxO3-mediated manganese superoxide dismutase expression by negatively regulating PI3K/AKT pathway during tacrolimus-induced oxidative stress. Tacrolimus 122-132 forkhead box O3 Homo sapiens 16-21 28771227-0 2017 Klotho enhances FoxO3-mediated manganese superoxide dismutase expression by negatively regulating PI3K/AKT pathway during tacrolimus-induced oxidative stress. Tacrolimus 122-132 AKT serine/threonine kinase 1 Homo sapiens 103-106 28663197-6 2017 Treatment of neurons with the calcineurin inhibitors FK506 or cyclosporin A resulted in nuclear accumulation of phospho-HDAC1 and was neuroprotective. Tacrolimus 53-58 histone deacetylase 1 Mus musculus 120-125 28901186-11 2017 Analysis of recipient peripheral blood revealed that transforming growth factor beta1 (TGFbeta1) was significantly increased in the rADSC-IR-FK506 group. Tacrolimus 141-146 transforming growth factor beta 1 Homo sapiens 53-85 28901186-11 2017 Analysis of recipient peripheral blood revealed that transforming growth factor beta1 (TGFbeta1) was significantly increased in the rADSC-IR-FK506 group. Tacrolimus 141-146 transforming growth factor beta 1 Homo sapiens 87-95 28050888-0 2017 A New CYP3A5*3 and CYP3A4*22 Cluster Influencing Tacrolimus Target Concentrations: A Population Approach. Tacrolimus 49-59 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 6-12 28050888-0 2017 A New CYP3A5*3 and CYP3A4*22 Cluster Influencing Tacrolimus Target Concentrations: A Population Approach. Tacrolimus 49-59 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 19-25 28050888-1 2017 BACKGROUND: Single nucleotide polymorphisms (SNPs) in the CYP3A5 and CYP3A4 genes have been reported to be an important cause of variability in the pharmacokinetics of tacrolimus in renal transplant patients. Tacrolimus 168-178 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 58-64 28050888-1 2017 BACKGROUND: Single nucleotide polymorphisms (SNPs) in the CYP3A5 and CYP3A4 genes have been reported to be an important cause of variability in the pharmacokinetics of tacrolimus in renal transplant patients. Tacrolimus 168-178 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-75 28050888-8 2017 CONCLUSIONS: Tacrolimus disposition in renal transplant recipients was described using a new population pharmacokinetic model that included the CYP3A5*3 and CYP3A4*22 genotype, age, and hematocrit. Tacrolimus 13-23 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 144-150 28050888-8 2017 CONCLUSIONS: Tacrolimus disposition in renal transplant recipients was described using a new population pharmacokinetic model that included the CYP3A5*3 and CYP3A4*22 genotype, age, and hematocrit. Tacrolimus 13-23 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 157-163 28533324-0 2017 CRISPR/Cas9 Genetic Modification of CYP3A5 *3 in HuH-7 Human Hepatocyte Cell Line Leads to Cell Lines with Increased Midazolam and Tacrolimus Metabolism. Tacrolimus 131-141 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 36-42 28533324-0 2017 CRISPR/Cas9 Genetic Modification of CYP3A5 *3 in HuH-7 Human Hepatocyte Cell Line Leads to Cell Lines with Increased Midazolam and Tacrolimus Metabolism. Tacrolimus 131-141 MIR7-3 host gene Homo sapiens 49-54 28533324-3 2017 In metabolism assays, HuH-7 had less tacrolimus (all P < 0.05) or midazolam (MDZ) (all P < 0.005) disappearance than all engineered cell lines. Tacrolimus 37-47 MIR7-3 host gene Homo sapiens 22-27 28299629-0 2017 Inhibition of Calcineurin A by FK506 Suppresses Seizures and Reduces the Expression of GluN2B in Membrane Fraction. Tacrolimus 31-36 glutamate ionotropic receptor NMDA type subunit 2B Rattus norvegicus 87-93 28135009-0 2017 ATP-binding cassette subfamily B member 1 1236C/T polymorphism significantly affects the therapeutic outcome of tacrolimus in patients with refractory ulcerative colitis. Tacrolimus 112-122 ATP binding cassette subfamily B member 1 Homo sapiens 0-41 28135009-2 2017 Both cytochrome P-450 3A5 (CYP3A5) and ATP-binding cassette subfamily B member 1 (ABCB1) associated with tacrolimus metabolism are known to have several genetic polymorphisms. Tacrolimus 105-115 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 5-25 28135009-2 2017 Both cytochrome P-450 3A5 (CYP3A5) and ATP-binding cassette subfamily B member 1 (ABCB1) associated with tacrolimus metabolism are known to have several genetic polymorphisms. Tacrolimus 105-115 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 27-33 28135009-2 2017 Both cytochrome P-450 3A5 (CYP3A5) and ATP-binding cassette subfamily B member 1 (ABCB1) associated with tacrolimus metabolism are known to have several genetic polymorphisms. Tacrolimus 105-115 ATP binding cassette subfamily B member 1 Homo sapiens 39-80 28135009-2 2017 Both cytochrome P-450 3A5 (CYP3A5) and ATP-binding cassette subfamily B member 1 (ABCB1) associated with tacrolimus metabolism are known to have several genetic polymorphisms. Tacrolimus 105-115 ATP binding cassette subfamily B member 1 Homo sapiens 82-87 28135009-4 2017 We aimed to investigate the influence of both CYP3A5 and ABCB1 polymorphisms on the efficacy of tacrolimus in ulcerative colitis treatment under the tight dose-adjusting strategy. Tacrolimus 96-106 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 46-52 28401703-0 2017 Tacrolimus population pharmacokinetics according to CYP3A5 genotype and clinical factors in Chinese adult kidney transplant recipients. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 52-58 28401703-7 2017 In this study, we observed that POD, HCT and CYP3A5*3 genotype were determinant factors in CL/F and POD related with V/F of tacrolimus significantly. Tacrolimus 124-134 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 45-51 28401703-10 2017 WHAT IS NEW AND CONCLUSION: The HCT, CYP3A5*3 genetic polymorphism and POD contributed to the interindividual variability of oral tacrolimus in Chinese adult renal transplant patients. Tacrolimus 130-140 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 37-43 28299629-4 2017 Thus, we hypothesized that one of the potential anti-epileptic mechanisms of FK506 is mediated by its ability to promote the phosphorylation of GluN2B and reduce the expression of GluN2B in membrane fraction by down-regulating CaNA. Tacrolimus 77-82 glutamate ionotropic receptor NMDA type subunit 2B Rattus norvegicus 144-150 28299629-4 2017 Thus, we hypothesized that one of the potential anti-epileptic mechanisms of FK506 is mediated by its ability to promote the phosphorylation of GluN2B and reduce the expression of GluN2B in membrane fraction by down-regulating CaNA. Tacrolimus 77-82 glutamate ionotropic receptor NMDA type subunit 2B Rattus norvegicus 180-186 28299629-8 2017 The levels of phosphorylated GluN2B were decreased in epileptic rats but increased after the FK506 treatment. Tacrolimus 93-98 glutamate ionotropic receptor NMDA type subunit 2B Rattus norvegicus 29-35 28299629-10 2017 However, the expression of GluN2B in membrane fraction was suppressed after FK506 treatment. Tacrolimus 76-81 glutamate ionotropic receptor NMDA type subunit 2B Rattus norvegicus 27-33 28299629-11 2017 Based on these results, FK506 may reduce the severity and frequency of seizures by reducing the expression of GluN2B in membrane fraction. Tacrolimus 24-29 glutamate ionotropic receptor NMDA type subunit 2B Rattus norvegicus 110-116 29050276-0 2017 A new donors" CYP3A5 and recipients" CYP3A4 cluster predicting tacrolimus disposition, and new-onset hypertension in Chinese liver transplant patients. Tacrolimus 63-73 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 14-20 29050276-0 2017 A new donors" CYP3A5 and recipients" CYP3A4 cluster predicting tacrolimus disposition, and new-onset hypertension in Chinese liver transplant patients. Tacrolimus 63-73 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 28738959-10 2017 Moreover, FK506 increased the expression of P27 and RB1, and reduced the expression of CDK4, CDK6 and MMP9. Tacrolimus 10-15 dynactin subunit 6 Homo sapiens 44-47 28738959-10 2017 Moreover, FK506 increased the expression of P27 and RB1, and reduced the expression of CDK4, CDK6 and MMP9. Tacrolimus 10-15 RB transcriptional corepressor 1 Homo sapiens 52-55 28738959-10 2017 Moreover, FK506 increased the expression of P27 and RB1, and reduced the expression of CDK4, CDK6 and MMP9. Tacrolimus 10-15 cyclin dependent kinase 4 Homo sapiens 87-91 28738959-10 2017 Moreover, FK506 increased the expression of P27 and RB1, and reduced the expression of CDK4, CDK6 and MMP9. Tacrolimus 10-15 cyclin dependent kinase 6 Homo sapiens 93-97 28738959-10 2017 Moreover, FK506 increased the expression of P27 and RB1, and reduced the expression of CDK4, CDK6 and MMP9. Tacrolimus 10-15 matrix metallopeptidase 9 Homo sapiens 102-106 28673995-3 2017 Abrogation of host IDO expression by deletion of the IDO gene or the IFN-gamma gene in donor T cells or by FK506 treatment resulted in acute lethal pulmonary inflammation known as idiopathic pneumonia syndrome (IPS). Tacrolimus 107-112 indoleamine 2,3-dioxygenase 1 Homo sapiens 19-22 28673995-5 2017 Accordingly, a histone deacetylase inhibitor (HDACi) could reduce IPS in the state where IFN-gamma expression was suppressed by FK506. Tacrolimus 128-133 interferon gamma Homo sapiens 89-98 28146606-2 2017 Tacrolimus dosing is challenged by considerable pharmacokinetic variability, both between patients and over time after transplantation, partly due to variability in cytochrome P450 3A (CYP3A) activity. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 165-183 28747916-4 2017 Here, we determined the effect of tacrolimus and MPA on DNA methylation of the gene promoter region of interferon gamma (IFNgamma), a pro-inflammatory cytokine. Tacrolimus 34-44 interferon gamma Homo sapiens 103-130 28747916-12 2017 IFNgamma protein production was suppressed by tacrolimus. Tacrolimus 46-56 interferon gamma Homo sapiens 0-8 27572744-9 2017 Moreover, the results in hypoxia-treated primary spinal cord microglia confirmed the effect of FK-506 on TNF-a, IL-1b, and IL-6 expression and NF-kappaB activation. Tacrolimus 95-101 interleukin 1 beta Rattus norvegicus 112-117 27572744-9 2017 Moreover, the results in hypoxia-treated primary spinal cord microglia confirmed the effect of FK-506 on TNF-a, IL-1b, and IL-6 expression and NF-kappaB activation. Tacrolimus 95-101 interleukin 6 Rattus norvegicus 123-127 28257599-7 2017 Treatment with tacrolimus and cyclosporin render CD4+ CD25- cells more susceptible to Treg control. Tacrolimus 15-25 CD4 molecule Homo sapiens 49-52 28257599-7 2017 Treatment with tacrolimus and cyclosporin render CD4+ CD25- cells more susceptible to Treg control. Tacrolimus 15-25 interleukin 2 receptor subunit alpha Homo sapiens 54-58 28672892-10 2017 On day 30 following intervention, the expression of IL-17 and CCL2 in the prostate of rats in the tacrolimus and celecoxib groups was significantly downregulated compared with the NS group (P<0.05). Tacrolimus 98-108 interleukin 17A Rattus norvegicus 52-57 28672892-10 2017 On day 30 following intervention, the expression of IL-17 and CCL2 in the prostate of rats in the tacrolimus and celecoxib groups was significantly downregulated compared with the NS group (P<0.05). Tacrolimus 98-108 C-C motif chemokine ligand 2 Rattus norvegicus 62-66 28621555-0 2017 SLC28A3 rs7853758 as a new biomarker of tacrolimus elimination and new-onset hypertension in Chinese liver transplantation patients. Tacrolimus 40-50 solute carrier family 28 member 3 Homo sapiens 0-7 28621555-4 2017 The model of donors" CYP3A5 rs776746 and recipients" CYP3A4 rs2242480 could predict tacrolimus metabolism at week 1 and the model of donors" CYP3A5 rs776746, recipients" CYP3A4 rs2242480, recipients" SLC28A3 rs7853758 and hemoglobin could predict tacrolimus disposition at weeks 2, 3 and 4. Tacrolimus 84-94 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 21-27 28621555-4 2017 The model of donors" CYP3A5 rs776746 and recipients" CYP3A4 rs2242480 could predict tacrolimus metabolism at week 1 and the model of donors" CYP3A5 rs776746, recipients" CYP3A4 rs2242480, recipients" SLC28A3 rs7853758 and hemoglobin could predict tacrolimus disposition at weeks 2, 3 and 4. Tacrolimus 84-94 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-59 28621555-4 2017 The model of donors" CYP3A5 rs776746 and recipients" CYP3A4 rs2242480 could predict tacrolimus metabolism at week 1 and the model of donors" CYP3A5 rs776746, recipients" CYP3A4 rs2242480, recipients" SLC28A3 rs7853758 and hemoglobin could predict tacrolimus disposition at weeks 2, 3 and 4. Tacrolimus 84-94 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 141-147 28621555-4 2017 The model of donors" CYP3A5 rs776746 and recipients" CYP3A4 rs2242480 could predict tacrolimus metabolism at week 1 and the model of donors" CYP3A5 rs776746, recipients" CYP3A4 rs2242480, recipients" SLC28A3 rs7853758 and hemoglobin could predict tacrolimus disposition at weeks 2, 3 and 4. Tacrolimus 84-94 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 170-176 28621555-4 2017 The model of donors" CYP3A5 rs776746 and recipients" CYP3A4 rs2242480 could predict tacrolimus metabolism at week 1 and the model of donors" CYP3A5 rs776746, recipients" CYP3A4 rs2242480, recipients" SLC28A3 rs7853758 and hemoglobin could predict tacrolimus disposition at weeks 2, 3 and 4. Tacrolimus 84-94 solute carrier family 28 member 3 Homo sapiens 200-207 28621555-6 2017 CONCLUSION: Rs7853758 in recipients" SLC28A3 has a correlation with tacrolimus pharmacokinetics and the risk of NOHP in Chinese LT patients. Tacrolimus 68-78 solute carrier family 28 member 3 Homo sapiens 37-44 28146606-2 2017 Tacrolimus dosing is challenged by considerable pharmacokinetic variability, both between patients and over time after transplantation, partly due to variability in cytochrome P450 3A (CYP3A) activity. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 185-190 28146606-3 2017 The aim of this study was to assess the value of the endogenous CYP3A marker 4beta-hydroxycholesterol (4betaOHC) for tacrolimus dose individualization early after kidney transplantation. Tacrolimus 117-127 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 64-69 28560399-8 2017 Verification of the miRNA-target genes revealed that Smad5, Jagged 1 and MAPK9 were significantly upregulated, whereas Smad7, BMP and activin membrane-bound inhibitor, and dual-specificity phosphatase 2 were significantly downregulated during FK506-induced osteodifferentiation. Tacrolimus 243-248 dual specificity phosphatase 2 Rattus norvegicus 134-202 28584011-2 2017 We and others have reported that cyclosporine A and tacrolimus decrease anti-inflammatory regulatory T cells and increase proinflammatory interleukin-17-producing T cells; therefore, we hypothesized that inhibition of these effects using noncellular therapies would prevent the hypertension, endothelial dysfunction, and renal glomerular injury induced by calcineurin inhibitor therapy. Tacrolimus 52-62 calcineurin binding protein 1 Mus musculus 356-377 28584011-3 2017 Daily treatment of mice with cyclosporine A or tacrolimus for 1 week significantly decreased CD4+/FoxP3+ regulatory T cells in the spleen and lymph nodes, as well as induced hypertension, vascular injury and dysfunction, and glomerular mesangial expansion in mice. Tacrolimus 47-57 forkhead box P3 Mus musculus 98-103 28642710-0 2017 Tacrolimus Updated Guidelines through popPK Modeling: How to Benefit More from CYP3A Pre-emptive Genotyping Prior to Kidney Transplantation. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 79-84 28706520-7 2017 Notably, NFAT antagonism by cyclosporin A or FK506 impaired IL-22 upregulation at normothermia and entirely prevented its enhanced expression upon hypothermic culture conditions. Tacrolimus 45-50 interleukin 22 Mus musculus 60-65 28672869-4 2017 Here, we showed that mutations of tax-6 and cnb-1, which respectively encode the catalytic subunit and the regulatory subunit of calcineurin, together with tacrolimus treatment, consistently led to decreased fat accumulation and delayed growth in the nematode Caenorhabditis elegans. Tacrolimus 156-166 Serine/threonine-protein phosphatase 2B catalytic subunit Caenorhabditis elegans 34-39 29259481-8 2017 Conclusion: For recurrent miscarriage cases that show an elevated Th1/Th2 cell ratio after achieving pregnancy, immunosuppressive treatment with tacrolimus could be effective. Tacrolimus 145-155 negative elongation factor complex member C/D Homo sapiens 66-69 28669959-0 2017 [Correlation of blood concentration of tacrolimus with serum cystatin C in renal transplant recipients and effect of tacrolimus on glucose and lipid metabolism]. Tacrolimus 39-49 cystatin C Homo sapiens 61-71 28669959-1 2017 OBJECTIVE: To investigate the correlation between blood concentrations of tacrolimus (FK506) and cystatin C (Cys C) and the effect of FK506 on glycolipid metabolism in renal transplant recipients. Tacrolimus 74-84 cystatin C Homo sapiens 97-107 28669959-1 2017 OBJECTIVE: To investigate the correlation between blood concentrations of tacrolimus (FK506) and cystatin C (Cys C) and the effect of FK506 on glycolipid metabolism in renal transplant recipients. Tacrolimus 74-84 cystatin C Homo sapiens 109-114 28669959-1 2017 OBJECTIVE: To investigate the correlation between blood concentrations of tacrolimus (FK506) and cystatin C (Cys C) and the effect of FK506 on glycolipid metabolism in renal transplant recipients. Tacrolimus 86-91 cystatin C Homo sapiens 97-107 28669959-4 2017 Results Plasma FK506 concentration decreased with age in the recipients and showed a positive correlation with Cys C (r=0.985, P=0.015) but no obvious correlation with Scr (r=0.259, P=0.741). Tacrolimus 15-20 cystatin C Homo sapiens 111-116 28669959-7 2017 Cys C is positively related to blood concentration of FK506 in the renal transplantation recipients. Tacrolimus 54-59 cystatin C Homo sapiens 0-5 28642710-4 2017 The integration of CYP3A4 and CY3A5 genotype in tacrolimus population-based PK (PopPK) modeling approaches has been proven to accurately predict the dose requirement to reach the therapeutic window. Tacrolimus 48-58 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 19-25 28642710-10 2017 Our model estimated that tacrolimus concentrations were 33% IC95%[20-26%], 41% IC95%[36-45%] lower in CYP3A IM and EM when compared to PM, respectively. Tacrolimus 25-35 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 102-107 28008657-0 2017 Bodyweight-adjustments introduce significant correlations between CYP3A metrics and tacrolimus clearance. Tacrolimus 84-94 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 66-71 29270498-12 2017 Proteinuria (urinary protein-to-creatinine ratio) was significantly reduced in both patients with MGN and those with FSGS after 6 months of ACTHar gel alone and was further reduced among the patients with MGN with the addition of tacrolimus. Tacrolimus 230-240 actinin alpha 4 Homo sapiens 117-121 29270498-14 2017 Discussion: Combination therapy with ACTHar gel and tacrolimus was well tolerated by patients with treatment-resistant MGN and FSGS and significantly reduced proteinuria and improved clinical response rates compared with ACTHar gel alone. Tacrolimus 52-62 actinin alpha 4 Homo sapiens 127-131 28324194-0 2017 Sex Differences in the Blood Concentration of Tacrolimus in Systemic Lupus Erythematosus and Rheumatoid Arthritis Patients with CYP3A5*3/*3. Tacrolimus 46-56 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 128-134 28324194-1 2017 The purpose of this study was to describe the impact of sex and cytochrome P450 3A5 (CYP3A5) variant on the blood concentration of tacrolimus in patients with systemic lupus erythematosus or rheumatoid arthritis. Tacrolimus 131-141 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 64-83 28324194-1 2017 The purpose of this study was to describe the impact of sex and cytochrome P450 3A5 (CYP3A5) variant on the blood concentration of tacrolimus in patients with systemic lupus erythematosus or rheumatoid arthritis. Tacrolimus 131-141 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 85-91 28324194-5 2017 In the CYP3A5*3/*3 group, the concentration of tacrolimus was significantly higher in men than in women (p < 0.05, effect size: d = 1.78). Tacrolimus 47-57 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 7-13 28324194-6 2017 Furthermore, in the CYP3A5*3/*3 group, the concentration of tacrolimus was significantly higher in women aged over 50 years than in women aged under 50 years (p < 0.05, effect size: d = 1.18). Tacrolimus 60-70 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 20-26 28324194-8 2017 Since the blood concentration of tacrolimus in patients with CYP3A5*3/*3 varies depending on sex and age, these factors should be considered when studying the difference of sex in CYP3A. Tacrolimus 33-43 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 61-67 28324194-8 2017 Since the blood concentration of tacrolimus in patients with CYP3A5*3/*3 varies depending on sex and age, these factors should be considered when studying the difference of sex in CYP3A. Tacrolimus 33-43 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 61-66 28374426-0 2017 Response to: "Response to: Bodyweight-adjustments introduce significant correlations between CYP3A metrics and tacrolimus clearance". Tacrolimus 111-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 93-98 28044353-0 2017 Donor CYP3A5 genotype influences tacrolimus disposition on the first day after paediatric liver transplantation. Tacrolimus 33-43 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 6-12 28044353-2 2017 METHODS: The contribution of the CYP3A4/5 genotype in paediatric liver transplant recipients and donors to the tacrolimus blood trough concentrations (C0 ) and the tacrolimus concentration/weight-adjusted dose ratio on day 1 was evaluated in 67 liver-transplanted children: 33 boys and 34 girls, mean age 4.5 years. Tacrolimus 111-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 33-39 28044353-3 2017 RESULTS: Donor CYP3A5 genotype appears to be significantly associated with tacrolimus disposition on the first day after liver transplantation (P < 0.0002). Tacrolimus 75-85 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 15-21 28044353-7 2017 CONCLUSIONS: Donor CYP3A5 genotype, recipient age and, to a lesser extent, donor gender appear to be associated with tacrolimus disposition on day 1 after transplant. Tacrolimus 117-127 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 19-25 28168728-0 2017 Response to: "Bodyweight-adjustments introduce significant correlations between CYP3A metrics and tacrolimus clearance". Tacrolimus 98-108 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 80-85 28611128-6 2017 Knockdown of KCNE2 increased intracellular Ca2+ transient, calcineurin activity, and nuclear NFAT (nuclear factor of activated T cells) protein levels, and pretreatment with inhibitor of L-type Ca2+ channel (nifedipine) or calcineurin (FK506) attenuated the activation of calcineurin-NFAT pathway and cardiomyocyte hypertrophy. Tacrolimus 236-241 potassium voltage-gated channel subfamily E regulatory subunit 2 Rattus norvegicus 13-18 28229376-1 2017 INTRODUCTION: Tacrolimus is a calcineurin inhibitor used as an immunosuppressant drug in solid organ transplantation, and is mainly metabolized by cytochrome P450 (CYP) 3A4 and CYP3A5. Tacrolimus 14-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 147-172 28342282-10 2017 Patients expressing CYP3A5*1 genotypes had lower tacrolimus AUC0-24 values vs those with CYP3A5*3/*3 (IR-TACP<.001; ER-TACP=.008). Tacrolimus 49-59 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 20-26 29123971-4 2017 Genome wide association study data for the immunosuppressant tacrolimus have identified multiple variants in the CYP3A5 gene associated with trough concentrations. Tacrolimus 61-71 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 113-119 28229376-1 2017 INTRODUCTION: Tacrolimus is a calcineurin inhibitor used as an immunosuppressant drug in solid organ transplantation, and is mainly metabolized by cytochrome P450 (CYP) 3A4 and CYP3A5. Tacrolimus 14-24 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 177-183 28229376-2 2017 Studies have shown an association between the CYP3A5 genotype and tacrolimus dose-adjusted trough concentrations. Tacrolimus 66-76 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 46-52 28229376-3 2017 Variants in the genes PPARA, POR and CYP3A4 have recently been shown to influence tacrolimus metabolism. Tacrolimus 82-92 peroxisome proliferator activated receptor alpha Homo sapiens 22-27 28229376-3 2017 Variants in the genes PPARA, POR and CYP3A4 have recently been shown to influence tacrolimus metabolism. Tacrolimus 82-92 cytochrome p450 oxidoreductase Homo sapiens 29-32 28229376-3 2017 Variants in the genes PPARA, POR and CYP3A4 have recently been shown to influence tacrolimus metabolism. Tacrolimus 82-92 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 28229376-5 2017 In the present study, we investigated a potential association between CYP3A5*3, PPARA c.209-1003G>A, POR*28 and CYP3A4*22 and dose-adjusted tacrolimus trough concentrations in a primarily corticosteroid-free (>85%) population of Danish pediatric and adult kidney transplant recipients. Tacrolimus 143-153 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 70-76 28229376-5 2017 In the present study, we investigated a potential association between CYP3A5*3, PPARA c.209-1003G>A, POR*28 and CYP3A4*22 and dose-adjusted tacrolimus trough concentrations in a primarily corticosteroid-free (>85%) population of Danish pediatric and adult kidney transplant recipients. Tacrolimus 143-153 peroxisome proliferator activated receptor alpha Homo sapiens 80-85 28229376-5 2017 In the present study, we investigated a potential association between CYP3A5*3, PPARA c.209-1003G>A, POR*28 and CYP3A4*22 and dose-adjusted tacrolimus trough concentrations in a primarily corticosteroid-free (>85%) population of Danish pediatric and adult kidney transplant recipients. Tacrolimus 143-153 cytochrome p450 oxidoreductase Homo sapiens 104-107 28229376-5 2017 In the present study, we investigated a potential association between CYP3A5*3, PPARA c.209-1003G>A, POR*28 and CYP3A4*22 and dose-adjusted tacrolimus trough concentrations in a primarily corticosteroid-free (>85%) population of Danish pediatric and adult kidney transplant recipients. Tacrolimus 143-153 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 115-121 28229376-8 2017 RESULTS: It was confirmed that CYP3A5*1 wild-type carriers had lower median dose-adjusted tacrolimus trough concentrations compared with noncarriers. Tacrolimus 90-100 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 31-37 28229376-13 2017 CONCLUSION: This study shows that the known association of the CYP3A5 genotype with tacrolimus dose-adjusted trough concentrations has the same impact in a corticosteroid-sparse population. Tacrolimus 84-94 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 63-69 28620390-7 2017 The proportion of IL-21+-activated Tfh-cells was partially decreased by in vitro addition of belatacept or tacrolimus (by ~60%). Tacrolimus 107-117 interleukin 21 Homo sapiens 18-23 29113387-0 2017 Tacrolimus dose requirement based on the CYP3A5 genotype in renal transplant patients. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 41-47 29113387-2 2017 The aim of the present study is to determine whether the single nucleotide polymorphism of CYP3A5 is a predictive index of FK506 dose requirement, and also the selection yardstick of FK506 or CsA treatment.We tested archival peripheral blood of 218 kidney recipients for CYP3A5 genotyping with PCR-SSP. Tacrolimus 123-128 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 91-97 29113387-3 2017 Meanwhile, the dose of FK506 and CsA was recorded, blood concentration of the drugs was measured, and graft outcome was monitored.These results indicate that CYP3A5*AA/AG carriers need higher FK506 dose than CYP3A5*GG homozygote to achieve the target blood concentration. Tacrolimus 23-28 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 158-164 28316087-11 2017 Further, CYP2C8*3 and CYP2J2 c.-76G>T SNPs influenced the renal function of these patients and the occurrence of adverse events during treatment with tacrolimus and mycophenolate sodium. Tacrolimus 153-163 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 9-15 28611384-7 2017 Compared to the high tacrolimus group, expression levels of six cytochrome P450 enzymes, CYP1A1, CYP2B6, CYP3A5, CYP4A11, CYP19A1, and CYP17A1 were significantly higher in the low tacrolimus group. Tacrolimus 180-190 cytochrome P450 family 1 subfamily A member 1 Homo sapiens 89-95 28611384-7 2017 Compared to the high tacrolimus group, expression levels of six cytochrome P450 enzymes, CYP1A1, CYP2B6, CYP3A5, CYP4A11, CYP19A1, and CYP17A1 were significantly higher in the low tacrolimus group. Tacrolimus 180-190 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 97-103 28611384-7 2017 Compared to the high tacrolimus group, expression levels of six cytochrome P450 enzymes, CYP1A1, CYP2B6, CYP3A5, CYP4A11, CYP19A1, and CYP17A1 were significantly higher in the low tacrolimus group. Tacrolimus 180-190 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 105-111 28611384-7 2017 Compared to the high tacrolimus group, expression levels of six cytochrome P450 enzymes, CYP1A1, CYP2B6, CYP3A5, CYP4A11, CYP19A1, and CYP17A1 were significantly higher in the low tacrolimus group. Tacrolimus 180-190 cytochrome P450 family 4 subfamily A member 11 Homo sapiens 113-120 28611384-7 2017 Compared to the high tacrolimus group, expression levels of six cytochrome P450 enzymes, CYP1A1, CYP2B6, CYP3A5, CYP4A11, CYP19A1, and CYP17A1 were significantly higher in the low tacrolimus group. Tacrolimus 180-190 cytochrome P450 family 19 subfamily A member 1 Homo sapiens 122-129 28611384-7 2017 Compared to the high tacrolimus group, expression levels of six cytochrome P450 enzymes, CYP1A1, CYP2B6, CYP3A5, CYP4A11, CYP19A1, and CYP17A1 were significantly higher in the low tacrolimus group. Tacrolimus 180-190 cytochrome P450 family 17 subfamily A member 1 Homo sapiens 135-142 28611384-9 2017 Enzyme assays showed that CYP3A5 and CYP17A1 exerted direct metabolic effects on tacrolimus and mycophenolate mofetil, respectively. Tacrolimus 81-91 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 26-32 28611384-9 2017 Enzyme assays showed that CYP3A5 and CYP17A1 exerted direct metabolic effects on tacrolimus and mycophenolate mofetil, respectively. Tacrolimus 81-91 cytochrome P450 family 17 subfamily A member 1 Homo sapiens 37-44 27754593-2 2017 Here, we assessed age-specific effects of the calcineurin inhibitor tacrolimus (TAC) in a murine transplant model and assessed its clinical relevance on human T cells. Tacrolimus 68-78 calcineurin binding protein 1 Mus musculus 46-67 28339015-7 2017 It was hypothesized that FK506 may inhibit the activity of DAPK1 by inhibiting calcineurin activity, which may be primarily involved in anti-apoptosis following DAI induction. Tacrolimus 25-30 death associated protein kinase 1 Homo sapiens 59-64 28339015-8 2017 Through researching the expression of nerve regeneration associated proteins (NF-H and GAP-43) following DAI, the present study provides novel data to suggest that FK506 promotes axon formation and nerve regeneration following experimental DAI. Tacrolimus 164-169 neurofilament heavy chain Homo sapiens 78-82 28339015-8 2017 Through researching the expression of nerve regeneration associated proteins (NF-H and GAP-43) following DAI, the present study provides novel data to suggest that FK506 promotes axon formation and nerve regeneration following experimental DAI. Tacrolimus 164-169 growth associated protein 43 Homo sapiens 87-93 28339051-15 2017 Tacrolimus reduced urinary protein and slowed the progression of DN, partially by recovering the protein expression of nephrin in the renal tissue of diabetic rats, and maintaining the integrity of the structure and function of podocytes. Tacrolimus 0-10 NPHS1 adhesion molecule, nephrin Rattus norvegicus 119-126 28316087-1 2017 STUDY OBJECTIVE: To investigate the influence of single nucleotide polymorphisms (SNPs) in genes encoding metabolizing enzymes (CYP2C8, CYP2J2, and UGT2B7) and transporters (ABCC2 and ABCG2) on dose and dose-adjusted trough blood concentrations (C:D ratio), clinical outcomes, and occurrence of adverse events of tacrolimus and mycophenolate sodium in Brazilian kidney transplant recipients. Tacrolimus 313-323 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 128-134 28316087-6 2017 ABCC2 c.3972T allele carriers showed higher tacrolimus C:D values than did carriers of the c.3972CC genotype. Tacrolimus 44-54 ATP binding cassette subfamily C member 2 Homo sapiens 0-5 28316087-7 2017 The CYP2C8*3 variant was also associated with slightly higher tacrolimus C:D values and higher estimated glomerular filtration rate but only in CYP3A5-nonexpressing patients (CYP3A5*3C/*3C carriers). Tacrolimus 62-72 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 4-10 28316087-10 2017 CONCLUSION: The ABCC2 c.3972C >T polymorphism affected tacrolimus C:D in Brazilian kidney transplant recipients. Tacrolimus 58-68 ATP binding cassette subfamily C member 2 Homo sapiens 16-21 28457398-10 2017 On the subgroup with GFR <45 mL/min/1.73 m2, those on tacrolimus had lower MgS than those on cyclosporine, but those same patients presented with significantly different GFR, higher in the tacrolimus subgroup. Tacrolimus 57-67 CD59 molecule (CD59 blood group) Homo sapiens 35-40 28457398-13 2017 A significant difference on MgS levels between patients on tacrolimus and cyclosporine was found only when considering GFR <45 mL/min/1.73 m2, in which patients on tacrolimus had significantly higher GFR than patients on cyclosporine, which may explain these results. Tacrolimus 167-177 CD59 molecule (CD59 blood group) Homo sapiens 133-138 28414795-4 2017 Cadm1 expression was upregulated in BMMs by receptor activator of nuclear factor kappa B ligand (RANKL), and blocked by a calcineurin/NFATc1 inhibitor, FK506. Tacrolimus 152-157 cell adhesion molecule 1 Mus musculus 0-5 28414795-4 2017 Cadm1 expression was upregulated in BMMs by receptor activator of nuclear factor kappa B ligand (RANKL), and blocked by a calcineurin/NFATc1 inhibitor, FK506. Tacrolimus 152-157 nuclear factor of activated T cells, cytoplasmic, calcineurin dependent 1 Mus musculus 134-140 28400553-5 2017 Relapses in tacrolimus treatment were associated with serum titers of aquaporin 4 antibody (AQP4-IgG) (P = 0.028). Tacrolimus 12-22 aquaporin 4 Homo sapiens 70-81 28400553-5 2017 Relapses in tacrolimus treatment were associated with serum titers of aquaporin 4 antibody (AQP4-IgG) (P = 0.028). Tacrolimus 12-22 aquaporin 4 Homo sapiens 92-96 28378777-1 2017 Bruck Syndrome is a connective tissue disease associated with inactivating mutations in lysyl hydroxylase 2 (LH2/PLOD2) or FK506 binding protein 65 (FKBP65/FKBP10). Tacrolimus 123-128 FK506 binding protein 10 Mus musculus 149-155 28378777-1 2017 Bruck Syndrome is a connective tissue disease associated with inactivating mutations in lysyl hydroxylase 2 (LH2/PLOD2) or FK506 binding protein 65 (FKBP65/FKBP10). Tacrolimus 123-128 FK506 binding protein 10 Mus musculus 156-162 28316087-11 2017 Further, CYP2C8*3 and CYP2J2 c.-76G>T SNPs influenced the renal function of these patients and the occurrence of adverse events during treatment with tacrolimus and mycophenolate sodium. Tacrolimus 153-163 cytochrome P450 family 2 subfamily J member 2 Homo sapiens 22-28 27779452-9 2017 A beneficial angiogenic response to potential therapies, FK506 and Elafin, was related to reduced slit guidance ligand 3 (SLIT3), an antimigratory factor. Tacrolimus 57-62 slit guidance ligand 3 Homo sapiens 122-127 29113387-3 2017 Meanwhile, the dose of FK506 and CsA was recorded, blood concentration of the drugs was measured, and graft outcome was monitored.These results indicate that CYP3A5*AA/AG carriers need higher FK506 dose than CYP3A5*GG homozygote to achieve the target blood concentration. Tacrolimus 192-197 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 158-164 29113387-4 2017 For CYP3A5*GG carriers, taking FK506 or CsA are both advisable. Tacrolimus 31-36 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 4-10 29113387-6 2017 CYP3A5 genotyping is a new approach to detecting FK506 dose requirement and a predictive index for the FK506 or CsA treatment selection in kidney recipients. Tacrolimus 49-54 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 29113387-6 2017 CYP3A5 genotyping is a new approach to detecting FK506 dose requirement and a predictive index for the FK506 or CsA treatment selection in kidney recipients. Tacrolimus 103-108 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 28157649-1 2017 OBJECTIVE: This study is to analyze concentration changes of the prolonged-release and shorter-acting formulation of tacrolimus in patients with different CYP3A5 genotypes after kidney transplantation. Tacrolimus 117-127 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 155-161 28157649-13 2017 CONCLUSION: Tacrolimus of different formulations had different impact on patients with different CYP3A5 genotypes after kidney transplantation. Tacrolimus 12-22 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 97-103 27503321-7 2017 CONCLUSIONS: These results strongly suggest that the interaction of FK506 with GDNF and NGF mediates distinct enhancement of neurite growth. Tacrolimus 68-73 glial cell derived neurotrophic factor Gallus gallus 79-83 27503321-7 2017 CONCLUSIONS: These results strongly suggest that the interaction of FK506 with GDNF and NGF mediates distinct enhancement of neurite growth. Tacrolimus 68-73 nerve growth factor Gallus gallus 88-91 26882121-3 2017 Aside from CYP3A5*3, the rs3814055 polymorphism in the NR1I2 gene was associated with the tacrolimus pharmacokinetics based on false discovery rate-corrected multiple tests and the least absolute shrinkage and selection operator analysis. Tacrolimus 90-100 nuclear receptor subfamily 1 group I member 2 Homo sapiens 55-60 28362060-17 2017 In the direct comparison, based on a single trial including 222 participants, tacrolimus plus sirolimus had increased mortality (HR 2.76, 95% CrI 1.30 to 6.69) and graft loss (HR 2.34, 95% CrI 1.28 to 4.61) at maximal follow-up compared with tacrolimus. Tacrolimus 78-88 EP300 interacting inhibitor of differentiation 1 Homo sapiens 142-147 28362060-17 2017 In the direct comparison, based on a single trial including 222 participants, tacrolimus plus sirolimus had increased mortality (HR 2.76, 95% CrI 1.30 to 6.69) and graft loss (HR 2.34, 95% CrI 1.28 to 4.61) at maximal follow-up compared with tacrolimus. Tacrolimus 78-88 EP300 interacting inhibitor of differentiation 1 Homo sapiens 189-194 28405602-12 2017 After drug conversion of a twice-daily CNI formulation to a once-daily tacrolimus formulation, CSA-treated patients needed longer to improve their cognitive functioning. Tacrolimus 71-81 ERCC excision repair 8, CSA ubiquitin ligase complex subunit Homo sapiens 95-98 28405602-14 2017 CONCLUSIONS: Patients with once-daily tacrolimus formulation had a better psychomotor speed than CSA-treated patients. Tacrolimus 38-48 ERCC excision repair 8, CSA ubiquitin ligase complex subunit Homo sapiens 97-100 28112181-0 2017 IL-3 and CTLA4 gene polymorphisms may influence the tacrolimus dose requirement in Chinese kidney transplant recipients. Tacrolimus 52-62 interleukin 3 Homo sapiens 0-4 28112181-0 2017 IL-3 and CTLA4 gene polymorphisms may influence the tacrolimus dose requirement in Chinese kidney transplant recipients. Tacrolimus 52-62 cytotoxic T-lymphocyte associated protein 4 Homo sapiens 9-14 28435308-0 2017 Association of the PPP3CA c.249G>A variant with clinical outcomes of tacrolimus-based therapy in kidney transplant recipients. Tacrolimus 72-82 protein phosphatase 3 catalytic subunit alpha Homo sapiens 19-25 27598231-8 2017 Moreover, higher frequencies of FoxP3-positive regulatory T cells in renal allografts were observed in ASP2409- and belatacept-based regimens compared with tacrolimus-based regimens. Tacrolimus 156-166 forkhead box protein P3 Macaca fascicularis 32-37 27822915-4 2017 Multiple regression analysis showed that concomitant use of oral itraconazole or voriconazole significantly increased the (C/Dpo)/(C/Div) of tacrolimus (p = 0.002), probably owing to the inhibition of enterohepatic cytochrome P450 3A4. Tacrolimus 141-151 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 215-234 28219593-0 2017 Betel Nut Chewing Is Associated With Reduced Tacrolimus Concentration in Taiwanese Liver Transplant Recipients. Tacrolimus 45-55 NUT midline carcinoma family member 1 Homo sapiens 6-9 28219593-2 2017 Tacrolimus, an immunosuppressant that protects against organ rejection in transplant recipients, not only is mainly metabolized by CYP3A enzymes but also has a narrow therapeutic range. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 131-136 28219593-6 2017 RESULTS: Dose-adjusted blood trough levels of tacrolimus tended to be significantly (P = .04) lower in betel nut chewers (mean = 0.81, medium = 0.7, 95% confidence interval [CI] = 0.73 to 0.90) than in nonchewers (mean = 1.12, medium = 0.88, 95% CI = 1.03 to 1.22) during the 18-month study period. Tacrolimus 46-56 NUT midline carcinoma family member 1 Homo sapiens 109-112 26882121-6 2017 An in vitro luciferase reporter assay indicated that downregulation of PXR expression is the likely molecular mechanism responsible for the increased exposure to tacrolimus in subjects carrying the rs3814055 C>T variant. Tacrolimus 162-172 nuclear receptor subfamily 1 group I member 2 Homo sapiens 71-74 28243539-7 2017 As expected, FK506 could induce a significant elevation of GVBD rate and increase the MPF level of denuded oocytes (DOs). Tacrolimus 13-18 mesothelin Mus musculus 86-89 27885697-16 2017 CYP3A5 expressers have decreased dose-adjusted tacrolimus C0 when compared to non-expressers. Tacrolimus 47-57 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 0-6 28108248-10 2017 We herein demonstrated that the new FK506-immobilized beads specifically isolated more FKBP12 than the original beads, thereby proving our method to be applicable to target identification experiments. Tacrolimus 36-41 FKBP prolyl isomerase 1A pseudogene 4 Homo sapiens 87-93 28196514-9 2017 Interestingly, FK506 injections significantly attenuated the MPTP-induced effects in the humanized CD34+ mice compared the C57BL/6 mice. Tacrolimus 15-20 CD34 antigen Mus musculus 99-103 28193233-8 2017 Placental production of TNFalphaand IL16 in the tacrolimus-treated HFD-dNONcNZO dams were restored to non-diabetic levels and the treatment resulted in the inhibition of aberrant monocyte/macrophage activation during pregnancy in the HFD-dNONcNZO dams. Tacrolimus 48-58 interleukin 16 Mus musculus 36-40 29371918-8 2017 TC improved Bcl2/Bax ratio, decreased apoptosis, CYP2E1 protein expression and liver fibrosis levels, however, EV offered no such protection. Tacrolimus 0-2 B cell leukemia/lymphoma 2 Mus musculus 12-16 29371918-8 2017 TC improved Bcl2/Bax ratio, decreased apoptosis, CYP2E1 protein expression and liver fibrosis levels, however, EV offered no such protection. Tacrolimus 0-2 BCL2-associated X protein Mus musculus 17-20 29371918-8 2017 TC improved Bcl2/Bax ratio, decreased apoptosis, CYP2E1 protein expression and liver fibrosis levels, however, EV offered no such protection. Tacrolimus 0-2 cytochrome P450, family 2, subfamily e, polypeptide 1 Mus musculus 49-55 29260042-6 2017 We hypothesize that use of tacrolimus may have contributed to the lack of response to topical interferon-alpha2b. Tacrolimus 27-37 interferon alpha 2 Homo sapiens 94-112 27885697-0 2017 Dynamic effects of CYP3A5 polymorphism on dose requirement and trough concentration of tacrolimus in renal transplant recipients. Tacrolimus 87-97 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 19-25 27885697-1 2017 WHAT IS KNOWN AND OBJECTIVE: Tacrolimus is a widely used immunosuppressive drug with marked pharmacokinetic variability partly due to CYP3A5 polymorphism. Tacrolimus 29-39 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 134-140 28280692-1 2017 The calcineurin inhibitor (CNI) tacrolimus (TAC) is an integral part of the immunosuppressive regimen after solid organ transplantation. Tacrolimus 32-42 calcineurin binding protein 1 Homo sapiens 4-25 28280692-1 2017 The calcineurin inhibitor (CNI) tacrolimus (TAC) is an integral part of the immunosuppressive regimen after solid organ transplantation. Tacrolimus 32-42 calcineurin binding protein 1 Homo sapiens 27-30 28084894-0 2017 Donors FMO3 polymorphisms affect tacrolimus elimination in Chinese liver transplant patients. Tacrolimus 33-43 flavin containing dimethylaniline monoxygenase 3 Homo sapiens 7-11 28084894-4 2017 RESULTS: Donor FMO3 rs1800822 allele T and rs909530 allele T were associated with fast tacrolimus elimination. Tacrolimus 87-97 flavin containing dimethylaniline monoxygenase 3 Homo sapiens 15-19 28084894-5 2017 Combination of polymorphisms of donor FMO3 rs1800822 and rs909530 genotype impacted on tacrolimus elimination (p = 0.0221). Tacrolimus 87-97 flavin containing dimethylaniline monoxygenase 3 Homo sapiens 38-42 28084894-7 2017 CONCLUSION: Donor"s FMO3 polymorphisms might affect tacrolimus elimination. Tacrolimus 52-62 flavin containing dimethylaniline monoxygenase 3 Homo sapiens 20-24 28030534-0 2017 Single-Nucleotide Polymorphism of CYP3A5 Impacts the Exposure to Tacrolimus in Pediatric Renal Transplant Recipients: A Pharmacogenetic Substudy of the TWIST Trial. Tacrolimus 65-75 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 34-40 28118317-0 2017 CD45RA Distinguishes CD4+CD25+CD127-/low TSDR Demethylated Regulatory T Cell Subpopulations With Differential Stability and Susceptibility to Tacrolimus-Mediated Inhibition of Suppression. Tacrolimus 142-152 protein tyrosine phosphatase receptor type C Homo sapiens 0-4 28118317-0 2017 CD45RA Distinguishes CD4+CD25+CD127-/low TSDR Demethylated Regulatory T Cell Subpopulations With Differential Stability and Susceptibility to Tacrolimus-Mediated Inhibition of Suppression. Tacrolimus 142-152 interferon stimulated exonuclease gene 20 Homo sapiens 25-29 28118317-0 2017 CD45RA Distinguishes CD4+CD25+CD127-/low TSDR Demethylated Regulatory T Cell Subpopulations With Differential Stability and Susceptibility to Tacrolimus-Mediated Inhibition of Suppression. Tacrolimus 142-152 interleukin 7 receptor Homo sapiens 30-35 29762990-0 2017 [Tacrolimus down-regulates the mRNA levels of IL-17 and IL-23 in the muscle tissues of mice with experimental autoimmune myositis]. Tacrolimus 1-11 interleukin 17A Mus musculus 46-51 29762990-0 2017 [Tacrolimus down-regulates the mRNA levels of IL-17 and IL-23 in the muscle tissues of mice with experimental autoimmune myositis]. Tacrolimus 1-11 interleukin 23, alpha subunit p19 Mus musculus 56-61 28122021-0 2017 The Effect of Tacrolimus and Mycophenolic Acid on CD14+ Monocyte Activation and Function. Tacrolimus 14-24 CD14 molecule Homo sapiens 50-54 28122021-7 2017 Tacrolimus (200 ng/ml) inhibited phosphorylation of p38MAPK by 30% (mean) in CD14+ monocytes which was significantly less than in activated CD3+ T cells (max 60%; p < 0.05). Tacrolimus 0-10 CD14 molecule Homo sapiens 77-81 28122021-10 2017 p-ERK was inhibited with a maximum of 15% after spiking with either tacrolimus or MPA. Tacrolimus 68-78 mitogen-activated protein kinase 1 Homo sapiens 2-5 27890698-7 2017 Thus, inhibition of CYP3A4 is presumably the underlying reason for the observed increase in the concentrations of the CYP3A4 substrate tacrolimus in the patient. Tacrolimus 135-145 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 20-26 27890698-7 2017 Thus, inhibition of CYP3A4 is presumably the underlying reason for the observed increase in the concentrations of the CYP3A4 substrate tacrolimus in the patient. Tacrolimus 135-145 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 118-124 28056508-4 2017 Using DARTS and LC-MS/MS analyses in combination with reference studies, V-ATPase catalytic subunit A (ATP6V1A) was identified as a new target protein of FK506. Tacrolimus 154-159 ATPase H+ transporting V1 subunit A Homo sapiens 103-110 28056508-5 2017 The biological relevance of ATP6V1A in mediating the neuroprotective effects of FK506 was validated by analyzing FK506 activity with respect to autophagy via acridine orange staining and transcription factor EB (TFEB) translocation assay. Tacrolimus 80-85 ATPase H+ transporting V1 subunit A Homo sapiens 28-35 28056508-5 2017 The biological relevance of ATP6V1A in mediating the neuroprotective effects of FK506 was validated by analyzing FK506 activity with respect to autophagy via acridine orange staining and transcription factor EB (TFEB) translocation assay. Tacrolimus 80-85 transcription factor EB Homo sapiens 187-210 28056508-5 2017 The biological relevance of ATP6V1A in mediating the neuroprotective effects of FK506 was validated by analyzing FK506 activity with respect to autophagy via acridine orange staining and transcription factor EB (TFEB) translocation assay. Tacrolimus 80-85 transcription factor EB Homo sapiens 212-216 28056508-5 2017 The biological relevance of ATP6V1A in mediating the neuroprotective effects of FK506 was validated by analyzing FK506 activity with respect to autophagy via acridine orange staining and transcription factor EB (TFEB) translocation assay. Tacrolimus 113-118 ATPase H+ transporting V1 subunit A Homo sapiens 28-35 28056508-6 2017 These analyses demonstrated that the binding of FK506 with ATP6V1A induces autophagy by activating the translocation of TFEB from the cytosol into the nucleus. Tacrolimus 48-53 ATPase H+ transporting V1 subunit A Homo sapiens 59-66 28056508-6 2017 These analyses demonstrated that the binding of FK506 with ATP6V1A induces autophagy by activating the translocation of TFEB from the cytosol into the nucleus. Tacrolimus 48-53 transcription factor EB Homo sapiens 120-124 28060893-8 2017 Molecular features involved in inflammation and immune response contributing to DN progression were significantly downregulated by tacrolimus (e.g. the tumor necrosis factor alpha (TNF), interleukin 4, or interleukin 10). Tacrolimus 131-141 tumor necrosis factor Homo sapiens 152-179 28060893-8 2017 Molecular features involved in inflammation and immune response contributing to DN progression were significantly downregulated by tacrolimus (e.g. the tumor necrosis factor alpha (TNF), interleukin 4, or interleukin 10). Tacrolimus 131-141 tumor necrosis factor Homo sapiens 181-184 28060893-8 2017 Molecular features involved in inflammation and immune response contributing to DN progression were significantly downregulated by tacrolimus (e.g. the tumor necrosis factor alpha (TNF), interleukin 4, or interleukin 10). Tacrolimus 131-141 interleukin 4 Homo sapiens 187-200 28060893-8 2017 Molecular features involved in inflammation and immune response contributing to DN progression were significantly downregulated by tacrolimus (e.g. the tumor necrosis factor alpha (TNF), interleukin 4, or interleukin 10). Tacrolimus 131-141 interleukin 10 Homo sapiens 205-219 28060893-9 2017 On the other hand, pro-fibrotic stimuli being detrimental to renal function were induced by tacrolimus like the transforming growth factor beta 1 (TGFB1), endothelin 1 (EDN1), or type IV collagen alpha 1 (COL4A1). Tacrolimus 92-102 transforming growth factor beta 1 Homo sapiens 112-145 28060893-9 2017 On the other hand, pro-fibrotic stimuli being detrimental to renal function were induced by tacrolimus like the transforming growth factor beta 1 (TGFB1), endothelin 1 (EDN1), or type IV collagen alpha 1 (COL4A1). Tacrolimus 92-102 transforming growth factor beta 1 Homo sapiens 147-152 28060893-9 2017 On the other hand, pro-fibrotic stimuli being detrimental to renal function were induced by tacrolimus like the transforming growth factor beta 1 (TGFB1), endothelin 1 (EDN1), or type IV collagen alpha 1 (COL4A1). Tacrolimus 92-102 endothelin 1 Homo sapiens 155-167 28060893-9 2017 On the other hand, pro-fibrotic stimuli being detrimental to renal function were induced by tacrolimus like the transforming growth factor beta 1 (TGFB1), endothelin 1 (EDN1), or type IV collagen alpha 1 (COL4A1). Tacrolimus 92-102 endothelin 1 Homo sapiens 169-173 28060893-9 2017 On the other hand, pro-fibrotic stimuli being detrimental to renal function were induced by tacrolimus like the transforming growth factor beta 1 (TGFB1), endothelin 1 (EDN1), or type IV collagen alpha 1 (COL4A1). Tacrolimus 92-102 collagen type IV alpha 1 chain Homo sapiens 205-211 28060893-10 2017 CONCLUSION: Patients with DN and elevated TNF levels might benefit from tacrolimus treatment regarding maintaining GFR and reducing inflammation. Tacrolimus 72-82 tumor necrosis factor Homo sapiens 42-45 28056860-8 2017 A decline in eGFR was the most frequent adverse event during tacrolimus treatment. Tacrolimus 61-71 epidermal growth factor receptor Homo sapiens 13-17 28056860-9 2017 During tacrolimus treatment, a >=40% decrease in eGFR was observed in 43 (10.5%) patients. Tacrolimus 7-17 epidermal growth factor receptor Homo sapiens 52-56 27458792-8 2017 We also observed dysregulation of miRNAs (e.g. let-7, miR-26b, miR-145, and miR-183) in cultured human hepatocytes treated with tacrolimus or high glucose, the two independent risk factors of NODALT identified in this cohort. Tacrolimus 128-138 microRNA 26b Homo sapiens 54-61 27458792-8 2017 We also observed dysregulation of miRNAs (e.g. let-7, miR-26b, miR-145, and miR-183) in cultured human hepatocytes treated with tacrolimus or high glucose, the two independent risk factors of NODALT identified in this cohort. Tacrolimus 128-138 microRNA 145 Homo sapiens 63-70 27458792-8 2017 We also observed dysregulation of miRNAs (e.g. let-7, miR-26b, miR-145, and miR-183) in cultured human hepatocytes treated with tacrolimus or high glucose, the two independent risk factors of NODALT identified in this cohort. Tacrolimus 128-138 microRNA 183 Homo sapiens 76-83 27458792-9 2017 The hepatic miRNA profiles altered by tacrolimus or hyperglycemia were associated with insulin resistance and glucose homeostatic imbalance as revealed by enrichment analysis. Tacrolimus 38-48 insulin Homo sapiens 87-94 27885697-2 2017 Our study aimed to investigate the dynamic effects of CYP3A5 genotypes on dose requirement and trough concentration (C0 ) of tacrolimus in renal transplant recipients. Tacrolimus 125-135 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 54-60 28655393-0 2017 The role of single nucleotide polymorphisms of CYP3A and ABCB1 on tacrolimus predose concentration in kidney transplant recipients. Tacrolimus 66-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 47-52 28655393-0 2017 The role of single nucleotide polymorphisms of CYP3A and ABCB1 on tacrolimus predose concentration in kidney transplant recipients. Tacrolimus 66-76 ATP binding cassette subfamily B member 1 Homo sapiens 57-62 28655393-8 2017 On the other hand, less than 1% of our transplant recipients possess the <italic>CYP3A</italic> genotype, which requires high daily tacrolimus dose. Tacrolimus 144-154 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 87-92 28246425-0 2017 Influence of IL-18 and IL-10 Polymorphisms on Tacrolimus Elimination in Chinese Lung Transplant Patients. Tacrolimus 46-56 interleukin 10 Homo sapiens 23-28 28246425-2 2017 The influence of interleukin-10 (IL-10) and interleukin-18 (IL-18) polymorphisms on tacrolimus pharmacokinetics had been described in liver and kidney transplantation. Tacrolimus 84-94 interleukin 18 Homo sapiens 44-58 28246425-2 2017 The influence of interleukin-10 (IL-10) and interleukin-18 (IL-18) polymorphisms on tacrolimus pharmacokinetics had been described in liver and kidney transplantation. Tacrolimus 84-94 interleukin 18 Homo sapiens 60-65 28246425-10 2017 IL-18 rs5744247 allele C and rs1946518 allele A were associated with fast tacrolimus metabolism. Tacrolimus 74-84 interleukin 18 Homo sapiens 0-5 28246425-11 2017 Combined analysis showed that the numbers of low IL-18 mRNA expression alleles had positive correlation with tacrolimus C/D ratios in lung transplant recipients. Tacrolimus 109-119 interleukin 18 Homo sapiens 49-54 28246425-12 2017 The influence of IL-18 polymorphisms on tacrolimus C/D ratios was observed in CYP3A5 expresser recipients, but not in CYP3A5 nonexpresser recipients. Tacrolimus 40-50 interleukin 18 Homo sapiens 17-22 28246425-12 2017 The influence of IL-18 polymorphisms on tacrolimus C/D ratios was observed in CYP3A5 expresser recipients, but not in CYP3A5 nonexpresser recipients. Tacrolimus 40-50 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 78-84 28246425-15 2017 IL-18 polymorphisms may influence tacrolimus elimination in lung transplantation patients. Tacrolimus 34-44 interleukin 18 Homo sapiens 0-5 28805561-4 2017 The aim of this study was to examine the association between KCNJ11 and KCNQ1 gene polymorphisms and posttransplant diabetes mellitus in kidney allograft recipients treated with tacrolimus. Tacrolimus 178-188 potassium inwardly rectifying channel subfamily J member 11 Homo sapiens 61-67 27717793-0 2017 The effect of CYP3A5 genetic polymorphisms on adverse events in patients with ulcerative colitis treated with tacrolimus. Tacrolimus 110-120 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 14-20 27747372-0 2017 FOXP3 rs3761548 polymorphism is associated with tacrolimus-induced acute nephrotoxicity in renal transplant patients. Tacrolimus 48-58 forkhead box P3 Homo sapiens 0-5 27747372-1 2017 PURPOSE: The purpose of this study was to investigate the potential impact of FOXP3 and CCDC22 gene polymorphisms on efficacy and safety of tacrolimus (TAC) in renal transplant patients. Tacrolimus 140-150 forkhead box P3 Homo sapiens 78-83 27747372-1 2017 PURPOSE: The purpose of this study was to investigate the potential impact of FOXP3 and CCDC22 gene polymorphisms on efficacy and safety of tacrolimus (TAC) in renal transplant patients. Tacrolimus 140-150 coiled-coil domain containing 22 Homo sapiens 88-94 28805561-4 2017 The aim of this study was to examine the association between KCNJ11 and KCNQ1 gene polymorphisms and posttransplant diabetes mellitus in kidney allograft recipients treated with tacrolimus. Tacrolimus 178-188 potassium voltage-gated channel subfamily Q member 1 Homo sapiens 72-77 29179182-11 2017 FK506 could significantly decrease TRPCs, CaN, phosphorylation of ERK1/2 and alpha-SMA expression. Tacrolimus 0-5 mitogen activated protein kinase 3 Rattus norvegicus 66-72 29279557-11 2017 It is notable that genotypes in patients where tacrolimus was not detected in the blood were wild types: 2677G/G and 3435C/C in MDR1. Tacrolimus 47-57 ATP binding cassette subfamily B member 1 Homo sapiens 128-132 29179182-12 2017 CONCLUSION: Taken together, these results suggest that the therapeutic effect of FK506 on IgAN might be partially associated with the down-regulated expression of TRPC channels, CaN and phosphorylation of ERK1/2. Tacrolimus 81-86 mitogen activated protein kinase 3 Rattus norvegicus 205-211 28092916-9 2017 However, the levels of CD4+Foxp3+ and CD3-CD56+ T cells were higher in the brand-name tacrolimus group than in the generic tacrolimus group 8 weeks after transplantation (p < 0.05). Tacrolimus 86-96 CD4 molecule Homo sapiens 23-26 28092916-10 2017 CONCLUSIONS: The level of CD4+Foxp3+ T cells was higher in the brand-name tacrolimus group than in the generic tacrolimus group after transplantation. Tacrolimus 74-84 CD4 molecule Homo sapiens 26-29 28092916-10 2017 CONCLUSIONS: The level of CD4+Foxp3+ T cells was higher in the brand-name tacrolimus group than in the generic tacrolimus group after transplantation. Tacrolimus 111-121 CD4 molecule Homo sapiens 26-29 28092916-11 2017 This finding showed that brand-name tacrolimus could have more potential immunosuppressive activity than generic tacrolimus regarding the contribution of CD4+Foxp3+ T cells to graft tolerance in liver transplant recipients. Tacrolimus 36-46 CD4 molecule Homo sapiens 154-157 27181115-2 2017 Tacrolimus (TAC) has proved to show efficacy against inadequate response to tumor necrosis factor alpha inhibitors, yet its add-on effects on TCZ remain unknown. Tacrolimus 0-10 tumor necrosis factor Homo sapiens 76-103 27977332-1 2017 AIM: Meta-analyses and large cohort studies provide confusing results on the association of the CYP3A5 6986A>G allelic variant and adverse outcomes in kidney transplant recipients under tacrolimus-based immunosuppressive regimen. Tacrolimus 189-199 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 96-102 26667830-1 2017 Tacrolimus is dependent on CYP3A5 enzyme for metabolism. Tacrolimus 0-10 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 27-33 27977332-2 2017 A residual effect of CYP3A5 recipient genotype is unexpected if kidney transplant recipients have similar exposure of tacrolimus. Tacrolimus 118-128 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 21-27 27977332-5 2017 We found a significant association of CYP3A5 genotypes with tacrolimus daily dose as well as with tacrolimus dose-adjusted concentrations. Tacrolimus 60-70 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 38-44 27977332-5 2017 We found a significant association of CYP3A5 genotypes with tacrolimus daily dose as well as with tacrolimus dose-adjusted concentrations. Tacrolimus 98-108 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 38-44 28101175-10 2016 FK506 treatment altered the expression levels of miR-146a and miR-155, indicating that they may have an important role in regulating the immune response to the rejection effect. Tacrolimus 0-5 microRNA 146a Rattus norvegicus 49-57 28253495-0 2017 Tacrolimus Triggers Transient Receptor Potential Vanilloid-1-Dependent Relapse of Pancreatitis-Related Pain in Mice. Tacrolimus 0-10 transient receptor potential cation channel, subfamily V, member 1 Mus musculus 20-60 28253495-3 2017 Calcineurin, a phosphatase, negatively regulates various channel functions including TRPV1, and calcineurin inhibitor-induced pain syndrome by tacrolimus, a calcineurin inhibitor, used as an immunosuppressant, has been a clinical problem. Tacrolimus 143-153 calcineurin binding protein 1 Mus musculus 96-117 28253495-3 2017 Calcineurin, a phosphatase, negatively regulates various channel functions including TRPV1, and calcineurin inhibitor-induced pain syndrome by tacrolimus, a calcineurin inhibitor, used as an immunosuppressant, has been a clinical problem. Tacrolimus 143-153 calcineurin binding protein 1 Mus musculus 157-178 28253495-6 2017 Pancreatitis-related symptoms disappeared in 24 h, whereas the referred hyperalgesia recurred following the administration of tacrolimus, which was abolished by the blockers of TRPV1 but not T-type Ca2+ channels. Tacrolimus 126-136 transient receptor potential cation channel, subfamily V, member 1 Mus musculus 177-182 28253495-7 2017 Thus, tacrolimus appears to cause the TRPV1-dependent relapse of pancreatitis-related pain, suggesting the involvement of calcineurin in the termination of pancreatic pain. Tacrolimus 6-16 transient receptor potential cation channel, subfamily V, member 1 Mus musculus 38-43 28736028-0 2017 Association Between Tacrolimus Pharmacokinetics and Cytochrome P450 3A5 and Multidrug Resistance Protein 1 Exon 21 Polymorphisms. Tacrolimus 20-30 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 52-71 28736028-0 2017 Association Between Tacrolimus Pharmacokinetics and Cytochrome P450 3A5 and Multidrug Resistance Protein 1 Exon 21 Polymorphisms. Tacrolimus 20-30 ATP binding cassette subfamily B member 1 Homo sapiens 76-106 28736028-1 2017 BACKGROUND: Individual differences in the pharmacokinetics (PK) of tacrolimus (TAC), an immunosuppressive drug, are reportedly associated with single-nucleotide polymorphisms (SNPs) of cytochrome P450 (CYP) 3A5 and multidrug resistance protein 1 (MDR1). Tacrolimus 67-77 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 185-210 28736028-1 2017 BACKGROUND: Individual differences in the pharmacokinetics (PK) of tacrolimus (TAC), an immunosuppressive drug, are reportedly associated with single-nucleotide polymorphisms (SNPs) of cytochrome P450 (CYP) 3A5 and multidrug resistance protein 1 (MDR1). Tacrolimus 67-77 ATP binding cassette subfamily B member 1 Homo sapiens 215-245 28736028-1 2017 BACKGROUND: Individual differences in the pharmacokinetics (PK) of tacrolimus (TAC), an immunosuppressive drug, are reportedly associated with single-nucleotide polymorphisms (SNPs) of cytochrome P450 (CYP) 3A5 and multidrug resistance protein 1 (MDR1). Tacrolimus 67-77 ATP binding cassette subfamily B member 1 Homo sapiens 247-251 27930655-8 2016 According to median regression analysis, AUC of prednisone t0-6 was significantly associated with the decrease of Gd-IgA1 t0-6 (P = 0.01) and IgA1 t0-6 (p = 0.002), whereas AUC of tacrolimus t0-6 was associated with the decrease of IgA1 t0-6 (p = 0.02). Tacrolimus 180-190 immunoglobulin heavy constant alpha 1 Homo sapiens 117-121 27930655-8 2016 According to median regression analysis, AUC of prednisone t0-6 was significantly associated with the decrease of Gd-IgA1 t0-6 (P = 0.01) and IgA1 t0-6 (p = 0.002), whereas AUC of tacrolimus t0-6 was associated with the decrease of IgA1 t0-6 (p = 0.02). Tacrolimus 180-190 immunoglobulin heavy constant alpha 1 Homo sapiens 142-146 27930655-8 2016 According to median regression analysis, AUC of prednisone t0-6 was significantly associated with the decrease of Gd-IgA1 t0-6 (P = 0.01) and IgA1 t0-6 (p = 0.002), whereas AUC of tacrolimus t0-6 was associated with the decrease of IgA1 t0-6 (p = 0.02). Tacrolimus 180-190 immunoglobulin heavy constant alpha 1 Homo sapiens 142-146 27488997-9 2016 Tacrolimus also did not change total AQP2 abundance but significantly increased the abundances of pS261-AQP2 and pS264-AQP2. Tacrolimus 0-10 aquaporin 2 Rattus norvegicus 104-108 27488997-9 2016 Tacrolimus also did not change total AQP2 abundance but significantly increased the abundances of pS261-AQP2 and pS264-AQP2. Tacrolimus 0-10 aquaporin 2 Rattus norvegicus 104-108 27488997-11 2016 Tacrolimus did increase the expression of pS264-AQP2 in the apical plasma membrane (by immunohistochemistry). Tacrolimus 0-10 aquaporin 2 Rattus norvegicus 48-52 28101175-10 2016 FK506 treatment altered the expression levels of miR-146a and miR-155, indicating that they may have an important role in regulating the immune response to the rejection effect. Tacrolimus 0-5 microRNA 155 Rattus norvegicus 62-69 27152719-12 2016 In OLP, tacrolimus treatment reduced the expression of Cat K in the epithelium but increased it in the stroma. Tacrolimus 8-18 cathepsin K Homo sapiens 55-60 27658575-4 2016 Yak FKBP6 encodes a polypeptide of 295 amino acid residues with an FK506-binding domain (FKBP_C) and three tetratricopeptide repeat domains. Tacrolimus 67-72 FKBP prolyl isomerase family member 6 (inactive) Bos taurus 4-9 27386875-0 2016 Repair of Neurological Function in Response to FK506 Through CaN/NFATc1 Pathway Following Traumatic Brain Injury in Rats. Tacrolimus 47-52 nuclear factor of activated T-cells 1 Rattus norvegicus 65-71 27030163-2 2016 PURPOSE: Herein, we prepared ovalbumin (OVA)-modified liposomes encapsulating the immunosuppressive drug FK506 (OVA-LipFK) and aimed to demonstrate the delivery selectivity of the liposomes to splenic B cells, and its antiallergic effect in an OVA-sensitized allergic model mouse. Tacrolimus 105-110 serine (or cysteine) peptidase inhibitor, clade B, member 1, pseudogene Mus musculus 29-38 27633115-0 2016 Mechanism of tacrolimus-induced chronic renal fibrosis following transplantation is regulated by ox-LDL and its receptor, LOX-1. Tacrolimus 13-23 oxidized low density lipoprotein receptor 1 Rattus norvegicus 122-127 28031829-1 2016 A 59-year-old woman receiving methotrexate and tacrolimus for rheumatoid arthritis (RA) was referred to our hospital following bilateral ground-glass opacity observed in her chest X-ray and elevated serum KL-6. Tacrolimus 47-57 mucin 1, cell surface associated Homo sapiens 205-209 27473149-7 2016 In cultured human cells, treatment with FK506 (tacrolimus), a calcineurin inhibitor, results in accumulation of pTDP species. Tacrolimus 40-45 calcineurin binding protein 1 Homo sapiens 62-83 27473149-7 2016 In cultured human cells, treatment with FK506 (tacrolimus), a calcineurin inhibitor, results in accumulation of pTDP species. Tacrolimus 47-57 calcineurin binding protein 1 Homo sapiens 62-83 28164520-0 2016 The Effect of ABCB1 Polymorphisms on Serial Tacrolimus Concentrations in Stable Austrian Long-Term Kidney Transplant Recipients. Tacrolimus 44-54 ATP binding cassette subfamily B member 1 Homo sapiens 14-19 28164520-1 2016 BACKGROUND: The multidrug resistance 1 gene (ABCB1) encodes P-glycoprotein (PGP), mainly expressed in the liver and engaged in metabolism of drugs including the immunosuppressant tacrolimus (TAC). Tacrolimus 179-189 ATP binding cassette subfamily B member 1 Homo sapiens 16-38 28164520-1 2016 BACKGROUND: The multidrug resistance 1 gene (ABCB1) encodes P-glycoprotein (PGP), mainly expressed in the liver and engaged in metabolism of drugs including the immunosuppressant tacrolimus (TAC). Tacrolimus 179-189 ATP binding cassette subfamily B member 1 Homo sapiens 45-50 28164520-1 2016 BACKGROUND: The multidrug resistance 1 gene (ABCB1) encodes P-glycoprotein (PGP), mainly expressed in the liver and engaged in metabolism of drugs including the immunosuppressant tacrolimus (TAC). Tacrolimus 179-189 ATP binding cassette subfamily B member 1 Homo sapiens 60-74 28164520-1 2016 BACKGROUND: The multidrug resistance 1 gene (ABCB1) encodes P-glycoprotein (PGP), mainly expressed in the liver and engaged in metabolism of drugs including the immunosuppressant tacrolimus (TAC). Tacrolimus 179-189 ATP binding cassette subfamily B member 1 Homo sapiens 76-79 27338269-0 2016 Pure red cell aplasia induced by anti-erythropoietin antibodies, well-controlled with tacrolimus. Tacrolimus 86-96 erythropoietin Homo sapiens 38-52 27338269-3 2016 The efficacy of tacrolimus, another calcineurin inhibitor, in patients with anti-EPO PRCA has not been determined. Tacrolimus 16-26 erythropoietin Homo sapiens 81-84 27338269-4 2016 The present report is the first our knowledge to describe the successful treatment of a patient with anti-EPO PRCA using tacrolimus. Tacrolimus 121-131 erythropoietin Homo sapiens 106-109 27399255-10 2016 Everolimus and tacrolimus are two immunosuppressive drugs metabolized by CYP3A4. Tacrolimus 15-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 73-79 27386875-2 2016 The nuclear factor of activated T cells (NFATc1) pathway plays an important role in regenerating neurological function following traumatic brain injury (TBI), but the precise mechanism underlying FK506-induced repair of neurological functions remains unclear. Tacrolimus 196-201 nuclear factor of activated T-cells 1 Rattus norvegicus 41-47 27386875-8 2016 Moreover, the cortical mRNA and serum protein expression levels of interleukin-2 (IL-2) and interferon-gamma (IFN-gamma) were decreased in FK506 group, especially at 6 h and at 1 day after TBI. Tacrolimus 139-144 interleukin 2 Rattus norvegicus 67-80 27386875-8 2016 Moreover, the cortical mRNA and serum protein expression levels of interleukin-2 (IL-2) and interferon-gamma (IFN-gamma) were decreased in FK506 group, especially at 6 h and at 1 day after TBI. Tacrolimus 139-144 interleukin 2 Rattus norvegicus 82-86 27386875-8 2016 Moreover, the cortical mRNA and serum protein expression levels of interleukin-2 (IL-2) and interferon-gamma (IFN-gamma) were decreased in FK506 group, especially at 6 h and at 1 day after TBI. Tacrolimus 139-144 interferon gamma Rattus norvegicus 92-108 27386875-8 2016 Moreover, the cortical mRNA and serum protein expression levels of interleukin-2 (IL-2) and interferon-gamma (IFN-gamma) were decreased in FK506 group, especially at 6 h and at 1 day after TBI. Tacrolimus 139-144 interferon gamma Rattus norvegicus 110-119 27386875-10 2016 Mechanistically, FK506 significantly down-regulated the mRNA and protein levels of calcium-regulated phosphatase (calcineurin, CaN) and inhibited the activation of NFATc1. Tacrolimus 17-22 nuclear factor of activated T-cells 1 Rattus norvegicus 164-170 27386875-11 2016 These results demonstrate that FK506 relieved inflammatory responses by regulating the NFATc1 signaling pathway and promoting the synaptic reconstruction of neurons and glial cells by regulating cell apoptosis, thereby facilitated improvements in neurological function. Tacrolimus 31-36 nuclear factor of activated T-cells 1 Rattus norvegicus 87-93 27372923-3 2016 Therefore, the aim of this study was to investigate the expression profile of TGFbeta isoforms, their receptors, and TGFbeta-related genes in human retinal pigment epithelial cells (RPE) after tacrolimus (FK-506) treatment in the presence or absence of lipopolysaccharide (LPS)-induced inflammation. Tacrolimus 193-203 transforming growth factor beta 1 Homo sapiens 78-85 27372923-0 2016 Transforming growth factor beta-related genes in human retinal pigment epithelial cells after tacrolimus treatment. Tacrolimus 94-104 transforming growth factor beta 1 Homo sapiens 0-31 27372923-3 2016 Therefore, the aim of this study was to investigate the expression profile of TGFbeta isoforms, their receptors, and TGFbeta-related genes in human retinal pigment epithelial cells (RPE) after tacrolimus (FK-506) treatment in the presence or absence of lipopolysaccharide (LPS)-induced inflammation. Tacrolimus 205-211 transforming growth factor beta 1 Homo sapiens 117-124 27372923-5 2016 RESULTS: Analysis using oligonucleotide microarrays revealed 20 statistically significant differentially expressed TGFbeta-related genes after LPS treatment in relation to control cells, and after tacrolimus and LPS treatment in relation to LPS-treated cells. Tacrolimus 197-207 transforming growth factor beta 1 Homo sapiens 115-122 27372923-6 2016 Moreover, our results showed that mRNA levels for TGFbeta2 and TGFbetaR3 after tacrolimus treatment, and for TGFbetaR3 after tacrolimus and LPS treatment in RPE cells were decreased. Tacrolimus 79-89 transforming growth factor beta 2 Homo sapiens 50-58 29441922-0 2016 The impact of CYP3A5 on the metabolism of cyclosporine A and tacrolimus in the evaluation of efficiency and safety of immunosuppressive treatment in patients after kidney transplantation. Tacrolimus 61-71 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 14-20 29441922-1 2016 The aim of the study was to determine the impact of CYP3A5 mutation on the serum levels of immunosuppressive drugs (tacrolimus and cyclosporine A), and on the occurrence of acute rejection episodes among patients after kidney transplantation. Tacrolimus 116-126 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 52-58 27310200-8 2016 Cyclosporine predominantly inhibited CYP3A4 (half maximal inhibitory concentration = 0.71 microM) rather than CYP3A5 (>5 microM), whereas tacrolimus showed similar inhibition for CYP3A4 (0.29 microM) and CYP3A5 (0.41 microM). Tacrolimus 141-151 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 182-188 27653228-8 2016 CONCLUSIONS: This study confirms the effect of CYP3A5*3 on tacrolimus dose requirement in liver transplantation and shows unexpected associations between the type of, and exposure to, CNI and either chronic rejection or graft loss. Tacrolimus 59-69 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 47-53 27706725-0 2016 Effect of pregnane X receptor polymorphisms on tacrolimus blood concentrations and the resulting adverse reactions in kidney transplantation recipients. Tacrolimus 47-57 nuclear receptor subfamily 1 group I member 2 Homo sapiens 10-29 27746739-11 2016 ERK1/2 phosphorylation was inhibited by FK506 and C3. Tacrolimus 40-45 mitogen activated protein kinase 3 Rattus norvegicus 0-6 27706725-1 2016 We investigated the effect of pregnane X receptor (PXR) polymorphisms on tacrolimus (FK506) blood trough concentrations and the associated adverse reactions in kidney transplantation recipients (KTRs). Tacrolimus 73-83 nuclear receptor subfamily 1 group I member 2 Homo sapiens 30-49 27706725-1 2016 We investigated the effect of pregnane X receptor (PXR) polymorphisms on tacrolimus (FK506) blood trough concentrations and the associated adverse reactions in kidney transplantation recipients (KTRs). Tacrolimus 73-83 nuclear receptor subfamily 1 group I member 2 Homo sapiens 51-54 27706725-1 2016 We investigated the effect of pregnane X receptor (PXR) polymorphisms on tacrolimus (FK506) blood trough concentrations and the associated adverse reactions in kidney transplantation recipients (KTRs). Tacrolimus 85-90 nuclear receptor subfamily 1 group I member 2 Homo sapiens 30-49 27498776-0 2016 The POR rs1057868-rs2868177 GC-GT diplotype is associated with high tacrolimus concentrations in early post-renal transplant recipients. Tacrolimus 68-78 cytochrome p450 oxidoreductase Homo sapiens 4-7 27498776-2 2016 In this study we examined the association between 6 POR SNPs and tacrolimus concentrations in Chinese renal transplant recipients. Tacrolimus 65-75 cytochrome p450 oxidoreductase Homo sapiens 52-55 27498776-9 2016 The CYP3A5*3 and POR rs1057868-rs2868177 GC-GT diplotype explained 31.7% and 5.7%, respectively, of the inter-individual variability of tacrolimus C0D7/D, whereas the POR rs1057868-rs2868177 GC-GT diplotype could explain 10.9% of the inter-individual variability of tacrolimus C0D7/D in CYP3A5 non-expressers. Tacrolimus 136-146 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 4-10 27498776-9 2016 The CYP3A5*3 and POR rs1057868-rs2868177 GC-GT diplotype explained 31.7% and 5.7%, respectively, of the inter-individual variability of tacrolimus C0D7/D, whereas the POR rs1057868-rs2868177 GC-GT diplotype could explain 10.9% of the inter-individual variability of tacrolimus C0D7/D in CYP3A5 non-expressers. Tacrolimus 136-146 cytochrome p450 oxidoreductase Homo sapiens 17-20 27498776-9 2016 The CYP3A5*3 and POR rs1057868-rs2868177 GC-GT diplotype explained 31.7% and 5.7%, respectively, of the inter-individual variability of tacrolimus C0D7/D, whereas the POR rs1057868-rs2868177 GC-GT diplotype could explain 10.9% of the inter-individual variability of tacrolimus C0D7/D in CYP3A5 non-expressers. Tacrolimus 136-146 cytochrome p450 oxidoreductase Homo sapiens 167-170 27498776-9 2016 The CYP3A5*3 and POR rs1057868-rs2868177 GC-GT diplotype explained 31.7% and 5.7%, respectively, of the inter-individual variability of tacrolimus C0D7/D, whereas the POR rs1057868-rs2868177 GC-GT diplotype could explain 10.9% of the inter-individual variability of tacrolimus C0D7/D in CYP3A5 non-expressers. Tacrolimus 136-146 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 287-293 27498776-9 2016 The CYP3A5*3 and POR rs1057868-rs2868177 GC-GT diplotype explained 31.7% and 5.7%, respectively, of the inter-individual variability of tacrolimus C0D7/D, whereas the POR rs1057868-rs2868177 GC-GT diplotype could explain 10.9% of the inter-individual variability of tacrolimus C0D7/D in CYP3A5 non-expressers. Tacrolimus 266-276 cytochrome p450 oxidoreductase Homo sapiens 17-20 27498776-10 2016 CONCLUSION: The CYP3A5*3 and POR rs1057868-rs2868177 GC-GT diplotype accounted for the inter-individual variation of tacrolimus C0D7/D. Tacrolimus 117-127 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 16-22 27498776-10 2016 CONCLUSION: The CYP3A5*3 and POR rs1057868-rs2868177 GC-GT diplotype accounted for the inter-individual variation of tacrolimus C0D7/D. Tacrolimus 117-127 cytochrome p450 oxidoreductase Homo sapiens 29-32 27498776-11 2016 Genotyping of POR rs1057868-rs2868177 diplotypes would help to differentiate initial tacrolimus dose requirements and to achieve early target C0 ranges in Chinese renal transplant recipients. Tacrolimus 85-95 cytochrome p450 oxidoreductase Homo sapiens 14-17 26990694-0 2016 Long-Term Clinical Impact of Adaptation of Initial Tacrolimus Dosing to CYP3A5 Genotype. Tacrolimus 51-61 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 72-78 26990694-1 2016 Pretransplantation adaptation of the daily dose of tacrolimus to CYP3A5 genotype is associated with improved achievement of target trough concentration (C0 ), but whether this improvement affects clinical outcomes is unknown. Tacrolimus 51-61 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 65-71 27138785-0 2016 The Effect of Weight and CYP3A5 Genotype on the Population Pharmacokinetics of Tacrolimus in Stable Paediatric Renal Transplant Recipients. Tacrolimus 79-89 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 25-31 27138785-7 2016 Children with lower weight and CYP3A5 expressers required higher weight-normalised tacrolimus doses. Tacrolimus 83-93 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 31-37 27138785-10 2016 Dose simulations show that a daily tacrolimus dose of 0.2 mg/kg generates a pre-dose concentration (C 0) ranging from 5 to 10 microg/L depending on the weight and CYP3A5 polymorphism. Tacrolimus 35-45 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 163-169 27138785-12 2016 CONCLUSIONS: In patients beyond the first year after transplantation, there is a cumulative effect of CYP3A5*1 polymorphism and weight on the tacrolimus C 0. Tacrolimus 142-152 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 102-108 27138785-13 2016 Children with lower weight and carriers of the CYP3A5*1 allele have higher weight-normalised tacrolimus dose requirements. Tacrolimus 93-103 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 47-53 27314545-2 2016 We sought to determine the singular and combined impact of CYP3A4*22 and CYP3A5*3 variants on tacrolimus drug disposition in adult heart transplant recipients. Tacrolimus 94-104 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 59-65 27641617-7 2016 Calcineurin antagonist FK506 could weaken the neuroprotection and the dephosphorylation of NMDAR induced by TRPC1/4 overexpression. Tacrolimus 23-28 transient receptor potential cation channel, subfamily C, member 1 Rattus norvegicus 108-113 27602099-1 2016 Tacrolimus (TAC) has been shown to improve remission from proteinuria in patients with refractory IgA nephropathy (IgAN); however, the efficacy and safety of TAC in such patients have not been fully explored. Tacrolimus 0-10 IGAN1 Homo sapiens 115-119 27318696-9 2016 Moreover, calcineurin inhibitors, cyclosporine A and FK506, partially reversed TRPV2 activation-induced inhibition of brown adipocyte differentiation. Tacrolimus 53-58 transient receptor potential cation channel, subfamily V, member 2 Mus musculus 79-84 27604685-0 2016 Previous exposure to biologics and C-reactive protein are associated with the response to tacrolimus in inflammatory bowel disease. Tacrolimus 90-100 C-reactive protein Homo sapiens 35-53 27580845-4 2016 Our results showed that CsA and FK506 treatment decreased proteinuria via a mechanism associated to a reduction in the foot-process fusion and desmin, and a recovery of synaptopodin and podocin. Tacrolimus 32-37 nephrosis 2, podocin Mus musculus 186-193 27580845-5 2016 In PAN-treated mouse podocytes, pre-incubation with CsA and FK506 restored the distribution of the actin cytoskeleton, increased the expression of synaptopodin and podocin, improved podocyte viability, and reduced the migrating activities of podocytes. Tacrolimus 60-65 nephrosis 2, podocin Mus musculus 164-171 27580845-6 2016 Treatment with CsA and FK506 also inhibited PAN-induced podocytes apoptosis, which was associated with the induction of Bcl-xL and inhibition of Bax, cleaved caspase 3, and cleaved PARP expression. Tacrolimus 23-28 BCL2-like 1 Mus musculus 120-126 27580845-6 2016 Treatment with CsA and FK506 also inhibited PAN-induced podocytes apoptosis, which was associated with the induction of Bcl-xL and inhibition of Bax, cleaved caspase 3, and cleaved PARP expression. Tacrolimus 23-28 BCL2-associated X protein Mus musculus 145-148 27580845-6 2016 Treatment with CsA and FK506 also inhibited PAN-induced podocytes apoptosis, which was associated with the induction of Bcl-xL and inhibition of Bax, cleaved caspase 3, and cleaved PARP expression. Tacrolimus 23-28 poly (ADP-ribose) polymerase family, member 1 Mus musculus 181-185 27580845-7 2016 Further studies revealed that CsA and FK506 inhibited PAN-induced p38 and JNK signaling, thereby protecting podocytes from PAN-induced injury. Tacrolimus 38-43 mitogen-activated protein kinase 14 Mus musculus 66-69 27580845-7 2016 Further studies revealed that CsA and FK506 inhibited PAN-induced p38 and JNK signaling, thereby protecting podocytes from PAN-induced injury. Tacrolimus 38-43 mitogen-activated protein kinase 8 Mus musculus 74-77 27648296-11 2016 In all patients treated with tacrolimus, tacrolimus could be discontinued with SASP. Tacrolimus 29-39 aspartic peptidase retroviral like 1 Homo sapiens 79-83 27648296-11 2016 In all patients treated with tacrolimus, tacrolimus could be discontinued with SASP. Tacrolimus 41-51 aspartic peptidase retroviral like 1 Homo sapiens 79-83 27518575-4 2016 Tacrolimus and Everolimus exerted potent antiproliferative properties in Huh 7 and Hep3B in which cells Sirolimus was inactive. Tacrolimus 0-10 MIR7-3 host gene Homo sapiens 73-78 27503662-1 2016 BACKGROUND The aim of the present study was to investigate the pharmacokinetics of the once-daily tacrolimus formulation (QD form) in relation to polymorphisms of the donor cytochrome P450 family 3 sub-family A polypeptide 5 (CYP3A5) gene and recipient adenosine triphosphate-binding cassette sub-family B member 1 (ABCB1) gene. Tacrolimus 98-108 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 173-224 27503662-1 2016 BACKGROUND The aim of the present study was to investigate the pharmacokinetics of the once-daily tacrolimus formulation (QD form) in relation to polymorphisms of the donor cytochrome P450 family 3 sub-family A polypeptide 5 (CYP3A5) gene and recipient adenosine triphosphate-binding cassette sub-family B member 1 (ABCB1) gene. Tacrolimus 98-108 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 226-232 27503662-1 2016 BACKGROUND The aim of the present study was to investigate the pharmacokinetics of the once-daily tacrolimus formulation (QD form) in relation to polymorphisms of the donor cytochrome P450 family 3 sub-family A polypeptide 5 (CYP3A5) gene and recipient adenosine triphosphate-binding cassette sub-family B member 1 (ABCB1) gene. Tacrolimus 98-108 ATP binding cassette subfamily B member 1 Homo sapiens 253-314 27503662-1 2016 BACKGROUND The aim of the present study was to investigate the pharmacokinetics of the once-daily tacrolimus formulation (QD form) in relation to polymorphisms of the donor cytochrome P450 family 3 sub-family A polypeptide 5 (CYP3A5) gene and recipient adenosine triphosphate-binding cassette sub-family B member 1 (ABCB1) gene. Tacrolimus 98-108 ATP binding cassette subfamily B member 1 Homo sapiens 316-321 27501378-9 2016 The administration of liposomal FK506 markedly suppressed the expression of cytokines, such as interferon-gamma and tumor necrosis factor-alpha, and reduced inflammation and fibrosis in the myocardium on day 21 compared to free FK506. Tacrolimus 32-37 interferon gamma Rattus norvegicus 95-143 27314545-2 2016 We sought to determine the singular and combined impact of CYP3A4*22 and CYP3A5*3 variants on tacrolimus drug disposition in adult heart transplant recipients. Tacrolimus 94-104 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 73-79 27314545-7 2016 However, tacrolimus C0 /D was 1.8-fold lower (P<.001) in CYP3A5 expressers vs non-expressers. Tacrolimus 9-19 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 60-66 27314545-8 2016 When combined CYP3A genotypes were evaluated, tacrolimus C0 /D was 1.8-fold lower in EMs vs IMs (P<.001) and EMs vs PMs (P=.001). Tacrolimus 46-56 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-19 27314545-10 2016 CONCLUSION: Combined CYP3A genotype was associated with tacrolimus drug disposition in adult heart transplant recipients, but the effect was largely driven by CYP3A5*3. Tacrolimus 56-66 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 21-26 27314545-10 2016 CONCLUSION: Combined CYP3A genotype was associated with tacrolimus drug disposition in adult heart transplant recipients, but the effect was largely driven by CYP3A5*3. Tacrolimus 56-66 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 159-165