PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 30912163-0 2019 Perpetrator effects of ciclosporin (P-glycoprotein inhibitor) and its combination with fluconazole (CYP3A inhibitor) on the pharmacokinetics of rivaroxaban in healthy volunteers. Cyclosporine 23-34 ATP binding cassette subfamily B member 1 Homo sapiens 36-50 30912163-2 2019 The aim of the present study was to investigate the effects of the potent P-gp inhibitor ciclosporin and its combination with the moderate CYP3A inhibitor fluconazole on rivaroxaban pharmacokinetics and on CYP3A activity. Cyclosporine 89-100 ATP binding cassette subfamily B member 1 Homo sapiens 74-78 31261526-6 2019 MDR1 C3435T CC was also associated with CNI use, especially with CsA therapy. Cyclosporine 65-68 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 30109442-8 2018 The apparent permeability of the fluorescent P-gp substrate rhodamine 123 was decreased by 35% by co-incubation with cyclosporin A. Cyclosporine 117-130 ATP binding cassette subfamily B member 1 Homo sapiens 45-49 31156436-2 2019 Metabolized mainly by CYP3A and being a substrate of P-glycoprotein (P-gp), CsA is susceptible to drug-drug interactions. Cyclosporine 76-79 ATP binding cassette subfamily B member 1 Homo sapiens 53-67 31156436-2 2019 Metabolized mainly by CYP3A and being a substrate of P-glycoprotein (P-gp), CsA is susceptible to drug-drug interactions. Cyclosporine 76-79 ATP binding cassette subfamily B member 1 Homo sapiens 69-73 30690767-0 2019 Relationship between allograft cyclosporin concentrations and P-glycoprotein expression in the 1st month following renal transplantation. Cyclosporine 31-42 ATP binding cassette subfamily B member 1 Homo sapiens 62-76 30690767-1 2019 The immunosuppressant cyclosporin is a P-glycoprotein (P-gp) substrate whose impaired function has been associated with an increased risk of cyclosporin-induced nephrotoxicity following renal transplantation. Cyclosporine 22-33 ATP binding cassette subfamily B member 1 Homo sapiens 39-53 30690767-1 2019 The immunosuppressant cyclosporin is a P-glycoprotein (P-gp) substrate whose impaired function has been associated with an increased risk of cyclosporin-induced nephrotoxicity following renal transplantation. Cyclosporine 22-33 ATP binding cassette subfamily B member 1 Homo sapiens 55-59 30690767-1 2019 The immunosuppressant cyclosporin is a P-glycoprotein (P-gp) substrate whose impaired function has been associated with an increased risk of cyclosporin-induced nephrotoxicity following renal transplantation. Cyclosporine 141-152 ATP binding cassette subfamily B member 1 Homo sapiens 39-53 30690767-1 2019 The immunosuppressant cyclosporin is a P-glycoprotein (P-gp) substrate whose impaired function has been associated with an increased risk of cyclosporin-induced nephrotoxicity following renal transplantation. Cyclosporine 141-152 ATP binding cassette subfamily B member 1 Homo sapiens 55-59 30799432-4 2019 The aim of this study was to determine the relationship between CYP3A4*1B and MDR1 polymorphisms and dose requirements to achieve the target therapeutic range for CsA. Cyclosporine 163-166 ATP binding cassette subfamily B member 1 Homo sapiens 78-82 30799432-8 2019 In the case of MDR1 3435C>T polymorphism, we observed that patients with the CC genotype received lower doses of CsA than patients with the CT and TT genotypes. Cyclosporine 116-119 ATP binding cassette subfamily B member 1 Homo sapiens 15-19 29352737-7 2018 The addition of 2 5 ng/ml cyclosporin A and 1 microM prednisolone inhibit IFN-gamma/TNF-alpha production significantly by CD8+ Pgp+ T cells from BOS patients. Cyclosporine 26-39 ATP binding cassette subfamily B member 1 Homo sapiens 127-130 29222397-9 2018 These findings suggest that increased activity of P-gp could be responsible for increased hepatic cyclosporin clearance. Cyclosporine 98-109 ATP binding cassette subfamily B member 1 Homo sapiens 50-54 29623717-4 2018 The results show a multifactorial origin of thrombocytopenia and a possible effect on refractivity to cyclosporine A therapy caused by long-term smoking, MDR-1 gene polymorphism, genetic predisposition to autoimmune diseases, allergic reactions as a manifestation of hypersensitivity in the immune system, controversial compliance of the patient, overcome infections as well as impact of drugs taken.Key words: immune thrombocytopenia refractery form cyclosporine A therapy platelets. Cyclosporine 102-116 ATP binding cassette subfamily B member 1 Homo sapiens 154-159 28164520-3 2016 METHODS: The genotype distribution of ABCB1 1236C>T, 2677G>T/A and 3435C>T was investigated among 96 Austrian KTR who were converted from cyclosporin to TAC. Cyclosporine 147-158 ATP binding cassette subfamily B member 1 Homo sapiens 38-43 28214069-4 2017 Immunosuppressive agents, such as calcineurin inhibitors (tacrolimus, cyclosporine) are substrates of cytochromes P450 3A4 and P-gp. Cyclosporine 70-82 ATP binding cassette subfamily B member 1 Homo sapiens 127-131 28739698-12 2017 CONCLUSION: These results suggest that highly HAL-resistant cancer cells can be sensitized with cyclosporine A or elacridar, specific P-gp inhibitors that exert their effects at a low dose. Cyclosporine 96-110 ATP binding cassette subfamily B member 1 Homo sapiens 134-138 28739760-4 2017 Its mechanism is not completely clear, but the hypothesis of CsA inhibiting P-glycoprotein mediated drug efflux is the most acceptable. Cyclosporine 61-64 ATP binding cassette subfamily B member 1 Homo sapiens 76-90 28623111-6 2017 Among the well-known ABCB1 inhibitors, a similar effect was found for cyclosporin A (CsA) but not for zosuquidar. Cyclosporine 85-88 ATP binding cassette subfamily B member 1 Homo sapiens 21-26 28736004-2 2017 However, the effect of TGF-beta1 and MDR1 gene polymorphisms on the pathogenesis of CsA-induced GO remains to be determined. Cyclosporine 84-87 ATP binding cassette subfamily B member 1 Homo sapiens 37-41 27283486-0 2016 Imaging the impact of cyclosporin A and dipyridamole on P-glycoprotein (ABCB1) function at the blood-brain barrier: A [(11)C]-N-desmethyl-loperamide PET study in nonhuman primates. Cyclosporine 22-35 ATP binding cassette subfamily B member 1 Homo sapiens 72-77 27283486-1 2016 Cyclosporin A (CsA) and dipyridamole (DPy) are potent inhibitors of the P-glycoprotein (P-gp; ABCB1) in vitro. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 72-86 27283486-1 2016 Cyclosporin A (CsA) and dipyridamole (DPy) are potent inhibitors of the P-glycoprotein (P-gp; ABCB1) in vitro. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 88-92 27283486-1 2016 Cyclosporin A (CsA) and dipyridamole (DPy) are potent inhibitors of the P-glycoprotein (P-gp; ABCB1) in vitro. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 94-99 29568367-4 2018 Sensitivity was completely restored with specific inhibitors cyclosporine (ABCB1) and Ko143 (ABCG2): K562-Dox LD50asciminib+cyclosporine = 13 nM, K562-ABCG2 LD50asciminib+Ko143 = 15 nM (p < 0.001). Cyclosporine 61-73 ATP binding cassette subfamily B member 1 Homo sapiens 75-80 29381954-0 2017 Effect of MDR1 C1236T polymorphism on cyclosporine pharmacokinetics: A systematic review and meta-analysis. Cyclosporine 38-50 ATP binding cassette subfamily B member 1 Homo sapiens 10-14 29381954-2 2017 The published data reveal conflicting effects of the polymorphism of MDR1 exon 12 SNP C1236T on the pharmacokinetics of cyclosporine.This study aims to conduct a meta-analysis to investigate the effect of SNP C1236T on the pharmacokinetics of cyclosporine. Cyclosporine 120-132 ATP binding cassette subfamily B member 1 Homo sapiens 69-73 29381954-2 2017 The published data reveal conflicting effects of the polymorphism of MDR1 exon 12 SNP C1236T on the pharmacokinetics of cyclosporine.This study aims to conduct a meta-analysis to investigate the effect of SNP C1236T on the pharmacokinetics of cyclosporine. Cyclosporine 243-255 ATP binding cassette subfamily B member 1 Homo sapiens 69-73 29381954-9 2017 CONCLUSIONS: MDR1 C1236T polymorphism may have a minor effect on cyclosporine pharmacokinetics in transplantation patients. Cyclosporine 65-77 ATP binding cassette subfamily B member 1 Homo sapiens 13-17 28952408-0 2017 Influence of CYP3A and ABCB1 polymorphisms on cyclosporine concentrations in renal transplant recipients. Cyclosporine 46-58 ATP binding cassette subfamily B member 1 Homo sapiens 23-28 28952408-1 2017 AIM: Cyclosporine is a substrate of CYP3A and ABCB1. Cyclosporine 5-17 ATP binding cassette subfamily B member 1 Homo sapiens 46-51 27836711-4 2016 In type I-like cells, rhodamine 123 (Rho123) accumulation was enhanced by various P-gp inhibitors such as verapamil and cyclosporine A. Cyclosporine 120-134 ATP binding cassette subfamily B member 1 Homo sapiens 82-86 26618109-6 2015 However, the use of biological agents that reduce P-gp expression as well as P-gp antagonists (e.g., cyclosporine) can successfully reduce the efflux of corticosteroids from lymphocytes in vitro, suggesting that both types of drugs can be used to overcome drug-resistance and improve clinical outcome. Cyclosporine 101-113 ATP binding cassette subfamily B member 1 Homo sapiens 77-81 26353895-8 2016 Cyclosporine is an inhibitor of OATP1B1/3, BCRP and P-gp, and a mild inhibitor of CYP3A; cyclosporine causes a significant increase in simeprevir plasma concentrations, and coadministration is not recommended. Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 52-56 26563728-6 2016 Fluoromethyl compound [(18)F]-6 is classified as a non-transported P-gp substrate, because its efflux increases after cyclosporine A modulation. Cyclosporine 118-132 ATP binding cassette subfamily B member 1 Homo sapiens 67-71 26912097-6 2016 Cyclosporine disposition is less susceptible to these interactions compared with tacrolimus, possibly because cyclosporine is itself a moderately strong CYP3A4- and strong P-gp inhibitor, blunting the effect of additional inhibitors. Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 172-176 26912097-6 2016 Cyclosporine disposition is less susceptible to these interactions compared with tacrolimus, possibly because cyclosporine is itself a moderately strong CYP3A4- and strong P-gp inhibitor, blunting the effect of additional inhibitors. Cyclosporine 110-122 ATP binding cassette subfamily B member 1 Homo sapiens 172-176 27016408-6 2016 Concentration-dependent uptake of DLM in 0.01% HSA was non-linear and was reduced at 4 C and by the P-gp inhibitor cyclosporine (CSA), indicative of a specific transport process. Cyclosporine 115-127 ATP binding cassette subfamily B member 1 Homo sapiens 100-104 27016408-6 2016 Concentration-dependent uptake of DLM in 0.01% HSA was non-linear and was reduced at 4 C and by the P-gp inhibitor cyclosporine (CSA), indicative of a specific transport process. Cyclosporine 129-132 ATP binding cassette subfamily B member 1 Homo sapiens 100-104 27016408-7 2016 Cellular accumulation of [(3)H]-paclitaxel, a P-glycoprotein (P-gp) substrate, was increased by CSA but not by DLM, suggesting that DLM is neither a substrate nor an inhibitor of P-gp. Cyclosporine 96-99 ATP binding cassette subfamily B member 1 Homo sapiens 46-60 27016408-7 2016 Cellular accumulation of [(3)H]-paclitaxel, a P-glycoprotein (P-gp) substrate, was increased by CSA but not by DLM, suggesting that DLM is neither a substrate nor an inhibitor of P-gp. Cyclosporine 96-99 ATP binding cassette subfamily B member 1 Homo sapiens 62-66 26585254-2 2016 To evaluate the brain expression of p-glycoprotein in patients with drug-resistant epilepsy, including neocortical epilepsy, we developed a noninvsive quantitative analysis including asymmetry indices based on (R)-[(11)C]-verapamil PET/MR imaging with cyclosporin A, a p-glycoprotein inhibitor. Cyclosporine 252-265 ATP binding cassette subfamily B member 1 Homo sapiens 36-50 27374283-1 2016 Cyclosporine (CSA), which is one of the substrates of ATP binding cassette subfamily B member 1 (ABCB1), is widely used as an immunosuppressant in patients undergoing transplantation. Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 54-95 27374283-1 2016 Cyclosporine (CSA), which is one of the substrates of ATP binding cassette subfamily B member 1 (ABCB1), is widely used as an immunosuppressant in patients undergoing transplantation. Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 97-102 25536375-0 2015 The Effect of ABCB1 C3435T Polymorphism on Cyclosporine Dose Requirements in Kidney Transplant Recipients: A Meta-Analysis. Cyclosporine 43-55 ATP binding cassette subfamily B member 1 Homo sapiens 14-19 27022464-2 2015 Specifically, acute administration of P-gp inhibitors, such as verapamil and cyclosporin A (CsA), has been shown to augment brain concentrations and functional activity of the antidepressant escitalopram in rodents. Cyclosporine 77-90 ATP binding cassette subfamily B member 1 Homo sapiens 38-42 27022464-2 2015 Specifically, acute administration of P-gp inhibitors, such as verapamil and cyclosporin A (CsA), has been shown to augment brain concentrations and functional activity of the antidepressant escitalopram in rodents. Cyclosporine 92-95 ATP binding cassette subfamily B member 1 Homo sapiens 38-42 26153782-9 2015 The efflux was inhibited by treatment with a P-gp inhibitor, cyclosporine A (CsA). Cyclosporine 61-75 ATP binding cassette subfamily B member 1 Homo sapiens 45-49 26153782-9 2015 The efflux was inhibited by treatment with a P-gp inhibitor, cyclosporine A (CsA). Cyclosporine 77-80 ATP binding cassette subfamily B member 1 Homo sapiens 45-49 26153782-12 2015 Inhibition and knock down of P-gp by CsA and siRNA, respectively, enhanced etoposide- and doxorubicin-induced cell death in the EBV-positive T-cell lines. Cyclosporine 37-40 ATP binding cassette subfamily B member 1 Homo sapiens 29-33 25536375-1 2015 Cyclosporine A (CsA) is a substrate of the multi-drug efflux pump P-glycoprotein (P-gp) encoded by ABCB1. Cyclosporine 0-14 ATP binding cassette subfamily B member 1 Homo sapiens 66-80 25536375-1 2015 Cyclosporine A (CsA) is a substrate of the multi-drug efflux pump P-glycoprotein (P-gp) encoded by ABCB1. Cyclosporine 0-14 ATP binding cassette subfamily B member 1 Homo sapiens 82-86 25536375-1 2015 Cyclosporine A (CsA) is a substrate of the multi-drug efflux pump P-glycoprotein (P-gp) encoded by ABCB1. Cyclosporine 0-14 ATP binding cassette subfamily B member 1 Homo sapiens 99-104 25536375-1 2015 Cyclosporine A (CsA) is a substrate of the multi-drug efflux pump P-glycoprotein (P-gp) encoded by ABCB1. Cyclosporine 16-19 ATP binding cassette subfamily B member 1 Homo sapiens 66-80 25536375-1 2015 Cyclosporine A (CsA) is a substrate of the multi-drug efflux pump P-glycoprotein (P-gp) encoded by ABCB1. Cyclosporine 16-19 ATP binding cassette subfamily B member 1 Homo sapiens 82-86 25536375-1 2015 Cyclosporine A (CsA) is a substrate of the multi-drug efflux pump P-glycoprotein (P-gp) encoded by ABCB1. Cyclosporine 16-19 ATP binding cassette subfamily B member 1 Homo sapiens 99-104 25536375-2 2015 Among the various single nucleotide polymorphisms (SNPs) of ABCB1, C3435T has been extensively investigated to determine the relationship with the pharmacokinetics of CsA. Cyclosporine 167-170 ATP binding cassette subfamily B member 1 Homo sapiens 60-65 25536375-9 2015 Therefore, this meta-analysis showed a correlation between ABCB1 C3435T polymorphism and the dose-adjusted concentration of CsA. Cyclosporine 124-127 ATP binding cassette subfamily B member 1 Homo sapiens 59-64 25857708-9 2015 Pgp(+) cells exhibited very low R123 and (18)FRB accumulation (around 1-8% of the Pgp(-) cell lines) which was not sensitive to the mitochondrial proton gradient; rather it was increased by the Pgp inhibitor cyclosporine A (CsA). Cyclosporine 208-222 ATP binding cassette subfamily B member 1 Homo sapiens 0-3 25857708-9 2015 Pgp(+) cells exhibited very low R123 and (18)FRB accumulation (around 1-8% of the Pgp(-) cell lines) which was not sensitive to the mitochondrial proton gradient; rather it was increased by the Pgp inhibitor cyclosporine A (CsA). Cyclosporine 224-227 ATP binding cassette subfamily B member 1 Homo sapiens 0-3 25240575-0 2015 Impact of CYP3A4 and MDR1 gene (G2677T) polymorphisms on dose requirement of the cyclosporine in renal transplant Egyptian recipients. Cyclosporine 81-93 ATP binding cassette subfamily B member 1 Homo sapiens 21-25 26004871-10 2015 Cell surface Gb3 expression of resistant cells was annihilated by PPMP whereas cyclosporin A decreased Gb3 and MDR1 expression in H1299 cells. Cyclosporine 79-92 ATP binding cassette subfamily B member 1 Homo sapiens 111-115 25891084-0 2015 Diltiazem augments the influence of MDR1 genotype status on cyclosporine concentration in Chinese patients with renal transplantation. Cyclosporine 60-72 ATP binding cassette subfamily B member 1 Homo sapiens 36-40 25891084-2 2015 In this study, we investigated how diltiazem altered the relationship between MDR1 genetic polymorphisms and CsA concentration in Chinese patients with renal transplantation. Cyclosporine 109-112 ATP binding cassette subfamily B member 1 Homo sapiens 78-82 25891084-8 2015 With regard to MDR1-3435, the adjusted CsA trough concentration was significantly higher in TT carriers than in CC and CT carriers when diltiazam was co-administered (58.83+-13.95 versus 46.14+-7.55 and 45.18+-12.35 ng/mL per mg/kg, P=0.011), and the differences were not observed in patients without diltiazam co-administered. Cyclosporine 39-42 ATP binding cassette subfamily B member 1 Homo sapiens 15-19 25891084-9 2015 With regard to MDR1-2677, the adjusted CsA trough concentration was significantly higher in TT carriers than in GG and GT carriers when diltiazam was co-administered (61.31+-12.93 versus 52.25+-7.83 and 39.70+-7.26 ng/mL per mg/kg, P=0.0001). Cyclosporine 39-42 ATP binding cassette subfamily B member 1 Homo sapiens 15-19 25891084-12 2015 CONCLUSION: MDR1 variants influence the adjusted CsA trough concentration in Chinese patients with renal transplant, and the influence more prominent when diltiazem is co-administered. Cyclosporine 49-52 ATP binding cassette subfamily B member 1 Homo sapiens 12-16 25673014-2 2015 The donor ABCB1 polymorphisms have been related with chronic histological damage and long-term renal function among kidney transplanted patients who received cyclosporine A and tacrolimus (Tac). Cyclosporine 158-172 ATP binding cassette subfamily B member 1 Homo sapiens 10-15 25407255-2 2015 Canagliflozin exposures may be affected by coadministration of drugs that induce (e.g., rifampin for UGT) or inhibit (e.g. probenecid for UGT; cyclosporine A for P-gp) these pathways. Cyclosporine 143-157 ATP binding cassette subfamily B member 1 Homo sapiens 162-166 25240575-6 2015 Interindividual heterogeneity in expression of ABCB1 and CYP3A4 has been suspected to be one of the factors resulting in cyclosporine (CsA) pharmacokinetic variation. Cyclosporine 121-133 ATP binding cassette subfamily B member 1 Homo sapiens 47-52 25240575-6 2015 Interindividual heterogeneity in expression of ABCB1 and CYP3A4 has been suspected to be one of the factors resulting in cyclosporine (CsA) pharmacokinetic variation. Cyclosporine 135-138 ATP binding cassette subfamily B member 1 Homo sapiens 47-52 25240575-7 2015 This study aimed to investigate the impact of inter-individual CYP3A4 rs4646437C>T and MDR1 G2677T/A polymorphisms on cyclosporine dose requirements among a sample of renal transplant Egyptian recipients. Cyclosporine 121-133 ATP binding cassette subfamily B member 1 Homo sapiens 90-94 25240575-8 2015 Fifty adult Egyptian patients on CsA were genotyped for CYP3A4 rs4646437C>T and MDR1 G2677T/A and correlated with CsA dose requirement and dose-adjusted CsA (C0) blood levels at 3, 6, and 9 months post transplantation. Cyclosporine 117-120 ATP binding cassette subfamily B member 1 Homo sapiens 83-87 25240575-8 2015 Fifty adult Egyptian patients on CsA were genotyped for CYP3A4 rs4646437C>T and MDR1 G2677T/A and correlated with CsA dose requirement and dose-adjusted CsA (C0) blood levels at 3, 6, and 9 months post transplantation. Cyclosporine 117-120 ATP binding cassette subfamily B member 1 Homo sapiens 83-87 25240575-11 2015 Genotyping of both CYP3A4 and MDR1 SNPs may be helpful in providing pre-transplant pharmacogenetic information to individualize CsA dosing. Cyclosporine 128-131 ATP binding cassette subfamily B member 1 Homo sapiens 30-34 26107754-3 2015 RESULTS: The presence of serious infections was correlated to ABCB1 rs1128503 (p = 0.012), CC genotype reduced the probability of infections being also associated with lower blood cyclosporine concentrations. Cyclosporine 180-192 ATP binding cassette subfamily B member 1 Homo sapiens 62-67 25456855-10 2014 Tariquidar was also a more potent pharmacological chaperone than other P-gp substrates/modulators such as cyclosporine A. Cyclosporine 106-120 ATP binding cassette subfamily B member 1 Homo sapiens 71-75 24739669-3 2014 We thus assessed the role of genetic variation in CYP3A4, CYP3A5, POR, NR1I2, and ABCB1 acting jointly in immunosuppressive drug pathways in tacrolimus (TAC) and ciclosporin (CSA) dose requirement in HTx recipients. Cyclosporine 162-173 ATP binding cassette subfamily B member 1 Homo sapiens 82-87 24120885-5 2013 Additionally, the P-gp inhibitors, verapamil and cyclosporin A, significantly decreased the efflux of AC. Cyclosporine 49-62 ATP binding cassette subfamily B member 1 Homo sapiens 18-22 24889923-4 2014 The aim of the present study was to assess the ABCB1 T-129C, G1199A, C1236T, G2677T and C3435T single-nucleotide polymorphisms (SNPs) as candidate predictive markers of response to cyclosporine treatment in 84 psoriasis patients. Cyclosporine 181-193 ATP binding cassette subfamily B member 1 Homo sapiens 47-52 25238617-4 2014 The combined addition of UIC2 and 10 times lower concentrations of CsA than what is necessary for Pgp inhibition when the modulator is applied alone, decreased the EC50 of doxorubicin (DOX) in KB-V1 (Pgp+) cells in vitro almost to the level of KB-3-1 (Pgp-) cells. Cyclosporine 67-70 ATP binding cassette subfamily B member 1 Homo sapiens 98-101 25238617-4 2014 The combined addition of UIC2 and 10 times lower concentrations of CsA than what is necessary for Pgp inhibition when the modulator is applied alone, decreased the EC50 of doxorubicin (DOX) in KB-V1 (Pgp+) cells in vitro almost to the level of KB-3-1 (Pgp-) cells. Cyclosporine 67-70 ATP binding cassette subfamily B member 1 Homo sapiens 200-203 25238617-4 2014 The combined addition of UIC2 and 10 times lower concentrations of CsA than what is necessary for Pgp inhibition when the modulator is applied alone, decreased the EC50 of doxorubicin (DOX) in KB-V1 (Pgp+) cells in vitro almost to the level of KB-3-1 (Pgp-) cells. Cyclosporine 67-70 ATP binding cassette subfamily B member 1 Homo sapiens 200-203 24903378-9 2014 In addition, chloroform extract had the ability to inhibit human P-glycoprotein-mediated daunorubicin in K562/R7 leukaemic cells in a dose-dependent manner compared to the positive control, cyclosporin A. Cyclosporine 190-203 ATP binding cassette subfamily B member 1 Homo sapiens 65-79 24641346-4 2014 Accumulation decreased in spheroids overexpressing Pgp (HEK-MDR) and was increased in the presence of Pgp inhibitors (verapamil, loperamide, cyclosporin A). Cyclosporine 141-154 ATP binding cassette subfamily B member 1 Homo sapiens 51-54 24641346-4 2014 Accumulation decreased in spheroids overexpressing Pgp (HEK-MDR) and was increased in the presence of Pgp inhibitors (verapamil, loperamide, cyclosporin A). Cyclosporine 141-154 ATP binding cassette subfamily B member 1 Homo sapiens 102-105 24219005-1 2014 INTRODUCTION: Previously, we demonstrated that oral docetaxel plus the P-glycoprotein (Pgp; ABCB1) inhibitor cyclosporin A (CsA) is safe and results in adequate exposure to docetaxel. Cyclosporine 124-127 ATP binding cassette subfamily B member 1 Homo sapiens 71-85 25242754-1 2014 BACKGROUND: The single-nucleotide polymorphisms (SNPs) of the Multidrug resistance 1 (MDR1) gene have been associated with changes in the pharmacokinetics of cyclosporine (CsA) and tacrolimus (FK506). Cyclosporine 158-170 ATP binding cassette subfamily B member 1 Homo sapiens 62-84 25242754-1 2014 BACKGROUND: The single-nucleotide polymorphisms (SNPs) of the Multidrug resistance 1 (MDR1) gene have been associated with changes in the pharmacokinetics of cyclosporine (CsA) and tacrolimus (FK506). Cyclosporine 158-170 ATP binding cassette subfamily B member 1 Homo sapiens 86-90 25242754-1 2014 BACKGROUND: The single-nucleotide polymorphisms (SNPs) of the Multidrug resistance 1 (MDR1) gene have been associated with changes in the pharmacokinetics of cyclosporine (CsA) and tacrolimus (FK506). Cyclosporine 172-175 ATP binding cassette subfamily B member 1 Homo sapiens 62-84 25242754-1 2014 BACKGROUND: The single-nucleotide polymorphisms (SNPs) of the Multidrug resistance 1 (MDR1) gene have been associated with changes in the pharmacokinetics of cyclosporine (CsA) and tacrolimus (FK506). Cyclosporine 172-175 ATP binding cassette subfamily B member 1 Homo sapiens 86-90 25242754-8 2014 CONCLUSIONS: Pretransplantation determination of MDR1 SNPs may be helpful to optimize the starting dose of CsA but can not predict long-term graft survival. Cyclosporine 107-110 ATP binding cassette subfamily B member 1 Homo sapiens 49-53 24219005-1 2014 INTRODUCTION: Previously, we demonstrated that oral docetaxel plus the P-glycoprotein (Pgp; ABCB1) inhibitor cyclosporin A (CsA) is safe and results in adequate exposure to docetaxel. Cyclosporine 124-127 ATP binding cassette subfamily B member 1 Homo sapiens 87-90 24219005-1 2014 INTRODUCTION: Previously, we demonstrated that oral docetaxel plus the P-glycoprotein (Pgp; ABCB1) inhibitor cyclosporin A (CsA) is safe and results in adequate exposure to docetaxel. Cyclosporine 124-127 ATP binding cassette subfamily B member 1 Homo sapiens 92-97 24658440-5 2014 Recently, different authors have demonstrated that P-gp inhibitors, such as cyclosporine A (CsA) and its analogue Tacrolimus, are able to reduce P-gp expression and or function in SLE, RA and PsA patients. Cyclosporine 76-90 ATP binding cassette subfamily B member 1 Homo sapiens 51-55 24658440-5 2014 Recently, different authors have demonstrated that P-gp inhibitors, such as cyclosporine A (CsA) and its analogue Tacrolimus, are able to reduce P-gp expression and or function in SLE, RA and PsA patients. Cyclosporine 76-90 ATP binding cassette subfamily B member 1 Homo sapiens 145-149 24658440-5 2014 Recently, different authors have demonstrated that P-gp inhibitors, such as cyclosporine A (CsA) and its analogue Tacrolimus, are able to reduce P-gp expression and or function in SLE, RA and PsA patients. Cyclosporine 92-95 ATP binding cassette subfamily B member 1 Homo sapiens 51-55 24658440-5 2014 Recently, different authors have demonstrated that P-gp inhibitors, such as cyclosporine A (CsA) and its analogue Tacrolimus, are able to reduce P-gp expression and or function in SLE, RA and PsA patients. Cyclosporine 92-95 ATP binding cassette subfamily B member 1 Homo sapiens 145-149 24621983-1 2014 OBJECTIVE: ATP-binding cassette, subfamily B, member 1 (ABCB1) transporter, or P-glycoprotein, is an efflux protein implicated in the absorption and the distribution of various compounds, including tacrolimus and cyclosporine A. Cyclosporine 213-227 ATP binding cassette subfamily B member 1 Homo sapiens 11-54 24621983-1 2014 OBJECTIVE: ATP-binding cassette, subfamily B, member 1 (ABCB1) transporter, or P-glycoprotein, is an efflux protein implicated in the absorption and the distribution of various compounds, including tacrolimus and cyclosporine A. Cyclosporine 213-227 ATP binding cassette subfamily B member 1 Homo sapiens 56-61 24621983-1 2014 OBJECTIVE: ATP-binding cassette, subfamily B, member 1 (ABCB1) transporter, or P-glycoprotein, is an efflux protein implicated in the absorption and the distribution of various compounds, including tacrolimus and cyclosporine A. Cyclosporine 213-227 ATP binding cassette subfamily B member 1 Homo sapiens 79-93 24621983-5 2014 The impact of the 1199G>A SNP on ABCB1 activity towards rhodamine (Rh123), doxorubicin, vinblastine, tacrolimus and cyclosporine A was assessed by accumulation, cytotoxicity and/or kinetic experiments. Cyclosporine 119-133 ATP binding cassette subfamily B member 1 Homo sapiens 36-41 24621983-8 2014 Unlike tacrolimus, our results also indicate that cyclosporine A, Rh123 and doxorubicin are transported in a similar extent by the wild-type and variant ABCB1 proteins while the variant protein seems to be more efficient for the transport of vinblastine. Cyclosporine 50-64 ATP binding cassette subfamily B member 1 Homo sapiens 153-158 24364805-1 2014 Using positron emission tomography (PET), (11)C-verapamil as the P-gp substrate, and cyclosporine A (CsA) as the P-gp inhibitor, we showed that the magnitude of P-gp-based drug interactions at the human blood-brain barrier (BBB) is modest. Cyclosporine 101-104 ATP binding cassette subfamily B member 1 Homo sapiens 113-117 24364805-1 2014 Using positron emission tomography (PET), (11)C-verapamil as the P-gp substrate, and cyclosporine A (CsA) as the P-gp inhibitor, we showed that the magnitude of P-gp-based drug interactions at the human blood-brain barrier (BBB) is modest. Cyclosporine 101-104 ATP binding cassette subfamily B member 1 Homo sapiens 113-117 24364805-2 2014 However, such interactions at clinically relevant CsA blood concentrations may be greater for substrates where P-gp plays an even larger role (fractional contribution of P-gp, ft > 0.97) in preventing the CNS entry of the drug (e.g., nelfinavir). Cyclosporine 50-53 ATP binding cassette subfamily B member 1 Homo sapiens 111-115 24364805-6 2014 Then, using these data, as well as in vitro data in LLCPK1 cells expressing the human P-gp, we predicted that CsA (at clinically relevant blood concentration of 1.5 muM) will increase the distribution of nelfinavir into the human brain by 236%. Cyclosporine 110-113 ATP binding cassette subfamily B member 1 Homo sapiens 86-90 24212378-4 2014 From a set of potential P-gp inhibitors, clarithromycin, cyclosporin A, itraconazole, ketoconazole, quinidine, and ritonavir inhibited P-gp-mediated transport of dabigatran etexilate over a concentration range that may hypothetically occur in the intestine. Cyclosporine 57-70 ATP binding cassette subfamily B member 1 Homo sapiens 24-28 24212378-4 2014 From a set of potential P-gp inhibitors, clarithromycin, cyclosporin A, itraconazole, ketoconazole, quinidine, and ritonavir inhibited P-gp-mediated transport of dabigatran etexilate over a concentration range that may hypothetically occur in the intestine. Cyclosporine 57-70 ATP binding cassette subfamily B member 1 Homo sapiens 135-139 24596624-7 2014 [(3)H]Paclitaxel uptake was markedly inhibited by cyclosporine and verapamil, well-known substrates of P-glycoprotein (P-gp) transporter. Cyclosporine 50-62 ATP binding cassette subfamily B member 1 Homo sapiens 103-117 24596624-7 2014 [(3)H]Paclitaxel uptake was markedly inhibited by cyclosporine and verapamil, well-known substrates of P-glycoprotein (P-gp) transporter. Cyclosporine 50-62 ATP binding cassette subfamily B member 1 Homo sapiens 119-123 24527031-3 2014 Cytochrome P-450 isoenzymes CYP3A4 and CYP3A5 and protein P-glycoprotein (P-gp) are involved in CyA bioavailability. Cyclosporine 96-99 ATP binding cassette subfamily B member 1 Homo sapiens 58-72 24527031-3 2014 Cytochrome P-450 isoenzymes CYP3A4 and CYP3A5 and protein P-glycoprotein (P-gp) are involved in CyA bioavailability. Cyclosporine 96-99 ATP binding cassette subfamily B member 1 Homo sapiens 74-78 23908147-1 2013 Cyclosporine exhibits pharmacokinetic and pharmacodynamic variability in renal transplant recipients (RTR) attributed to P-glycoprotein (P-gp), an ABCB1 efflux transporter that influences bioavailability and intracellular distribution. Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 121-135 23851346-4 2013 METHODS: Fourteen healthy volunteers received morphine (0.1 mg/kg, 1-h IV infusion) in a crossover study without (control) or with the infusion of validated P-glycoprotein inhibitor cyclosporine (5 mg/kg, 2-h infusion). Cyclosporine 182-194 ATP binding cassette subfamily B member 1 Homo sapiens 157-171 24064216-0 2013 Mutations in intracellular loops 1 and 3 lead to misfolding of human P-glycoprotein (ABCB1) that can be rescued by cyclosporine A, which reduces its association with chaperone Hsp70. Cyclosporine 115-129 ATP binding cassette subfamily B member 1 Homo sapiens 69-83 24064216-0 2013 Mutations in intracellular loops 1 and 3 lead to misfolding of human P-glycoprotein (ABCB1) that can be rescued by cyclosporine A, which reduces its association with chaperone Hsp70. Cyclosporine 115-129 ATP binding cassette subfamily B member 1 Homo sapiens 85-90 24064216-7 2013 The intracellularly trapped misprocessed protein associates more with chaperone Hsp70, and the treatment with cyclosporine A reduces the association of mutant P-gp, thus allowing it to be trafficked to the cell surface. Cyclosporine 110-124 ATP binding cassette subfamily B member 1 Homo sapiens 159-163 23953030-3 2013 The canalicular transport of irinotecan and SN-38G is mediated by ABCC2 (MRP2) and ABCB1 (MDR1) which are both inhibited by ciclosporin. Cyclosporine 124-135 ATP binding cassette subfamily B member 1 Homo sapiens 83-88 23953030-3 2013 The canalicular transport of irinotecan and SN-38G is mediated by ABCC2 (MRP2) and ABCB1 (MDR1) which are both inhibited by ciclosporin. Cyclosporine 124-135 ATP binding cassette subfamily B member 1 Homo sapiens 90-94 23908147-1 2013 Cyclosporine exhibits pharmacokinetic and pharmacodynamic variability in renal transplant recipients (RTR) attributed to P-glycoprotein (P-gp), an ABCB1 efflux transporter that influences bioavailability and intracellular distribution. Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 137-141 23908147-1 2013 Cyclosporine exhibits pharmacokinetic and pharmacodynamic variability in renal transplant recipients (RTR) attributed to P-glycoprotein (P-gp), an ABCB1 efflux transporter that influences bioavailability and intracellular distribution. Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 147-152 23908147-5 2013 ABCB1 gene expression was assessed in PBMCs pre-dose and 4 hours after cyclosporine. Cyclosporine 71-83 ATP binding cassette subfamily B member 1 Homo sapiens 0-5 23503472-6 2013 RESULTS: The dose-adjusted trough concentration (C0) of cyclosporine in ABCB1 2677 TT carriers was significantly higher than that in GG carriers together with GT carriers [90.4+-24.5 vs 67.8+-26.8 (ng/mL)/(mg/kg), P=0.001]. Cyclosporine 56-68 ATP binding cassette subfamily B member 1 Homo sapiens 72-77 23720091-0 2013 Functional G1199A ABCB1 polymorphism may have an effect on cyclosporine blood concentration in renal transplanted patients. Cyclosporine 59-71 ATP binding cassette subfamily B member 1 Homo sapiens 18-23 23720091-1 2013 Cyclosporine A (CsA) shows significant inter-individual variability in its pharmacokinetics, which may be due to polymorphisms in ABCB-1 genes coding for P-glycoprotein. Cyclosporine 0-14 ATP binding cassette subfamily B member 1 Homo sapiens 130-136 23720091-1 2013 Cyclosporine A (CsA) shows significant inter-individual variability in its pharmacokinetics, which may be due to polymorphisms in ABCB-1 genes coding for P-glycoprotein. Cyclosporine 0-14 ATP binding cassette subfamily B member 1 Homo sapiens 154-168 23720091-1 2013 Cyclosporine A (CsA) shows significant inter-individual variability in its pharmacokinetics, which may be due to polymorphisms in ABCB-1 genes coding for P-glycoprotein. Cyclosporine 16-19 ATP binding cassette subfamily B member 1 Homo sapiens 130-136 23720091-1 2013 Cyclosporine A (CsA) shows significant inter-individual variability in its pharmacokinetics, which may be due to polymorphisms in ABCB-1 genes coding for P-glycoprotein. Cyclosporine 16-19 ATP binding cassette subfamily B member 1 Homo sapiens 154-168 23720091-6 2013 Polymorphisms of ABCB-1 have only a minor effect on CsA blood concentrations. Cyclosporine 52-55 ATP binding cassette subfamily B member 1 Homo sapiens 17-23 23353700-6 2013 The addition of either tamoxifen, VX-710, verapamil, or cyclosporin A, antagonists of P-gp, enhanced C6-ceramide cytotoxicity in all cell lines. Cyclosporine 56-69 ATP binding cassette subfamily B member 1 Homo sapiens 86-90 24088131-7 2013 CONCLUSION: The presence of specific ABCB1 and SXR SNPs could significantly affect cyclosporine exposure during a kidney transplant patient"s development from childhood to adulthood in a time-dependent fashion. Cyclosporine 83-95 ATP binding cassette subfamily B member 1 Homo sapiens 37-42 23562926-8 2013 Cyclosporin A and verapamil, both inhibitors of P-glycoprotein (P-gp), significantly decreased the efflux of AC. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 48-62 23562926-8 2013 Cyclosporin A and verapamil, both inhibitors of P-glycoprotein (P-gp), significantly decreased the efflux of AC. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 64-68 23756537-1 2013 OBJECTIVE: To investigate the occurrence of MDR1 C3435T gene polymorphisms in the Turkish renal transplant patients treated with cyclosporine (CsA), and correlate these findings with prevalence and degree of gingival hyperplasia (GH). Cyclosporine 129-141 ATP binding cassette subfamily B member 1 Homo sapiens 44-48 23756537-1 2013 OBJECTIVE: To investigate the occurrence of MDR1 C3435T gene polymorphisms in the Turkish renal transplant patients treated with cyclosporine (CsA), and correlate these findings with prevalence and degree of gingival hyperplasia (GH). Cyclosporine 143-146 ATP binding cassette subfamily B member 1 Homo sapiens 44-48 23731729-5 2013 We further hypothesized that treatment with cyclosporine A, a Pgp1 inhibitor, would render cells more sensitive to treatment with corticosteroids. Cyclosporine 44-58 ATP binding cassette subfamily B member 1 Homo sapiens 62-66 23593196-6 2013 Validation of the assay was performed with known ABCB1 inhibitors, XR9576, verapamil, and cyclosporin A, all of which displayed dose-dependent inhibition of ABCB1-mediated calcein AM efflux in this assay. Cyclosporine 90-103 ATP binding cassette subfamily B member 1 Homo sapiens 157-162 23593196-13 2013 Inhibition of ABCB1 with XR9576 and cyclosporin A enhanced the cytotoxicity of BI 2536 to ABCB1-overexpressing cancer cells, HCT-15-Pgp, and decreased the IC50 value of BI 2536 by several orders of magnitude. Cyclosporine 36-49 ATP binding cassette subfamily B member 1 Homo sapiens 90-95 23503472-7 2013 ABCB1 3435 TT carriers had a significantly higher dose-adjusted C0 of cyclosporine than CC carriers together with CT carriers [92.0+-24.0 vs 68.4+-26.5 (ng/mL)/(mg/kg), P=0.002]. Cyclosporine 70-82 ATP binding cassette subfamily B member 1 Homo sapiens 0-5 23503472-10 2013 CONCLUSION: These results illustrate that the ABCB1 and NFKB1 genotypes are closely correlated with cyclosporine trough concentrations, suggesting that these SNPs are useful for determining the appropriate dose of cyclosporine. Cyclosporine 100-112 ATP binding cassette subfamily B member 1 Homo sapiens 46-51 22886152-0 2013 ABCB1 polymorphisms are associated with cyclosporine-induced nephrotoxicity and gingival hyperplasia in renal transplant recipients. Cyclosporine 40-52 ATP binding cassette subfamily B member 1 Homo sapiens 0-5 22886152-5 2013 In terms of CsA-induced adverse effects, the incidence of nephrotoxicity was higher in carriers of the ABCB1 3435TT genotype and in those patients carrying four to six variants in the three ABCB1 loci [odds ratio (OR) 4.2, 95 % confidence interval (CI) 1.3-13.9, p = 0.02 and OR 3.6, 95 % CI 1.1-11.8, p = 0.05, respectively]. Cyclosporine 12-15 ATP binding cassette subfamily B member 1 Homo sapiens 103-108 22886152-5 2013 In terms of CsA-induced adverse effects, the incidence of nephrotoxicity was higher in carriers of the ABCB1 3435TT genotype and in those patients carrying four to six variants in the three ABCB1 loci [odds ratio (OR) 4.2, 95 % confidence interval (CI) 1.3-13.9, p = 0.02 and OR 3.6, 95 % CI 1.1-11.8, p = 0.05, respectively]. Cyclosporine 12-15 ATP binding cassette subfamily B member 1 Homo sapiens 190-195 22886152-8 2013 CONCLUSIONS: ABCB1 polymorphisms may be helpful in predicting certain CsA-related side effects in renal transplant recipients. Cyclosporine 70-73 ATP binding cassette subfamily B member 1 Homo sapiens 13-18 23216707-0 2013 Do drug transporter (ABCB1) SNPs and P-glycoprotein function influence cyclosporine and macrolides exposure in renal transplant patients? Cyclosporine 71-83 ATP binding cassette subfamily B member 1 Homo sapiens 21-26 23216707-8 2013 Pgp-high pumpers treated with cyclosporine showed lower values of Pgp function than macrolides. Cyclosporine 30-42 ATP binding cassette subfamily B member 1 Homo sapiens 0-3 23216707-8 2013 Pgp-high pumpers treated with cyclosporine showed lower values of Pgp function than macrolides. Cyclosporine 30-42 ATP binding cassette subfamily B member 1 Homo sapiens 66-69 23216707-12 2013 Pgp activity was influenced by cyclosporine but not macrolides exposure. Cyclosporine 31-43 ATP binding cassette subfamily B member 1 Homo sapiens 0-3 23085740-1 2012 AIM: To evaluate retrospectively the association of cytochrome P450 3A (CYP3A) and ATP-binding cassette sub-family B member 1 (ABCB1) gene polymorphisms with the pharmacokinetics of cyclosporine A (CsA) in Chinese renal transplant patients. Cyclosporine 182-196 ATP binding cassette subfamily B member 1 Homo sapiens 83-125 23359659-7 2013 The potency of CsA to inhibit P-gp was tissue-independent (maternal BBB half-maximal inhibitory concentration [IC50], 5.67 +- 1.07 muM, vs. BPB IC50, 7.63 +- 3.16 muM). Cyclosporine 15-18 ATP binding cassette subfamily B member 1 Homo sapiens 30-34 23085740-1 2012 AIM: To evaluate retrospectively the association of cytochrome P450 3A (CYP3A) and ATP-binding cassette sub-family B member 1 (ABCB1) gene polymorphisms with the pharmacokinetics of cyclosporine A (CsA) in Chinese renal transplant patients. Cyclosporine 182-196 ATP binding cassette subfamily B member 1 Homo sapiens 127-132 23085740-1 2012 AIM: To evaluate retrospectively the association of cytochrome P450 3A (CYP3A) and ATP-binding cassette sub-family B member 1 (ABCB1) gene polymorphisms with the pharmacokinetics of cyclosporine A (CsA) in Chinese renal transplant patients. Cyclosporine 198-201 ATP binding cassette subfamily B member 1 Homo sapiens 127-132 23217392-1 2012 BACKGROUND: Cyclosporin A (CsA) is a substrate of both cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp), some of the single nucleotide polymorphisms (SNPs) in these genes are associated with interindividual variations in CsA pharmacokinetics. Cyclosporine 27-30 ATP binding cassette subfamily B member 1 Homo sapiens 86-100 23217392-1 2012 BACKGROUND: Cyclosporin A (CsA) is a substrate of both cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp), some of the single nucleotide polymorphisms (SNPs) in these genes are associated with interindividual variations in CsA pharmacokinetics. Cyclosporine 27-30 ATP binding cassette subfamily B member 1 Homo sapiens 102-106 23217392-1 2012 BACKGROUND: Cyclosporin A (CsA) is a substrate of both cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp), some of the single nucleotide polymorphisms (SNPs) in these genes are associated with interindividual variations in CsA pharmacokinetics. Cyclosporine 225-228 ATP binding cassette subfamily B member 1 Homo sapiens 86-100 23217392-1 2012 BACKGROUND: Cyclosporin A (CsA) is a substrate of both cytochrome P450 3A (CYP3A) and P-glycoprotein (P-gp), some of the single nucleotide polymorphisms (SNPs) in these genes are associated with interindividual variations in CsA pharmacokinetics. Cyclosporine 225-228 ATP binding cassette subfamily B member 1 Homo sapiens 102-106 23217392-4 2012 Retrospective case control study was utilized to identify the association between CYP3A4 1G, CYP3A5 3, ABCB1 genetic polymorphisms and CsA-related outcomes. Cyclosporine 135-138 ATP binding cassette subfamily B member 1 Homo sapiens 103-108 23014881-10 2012 The efflux of Hoechst 33342, a substrate for MDR1, was blocked by MDR1 inhibitor cyclosporin A, suggesting the functional expression of this transporter. Cyclosporine 81-94 ATP binding cassette subfamily B member 1 Homo sapiens 45-49 23014881-10 2012 The efflux of Hoechst 33342, a substrate for MDR1, was blocked by MDR1 inhibitor cyclosporin A, suggesting the functional expression of this transporter. Cyclosporine 81-94 ATP binding cassette subfamily B member 1 Homo sapiens 66-70 23146540-4 2012 CsA inhibits P-glycoprotein resulting in decreased hepatic metabolism and renal excretion of colchicine. Cyclosporine 0-3 ATP binding cassette subfamily B member 1 Homo sapiens 13-27 23084335-7 2012 Although other confounding factors causing immunological modulation may exist, it is plausible that low serum and high intracellular cyclosporine concentrations, due to the inhibition of P-gp activity by voriconazole, also contribute to an immunosuppressive state. Cyclosporine 133-145 ATP binding cassette subfamily B member 1 Homo sapiens 187-191 22947591-6 2012 OBJECTIVE: To build a population pharmacokinetic model of cyclosporine in living donor renal transplant recipients and identify covariates including CYP3A5*3, ABCB1 genetic polymorphisms that affect cyclosporine pharmacokinetic parameters. Cyclosporine 199-211 ATP binding cassette subfamily B member 1 Homo sapiens 159-164 22584255-5 2012 To define the mechanisms responsible for this low bioavailability, two P-glycoprotein (P-gp) inhibitors, verapamil and cyclosporine A, were used, and their presence substantially decreased C-K"s efflux ratio in Caco-2 cells (from 26.6 to <3) and significantly increased intracellular concentrations (by as much as 40-fold). Cyclosporine 119-133 ATP binding cassette subfamily B member 1 Homo sapiens 87-91 22584255-5 2012 To define the mechanisms responsible for this low bioavailability, two P-glycoprotein (P-gp) inhibitors, verapamil and cyclosporine A, were used, and their presence substantially decreased C-K"s efflux ratio in Caco-2 cells (from 26.6 to <3) and significantly increased intracellular concentrations (by as much as 40-fold). Cyclosporine 119-133 ATP binding cassette subfamily B member 1 Homo sapiens 71-85 20641759-5 2004 Calcium channel blockers, cyclosporin A, and its non-immunosuppressive analog PSC 833 are MDR modulators, inhibiting transport of P-gp substrates out of the cells (5, 6). Cyclosporine 26-39 ATP binding cassette subfamily B member 1 Homo sapiens 130-134 22290425-4 2012 Based on that, the present study aimed to evaluate the reversal of MDR phenotype through modulation of Pgp efflux pump activity in leukemia multidrug-resistant cells, using a low dose of cyclosporine A (CsA). Cyclosporine 203-206 ATP binding cassette subfamily B member 1 Homo sapiens 103-106 22290425-5 2012 We showed that modulation of Pgp activity by using CsA did not induce cytotoxic effects in leukemia cells, independently of Pgp expression. Cyclosporine 51-54 ATP binding cassette subfamily B member 1 Homo sapiens 29-32 22764569-6 2012 Although verapamil and cyclosporine A as MDR1 substrates completely inhibited the basolateral-to-apical transport, probenecid as MRP1 inhibitor did not show an effect. Cyclosporine 23-37 ATP binding cassette subfamily B member 1 Homo sapiens 41-45 22420656-9 2012 However, repeated pretreatment (7 days) with oral ETP significantly decreased the oral morphine-induced analgesia, in a cyclosporine A (a P-gp inhibitor) reversible manner. Cyclosporine 120-134 ATP binding cassette subfamily B member 1 Homo sapiens 138-142 22974789-8 2012 Pgp activity was also reduced in CsA and CsA+Rapa compared to the other immunosupressants but it was only significant in the CsA group for CD8+ subset. Cyclosporine 33-36 ATP binding cassette subfamily B member 1 Homo sapiens 0-3 22088485-8 2012 Inhibition of the multi-drug resistance pump ABCB1 with cyclosporine or knockdown with shRNA prior to treatment with YM155 demonstrated that cell lines with ABCB1 expression became 27-695 times more sensitive to YM155 treatment. Cyclosporine 56-68 ATP binding cassette subfamily B member 1 Homo sapiens 45-50 22088485-8 2012 Inhibition of the multi-drug resistance pump ABCB1 with cyclosporine or knockdown with shRNA prior to treatment with YM155 demonstrated that cell lines with ABCB1 expression became 27-695 times more sensitive to YM155 treatment. Cyclosporine 56-68 ATP binding cassette subfamily B member 1 Homo sapiens 157-162 20641391-4 2004 Calcium channel blockers, cyclosporin A, and its non-immunosuppressive analog PSC 833 are MDR modulators that inhibit transport of P-gp substrates out of cells (6, 7). Cyclosporine 26-39 ATP binding cassette subfamily B member 1 Homo sapiens 131-135 20641391-10 2004 Brain accumulation of [(11)C]CARV is reported to be highly sensitive to P-gp modulation by cyclosporin A (10). Cyclosporine 91-104 ATP binding cassette subfamily B member 1 Homo sapiens 72-76 20641916-5 2004 Calcium channel blockers, cyclosporin A, and its non-immunosuppressive analog PSC 833 are MDR modulators that inhibit transport of P-gp substrates out of cells (6, 7). Cyclosporine 26-39 ATP binding cassette subfamily B member 1 Homo sapiens 131-135 22974789-11 2012 CONCLUSIONS: Our data indicate that small molecules immunosuppressants, especially CsA, inhibit Pgp activity and T-cell function being the CD8+ T cells more susceptible to this effect. Cyclosporine 83-86 ATP binding cassette subfamily B member 1 Homo sapiens 96-99 21757611-4 2011 Two P-glycoprotein (P-gp) inhibitors, verapamil and cyclosporine A, substantially decreased the efflux ratio of Rh2s from 28.5 to 1.0 and 1.2, respectively, in Caco-2 cells. Cyclosporine 52-66 ATP binding cassette subfamily B member 1 Homo sapiens 4-18 21660974-6 2011 In co-treatment with beta-cyclodextrins, the apical to basolateral taxol flux was 4 to 6 times greater than in untreated monolayers and it was also higher than in cells treated with Pgp inhibitor cyclosporin A. Cyclosporine 196-209 ATP binding cassette subfamily B member 1 Homo sapiens 182-185 22016125-8 2011 Calcineurin inhibitors (cyclosporine, tacrolimus) and mTOR inhibitors (sirolimus, everolimus) are particularly susceptible to the effects of substances that inhibit or induce cytochrome P450 (CYP) 3A4 and P-glycoprotein. Cyclosporine 24-36 ATP binding cassette subfamily B member 1 Homo sapiens 205-219 21757611-4 2011 Two P-glycoprotein (P-gp) inhibitors, verapamil and cyclosporine A, substantially decreased the efflux ratio of Rh2s from 28.5 to 1.0 and 1.2, respectively, in Caco-2 cells. Cyclosporine 52-66 ATP binding cassette subfamily B member 1 Homo sapiens 20-24 21806386-1 2011 AIM: Polymorphisms in the CYP3A5 and ABCB1 genes have been investigated as modulators of the pharmacokinetics and clinical effects of cyclosporine (CSA) and tacrolimus (TAC) in European, North American and Asian populations, with controversial results. Cyclosporine 134-146 ATP binding cassette subfamily B member 1 Homo sapiens 37-42 21974705-12 2011 While cyclosporine A therapy gradually decreased MDR-1 expression, LDL adsorption therapy decreased expression sharply. Cyclosporine 6-20 ATP binding cassette subfamily B member 1 Homo sapiens 49-54 21538216-8 2011 This effect is prevented by Pgp inhibitors verapamil and cyclosporin A, as well as siRNA to ABCB1, with concomitant re-sensitization to silvestrol. Cyclosporine 57-70 ATP binding cassette subfamily B member 1 Homo sapiens 28-31 21806386-1 2011 AIM: Polymorphisms in the CYP3A5 and ABCB1 genes have been investigated as modulators of the pharmacokinetics and clinical effects of cyclosporine (CSA) and tacrolimus (TAC) in European, North American and Asian populations, with controversial results. Cyclosporine 148-151 ATP binding cassette subfamily B member 1 Homo sapiens 37-42 20571034-0 2011 Do drug transporter (ABCB1) SNPs influence cyclosporine and tacrolimus dose requirements and renal allograft outcome in the posttransplantation period? Cyclosporine 43-55 ATP binding cassette subfamily B member 1 Homo sapiens 21-26 21466223-0 2011 Quercetin and rutin reduced the bioavailability of cyclosporine from Neoral, an immunosuppressant, through activating P-glycoprotein and CYP 3A4. Cyclosporine 51-63 ATP binding cassette subfamily B member 1 Homo sapiens 118-132 21466223-2 2011 Cyclosporine (CSP), an immunosuppressant with a narrow therapeutic window, is a substrate of P-glycoprotein (P-gp) and cytochrome P-450 3A4 (CYP3A4). Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 93-107 21466223-2 2011 Cyclosporine (CSP), an immunosuppressant with a narrow therapeutic window, is a substrate of P-glycoprotein (P-gp) and cytochrome P-450 3A4 (CYP3A4). Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 109-113 21466223-2 2011 Cyclosporine (CSP), an immunosuppressant with a narrow therapeutic window, is a substrate of P-glycoprotein (P-gp) and cytochrome P-450 3A4 (CYP3A4). Cyclosporine 14-17 ATP binding cassette subfamily B member 1 Homo sapiens 93-107 21466223-2 2011 Cyclosporine (CSP), an immunosuppressant with a narrow therapeutic window, is a substrate of P-glycoprotein (P-gp) and cytochrome P-450 3A4 (CYP3A4). Cyclosporine 14-17 ATP binding cassette subfamily B member 1 Homo sapiens 109-113 21839244-0 2011 Pharmacogenetic study of ABCB1 and CYP3A5 genes during the first year following heart transplantation regarding tacrolimus or cyclosporine levels. Cyclosporine 126-138 ATP binding cassette subfamily B member 1 Homo sapiens 25-30 21839244-3 2011 We evaluated the SNPs in ABCB1 (glycoprotein P) and CYP3A5 (metabolic enzyme) genes, seeking correlate them with tacrolimus or cyclosporine levels during the first year after heart transplantation. Cyclosporine 127-139 ATP binding cassette subfamily B member 1 Homo sapiens 25-30 21839244-8 2011 To correlate ABCB1 SNPs, the variants described to cause higher blood levels in rs1045642, 1128503, 2032582 (in linkage disequilibrium) showed this effect only until 4 months posttransplantation among patients treated with cyclosporine (more than 100% higher than the other variant). Cyclosporine 223-235 ATP binding cassette subfamily B member 1 Homo sapiens 13-18 20571034-1 2011 Polymorphisms in the drug transporter gene (ABCB1) may play a significant role in individualizing cyclosporine (CsA) and tacrolimus (Tac) dosage and subsequently the allograft outcome in renal transplant recipients. Cyclosporine 98-110 ATP binding cassette subfamily B member 1 Homo sapiens 44-49 20571034-1 2011 Polymorphisms in the drug transporter gene (ABCB1) may play a significant role in individualizing cyclosporine (CsA) and tacrolimus (Tac) dosage and subsequently the allograft outcome in renal transplant recipients. Cyclosporine 112-115 ATP binding cassette subfamily B member 1 Homo sapiens 44-49 21318225-5 2011 The cyclosporin derivative PSC833, a potent inhibitor of P-glycoprotein, sensitized DX5 but not GARF cells to the cytotoxic effects of daunorubicin. Cyclosporine 4-15 ATP binding cassette subfamily B member 1 Homo sapiens 57-71 21383650-1 2011 BACKGROUND: The association of CYP3A5, CYP3A4, and ABCB1 single nucleotide polymorphisms (SNPs) with cyclosporine (CsA) pharmacokinetics is controversial. Cyclosporine 101-113 ATP binding cassette subfamily B member 1 Homo sapiens 51-56 21383650-1 2011 BACKGROUND: The association of CYP3A5, CYP3A4, and ABCB1 single nucleotide polymorphisms (SNPs) with cyclosporine (CsA) pharmacokinetics is controversial. Cyclosporine 115-118 ATP binding cassette subfamily B member 1 Homo sapiens 51-56 21857093-1 2011 The aim of this study was to retrospectively evaluate the effect of polymorphisms in the CYP3A4, CYP3A5 and ABCB1 genes on the dose-adjusted concentration and dose requirement of cyclosporine A(CsA) in Chinese recipients during the early period after bone marrow or hematopoietic stem cell transplantation. Cyclosporine 179-193 ATP binding cassette subfamily B member 1 Homo sapiens 108-113 21062675-0 2011 Reversion of resistance to immunosuppressive agents in three patients with psoriatic arthritis by cyclosporine A: modulation of P-glycoprotein function. Cyclosporine 98-112 ATP binding cassette subfamily B member 1 Homo sapiens 128-142 21062675-3 2011 P-gp function can in vitro be inhibited by cyclosporine A (CSA) and verapamil; moreover, P-gp reduction by CSA in systemic lupus erythematosus and rheumatoid arthritis has been demonstrated. Cyclosporine 43-57 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 21062675-3 2011 P-gp function can in vitro be inhibited by cyclosporine A (CSA) and verapamil; moreover, P-gp reduction by CSA in systemic lupus erythematosus and rheumatoid arthritis has been demonstrated. Cyclosporine 59-62 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 21062675-3 2011 P-gp function can in vitro be inhibited by cyclosporine A (CSA) and verapamil; moreover, P-gp reduction by CSA in systemic lupus erythematosus and rheumatoid arthritis has been demonstrated. Cyclosporine 107-110 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 21062675-3 2011 P-gp function can in vitro be inhibited by cyclosporine A (CSA) and verapamil; moreover, P-gp reduction by CSA in systemic lupus erythematosus and rheumatoid arthritis has been demonstrated. Cyclosporine 107-110 ATP binding cassette subfamily B member 1 Homo sapiens 89-93 21062675-6 2011 CSA treatment resulted in good clinical outcome that was related with a significant P-gp function reduction at CD3+ and CD8+ levels. Cyclosporine 0-3 ATP binding cassette subfamily B member 1 Homo sapiens 84-88 21062675-7 2011 In addition to its immunosuppressive activity, CSA results may also be related to MTX/SSA effect restoration through P-gp inhibition. Cyclosporine 47-50 ATP binding cassette subfamily B member 1 Homo sapiens 117-121 21273673-8 2010 None of the Tac pharmacokinetic parameters were associated with ABCB1 SNPs, but ABCB1 SNPs had early effects on the CsA exposure index and dose requirements. Cyclosporine 116-119 ATP binding cassette subfamily B member 1 Homo sapiens 80-85 20869436-2 2010 It has been shown earlier that the combined application of a class of Pgp modulators (e.g. cyclosporine A and SDZ PSC 833) used at low concentrations and UIC2 antibody is a novel, specific, and effective way of blocking Pgp function (Goda et al., 2007). Cyclosporine 91-105 ATP binding cassette subfamily B member 1 Homo sapiens 70-73 20869436-2 2010 It has been shown earlier that the combined application of a class of Pgp modulators (e.g. cyclosporine A and SDZ PSC 833) used at low concentrations and UIC2 antibody is a novel, specific, and effective way of blocking Pgp function (Goda et al., 2007). Cyclosporine 91-105 ATP binding cassette subfamily B member 1 Homo sapiens 220-223 20869436-4 2010 Co-incubation of cells with UIC2 and cyclosporine A (CSA, 2muM) increased the binding of UIC2 more than 3-fold and reverted the rhodamine 123 (R123), daunorubicin (DNR) and (99m)Tc-MIBI accumulation of the Pgp(+) 2780AD cells to approx. Cyclosporine 37-51 ATP binding cassette subfamily B member 1 Homo sapiens 206-209 20869436-4 2010 Co-incubation of cells with UIC2 and cyclosporine A (CSA, 2muM) increased the binding of UIC2 more than 3-fold and reverted the rhodamine 123 (R123), daunorubicin (DNR) and (99m)Tc-MIBI accumulation of the Pgp(+) 2780AD cells to approx. Cyclosporine 53-56 ATP binding cassette subfamily B member 1 Homo sapiens 206-209 20735140-8 2010 While 2-4 showed either no or very weak inhibition of cellular P-glycoprotein (P-gp) activity, they either activated or inhibited the actions of the first generation P-gp inhibitors verapamil or cyclosporin, respectively. Cyclosporine 195-206 ATP binding cassette subfamily B member 1 Homo sapiens 166-170 20862795-5 2004 Calcium channel blockers (such as verapamil), cyclosporine (CsA, P-gp inhibitor) and CsA"s non-immunosuppressive analog PSC 833 (other mechanism) are MDR modulators that inhibit the transport of P-gp substrates out of the cells (6, 7). Cyclosporine 46-58 ATP binding cassette subfamily B member 1 Homo sapiens 65-69 20862795-5 2004 Calcium channel blockers (such as verapamil), cyclosporine (CsA, P-gp inhibitor) and CsA"s non-immunosuppressive analog PSC 833 (other mechanism) are MDR modulators that inhibit the transport of P-gp substrates out of the cells (6, 7). Cyclosporine 46-58 ATP binding cassette subfamily B member 1 Homo sapiens 195-199 20862794-5 2004 Calcium channel blockers (such as verapamil), cyclosporine (CsA, P-gp inhibitor) and CsA"s non-immunosuppressive analog PSC 833 (other mechanism) are MDR modulators that inhibit the transport of P-gp substrates out of the cells (6, 7). Cyclosporine 46-58 ATP binding cassette subfamily B member 1 Homo sapiens 65-69 20862794-5 2004 Calcium channel blockers (such as verapamil), cyclosporine (CsA, P-gp inhibitor) and CsA"s non-immunosuppressive analog PSC 833 (other mechanism) are MDR modulators that inhibit the transport of P-gp substrates out of the cells (6, 7). Cyclosporine 46-58 ATP binding cassette subfamily B member 1 Homo sapiens 195-199 20862794-5 2004 Calcium channel blockers (such as verapamil), cyclosporine (CsA, P-gp inhibitor) and CsA"s non-immunosuppressive analog PSC 833 (other mechanism) are MDR modulators that inhibit the transport of P-gp substrates out of the cells (6, 7). Cyclosporine 60-63 ATP binding cassette subfamily B member 1 Homo sapiens 195-199 20862795-5 2004 Calcium channel blockers (such as verapamil), cyclosporine (CsA, P-gp inhibitor) and CsA"s non-immunosuppressive analog PSC 833 (other mechanism) are MDR modulators that inhibit the transport of P-gp substrates out of the cells (6, 7). Cyclosporine 60-63 ATP binding cassette subfamily B member 1 Homo sapiens 195-199 19763573-0 2010 PSC833, cyclosporine analogue, downregulates MDR1 expression by activating JNK/c-Jun/AP-1 and suppressing NF-kappaB. Cyclosporine 8-20 ATP binding cassette subfamily B member 1 Homo sapiens 45-49 20505666-1 2010 Cyclosporin A (CsA) is a substrate for cytochrome P450 3A and the efflux transporter P-glycoprotein (P-gp; ABCB1), both abundantly expressed in the kidney. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 107-112 20505666-1 2010 Cyclosporin A (CsA) is a substrate for cytochrome P450 3A and the efflux transporter P-glycoprotein (P-gp; ABCB1), both abundantly expressed in the kidney. Cyclosporine 15-18 ATP binding cassette subfamily B member 1 Homo sapiens 107-112 20505666-6 2010 The study showed that the presence of ABCB1 polymorphisms in donors influences long-term graft outcome adversely with decrease in renal function and graft loss in transplant recipients receiving CsA. Cyclosporine 195-198 ATP binding cassette subfamily B member 1 Homo sapiens 38-43 20121715-8 2010 Inhibitors of P-gp, including cyclosporine A (CsA) and verapamil (Vpa), increased the intracellular level of IB-MECA and reversed the resistance of K562/HHT cells to this drug. Cyclosporine 30-44 ATP binding cassette subfamily B member 1 Homo sapiens 14-18 20121715-8 2010 Inhibitors of P-gp, including cyclosporine A (CsA) and verapamil (Vpa), increased the intracellular level of IB-MECA and reversed the resistance of K562/HHT cells to this drug. Cyclosporine 46-49 ATP binding cassette subfamily B member 1 Homo sapiens 14-18 20431509-4 2010 There are also genetic predictors of pharmacodynamics, including IMPDH1 for mycophenolate and ABCB1 for cyclosporine that may identify individuals at particular risk of efficacy failure or toxicity with a given drug. Cyclosporine 104-116 ATP binding cassette subfamily B member 1 Homo sapiens 94-99 20336065-3 2010 Regional P-gp inhibition was expressed as cyclosporine A-induced percentage change in the distributional clearance of verapamil (K(1)) in the brain, normalized to the regional blood flow (rCBF). Cyclosporine 42-56 ATP binding cassette subfamily B member 1 Homo sapiens 9-13 19763573-2 2010 PSC833 is well known as a non-immunosuppressant cyclosporine analogue that functionally inhibits P-glycoprotein (Pgp), a product of the MDR1 gene. Cyclosporine 48-60 ATP binding cassette subfamily B member 1 Homo sapiens 97-111 19763573-2 2010 PSC833 is well known as a non-immunosuppressant cyclosporine analogue that functionally inhibits P-glycoprotein (Pgp), a product of the MDR1 gene. Cyclosporine 48-60 ATP binding cassette subfamily B member 1 Homo sapiens 113-116 19763573-2 2010 PSC833 is well known as a non-immunosuppressant cyclosporine analogue that functionally inhibits P-glycoprotein (Pgp), a product of the MDR1 gene. Cyclosporine 48-60 ATP binding cassette subfamily B member 1 Homo sapiens 136-140 20170205-13 2010 Influence of ABCB1 3435C>T, 1236C>T and 2677G>T/A SNPs on the pharmacokinetics of ciclosporin and tacrolimus remains uncertain, with inconsistent results. Cyclosporine 91-102 ATP binding cassette subfamily B member 1 Homo sapiens 13-18 20109345-15 2010 After the cells were exposed to 10 mug/mL DDP for 24 h, the cell apoptosis rate of SK-Hep1/DDP was decreased in comparison with SK-Hep1, but it was increased in those with pretreatment of MDR1 inhibitor CsA as compared with those without pretreatment. Cyclosporine 203-206 ATP binding cassette subfamily B member 1 Homo sapiens 188-192 20641310-5 2004 Calcium channel blockers, cyclosporin and its non-immunosuppressive analogue PSC 833 are MDR modulators inhibiting transport of P-gp substrates out of the cells (6, 7). Cyclosporine 26-37 ATP binding cassette subfamily B member 1 Homo sapiens 128-132 20061922-1 2010 BACKGROUND: We hypothesized that genetic variation of ATP-binding cassette subfamily B member 1 (ABCB1) that encodes P-glycoprotein (involved in the uptake of cyclosporin A [CsA]) contributes to trough drug concentrations and thereby to CsA"s immunosuppressive and toxic effects. Cyclosporine 159-172 ATP binding cassette subfamily B member 1 Homo sapiens 54-95 20061922-1 2010 BACKGROUND: We hypothesized that genetic variation of ATP-binding cassette subfamily B member 1 (ABCB1) that encodes P-glycoprotein (involved in the uptake of cyclosporin A [CsA]) contributes to trough drug concentrations and thereby to CsA"s immunosuppressive and toxic effects. Cyclosporine 159-172 ATP binding cassette subfamily B member 1 Homo sapiens 97-102 20061922-1 2010 BACKGROUND: We hypothesized that genetic variation of ATP-binding cassette subfamily B member 1 (ABCB1) that encodes P-glycoprotein (involved in the uptake of cyclosporin A [CsA]) contributes to trough drug concentrations and thereby to CsA"s immunosuppressive and toxic effects. Cyclosporine 174-177 ATP binding cassette subfamily B member 1 Homo sapiens 54-95 20061922-1 2010 BACKGROUND: We hypothesized that genetic variation of ATP-binding cassette subfamily B member 1 (ABCB1) that encodes P-glycoprotein (involved in the uptake of cyclosporin A [CsA]) contributes to trough drug concentrations and thereby to CsA"s immunosuppressive and toxic effects. Cyclosporine 174-177 ATP binding cassette subfamily B member 1 Homo sapiens 97-102 20061922-1 2010 BACKGROUND: We hypothesized that genetic variation of ATP-binding cassette subfamily B member 1 (ABCB1) that encodes P-glycoprotein (involved in the uptake of cyclosporin A [CsA]) contributes to trough drug concentrations and thereby to CsA"s immunosuppressive and toxic effects. Cyclosporine 237-240 ATP binding cassette subfamily B member 1 Homo sapiens 54-95 20061922-1 2010 BACKGROUND: We hypothesized that genetic variation of ATP-binding cassette subfamily B member 1 (ABCB1) that encodes P-glycoprotein (involved in the uptake of cyclosporin A [CsA]) contributes to trough drug concentrations and thereby to CsA"s immunosuppressive and toxic effects. Cyclosporine 237-240 ATP binding cassette subfamily B member 1 Homo sapiens 97-102 20061922-7 2010 CONCLUSIONS: The association of ABCB1 12/1236, 21/2677, and 26/3435 CC/GG/CC haplotype with increased CsA dose- and weight-adjusted CsA trough concentrations in this group of adult white heart transplant recipients was not consistent over time and had no effect on the incidence of acute rejection or on the development of renal impairment. Cyclosporine 102-105 ATP binding cassette subfamily B member 1 Homo sapiens 32-37 20061922-7 2010 CONCLUSIONS: The association of ABCB1 12/1236, 21/2677, and 26/3435 CC/GG/CC haplotype with increased CsA dose- and weight-adjusted CsA trough concentrations in this group of adult white heart transplant recipients was not consistent over time and had no effect on the incidence of acute rejection or on the development of renal impairment. Cyclosporine 132-135 ATP binding cassette subfamily B member 1 Homo sapiens 32-37 19995330-2 2009 In addition, the efflux can be reversed by cyclosporine, indicating that S5 may be a human P-glycoprotein (P-gp) substrate. Cyclosporine 43-55 ATP binding cassette subfamily B member 1 Homo sapiens 91-105 19995330-2 2009 In addition, the efflux can be reversed by cyclosporine, indicating that S5 may be a human P-glycoprotein (P-gp) substrate. Cyclosporine 43-55 ATP binding cassette subfamily B member 1 Homo sapiens 107-111 20038391-1 2009 OBJECTIVE: To determine how single nucleotide polymorphisms located on genes MDR1, CYP3A4 and CYP3A5 affect the absorption kinetics of cyclosporine in cardiac transplant patients. Cyclosporine 135-147 ATP binding cassette subfamily B member 1 Homo sapiens 77-81 19925383-11 2009 MDR1 haplotypes and CYP3A5*3 genotypes can be related to C(2) and C(0) of CsA, respectively. Cyclosporine 74-77 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 19925383-0 2009 Influence of the MDR1 haplotype and CYP3A5 genotypes on cyclosporine blood level in Chinese renal transplant recipients. Cyclosporine 56-68 ATP binding cassette subfamily B member 1 Homo sapiens 17-21 20038391-5 2009 DISCUSSION: Our results show that genotype differences in MDR1 3435C > T can explain part of the variability in cyclosporine absorption among individuals in the population of Spanish cardiac transplant recipients. Cyclosporine 115-127 ATP binding cassette subfamily B member 1 Homo sapiens 58-62 19447222-6 2009 The effect was reversed by the MDR1 inhibitor cyclosporine. Cyclosporine 46-58 ATP binding cassette subfamily B member 1 Homo sapiens 31-35 19562680-6 2009 In the presence of cyclosporin A and verapamil, potent inhibitors of P-glycoprotein (P-gp), the P(ratio) decreased from 3.8 to 2.3 and 1.8, respectively, and permeation of apical to basolateral was enhanced. Cyclosporine 19-32 ATP binding cassette subfamily B member 1 Homo sapiens 69-83 19562680-6 2009 In the presence of cyclosporin A and verapamil, potent inhibitors of P-glycoprotein (P-gp), the P(ratio) decreased from 3.8 to 2.3 and 1.8, respectively, and permeation of apical to basolateral was enhanced. Cyclosporine 19-32 ATP binding cassette subfamily B member 1 Homo sapiens 85-89 19960055-5 2009 After the control phase of each experiment, the P-glycoprotein inhibitor ciclosporin A was added at middle perfusion (45 minutes). Cyclosporine 73-86 ATP binding cassette subfamily B member 1 Homo sapiens 48-62 19470683-0 2009 ABCB1 genotypes predict cyclosporine-related adverse events and kidney allograft outcome. Cyclosporine 24-36 ATP binding cassette subfamily B member 1 Homo sapiens 0-5 19470683-1 2009 Cyclosporine A (CsA) is a substrate of P-glycoprotein, an efflux transporter encoded by the ABCB1 gene. Cyclosporine 0-14 ATP binding cassette subfamily B member 1 Homo sapiens 39-53 19470683-1 2009 Cyclosporine A (CsA) is a substrate of P-glycoprotein, an efflux transporter encoded by the ABCB1 gene. Cyclosporine 0-14 ATP binding cassette subfamily B member 1 Homo sapiens 92-97 19470683-1 2009 Cyclosporine A (CsA) is a substrate of P-glycoprotein, an efflux transporter encoded by the ABCB1 gene. Cyclosporine 16-19 ATP binding cassette subfamily B member 1 Homo sapiens 39-53 19470683-1 2009 Cyclosporine A (CsA) is a substrate of P-glycoprotein, an efflux transporter encoded by the ABCB1 gene. Cyclosporine 16-19 ATP binding cassette subfamily B member 1 Homo sapiens 92-97 19470683-2 2009 Compared with carriers of the wild-type gene, carriers of T allelic variants in exons 21 or 26 have reduced P-glycoprotein activity and, secondarily, increased intracellular concentration of CsA; therefore, carriers of T variants might be at increased risk for CsA-related adverse events. Cyclosporine 191-194 ATP binding cassette subfamily B member 1 Homo sapiens 108-122 19470683-2 2009 Compared with carriers of the wild-type gene, carriers of T allelic variants in exons 21 or 26 have reduced P-glycoprotein activity and, secondarily, increased intracellular concentration of CsA; therefore, carriers of T variants might be at increased risk for CsA-related adverse events. Cyclosporine 261-264 ATP binding cassette subfamily B member 1 Homo sapiens 108-122 19470683-3 2009 We evaluated the associations between ABCB1 genotypes (in exons 12, 21, and 26) and CsA-related outcomes in 147 renal transplant recipients who were receiving CsA-based immunosuppression and were included in the Mycophenolate Steroids Sparing study. Cyclosporine 84-87 ATP binding cassette subfamily B member 1 Homo sapiens 38-43 19470683-7 2009 In conclusion, renal transplant recipients with T allelic variants in ABCB1 exons 21 or 26 are at increased risk for CsA-related adverse events. Cyclosporine 117-120 ATP binding cassette subfamily B member 1 Homo sapiens 70-75 19429419-3 2009 The change in the mRNA expression of MDR1 was accompanied by a change in the CsA-dependent intracellular accumulation of rhodamine 123. Cyclosporine 77-80 ATP binding cassette subfamily B member 1 Homo sapiens 37-41 19376366-0 2009 Genetic polymorphisms in CYP3A5 and MDR1 genes and their correlations with plasma levels of tacrolimus and cyclosporine in renal transplant recipients. Cyclosporine 107-119 ATP binding cassette subfamily B member 1 Homo sapiens 36-40 18936931-0 2009 Effect of genetic polymorphisms of CYP3A5 and MDR1 on cyclosporine concentration during the early stage after renal transplantation in Chinese patients co-treated with diltiazem. Cyclosporine 54-66 ATP binding cassette subfamily B member 1 Homo sapiens 46-50 18936931-8 2009 CONCLUSION: This study demonstrated that the G2677T/A single nucleotide polymorphisms in MDR1 and MDR1 haplotypes C-G-C, T-G-T and T-T-C are associated with the CsA concentration during the very early post-transplant period in Chinese renal transplant patients co-treated with diltiazem. Cyclosporine 161-164 ATP binding cassette subfamily B member 1 Homo sapiens 89-93 18936931-8 2009 CONCLUSION: This study demonstrated that the G2677T/A single nucleotide polymorphisms in MDR1 and MDR1 haplotypes C-G-C, T-G-T and T-T-C are associated with the CsA concentration during the very early post-transplant period in Chinese renal transplant patients co-treated with diltiazem. Cyclosporine 161-164 ATP binding cassette subfamily B member 1 Homo sapiens 98-102 20641209-5 2004 Calcium channel blockers, cyclosporin, and its non-immunosuppressive analog PSC 833 are MDR modulators that inhibit the transport of P-gp substrates out of the cells (6, 7). Cyclosporine 26-37 ATP binding cassette subfamily B member 1 Homo sapiens 133-137 19617341-0 2009 Imaging of cyclosporine inhibition of P-glycoprotein activity using 11C-verapamil in the brain: studies of healthy humans. Cyclosporine 11-23 ATP binding cassette subfamily B member 1 Homo sapiens 38-52 19617341-3 2009 We have previously demonstrated P-gp activity at the human BBB using PET of (11)C-verapamil distribution into the brain in the absence and presence of the P-gp inhibitor cyclosporine-A (CsA). Cyclosporine 170-184 ATP binding cassette subfamily B member 1 Homo sapiens 32-36 19530439-7 2009 After treatment of the MDR1-expressing HeLa cells with MDR1 substrate vinblastin or inhibitors cyclosporin A and verapamil, the amount of R-123 retained in the cells was increased to 2 to 2.3 times the level in untreated MDR1-expressing HeLa cells. Cyclosporine 95-108 ATP binding cassette subfamily B member 1 Homo sapiens 23-27 19047468-5 2009 The effect of P-gp inhibition was investigated by administering cyclosporin A (CsA). Cyclosporine 64-77 ATP binding cassette subfamily B member 1 Homo sapiens 14-18 19408691-8 2009 The P-glycoprotein inhibitor cyclosporine A significantly enhanced the transport amount of aripiprazole. Cyclosporine 29-43 ATP binding cassette subfamily B member 1 Homo sapiens 4-18 19728747-9 2009 Ciclosporin and tacrolimus have distinct pharmacokinetics, but both are metabolized by intestinal and hepatic CYP3A4/3A5 and transported across the cell membrane by P-glycoprotein. Cyclosporine 0-11 ATP binding cassette subfamily B member 1 Homo sapiens 165-179 19470292-10 2009 The effects produced by some of these components are found to be comparable to those of well-known P-gp inhibitors verapamil and cyclosporine. Cyclosporine 129-141 ATP binding cassette subfamily B member 1 Homo sapiens 99-103 18835257-4 2008 The efflux could be blocked by cyclosporine A, a specific P-glycoprotein (P-gp) inhibitor, suggesting that P-gp may be the responsible transporter. Cyclosporine 31-45 ATP binding cassette subfamily B member 1 Homo sapiens 58-72 18835257-4 2008 The efflux could be blocked by cyclosporine A, a specific P-glycoprotein (P-gp) inhibitor, suggesting that P-gp may be the responsible transporter. Cyclosporine 31-45 ATP binding cassette subfamily B member 1 Homo sapiens 74-78 18835257-4 2008 The efflux could be blocked by cyclosporine A, a specific P-glycoprotein (P-gp) inhibitor, suggesting that P-gp may be the responsible transporter. Cyclosporine 31-45 ATP binding cassette subfamily B member 1 Homo sapiens 107-111 19053888-6 2008 N-4-methylpiperazine- (10a-d) and tetrahydroisoquinoline- (11a-d) derivatives were Cyclosporin A-like ABCB1 nontransported substrates. Cyclosporine 83-96 ATP binding cassette subfamily B member 1 Homo sapiens 102-107 18702631-0 2008 Role of MDR1 gene polymorphisms in gingival overgrowth induced by cyclosporine in transplant patients. Cyclosporine 66-78 ATP binding cassette subfamily B member 1 Homo sapiens 8-12 18702631-1 2008 BACKGROUND AND OBJECTIVE: The aim of the present study was to determine the association between genotypes of the MDR1 gene, encoding P-glycoprotein, and gingival overgrowth in transplant patients treated with cyclosporine, and to evaluate the effect of periodontal treatment in these patients. Cyclosporine 209-221 ATP binding cassette subfamily B member 1 Homo sapiens 113-117 18978522-1 2008 Cyclosporine is a substrate of cytochrome P450 (CYP) 3A and of the transporter ABCB1, for which polymorphisms have been described. Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 79-84 18801030-0 2008 Meta-analysis of the effect of MDR1 C3435T polymorphism on cyclosporine pharmacokinetics. Cyclosporine 59-71 ATP binding cassette subfamily B member 1 Homo sapiens 31-35 19005401-1 2008 BACKGROUND: Bioavailability of tacrolimus (Tac) and cyclosporine is determined by cytochrome P450IIIA and by P-glycoprotein encoded by the CYP3A4/CYP3A5 and ABCB1 genes. Cyclosporine 52-64 ATP binding cassette subfamily B member 1 Homo sapiens 157-162 18801030-1 2008 The published data revealed conflicting results of the polymorphism of MDR1 exon 26 SNP C3435T on the pharmacokinetics of cyclosporine; thus, the aim was to conduct a meta-analysis of significant magnitude to investigate the influence of SNP C3435T on the pharmacokinetics of cyclosporine. Cyclosporine 122-134 ATP binding cassette subfamily B member 1 Homo sapiens 71-75 18801030-1 2008 The published data revealed conflicting results of the polymorphism of MDR1 exon 26 SNP C3435T on the pharmacokinetics of cyclosporine; thus, the aim was to conduct a meta-analysis of significant magnitude to investigate the influence of SNP C3435T on the pharmacokinetics of cyclosporine. Cyclosporine 276-288 ATP binding cassette subfamily B member 1 Homo sapiens 71-75 18801030-7 2008 In conclusion, our meta-analysis of available studies has thus far failed to demonstrate a definitive correlation between the SNP C3435T in MDR1 gene and alterations in P-glycoprotein function that can result in altered pharmacokinetics of cyclosporine, although it was indicated in this meta-analysis that the carrier of CC genotype of the SNP C3435T of MDR1 had lower cyclosporine exposure presented as AUC(0-12) than those with at least one T allele. Cyclosporine 240-252 ATP binding cassette subfamily B member 1 Homo sapiens 140-144 18801030-8 2008 There seems to be ethnic differences in the relationship between the SNP C3435T of MDR1 and cyclosporine pharmacokinetics. Cyclosporine 92-104 ATP binding cassette subfamily B member 1 Homo sapiens 83-87 18789739-3 2008 Cyclosporine A (CsA), aureobasidin A (AbA) and related analogues were reported to possess potent inhibitory actions against Pgp. Cyclosporine 0-14 ATP binding cassette subfamily B member 1 Homo sapiens 124-127 18636247-0 2008 Association of MDR1, CYP3A4*18B, and CYP3A5*3 polymorphisms with cyclosporine pharmacokinetics in Chinese renal transplant recipients. Cyclosporine 65-77 ATP binding cassette subfamily B member 1 Homo sapiens 15-19 18789739-0 2008 Development of predictive in silico model for cyclosporine- and aureobasidin-based P-glycoprotein inhibitors employing receptor surface analysis. Cyclosporine 46-58 ATP binding cassette subfamily B member 1 Homo sapiens 83-97 19213345-8 2008 The P-gp expression was down-regulated after treated with CsA, Tet and both (75.32%, 76.86% and 48.61%); mdr1 mRNA was also down-regulated, and the effect of their combination was more obvious. Cyclosporine 58-61 ATP binding cassette subfamily B member 1 Homo sapiens 4-8 19213345-8 2008 The P-gp expression was down-regulated after treated with CsA, Tet and both (75.32%, 76.86% and 48.61%); mdr1 mRNA was also down-regulated, and the effect of their combination was more obvious. Cyclosporine 58-61 ATP binding cassette subfamily B member 1 Homo sapiens 105-109 18760199-0 2008 ABCB1 G2677 allele is associated with high dose requirement of cyclosporin A to prevent renal allograft rejection in North India. Cyclosporine 63-76 ATP binding cassette subfamily B member 1 Homo sapiens 0-5 18760199-1 2008 BACKGROUND: Interindividual heterogeneity in expression of ABCB1 gene has been suspected to be one of the factors resulting in cyclosporin (CsA) pharmacokinetic variation. Cyclosporine 127-138 ATP binding cassette subfamily B member 1 Homo sapiens 59-64 18760199-1 2008 BACKGROUND: Interindividual heterogeneity in expression of ABCB1 gene has been suspected to be one of the factors resulting in cyclosporin (CsA) pharmacokinetic variation. Cyclosporine 140-143 ATP binding cassette subfamily B member 1 Homo sapiens 59-64 18760199-2 2008 The present study explored the association of ABCB1 SNPs on CsA dose requirements and dose-adjusted C2 levels (CsA level/daily dose requirement) in renal allograft recipients. Cyclosporine 60-63 ATP binding cassette subfamily B member 1 Homo sapiens 46-51 19100412-0 2008 Different effect of cyclosporine and tacrolimus on renal expression of P-glycoprotein in human kidney transplantation. Cyclosporine 20-32 ATP binding cassette subfamily B member 1 Homo sapiens 71-85 19100412-1 2008 OBJECTIVE: To investigate the differential effects of cyclosporine (CsA) and tacrolimus (TAC) on renal expression of P-glycoprotein (P-gp) in a cohort of kidney transplant recipients. Cyclosporine 54-66 ATP binding cassette subfamily B member 1 Homo sapiens 117-131 19100412-1 2008 OBJECTIVE: To investigate the differential effects of cyclosporine (CsA) and tacrolimus (TAC) on renal expression of P-glycoprotein (P-gp) in a cohort of kidney transplant recipients. Cyclosporine 54-66 ATP binding cassette subfamily B member 1 Homo sapiens 133-137 19100412-1 2008 OBJECTIVE: To investigate the differential effects of cyclosporine (CsA) and tacrolimus (TAC) on renal expression of P-glycoprotein (P-gp) in a cohort of kidney transplant recipients. Cyclosporine 68-71 ATP binding cassette subfamily B member 1 Homo sapiens 117-131 19100412-1 2008 OBJECTIVE: To investigate the differential effects of cyclosporine (CsA) and tacrolimus (TAC) on renal expression of P-glycoprotein (P-gp) in a cohort of kidney transplant recipients. Cyclosporine 68-71 ATP binding cassette subfamily B member 1 Homo sapiens 133-137 19100412-8 2008 CONCLUSION: Less P-gp expression in the CsA group than the TAC group may be the molecular action pathway of the high incidence of CsA nephrotoxicity and CsA-induced CAN. Cyclosporine 40-43 ATP binding cassette subfamily B member 1 Homo sapiens 17-21 19100412-8 2008 CONCLUSION: Less P-gp expression in the CsA group than the TAC group may be the molecular action pathway of the high incidence of CsA nephrotoxicity and CsA-induced CAN. Cyclosporine 130-133 ATP binding cassette subfamily B member 1 Homo sapiens 17-21 19100412-8 2008 CONCLUSION: Less P-gp expression in the CsA group than the TAC group may be the molecular action pathway of the high incidence of CsA nephrotoxicity and CsA-induced CAN. Cyclosporine 130-133 ATP binding cassette subfamily B member 1 Homo sapiens 17-21 18789739-3 2008 Cyclosporine A (CsA), aureobasidin A (AbA) and related analogues were reported to possess potent inhibitory actions against Pgp. Cyclosporine 16-19 ATP binding cassette subfamily B member 1 Homo sapiens 124-127 18789739-4 2008 In this work we employed receptor surface analysis (RSA) to construct two satisfactory receptor surface models (RSMs) for cyclosporine- and aureobasidin-based Pgp inhibitors. Cyclosporine 122-134 ATP binding cassette subfamily B member 1 Homo sapiens 159-162 18789739-7 2008 The resulting 3D-QSAR was employed to probe the structural factors that control the inhibitory activities of cyclosporine and aureobasidin analogues against Pgp. Cyclosporine 109-121 ATP binding cassette subfamily B member 1 Homo sapiens 157-160 18717915-0 2008 ABCB1 polymorphisms may have a minor effect on ciclosporin blood concentrations in myasthenia gravis patients. Cyclosporine 47-58 ATP binding cassette subfamily B member 1 Homo sapiens 0-5 18717915-3 2008 The aim was to determine the role of genetic polymorphisms in MDR-1 with respect to interindividual variability of CsA blood concentrations in myasthenia gravis (MG) patients. Cyclosporine 115-118 ATP binding cassette subfamily B member 1 Homo sapiens 62-67 18717915-7 2008 Furthermore, under the same CsA regimen, it was found that the trough concentrations of variant genotype (ABCB1 1236TT or ABCB1 2677TT) were significant greater than those of wild-type (ABCB1 1236CC or ABCB1 2677GG, respectively) (P = 0.0222 and 0.0081). Cyclosporine 28-31 ATP binding cassette subfamily B member 1 Homo sapiens 106-111 18717915-7 2008 Furthermore, under the same CsA regimen, it was found that the trough concentrations of variant genotype (ABCB1 1236TT or ABCB1 2677TT) were significant greater than those of wild-type (ABCB1 1236CC or ABCB1 2677GG, respectively) (P = 0.0222 and 0.0081). Cyclosporine 28-31 ATP binding cassette subfamily B member 1 Homo sapiens 122-127 18717915-7 2008 Furthermore, under the same CsA regimen, it was found that the trough concentrations of variant genotype (ABCB1 1236TT or ABCB1 2677TT) were significant greater than those of wild-type (ABCB1 1236CC or ABCB1 2677GG, respectively) (P = 0.0222 and 0.0081). Cyclosporine 28-31 ATP binding cassette subfamily B member 1 Homo sapiens 122-127 18717915-7 2008 Furthermore, under the same CsA regimen, it was found that the trough concentrations of variant genotype (ABCB1 1236TT or ABCB1 2677TT) were significant greater than those of wild-type (ABCB1 1236CC or ABCB1 2677GG, respectively) (P = 0.0222 and 0.0081). Cyclosporine 28-31 ATP binding cassette subfamily B member 1 Homo sapiens 122-127 18717915-9 2008 CONCLUSIONS: ABCB1 polymorphisms in both genotype and haplotype may have a minor effect on the CsA blood concentrations. Cyclosporine 95-98 ATP binding cassette subfamily B member 1 Homo sapiens 13-18 18594053-5 2008 DATA SYNTHESIS: Corticosteroids share common metabolic and transporter pathways, the cytochrome P450 and P-glycoprotein (P-gp/ABCB1) systems, respectively, with cyclosporine, tacrolimus, and sirolimus. Cyclosporine 161-173 ATP binding cassette subfamily B member 1 Homo sapiens 105-119 18594053-5 2008 DATA SYNTHESIS: Corticosteroids share common metabolic and transporter pathways, the cytochrome P450 and P-glycoprotein (P-gp/ABCB1) systems, respectively, with cyclosporine, tacrolimus, and sirolimus. Cyclosporine 161-173 ATP binding cassette subfamily B member 1 Homo sapiens 126-131 18589174-3 2008 Frequencies of CYP3A5*1 versus *3 and MDR1-C3435T were correlated with tacrolimus (TAC) and cyclosporine (CSA) concentration-to-dose (C/D) ratios. Cyclosporine 92-104 ATP binding cassette subfamily B member 1 Homo sapiens 38-42 18673531-8 2008 MTT assay showed that Pgp inhibitors such as cyclosporine A, verapamil and PSC833 sensitized Colo320HSR (colon, highest MDR1 expression) but not SNU-668 (gastric, highest) and SNU-C5 (gastric, no expression) to paclitaxel. Cyclosporine 45-59 ATP binding cassette subfamily B member 1 Homo sapiens 22-25 18673531-8 2008 MTT assay showed that Pgp inhibitors such as cyclosporine A, verapamil and PSC833 sensitized Colo320HSR (colon, highest MDR1 expression) but not SNU-668 (gastric, highest) and SNU-C5 (gastric, no expression) to paclitaxel. Cyclosporine 45-59 ATP binding cassette subfamily B member 1 Homo sapiens 120-124 18518855-7 2008 In adults, genetic polymorphisms in the genes encoding the cyclosporine-metabolizing enzymes CYP3A4 and CYP3A5, as well as the ABCB1 gene, which encodes the efflux-pump P-glycoprotein, seem to have a limited effect, if any, on cyclosporine pharmacokinetics. Cyclosporine 227-239 ATP binding cassette subfamily B member 1 Homo sapiens 169-183 18518855-8 2008 However, the authors have now reported for the first time an association between cyclosporine oral bioavailability and the ABCB1 c.1236C>T and c.2677G>T polymorphisms, as well as the related haplotype c.1199G-c.1236C-c.2677G-c.3435C, in children with end-stage renal disease older than 8 years of age. Cyclosporine 81-93 ATP binding cassette subfamily B member 1 Homo sapiens 123-128 18589174-3 2008 Frequencies of CYP3A5*1 versus *3 and MDR1-C3435T were correlated with tacrolimus (TAC) and cyclosporine (CSA) concentration-to-dose (C/D) ratios. Cyclosporine 106-109 ATP binding cassette subfamily B member 1 Homo sapiens 38-42 19356075-0 2008 Influence of ABCB1 gene polymorphisms and P-glycoprotein activity on cyclosporine pharmacokinetics in peripheral blood mononuclear cells in healthy volunteers. Cyclosporine 69-81 ATP binding cassette subfamily B member 1 Homo sapiens 13-18 18518855-12 2008 These data suggest that the effect of ABCB1 polymorphisms on cyclosporine pharmacokinetics is related to age, and thus developmental stage. Cyclosporine 61-73 ATP binding cassette subfamily B member 1 Homo sapiens 38-43 18518855-13 2008 Although further study is necessary to establish the predictive value of ABCB1 genotyping for individualization of cyclosporine therapy in children older than 8 years, an important step towards further personalized immunosuppressive drug therapy has been made. Cyclosporine 115-127 ATP binding cassette subfamily B member 1 Homo sapiens 73-78 18451510-3 2008 P-gp function was estimated by the transporter activity of the cells based on the efflux of Rhodamine-123 (Rh123) from the cells in the presence or absence of a P-gp inhibitor, cyclosporine A. Cyclosporine 177-191 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 19356075-0 2008 Influence of ABCB1 gene polymorphisms and P-glycoprotein activity on cyclosporine pharmacokinetics in peripheral blood mononuclear cells in healthy volunteers. Cyclosporine 69-81 ATP binding cassette subfamily B member 1 Homo sapiens 42-56 19356075-1 2008 The calcineurin inhibitor cyclosporine is removed from lymphocytes by the drug efflux transporter P-glycoprotein (P-gp) encoded by the ABCB1 gene for which several single nucleotide polymorphisms (SNPs) have been identified. Cyclosporine 26-38 ATP binding cassette subfamily B member 1 Homo sapiens 98-112 19356075-1 2008 The calcineurin inhibitor cyclosporine is removed from lymphocytes by the drug efflux transporter P-glycoprotein (P-gp) encoded by the ABCB1 gene for which several single nucleotide polymorphisms (SNPs) have been identified. Cyclosporine 26-38 ATP binding cassette subfamily B member 1 Homo sapiens 135-140 17934801-10 2008 Interestingly, cyclosporin A, a P-gp inhibitor, but not fumitremorgin C, a BCRP inhibitor, restored both imatinib-sensitivity and the intracellular imatinib level. Cyclosporine 15-28 ATP binding cassette subfamily B member 1 Homo sapiens 32-36 18518855-3 2008 : Pharmacogenetics of cyclosporine in children suggests an age-dependent influence of ABCB1polymorphisms. Cyclosporine 22-34 ATP binding cassette subfamily B member 1 Homo sapiens 86-91 17031644-5 2007 RESULTS: CsA increased cellular drug uptake in cells overexpressing Pgp, MRP-1 or BCRP and nuclear drug uptake in cells overexpressing LRP at the clinically achievable concentration of 2.5 microM. Cyclosporine 9-12 ATP binding cassette subfamily B member 1 Homo sapiens 68-71 18334915-0 2008 Influence of ABCB1 genetic polymorphisms on cyclosporine intracellular concentration in transplant recipients. Cyclosporine 44-56 ATP binding cassette subfamily B member 1 Homo sapiens 13-18 18334915-1 2008 OBJECTIVE: The expression on lymphocytes of P-glycoprotein, an efflux transporter encoded by the ABCB1 gene, might influence cyclosporine intracellular concentration. Cyclosporine 125-137 ATP binding cassette subfamily B member 1 Homo sapiens 44-58 18334915-1 2008 OBJECTIVE: The expression on lymphocytes of P-glycoprotein, an efflux transporter encoded by the ABCB1 gene, might influence cyclosporine intracellular concentration. Cyclosporine 125-137 ATP binding cassette subfamily B member 1 Homo sapiens 97-102 18334915-4 2008 The ABCB1 1199A carriers presented a 1.8-fold decreased cyclosporine intracellular concentration (P=0.04), whereas the 3435T carriers presented a 1.7-fold increase (P=0.02) as well as a 1.2-fold increased blood concentration (P=0.04). Cyclosporine 56-68 ATP binding cassette subfamily B member 1 Homo sapiens 4-9 18334915-6 2008 CONCLUSION: This is the first report demonstrating that ABCB1 polymorphisms influence cyclosporine intracellular concentration. Cyclosporine 86-98 ATP binding cassette subfamily B member 1 Homo sapiens 56-61 18057117-4 2008 Therefore, we developed a high throughput cell-based assay to determine the potential of putative P-gp inhibitors [including cyclosporine A (CsA)] to inhibit (EC(50)) the efflux of verapamil-bodipy, a model P-gp substrate. Cyclosporine 125-139 ATP binding cassette subfamily B member 1 Homo sapiens 98-102 18057117-4 2008 Therefore, we developed a high throughput cell-based assay to determine the potential of putative P-gp inhibitors [including cyclosporine A (CsA)] to inhibit (EC(50)) the efflux of verapamil-bodipy, a model P-gp substrate. Cyclosporine 125-139 ATP binding cassette subfamily B member 1 Homo sapiens 207-211 18057117-4 2008 Therefore, we developed a high throughput cell-based assay to determine the potential of putative P-gp inhibitors [including cyclosporine A (CsA)] to inhibit (EC(50)) the efflux of verapamil-bodipy, a model P-gp substrate. Cyclosporine 141-144 ATP binding cassette subfamily B member 1 Homo sapiens 98-102 18057117-4 2008 Therefore, we developed a high throughput cell-based assay to determine the potential of putative P-gp inhibitors [including cyclosporine A (CsA)] to inhibit (EC(50)) the efflux of verapamil-bodipy, a model P-gp substrate. Cyclosporine 141-144 ATP binding cassette subfamily B member 1 Homo sapiens 207-211 18057117-6 2008 Using this assay, quinine, quinidine, CsA, and amprenavir were predicted to be the most potent P-gp inhibitors in vivo at their respective therapeutic maximal unbound plasma concentrations. Cyclosporine 38-41 ATP binding cassette subfamily B member 1 Homo sapiens 95-99 18003606-7 2008 Cell surface MDR1 was up-regulated 1 h after treatment with CsA or adaGb3, but at 72 h, cell surface expression was lost. Cyclosporine 60-63 ATP binding cassette subfamily B member 1 Homo sapiens 13-17 18271955-8 2008 In addition, P-gp inhibition by zosuquidar was found to be more potent than cyclosporine A in cells with highly active P-gp. Cyclosporine 76-90 ATP binding cassette subfamily B member 1 Homo sapiens 119-123 17686907-4 2007 Considering that cyclosporin A and rifampicin inhibit multiple uptake/efflux transporters, the interactions of CP-671,305 with major human hepatic drug transporters, multidrug resistance protein 1 (MDR1), multidrug resistance-associated protein 2 (MRP2), breast cancer resistant protein (BCRP), and organic anion-transporting polypeptide (OATPs) were evaluated in vitro. Cyclosporine 17-30 ATP binding cassette subfamily B member 1 Homo sapiens 166-196 17958337-6 2007 P-glycoprotein inhibitors such as cyclosporine, tariquidar and verapamil significantly increased the influx of udenafil and decreased the efflux of udenafil. Cyclosporine 34-46 ATP binding cassette subfamily B member 1 Homo sapiens 0-14 17031644-1 2007 PURPOSE: We sought to determine the effects of the immunosuppressants, cyclosporin A (CsA), tacrolimus and sirolimus, on drug transport by the ATP-binding cassette proteins, P-glycoprotein (Pgp; ABCB1), multidrug resistance protein-1 (MRP-1; ABCC1) and breast cancer resistance protein (BCRP; ABCG2), and the major vault protein lung resistance protein (LRP). Cyclosporine 86-89 ATP binding cassette subfamily B member 1 Homo sapiens 174-188 17031644-1 2007 PURPOSE: We sought to determine the effects of the immunosuppressants, cyclosporin A (CsA), tacrolimus and sirolimus, on drug transport by the ATP-binding cassette proteins, P-glycoprotein (Pgp; ABCB1), multidrug resistance protein-1 (MRP-1; ABCC1) and breast cancer resistance protein (BCRP; ABCG2), and the major vault protein lung resistance protein (LRP). Cyclosporine 86-89 ATP binding cassette subfamily B member 1 Homo sapiens 190-193 17031644-1 2007 PURPOSE: We sought to determine the effects of the immunosuppressants, cyclosporin A (CsA), tacrolimus and sirolimus, on drug transport by the ATP-binding cassette proteins, P-glycoprotein (Pgp; ABCB1), multidrug resistance protein-1 (MRP-1; ABCC1) and breast cancer resistance protein (BCRP; ABCG2), and the major vault protein lung resistance protein (LRP). Cyclosporine 86-89 ATP binding cassette subfamily B member 1 Homo sapiens 195-200 17031644-1 2007 PURPOSE: We sought to determine the effects of the immunosuppressants, cyclosporin A (CsA), tacrolimus and sirolimus, on drug transport by the ATP-binding cassette proteins, P-glycoprotein (Pgp; ABCB1), multidrug resistance protein-1 (MRP-1; ABCC1) and breast cancer resistance protein (BCRP; ABCG2), and the major vault protein lung resistance protein (LRP). Cyclosporine 86-89 ATP binding cassette subfamily B member 1 Homo sapiens 203-233 17031644-1 2007 PURPOSE: We sought to determine the effects of the immunosuppressants, cyclosporin A (CsA), tacrolimus and sirolimus, on drug transport by the ATP-binding cassette proteins, P-glycoprotein (Pgp; ABCB1), multidrug resistance protein-1 (MRP-1; ABCC1) and breast cancer resistance protein (BCRP; ABCG2), and the major vault protein lung resistance protein (LRP). Cyclosporine 86-89 ATP binding cassette subfamily B member 1 Homo sapiens 235-240 17545536-1 2007 PURPOSE: Increased clearance of drugs, such as oral cyclosporine, that are CYP3A and/or ABCB1 (P-gp/MDR1) substrates was reported in African-American compared with Caucasian patients. Cyclosporine 52-64 ATP binding cassette subfamily B member 1 Homo sapiens 88-93 17545536-1 2007 PURPOSE: Increased clearance of drugs, such as oral cyclosporine, that are CYP3A and/or ABCB1 (P-gp/MDR1) substrates was reported in African-American compared with Caucasian patients. Cyclosporine 52-64 ATP binding cassette subfamily B member 1 Homo sapiens 100-104 18192894-0 2008 Pharmacogenetics of cyclosporine in children suggests an age-dependent influence of ABCB1 polymorphisms. Cyclosporine 20-32 ATP binding cassette subfamily B member 1 Homo sapiens 84-89 18192894-9 2008 CONCLUSIONS: Although these data suggest an age-related effect of ABCB1 polymorphism on oral bioavailability, further studies are required on the predictive value of genotyping for individualization of cyclosporine dosing in children. Cyclosporine 202-214 ATP binding cassette subfamily B member 1 Homo sapiens 66-71 18197554-1 2008 The hypothesis tested was that ketoconazole can modulate P-glycoprotein, thereby altering cellular uptake and apparent permeability (P(app)) of multidrug-resistant substrates, such as cyclosporin A (CSA) and digoxin, across Caco-2, MDCKII-MDR1, and MDCKII wild-type cell transport models. Cyclosporine 184-197 ATP binding cassette subfamily B member 1 Homo sapiens 57-71 18277615-4 2008 Moreover, the BL-AP transport in the Caco-2 cells was significantly reduced by the cis-presence of P-glycoprotein (P-gp) inhibitors such as cyclosporine A, verapamil, and digoxin. Cyclosporine 140-154 ATP binding cassette subfamily B member 1 Homo sapiens 99-113 18277615-4 2008 Moreover, the BL-AP transport in the Caco-2 cells was significantly reduced by the cis-presence of P-glycoprotein (P-gp) inhibitors such as cyclosporine A, verapamil, and digoxin. Cyclosporine 140-154 ATP binding cassette subfamily B member 1 Homo sapiens 115-119 17947497-6 2008 Pgp inhibitors verapamil, cyclosporine A, or PSC833 increased doxorubicin accumulation in the MDR cells up to 79%, and it reversed drug resistance in these cells. Cyclosporine 26-40 ATP binding cassette subfamily B member 1 Homo sapiens 0-3 19668484-0 2007 MDR1 polymorphisms effect cyclosporine AUC0-4 values in Behcet"s disease patients. Cyclosporine 26-38 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 17697052-7 2007 Cyclosporin A-mediated inhibition of Pgp enhanced the uptake of morphine in lambda-carrageenan and control animals. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 37-40 17031644-5 2007 RESULTS: CsA increased cellular drug uptake in cells overexpressing Pgp, MRP-1 or BCRP and nuclear drug uptake in cells overexpressing LRP at the clinically achievable concentration of 2.5 microM. Cyclosporine 9-12 ATP binding cassette subfamily B member 1 Homo sapiens 73-78 17031644-9 2007 CONCLUSIONS: CsA, tacrolimus and sirolimus modulate drug transport by Pgp, MRP-1 and BCRP and CsA and sirolimus modulate drug transport by LRP at concentrations that differ from immunosuppressive concentrations and maximum tolerated concentrations. Cyclosporine 13-16 ATP binding cassette subfamily B member 1 Homo sapiens 70-73 17031644-9 2007 CONCLUSIONS: CsA, tacrolimus and sirolimus modulate drug transport by Pgp, MRP-1 and BCRP and CsA and sirolimus modulate drug transport by LRP at concentrations that differ from immunosuppressive concentrations and maximum tolerated concentrations. Cyclosporine 13-16 ATP binding cassette subfamily B member 1 Homo sapiens 75-80 17105736-0 2007 Influence of the Plasmodium falciparum P-glycoprotein homologue 1 (pfmdr1 gene product) on the antimalarial action of cyclosporin. Cyclosporine 118-129 ATP binding cassette subfamily B member 1 Homo sapiens 39-53 17519790-1 2007 BACKGROUND: Several single nucleotide polymorphisms (SNPs) in the multidrug resistance (MDR1) gene may play a role in the interindividual variation of cyclosporine A (CsA) absorption in renal transplant patients. Cyclosporine 167-170 ATP binding cassette subfamily B member 1 Homo sapiens 88-92 17519790-10 2007 CONCLUSIONS: MDR1 polymorphisms are associated with differences in CsA exposure only in the first posttransplant week. Cyclosporine 67-70 ATP binding cassette subfamily B member 1 Homo sapiens 13-17 17024347-0 2007 Expression of multidrug resistance P-glycoprotein on lymphocytes from nephrotic children treated with cyclosporine A and ACE-inhibitor. Cyclosporine 102-116 ATP binding cassette subfamily B member 1 Homo sapiens 35-49 17024347-1 2007 The aim of this work was to determine the expression of P-glycoprotein (P-gp) on peripheral lymphocytes (CD3) in children with steroid-dependent nephrotic syndrome (SDNS) during cyclosporine A (CyA) and ACE-inhibitor (ACE-I) treatment. Cyclosporine 178-192 ATP binding cassette subfamily B member 1 Homo sapiens 56-70 17024347-1 2007 The aim of this work was to determine the expression of P-glycoprotein (P-gp) on peripheral lymphocytes (CD3) in children with steroid-dependent nephrotic syndrome (SDNS) during cyclosporine A (CyA) and ACE-inhibitor (ACE-I) treatment. Cyclosporine 178-192 ATP binding cassette subfamily B member 1 Homo sapiens 72-76 17314201-7 2007 Cyclosporine A significantly inhibited Pgp-mediated transport of sitagliptin (IC50=1 microM). Cyclosporine 0-14 ATP binding cassette subfamily B member 1 Homo sapiens 39-42 17290357-6 2007 However, the addition of P-gp antagonists such as ciclosporin A and inhibitors of P-gp synthesis successfully reduce efflux of corticosteroids from lymphocytes in vitro and these results imply that P-gp antagonists and P-gp synthesis inhibitors could work in order to overcome drug-resistance in vivo. Cyclosporine 50-63 ATP binding cassette subfamily B member 1 Homo sapiens 25-29 17425754-2 2007 Ciclosporin is a substrate for P-gp and is metabolized by cytochrome P450 (CYP) 3A enzymes. Cyclosporine 0-11 ATP binding cassette subfamily B member 1 Homo sapiens 31-35 17425754-4 2007 MDR-1 genotypes of SNPs C1236T, G2677T/A and C3435T, as well as haplotypes C-G-C and T-T-T and CYP3A5*1 genotype (predictive of CYP3A5 expression), were related to ciclosporin blood concentrations measured at both 0 and 2 h after drug dosing in 197 stable renal transplant patients. Cyclosporine 164-175 ATP binding cassette subfamily B member 1 Homo sapiens 0-5 17425754-5 2007 Significant differences (of a magnitude unlikely to be relevant clinically) in dose-normalized blood ciclosporin concentrations were found only between MDR-1 genotypes of the C1236T SNP and between haplotype groups C-G-C and T-T-T in patients that were expressers of CYP3A5. Cyclosporine 101-112 ATP binding cassette subfamily B member 1 Homo sapiens 152-157 17556798-0 2007 Polymorphism in the P-glycoprotein drug transporter MDR1 gene in renal transplant patients treated with cyclosporin A in a Polish population. Cyclosporine 104-117 ATP binding cassette subfamily B member 1 Homo sapiens 20-34 17556798-0 2007 Polymorphism in the P-glycoprotein drug transporter MDR1 gene in renal transplant patients treated with cyclosporin A in a Polish population. Cyclosporine 104-117 ATP binding cassette subfamily B member 1 Homo sapiens 52-56 17556798-1 2007 P-glycoprotein (P-gp), the product of MDR1 gene, is a protein which mediates transmembrane transport of a great number of xenobiotics including cyclosporin A used as an immunosuppressive drug in patients with allogenic kidney grafts. Cyclosporine 144-157 ATP binding cassette subfamily B member 1 Homo sapiens 0-14 17556798-1 2007 P-glycoprotein (P-gp), the product of MDR1 gene, is a protein which mediates transmembrane transport of a great number of xenobiotics including cyclosporin A used as an immunosuppressive drug in patients with allogenic kidney grafts. Cyclosporine 144-157 ATP binding cassette subfamily B member 1 Homo sapiens 16-20 17556798-1 2007 P-glycoprotein (P-gp), the product of MDR1 gene, is a protein which mediates transmembrane transport of a great number of xenobiotics including cyclosporin A used as an immunosuppressive drug in patients with allogenic kidney grafts. Cyclosporine 144-157 ATP binding cassette subfamily B member 1 Homo sapiens 38-42 17268068-5 2007 P-gp function was estimated by transporter activity that was inferred from a decrease in fluorescent P-gp substrate Rhodamine 123 (Rh123) and its inhibition by cyclosporine A (CsA). Cyclosporine 160-174 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 17268068-5 2007 P-gp function was estimated by transporter activity that was inferred from a decrease in fluorescent P-gp substrate Rhodamine 123 (Rh123) and its inhibition by cyclosporine A (CsA). Cyclosporine 176-179 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 17244767-3 2007 Cyclosporine was used as a probe P-glycoprotein inhibitor at a high dose to evaluate the potential effect of potent P-glycoprotein inhibition on single-dose sitagliptin pharmacokinetics in healthy male subjects. Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 33-47 17244767-9 2007 These results rationalize the use of a single high-dose cyclosporine as a probe inhibitor of P-glycoprotein for compound candidates whose elimination is less dependent on CYP3A4-mediated metabolism. Cyclosporine 56-68 ATP binding cassette subfamily B member 1 Homo sapiens 93-107 17045309-8 2007 The AEDs phenytoin and levetiracetam were directionally transported by mouse but not human Pgp, whereas CsA was transported by both types of Pgp. Cyclosporine 104-107 ATP binding cassette subfamily B member 1 Homo sapiens 141-144 16636798-12 2007 As compared to cyclosporin A, these compounds showed reduced cellular toxicity and increased potency of BCRP and Pgp inhibition. Cyclosporine 15-28 ATP binding cassette subfamily B member 1 Homo sapiens 113-116 17105736-5 2007 We therefore investigated the possibility that the antimalarial target of cyclosporin might be a P-glycoprotein homologue. Cyclosporine 74-85 ATP binding cassette subfamily B member 1 Homo sapiens 97-111 17050779-4 2007 The rest of the Pgp molecules become recognized by this antibody only in the presence of certain substrates or modulators, including vinblastine, cyclosporine A (CsA), and SDZ PSC 833 (valspodar). Cyclosporine 162-165 ATP binding cassette subfamily B member 1 Homo sapiens 16-19 17050779-6 2007 Remarkably, the inhibitory binding of the antibody is brought about by coincubation with concentrations of CsA or SDZ PSC 833 approximately 20 times lower than what is necessary for Pgp inhibition when the modulators are applied alone. Cyclosporine 107-110 ATP binding cassette subfamily B member 1 Homo sapiens 182-185 17050779-7 2007 The feasibility of such a combinative treatment for in vivo multidrug resistance reversal was substantiated by the dramatic increase of daunorubicin accumulation in xenotransplanted Pgp+ tumors in response to a combined treatment with UIC2 and CsA, both administered at doses ineffective when applied alone. Cyclosporine 244-247 ATP binding cassette subfamily B member 1 Homo sapiens 182-185 17038319-8 2006 Cyclosporin A, a competitive P-glycoprotein inhibitor, restored intracellular dexamethasone levels in CD4+ T cells. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 29-43 17178259-9 2006 Cyclosporine (INN, ciclosporin) inhibits CYP3A4, P-glycoprotein (multidrug resistance protein 1), organic anion transporting polypeptide 1B1 (OATP1B1), and some other hepatic uptake transporters. Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 49-63 17042920-0 2006 Effects of genetic polymorphisms of CYP3A4, CYP3A5 and MDR1 on cyclosporine pharmacokinetics after renal transplantation. Cyclosporine 63-75 ATP binding cassette subfamily B member 1 Homo sapiens 55-59 17042920-4 2006 Interindividual differences in the activity and expression of the metabolising enzymes cytochrome P450 (CYP) 3A4 and 3A5 and the multidrug efflux pump P-glycoprotein (P-gp) contribute considerably to cyclosporine pharmacokinetics. Cyclosporine 200-212 ATP binding cassette subfamily B member 1 Homo sapiens 151-165 17042920-4 2006 Interindividual differences in the activity and expression of the metabolising enzymes cytochrome P450 (CYP) 3A4 and 3A5 and the multidrug efflux pump P-glycoprotein (P-gp) contribute considerably to cyclosporine pharmacokinetics. Cyclosporine 200-212 ATP binding cassette subfamily B member 1 Homo sapiens 167-171 17042920-7 2006 The aim of the present study was to evaluate retrospectively the effects of genetic polymorphisms of CYP3A4, CYP3A5 and MDR1 on cyclosporine dose adjusted trough blood concentration during the early period after renal transplantation in Chinese patients. Cyclosporine 128-140 ATP binding cassette subfamily B member 1 Homo sapiens 120-124 17106006-6 2006 Using genetic markers to adjust initial doses of cyclosporine or tacrolimus may prove difficult, considering the variety of polymorphism known to affect CYP3A4, CYP3A5, and the multidrug resistance-1 (MDR1) gene (the gene that codes for PGP). Cyclosporine 49-61 ATP binding cassette subfamily B member 1 Homo sapiens 177-199 16892207-7 2006 On the other hand, the corrected V(max)/K(m) value of human P-gp for cyclosporin A transport was 3.8-fold higher than that of monkey P-gp. Cyclosporine 69-82 ATP binding cassette subfamily B member 1 Homo sapiens 60-64 16892207-7 2006 On the other hand, the corrected V(max)/K(m) value of human P-gp for cyclosporin A transport was 3.8-fold higher than that of monkey P-gp. Cyclosporine 69-82 ATP binding cassette subfamily B member 1 Homo sapiens 133-137 16873536-7 2006 Inhibition of P-gp-mediated glucocorticoid efflux by cyclosporin A in BeWoMDR cells returned GR activation to levels similar to those in BeWo cells. Cyclosporine 53-66 ATP binding cassette subfamily B member 1 Homo sapiens 14-18 17112845-0 2006 MDR1 C3435T polymorphisms correlate with cyclosporine levels in de novo renal recipients. Cyclosporine 41-53 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 17112845-2 2006 PGP serves as a hydrophobic export pump that extrudes cyclosporine (CsA) across the luminal membrane thus preventing CsA absorption. Cyclosporine 54-66 ATP binding cassette subfamily B member 1 Homo sapiens 0-3 17112845-2 2006 PGP serves as a hydrophobic export pump that extrudes cyclosporine (CsA) across the luminal membrane thus preventing CsA absorption. Cyclosporine 68-71 ATP binding cassette subfamily B member 1 Homo sapiens 0-3 17112845-2 2006 PGP serves as a hydrophobic export pump that extrudes cyclosporine (CsA) across the luminal membrane thus preventing CsA absorption. Cyclosporine 117-120 ATP binding cassette subfamily B member 1 Homo sapiens 0-3 17112845-10 2006 CONCLUSIONS: MDR1 SNPs are correlated with CsA exposure in the early post-transplant period. Cyclosporine 43-46 ATP binding cassette subfamily B member 1 Homo sapiens 13-17 16969354-3 2006 Previously, we demonstrated that oral paclitaxel plus the P-gp inhibitor cyclosporin (CsA) is safe and results in adequate exposure to paclitaxel. Cyclosporine 73-84 ATP binding cassette subfamily B member 1 Homo sapiens 58-62 17045162-8 2006 CsA restored sensitivity to DOX and CIS, and enhanced the accumulation and efflux half-life of radiotracers in MDR1-expressing cell lines. Cyclosporine 0-3 ATP binding cassette subfamily B member 1 Homo sapiens 111-115 17075191-6 2006 However, the addition of P-gp antagonists such as ciclosporin A and inhibitors of P-gp synthesis successfully reduce efflux of corticosteroids from lymphocytes in vitro and these results imply that P-gp antagonists and P-gp synthesis inhibitors could work in order to overcome drug-resistance in vivo. Cyclosporine 50-63 ATP binding cassette subfamily B member 1 Homo sapiens 25-29 16759707-5 2006 Both tacrolimus and cyclosporine are substrates of Pgp, CYP3A4 and CYP3A5, and therefore, these molecules are potential pharmacokinetic factors with which to establish personalized dosage regimens for these drugs. Cyclosporine 20-32 ATP binding cassette subfamily B member 1 Homo sapiens 51-54 17096884-6 2006 Cyclosporine A and raloxifene (alone or combination) elevated the intracellular DNR concentration in K562/A02, down regulated P-gp and mdr-1 mRNA expressions. Cyclosporine 0-14 ATP binding cassette subfamily B member 1 Homo sapiens 126-130 17096884-6 2006 Cyclosporine A and raloxifene (alone or combination) elevated the intracellular DNR concentration in K562/A02, down regulated P-gp and mdr-1 mRNA expressions. Cyclosporine 0-14 ATP binding cassette subfamily B member 1 Homo sapiens 135-140 17178259-9 2006 Cyclosporine (INN, ciclosporin) inhibits CYP3A4, P-glycoprotein (multidrug resistance protein 1), organic anion transporting polypeptide 1B1 (OATP1B1), and some other hepatic uptake transporters. Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 65-95 17178259-9 2006 Cyclosporine (INN, ciclosporin) inhibits CYP3A4, P-glycoprotein (multidrug resistance protein 1), organic anion transporting polypeptide 1B1 (OATP1B1), and some other hepatic uptake transporters. Cyclosporine 19-30 ATP binding cassette subfamily B member 1 Homo sapiens 49-63 17178259-9 2006 Cyclosporine (INN, ciclosporin) inhibits CYP3A4, P-glycoprotein (multidrug resistance protein 1), organic anion transporting polypeptide 1B1 (OATP1B1), and some other hepatic uptake transporters. Cyclosporine 19-30 ATP binding cassette subfamily B member 1 Homo sapiens 65-95 16837925-0 2006 Role of P-glycoprotein in cyclosporine cytotoxicity in the cyclosporine-sirolimus interaction. Cyclosporine 26-38 ATP binding cassette subfamily B member 1 Homo sapiens 8-22 16837925-0 2006 Role of P-glycoprotein in cyclosporine cytotoxicity in the cyclosporine-sirolimus interaction. Cyclosporine 59-71 ATP binding cassette subfamily B member 1 Homo sapiens 8-22 16837925-2 2006 Cyclosporine and sirolimus are P-glycoprotein (Pgp) substrates. Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 31-45 16837925-2 2006 Cyclosporine and sirolimus are P-glycoprotein (Pgp) substrates. Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 47-50 16837925-3 2006 We hypothesized that the Pgp activity level may affect cyclosporine cytotoxicity by interfering with the ability of Pgp to remove cyclosporine from within tubular cells, and that an interaction between cyclosporine and sirolimus on Pgp function may explain the enhancement of cyclosporine nephrotoxicity by sirolimus. Cyclosporine 55-67 ATP binding cassette subfamily B member 1 Homo sapiens 25-28 16837925-3 2006 We hypothesized that the Pgp activity level may affect cyclosporine cytotoxicity by interfering with the ability of Pgp to remove cyclosporine from within tubular cells, and that an interaction between cyclosporine and sirolimus on Pgp function may explain the enhancement of cyclosporine nephrotoxicity by sirolimus. Cyclosporine 55-67 ATP binding cassette subfamily B member 1 Homo sapiens 116-119 16837925-3 2006 We hypothesized that the Pgp activity level may affect cyclosporine cytotoxicity by interfering with the ability of Pgp to remove cyclosporine from within tubular cells, and that an interaction between cyclosporine and sirolimus on Pgp function may explain the enhancement of cyclosporine nephrotoxicity by sirolimus. Cyclosporine 55-67 ATP binding cassette subfamily B member 1 Homo sapiens 116-119 16837925-3 2006 We hypothesized that the Pgp activity level may affect cyclosporine cytotoxicity by interfering with the ability of Pgp to remove cyclosporine from within tubular cells, and that an interaction between cyclosporine and sirolimus on Pgp function may explain the enhancement of cyclosporine nephrotoxicity by sirolimus. Cyclosporine 130-142 ATP binding cassette subfamily B member 1 Homo sapiens 25-28 16837925-3 2006 We hypothesized that the Pgp activity level may affect cyclosporine cytotoxicity by interfering with the ability of Pgp to remove cyclosporine from within tubular cells, and that an interaction between cyclosporine and sirolimus on Pgp function may explain the enhancement of cyclosporine nephrotoxicity by sirolimus. Cyclosporine 130-142 ATP binding cassette subfamily B member 1 Homo sapiens 116-119 16837925-3 2006 We hypothesized that the Pgp activity level may affect cyclosporine cytotoxicity by interfering with the ability of Pgp to remove cyclosporine from within tubular cells, and that an interaction between cyclosporine and sirolimus on Pgp function may explain the enhancement of cyclosporine nephrotoxicity by sirolimus. Cyclosporine 130-142 ATP binding cassette subfamily B member 1 Homo sapiens 116-119 16837925-3 2006 We hypothesized that the Pgp activity level may affect cyclosporine cytotoxicity by interfering with the ability of Pgp to remove cyclosporine from within tubular cells, and that an interaction between cyclosporine and sirolimus on Pgp function may explain the enhancement of cyclosporine nephrotoxicity by sirolimus. Cyclosporine 130-142 ATP binding cassette subfamily B member 1 Homo sapiens 25-28 16837925-3 2006 We hypothesized that the Pgp activity level may affect cyclosporine cytotoxicity by interfering with the ability of Pgp to remove cyclosporine from within tubular cells, and that an interaction between cyclosporine and sirolimus on Pgp function may explain the enhancement of cyclosporine nephrotoxicity by sirolimus. Cyclosporine 130-142 ATP binding cassette subfamily B member 1 Homo sapiens 116-119 16783494-4 2006 Since P-glycoprotein transports a wide range of drugs (e.g. antidepressants, antiepileptics, HIV protease inhibitors, cyclosporine, digoxin), its location in these tissues limits bioavailability of orally administered drugs and prevents entry of xenobiotics into the brain, testis and the fetus. Cyclosporine 118-130 ATP binding cassette subfamily B member 1 Homo sapiens 6-20 16756642-1 2006 AIM AND METHODS: P-glycoprotein (gp-170, P-gp) is a transmembrane transporter involved in drug, for example cyclosporine A, efflux from the cells thus limiting their intracellular concentration. Cyclosporine 108-122 ATP binding cassette subfamily B member 1 Homo sapiens 17-31 16756642-1 2006 AIM AND METHODS: P-glycoprotein (gp-170, P-gp) is a transmembrane transporter involved in drug, for example cyclosporine A, efflux from the cells thus limiting their intracellular concentration. Cyclosporine 108-122 ATP binding cassette subfamily B member 1 Homo sapiens 33-39 16756642-1 2006 AIM AND METHODS: P-glycoprotein (gp-170, P-gp) is a transmembrane transporter involved in drug, for example cyclosporine A, efflux from the cells thus limiting their intracellular concentration. Cyclosporine 108-122 ATP binding cassette subfamily B member 1 Homo sapiens 41-45 16756642-3 2006 The aim of the present study was to evaluate P-gp expression on the surface of CD4(+), CD8(+), CD19(+) and CD56(+) cells in kidney transplant patients treated with cyclosporine A as a main immunosuppressant, using flow cytometry. Cyclosporine 164-178 ATP binding cassette subfamily B member 1 Homo sapiens 45-49 16568474-7 2006 Even in a small population of viable cells, P-gp positive cells emitting low red fluorescence, gained on red fluorescence after P-gp inhibition with CsA permitting an evaluation of P-gp activity. Cyclosporine 149-152 ATP binding cassette subfamily B member 1 Homo sapiens 44-48 16568474-7 2006 Even in a small population of viable cells, P-gp positive cells emitting low red fluorescence, gained on red fluorescence after P-gp inhibition with CsA permitting an evaluation of P-gp activity. Cyclosporine 149-152 ATP binding cassette subfamily B member 1 Homo sapiens 128-132 16568474-7 2006 Even in a small population of viable cells, P-gp positive cells emitting low red fluorescence, gained on red fluorescence after P-gp inhibition with CsA permitting an evaluation of P-gp activity. Cyclosporine 149-152 ATP binding cassette subfamily B member 1 Homo sapiens 128-132 16568474-9 2006 Most importantly, the apoptotic cells could be distinguished by the loss of red fluorescence and the increase of green fluorescence without any change after P-gp inhibition with CsA. Cyclosporine 178-181 ATP binding cassette subfamily B member 1 Homo sapiens 157-161 16911928-6 2006 RESULTS: The SNPs of CYP3A and P-gp are closely correlated to the large variations of cyclosporine and tacrolimus dosage between different patients, although conflicting results were obtained by some authors. Cyclosporine 86-98 ATP binding cassette subfamily B member 1 Homo sapiens 31-35 16858127-3 2006 The present objectives are to elucidate the dysfunction of P-glycoprotein (P-gp) in addition to the opening of TJ by t-BuOOH at a high concentration condition using rhodamine123 (Rho123) as a P-gp substrate and cyclosporine A (CyA) as a P-gp inhibitor. Cyclosporine 211-225 ATP binding cassette subfamily B member 1 Homo sapiens 59-73 16858127-3 2006 The present objectives are to elucidate the dysfunction of P-glycoprotein (P-gp) in addition to the opening of TJ by t-BuOOH at a high concentration condition using rhodamine123 (Rho123) as a P-gp substrate and cyclosporine A (CyA) as a P-gp inhibitor. Cyclosporine 211-225 ATP binding cassette subfamily B member 1 Homo sapiens 75-79 16858127-3 2006 The present objectives are to elucidate the dysfunction of P-glycoprotein (P-gp) in addition to the opening of TJ by t-BuOOH at a high concentration condition using rhodamine123 (Rho123) as a P-gp substrate and cyclosporine A (CyA) as a P-gp inhibitor. Cyclosporine 227-230 ATP binding cassette subfamily B member 1 Homo sapiens 59-73 16858127-3 2006 The present objectives are to elucidate the dysfunction of P-glycoprotein (P-gp) in addition to the opening of TJ by t-BuOOH at a high concentration condition using rhodamine123 (Rho123) as a P-gp substrate and cyclosporine A (CyA) as a P-gp inhibitor. Cyclosporine 227-230 ATP binding cassette subfamily B member 1 Homo sapiens 75-79 16827636-0 2006 Association between cyclosporine concentration and genetic polymorphisms of CYP3A5 and MDR1 during the early stage after renal transplantation. Cyclosporine 20-32 ATP binding cassette subfamily B member 1 Homo sapiens 87-91 16647797-6 2006 Treatment with quinidine or cyclosporine A, which are P-gp inhibitors, decreased the P(app) of Rho-123 to the same degree in both monolayers. Cyclosporine 28-42 ATP binding cassette subfamily B member 1 Homo sapiens 54-58 16837925-3 2006 We hypothesized that the Pgp activity level may affect cyclosporine cytotoxicity by interfering with the ability of Pgp to remove cyclosporine from within tubular cells, and that an interaction between cyclosporine and sirolimus on Pgp function may explain the enhancement of cyclosporine nephrotoxicity by sirolimus. Cyclosporine 130-142 ATP binding cassette subfamily B member 1 Homo sapiens 116-119 16837925-3 2006 We hypothesized that the Pgp activity level may affect cyclosporine cytotoxicity by interfering with the ability of Pgp to remove cyclosporine from within tubular cells, and that an interaction between cyclosporine and sirolimus on Pgp function may explain the enhancement of cyclosporine nephrotoxicity by sirolimus. Cyclosporine 130-142 ATP binding cassette subfamily B member 1 Homo sapiens 25-28 16837925-3 2006 We hypothesized that the Pgp activity level may affect cyclosporine cytotoxicity by interfering with the ability of Pgp to remove cyclosporine from within tubular cells, and that an interaction between cyclosporine and sirolimus on Pgp function may explain the enhancement of cyclosporine nephrotoxicity by sirolimus. Cyclosporine 130-142 ATP binding cassette subfamily B member 1 Homo sapiens 116-119 16837925-3 2006 We hypothesized that the Pgp activity level may affect cyclosporine cytotoxicity by interfering with the ability of Pgp to remove cyclosporine from within tubular cells, and that an interaction between cyclosporine and sirolimus on Pgp function may explain the enhancement of cyclosporine nephrotoxicity by sirolimus. Cyclosporine 130-142 ATP binding cassette subfamily B member 1 Homo sapiens 116-119 16837925-8 2006 Pgp expression and function were confirmed in HRECs and cyclosporine and sirolimus were shown to be Pgp inhibitors in this model. Cyclosporine 56-68 ATP binding cassette subfamily B member 1 Homo sapiens 100-103 16837925-9 2006 Verapamil-induced inhibition of Pgp led to a significant increase in cellular concentration of cyclosporine (P<0.05). Cyclosporine 95-107 ATP binding cassette subfamily B member 1 Homo sapiens 32-35 16837925-10 2006 Cyclosporine exerted a concentration-dependent cytotoxic effect on HRECs that was significantly increased by inhibition of Pgp activity. Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 123-126 16837925-12 2006 These data demonstrate that Pgp plays a critical role in protecting renal epithelial cells from cyclosporine toxicity. Cyclosporine 96-108 ATP binding cassette subfamily B member 1 Homo sapiens 28-31 16837925-13 2006 The inhibitory effect of sirolimus on Pgp-mediated efflux and the cellular concentration of cyclosporine could explain the exacerbation of cyclosporine nephrotoxicity observed clinically. Cyclosporine 139-151 ATP binding cassette subfamily B member 1 Homo sapiens 38-41 16254147-0 2006 Randomized use of cyclosporin A (CsA) to modulate P-glycoprotein in children with AML in remission: Pediatric Oncology Group Study 9421. Cyclosporine 33-36 ATP binding cassette subfamily B member 1 Homo sapiens 50-64 16221533-6 2006 The efflux rate significantly decreased in the presence of metabolic inhibitors sodium azide and 2-deoxy-d-glucose, P-gp inhibitors cyclosporin A and valspodar, but not in the presence of MRPs inhibitor MK571. Cyclosporine 132-145 ATP binding cassette subfamily B member 1 Homo sapiens 116-120 16522547-4 2006 This study was planned to study the expression of P-glycoprotein/170 in patients with acute leukemia and the effect of Cyclosporin A (CSA) as a modulator of P-glycoprotein functional activity. Cyclosporine 119-132 ATP binding cassette subfamily B member 1 Homo sapiens 157-171 16451059-7 2006 P-gp inhibition by CsA confirmed that these new analogues are no longer P-gp substrates. Cyclosporine 19-22 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 16299163-8 2006 Moreover, basal-to-apical transport of [3H]CsA in the Caco-2 cell monolayer was not affected by DHA but was decreased by valspodar (PSC 833), a P-gp inhibitor. Cyclosporine 43-46 ATP binding cassette subfamily B member 1 Homo sapiens 144-148 16522547-4 2006 This study was planned to study the expression of P-glycoprotein/170 in patients with acute leukemia and the effect of Cyclosporin A (CSA) as a modulator of P-glycoprotein functional activity. Cyclosporine 134-137 ATP binding cassette subfamily B member 1 Homo sapiens 157-171 16259758-5 2005 In the presence of ciclosporin and verapamil, potent inhibitors of P-glycoprotein (P-gp)/MRP2, the absorptive transport was enhanced and secretory efflux was diminished. Cyclosporine 19-30 ATP binding cassette subfamily B member 1 Homo sapiens 67-81 16455045-6 2006 Finally, we observed competitive and non-competitive interactions between one of such dihydro-beta-agarofurans (Mama12) and classical Pgp modulators such as cyclosporin A, verapamil, progesterone, vinblastine and GF120918. Cyclosporine 157-170 ATP binding cassette subfamily B member 1 Homo sapiens 134-137 16438909-0 2005 Relationship between MDR1 polymorphism and blood concentration of cyclosporine A. Cyclosporine 66-80 ATP binding cassette subfamily B member 1 Homo sapiens 21-25 16051742-1 2005 The peripheral benzodiazepine receptor (pBR) ligand, PK11195, promotes mitochondrial apoptosis and blocks P-glycoprotein (Pgp)-mediated drug efflux to chemosensitize cancer cells at least as well or better than the Pgp modulator, cyclosporine A (CSA). Cyclosporine 230-244 ATP binding cassette subfamily B member 1 Homo sapiens 122-125 16051742-1 2005 The peripheral benzodiazepine receptor (pBR) ligand, PK11195, promotes mitochondrial apoptosis and blocks P-glycoprotein (Pgp)-mediated drug efflux to chemosensitize cancer cells at least as well or better than the Pgp modulator, cyclosporine A (CSA). Cyclosporine 246-249 ATP binding cassette subfamily B member 1 Homo sapiens 122-125 16051742-5 2005 PK11195 and CSA bind noncompetitively in Pgp-expressing cells, indicating that PK11195 interacts with Pgp at sites that are distinct from CSA-binding sites. Cyclosporine 12-15 ATP binding cassette subfamily B member 1 Homo sapiens 41-44 16051742-5 2005 PK11195 and CSA bind noncompetitively in Pgp-expressing cells, indicating that PK11195 interacts with Pgp at sites that are distinct from CSA-binding sites. Cyclosporine 12-15 ATP binding cassette subfamily B member 1 Homo sapiens 102-105 16377671-5 2006 Hepatobiliary excretion experiments revealed that cyclosporine almost completely inhibited the biliary clearance of telithromycin, suggesting that telithromycin is a substrate of P glycoprotein and a potential substrate of Mrp2. Cyclosporine 50-62 ATP binding cassette subfamily B member 1 Homo sapiens 179-193 16364863-3 2005 However, recent reports have suggested that carvedilol, but not metoprolol, modulates P-glycoprotein (P-gp), a membrane protein that regulates CsA absorption. Cyclosporine 143-146 ATP binding cassette subfamily B member 1 Homo sapiens 86-100 16364863-3 2005 However, recent reports have suggested that carvedilol, but not metoprolol, modulates P-glycoprotein (P-gp), a membrane protein that regulates CsA absorption. Cyclosporine 143-146 ATP binding cassette subfamily B member 1 Homo sapiens 102-106 16364863-16 2005 Although carvedilol and CsA do not interact at the level of cytochrome P450 system, it appears that carvedilol influences CsA levels through its effects on P-gp. Cyclosporine 122-125 ATP binding cassette subfamily B member 1 Homo sapiens 156-160 16259758-5 2005 In the presence of ciclosporin and verapamil, potent inhibitors of P-glycoprotein (P-gp)/MRP2, the absorptive transport was enhanced and secretory efflux was diminished. Cyclosporine 19-30 ATP binding cassette subfamily B member 1 Homo sapiens 83-87 16159384-4 2005 Observations that cyclosporin A, and certain other substances, inhibit both the proteasome and P-glycoprotein led us to investigate whether anthracyclines, well known substrates of P-gp, also inhibit the function of the proteasome. Cyclosporine 18-31 ATP binding cassette subfamily B member 1 Homo sapiens 95-109 15876424-7 2005 In the Be-Wo cell line, methadone and paclitaxel uptake was also increased in the presence of the P-gp inhibitor cyclosporin A. Cyclosporine 113-126 ATP binding cassette subfamily B member 1 Homo sapiens 98-102 16020127-4 2005 The aim of this study was to analyze the P-gP-modulating effects of PSC 833, a cyclosporine derivate, and verapamil on the chemotherapy of HB in vivo. Cyclosporine 79-91 ATP binding cassette subfamily B member 1 Homo sapiens 41-45 16095503-8 2005 Concomitantly, a profound decrease of hepatic and intestinal PGP and an increase of intestinal CYP3A4 were noted with CsA, whereas no effect was seen after atorvastatin therapy with or without Tac. Cyclosporine 118-121 ATP binding cassette subfamily B member 1 Homo sapiens 61-64 16043202-12 2005 Inhibitors such as calcium-channel blockers (verapamil), cyclosporin A, ONT-093, and XR9576 can modulate the P-gp functionality. Cyclosporine 57-70 ATP binding cassette subfamily B member 1 Homo sapiens 109-113 15530432-8 2004 By contrast, all misprocessed P-gp mutants were rescued by the chemical chaperone/drug substrate cyclosporin A in a dose-dependent manner. Cyclosporine 97-110 ATP binding cassette subfamily B member 1 Homo sapiens 30-34 15772250-0 2005 ABCB1 genotype of the donor but not of the recipient is a major risk factor for cyclosporine-related nephrotoxicity after renal transplantation. Cyclosporine 80-92 ATP binding cassette subfamily B member 1 Homo sapiens 0-5 15772250-2 2005 Animal models and in vivo studies indicate that the transmembrane efflux pump P-glycoprotein contributes substantially to CsA nephrotoxicity. Cyclosporine 122-125 ATP binding cassette subfamily B member 1 Homo sapiens 78-92 15772250-3 2005 It was hypothesized that the TT genotype at the ABCB1 3435C-->T polymorphism, which is associated with decreased expression of P-glycoprotein in renal tissue, is a risk factor for developing CsA nephrotoxicity. Cyclosporine 194-197 ATP binding cassette subfamily B member 1 Homo sapiens 48-53 15772250-3 2005 It was hypothesized that the TT genotype at the ABCB1 3435C-->T polymorphism, which is associated with decreased expression of P-glycoprotein in renal tissue, is a risk factor for developing CsA nephrotoxicity. Cyclosporine 194-197 ATP binding cassette subfamily B member 1 Homo sapiens 130-144 15772250-7 2005 The P-glycoprotein low expressor genotype 3435TT only of renal organ donors but not of the recipients was overrepresented in patients with CsA nephrotoxicity as compared with patients without toxicity (chi2 = 10.5; P = 0.005). Cyclosporine 139-142 ATP binding cassette subfamily B member 1 Homo sapiens 4-18 15772250-9 2005 In a multivariate model that included several other nongenetic covariates, only the donor"s ABCB1 3435TT genotype was strongly associated with CsA nephrotoxicity (odds ratio, 13.4; 95% confidence interval, 1.2 to 148; P = 0.034). Cyclosporine 143-146 ATP binding cassette subfamily B member 1 Homo sapiens 92-97 15772250-10 2005 A dominant role of the donor"s ABCB1 genotype was identified for development of CsA nephrotoxicity. Cyclosporine 80-83 ATP binding cassette subfamily B member 1 Homo sapiens 31-36 15772250-11 2005 This suggests that P-glycoprotein is an important factor in CsA nephrotoxicity. Cyclosporine 60-63 ATP binding cassette subfamily B member 1 Homo sapiens 19-33 16019806-8 2005 CsA inhibits P-gp in a different way from its metabolites, whereas roquefortine C activates P-gp and also inhibits P450-3A and other haemoproteins. Cyclosporine 0-3 ATP binding cassette subfamily B member 1 Homo sapiens 13-17 15598974-3 2005 In this study, we demonstrate that human ABCG2 and P-glycoprotein, despite overlapping substrate specificities, differ in sensitivity to the immunomodulator cyclosporin A. Cyclosporine 157-170 ATP binding cassette subfamily B member 1 Homo sapiens 51-65 15598974-5 2005 By flow cytometric analysis using the fluorescent substrates rhodamine 123 and mitoxantrone, we showed that cyclosporin A inhibits P-gp function at low micromolar concentrations, whereas ABCG2 function was unaffected. Cyclosporine 108-121 ATP binding cassette subfamily B member 1 Homo sapiens 131-135 15882134-5 2005 This review describes polymorphisms of the genes coding for P-gp and CYPs, and focuses on the compounds cyclosporin and tacrolimus. Cyclosporine 104-115 ATP binding cassette subfamily B member 1 Homo sapiens 60-64 15542593-11 2005 Mutant L1260A P-gp exhibited drug-stimulated ATPase activities similar to that of wild-type enzyme after rescue with cyclosporin A. Cyclosporine 117-130 ATP binding cassette subfamily B member 1 Homo sapiens 14-18 15961982-11 2005 The modest inhibition of human BBB P-gp by cyclosporine has implications for P-gp-based drug interactions at the human BBB. Cyclosporine 43-55 ATP binding cassette subfamily B member 1 Homo sapiens 35-39 15961982-11 2005 The modest inhibition of human BBB P-gp by cyclosporine has implications for P-gp-based drug interactions at the human BBB. Cyclosporine 43-55 ATP binding cassette subfamily B member 1 Homo sapiens 77-81 15788683-2 2005 The Pgp modulator cyclosporin A has shown clinical efficacy in AML, whereas its analogue PSC-833 has not. Cyclosporine 18-31 ATP binding cassette subfamily B member 1 Homo sapiens 4-7 15788683-6 2005 RESULTS: Cyclosporin A enhanced retention of the substrate drug mitoxantrone in cells overexpressing Pgp (HL60/VCR), MRP-1 (HL60/ADR), and BCRP (8226/MR20, HEK-293 482R) and increased cytotoxicity 6-, 4-, 4-, and 3-fold, respectively. Cyclosporine 9-22 ATP binding cassette subfamily B member 1 Homo sapiens 101-104 15788683-10 2005 CONCLUSIONS: Cyclosporin A modulates Pgp, MRP-1, BCRP, and LRP, and this broad-spectrum activity may contribute to its clinical efficacy. Cyclosporine 13-26 ATP binding cassette subfamily B member 1 Homo sapiens 37-40 15744065-3 2005 Since cyclosporin A (MDR1 P-gp inhibitor) but not MK571 (MRP1 inhibitor) inhibited SAL-induced PS externalization, it was suggested that MDR1 P-gp is involved in this phenomenon. Cyclosporine 6-19 ATP binding cassette subfamily B member 1 Homo sapiens 21-25 15744065-3 2005 Since cyclosporin A (MDR1 P-gp inhibitor) but not MK571 (MRP1 inhibitor) inhibited SAL-induced PS externalization, it was suggested that MDR1 P-gp is involved in this phenomenon. Cyclosporine 6-19 ATP binding cassette subfamily B member 1 Homo sapiens 137-141 15886424-4 2005 Cyclosporine A which is used as an immunosuppressive drug in patients with allogenic kidney grafts is a substrate for P-gp. Cyclosporine 0-14 ATP binding cassette subfamily B member 1 Homo sapiens 118-122 15886424-6 2005 It was assumed that polymorphism of MDR1 gene which is associated with change in P-gp activity plays a role in induction of tremor in some patients with allogenic kidney graft treated with cyclosporine A. Cyclosporine 189-203 ATP binding cassette subfamily B member 1 Homo sapiens 36-40 15886424-6 2005 It was assumed that polymorphism of MDR1 gene which is associated with change in P-gp activity plays a role in induction of tremor in some patients with allogenic kidney graft treated with cyclosporine A. Cyclosporine 189-203 ATP binding cassette subfamily B member 1 Homo sapiens 81-85 15738623-8 2005 The inhibitory effects of QPA on P-gp were more effective than those of the typical P-gp inhibitors cyclosporin A and verapamil. Cyclosporine 100-113 ATP binding cassette subfamily B member 1 Homo sapiens 84-88 15661399-11 2005 P-gp inhibitors GF120918 and cyclosporin A enhanced ceramide-induced apoptosis in the p-gp expressing cells. Cyclosporine 29-42 ATP binding cassette subfamily B member 1 Homo sapiens 86-90 14962898-3 2004 We also previously reported that inhibition of drug transport by the Pgp modulator, cyclosporine A (CSA), can increase GO sensitivity in Pgp(+) AML cells and that the peripheral benzodiazepine receptor ligand, PK11195, sensitizes AML cells to standard chemotherapeutics both by inhibiting Pgp-mediated efflux and by promoting mitochondrial apoptosis. Cyclosporine 84-98 ATP binding cassette subfamily B member 1 Homo sapiens 69-72 15592326-1 2004 OBJECTIVE: Our objective was to determine the relationship between single nucleotide polymorphisms (SNPs) in the multidrug resistance 1 (MDR-1) gene and the cytochrome P450 (CYP) genes CYP3A4 and CYP3A5 and the pharmacokinetics of cyclosporine (INN, ciclosporin). Cyclosporine 231-243 ATP binding cassette subfamily B member 1 Homo sapiens 113-135 15592326-1 2004 OBJECTIVE: Our objective was to determine the relationship between single nucleotide polymorphisms (SNPs) in the multidrug resistance 1 (MDR-1) gene and the cytochrome P450 (CYP) genes CYP3A4 and CYP3A5 and the pharmacokinetics of cyclosporine (INN, ciclosporin). Cyclosporine 231-243 ATP binding cassette subfamily B member 1 Homo sapiens 137-142 15592326-1 2004 OBJECTIVE: Our objective was to determine the relationship between single nucleotide polymorphisms (SNPs) in the multidrug resistance 1 (MDR-1) gene and the cytochrome P450 (CYP) genes CYP3A4 and CYP3A5 and the pharmacokinetics of cyclosporine (INN, ciclosporin). Cyclosporine 250-261 ATP binding cassette subfamily B member 1 Homo sapiens 113-135 15592326-1 2004 OBJECTIVE: Our objective was to determine the relationship between single nucleotide polymorphisms (SNPs) in the multidrug resistance 1 (MDR-1) gene and the cytochrome P450 (CYP) genes CYP3A4 and CYP3A5 and the pharmacokinetics of cyclosporine (INN, ciclosporin). Cyclosporine 250-261 ATP binding cassette subfamily B member 1 Homo sapiens 137-142 15569157-7 2004 Cyclosporin A, a competitive inhibitor of P-glycoprotein, recovered intracellular dexamethasone levels in lymphocytes. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 42-56 15813023-0 2004 [Effect of MDR1 polymorphic expression on oral disposition of cyclosporine A]. Cyclosporine 62-76 ATP binding cassette subfamily B member 1 Homo sapiens 11-15 15307840-0 2004 CYP3A4 and P-glycoprotein activity in healthy controls and transplant patients on cyclosporin vs. tacrolimus vs. sirolimus. Cyclosporine 82-93 ATP binding cassette subfamily B member 1 Homo sapiens 11-25 15472471-3 2004 In both cells, the accumulation increased with the addition of PCB-126 and cyclosporine A (CYA), which are P-glycoprotein modulators, though the magnitudes were different in these two cell groups as well as for these two chemicals. Cyclosporine 75-89 ATP binding cassette subfamily B member 1 Homo sapiens 107-121 15472471-3 2004 In both cells, the accumulation increased with the addition of PCB-126 and cyclosporine A (CYA), which are P-glycoprotein modulators, though the magnitudes were different in these two cell groups as well as for these two chemicals. Cyclosporine 91-94 ATP binding cassette subfamily B member 1 Homo sapiens 107-121 15322232-4 2004 Moreover, exposing isolated capillaries to the PXR ligands pregnenolone-16alpha-carbonitrile (PCN) and dexamethasone increased p-glycoprotein expression and p-glycoprotein-specific transport of a fluorescent cyclosporine A derivative into capillary lumens. Cyclosporine 208-222 ATP binding cassette subfamily B member 1 Homo sapiens 157-171 15494300-8 2004 In clinical trials in MDS, first-generation Pgp blockers, such as cyclosporin-A and verapamil, were minimally effective, non-specific, and toxic. Cyclosporine 66-79 ATP binding cassette subfamily B member 1 Homo sapiens 44-47 15239129-5 2004 Furthermore, using rhodamine-123 efflux assays, we observed a significant decrease in P-glycoprotein activity in caveolin-1 overexpressing cells, similar to that observed with 5 microM cyclosporine A or 10 microM verapamil, 2 inhibitors of P-glycoprotein activity. Cyclosporine 185-199 ATP binding cassette subfamily B member 1 Homo sapiens 86-100 15307840-1 2004 This study aimed to determine the impact of maintenance immunosuppressive therapy with cyclosporin A (CsA), tacrolimus (FK506) and sirolimus (Rapa) on the in vivo activity of both intestinal and hepatic cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (PGP) in renal transplant patients. Cyclosporine 102-105 ATP binding cassette subfamily B member 1 Homo sapiens 236-250 15307840-1 2004 This study aimed to determine the impact of maintenance immunosuppressive therapy with cyclosporin A (CsA), tacrolimus (FK506) and sirolimus (Rapa) on the in vivo activity of both intestinal and hepatic cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (PGP) in renal transplant patients. Cyclosporine 102-105 ATP binding cassette subfamily B member 1 Homo sapiens 252-255 15307840-5 2004 A significant increase in intestinal CYP3A4 activity and a significant decrease in hepatic and intestinal PGP activity was seen in patients on CsA in comparison with those on FK506 or Rapa (p < 0.01). Cyclosporine 143-146 ATP binding cassette subfamily B member 1 Homo sapiens 106-109 14962898-3 2004 We also previously reported that inhibition of drug transport by the Pgp modulator, cyclosporine A (CSA), can increase GO sensitivity in Pgp(+) AML cells and that the peripheral benzodiazepine receptor ligand, PK11195, sensitizes AML cells to standard chemotherapeutics both by inhibiting Pgp-mediated efflux and by promoting mitochondrial apoptosis. Cyclosporine 84-98 ATP binding cassette subfamily B member 1 Homo sapiens 137-140 14962898-3 2004 We also previously reported that inhibition of drug transport by the Pgp modulator, cyclosporine A (CSA), can increase GO sensitivity in Pgp(+) AML cells and that the peripheral benzodiazepine receptor ligand, PK11195, sensitizes AML cells to standard chemotherapeutics both by inhibiting Pgp-mediated efflux and by promoting mitochondrial apoptosis. Cyclosporine 84-98 ATP binding cassette subfamily B member 1 Homo sapiens 137-140 14962898-3 2004 We also previously reported that inhibition of drug transport by the Pgp modulator, cyclosporine A (CSA), can increase GO sensitivity in Pgp(+) AML cells and that the peripheral benzodiazepine receptor ligand, PK11195, sensitizes AML cells to standard chemotherapeutics both by inhibiting Pgp-mediated efflux and by promoting mitochondrial apoptosis. Cyclosporine 100-103 ATP binding cassette subfamily B member 1 Homo sapiens 69-72 14962898-3 2004 We also previously reported that inhibition of drug transport by the Pgp modulator, cyclosporine A (CSA), can increase GO sensitivity in Pgp(+) AML cells and that the peripheral benzodiazepine receptor ligand, PK11195, sensitizes AML cells to standard chemotherapeutics both by inhibiting Pgp-mediated efflux and by promoting mitochondrial apoptosis. Cyclosporine 100-103 ATP binding cassette subfamily B member 1 Homo sapiens 137-140 14962898-3 2004 We also previously reported that inhibition of drug transport by the Pgp modulator, cyclosporine A (CSA), can increase GO sensitivity in Pgp(+) AML cells and that the peripheral benzodiazepine receptor ligand, PK11195, sensitizes AML cells to standard chemotherapeutics both by inhibiting Pgp-mediated efflux and by promoting mitochondrial apoptosis. Cyclosporine 100-103 ATP binding cassette subfamily B member 1 Homo sapiens 137-140 15116055-0 2004 CYP3A5 and MDR1 genetic polymorphisms and cyclosporine pharmacokinetics after renal transplantation. Cyclosporine 42-54 ATP binding cassette subfamily B member 1 Homo sapiens 11-15 15116055-1 2004 BACKGROUND: The immunosuppressive drug cyclosporine (INN, ciclosporin), whose pharmacokinetic characteristics vary greatly among individuals, is a substrate for cytochrome P450 (CYP) 3A and P-glycoprotein, the product of the multidrug resistance 1 (MDR1) gene. Cyclosporine 39-51 ATP binding cassette subfamily B member 1 Homo sapiens 190-204 15116055-1 2004 BACKGROUND: The immunosuppressive drug cyclosporine (INN, ciclosporin), whose pharmacokinetic characteristics vary greatly among individuals, is a substrate for cytochrome P450 (CYP) 3A and P-glycoprotein, the product of the multidrug resistance 1 (MDR1) gene. Cyclosporine 39-51 ATP binding cassette subfamily B member 1 Homo sapiens 225-247 15116055-1 2004 BACKGROUND: The immunosuppressive drug cyclosporine (INN, ciclosporin), whose pharmacokinetic characteristics vary greatly among individuals, is a substrate for cytochrome P450 (CYP) 3A and P-glycoprotein, the product of the multidrug resistance 1 (MDR1) gene. Cyclosporine 39-51 ATP binding cassette subfamily B member 1 Homo sapiens 249-253 15116055-1 2004 BACKGROUND: The immunosuppressive drug cyclosporine (INN, ciclosporin), whose pharmacokinetic characteristics vary greatly among individuals, is a substrate for cytochrome P450 (CYP) 3A and P-glycoprotein, the product of the multidrug resistance 1 (MDR1) gene. Cyclosporine 58-69 ATP binding cassette subfamily B member 1 Homo sapiens 190-204 15116055-1 2004 BACKGROUND: The immunosuppressive drug cyclosporine (INN, ciclosporin), whose pharmacokinetic characteristics vary greatly among individuals, is a substrate for cytochrome P450 (CYP) 3A and P-glycoprotein, the product of the multidrug resistance 1 (MDR1) gene. Cyclosporine 58-69 ATP binding cassette subfamily B member 1 Homo sapiens 225-247 15116055-1 2004 BACKGROUND: The immunosuppressive drug cyclosporine (INN, ciclosporin), whose pharmacokinetic characteristics vary greatly among individuals, is a substrate for cytochrome P450 (CYP) 3A and P-glycoprotein, the product of the multidrug resistance 1 (MDR1) gene. Cyclosporine 58-69 ATP binding cassette subfamily B member 1 Homo sapiens 249-253 14724652-6 2004 The modulation of Pgp by cyclosporin A (CSA) readily restored imatinib cytotoxicity in these cells. Cyclosporine 25-38 ATP binding cassette subfamily B member 1 Homo sapiens 18-21 14985103-4 2004 Here we have extended these observations to 44 Pgp interacting agents, and found that only 8 fall into the cyclosporin-like category, inducing a conformational state characterized by the complete UIC2 dominance. Cyclosporine 107-118 ATP binding cassette subfamily B member 1 Homo sapiens 47-50 15110230-3 2004 In contrast, many other compounds such as calcium channel blockers (verapamil) and immunosupressors (cyclosporine-A) are able to inhibit P-gp function. Cyclosporine 101-115 ATP binding cassette subfamily B member 1 Homo sapiens 137-141 14985103-3 2004 In the case of cyclosporin A, vinblastine or valinomycin, this up-shift was found to be concomitant with the near-complete suppression of labeling with other mAbs specific for Pgp epitopes overlapping with UIC2, while pre-treatment with verapamil or Tween 80 brings about a modest suppression. Cyclosporine 15-28 ATP binding cassette subfamily B member 1 Homo sapiens 176-179 14724652-6 2004 The modulation of Pgp by cyclosporin A (CSA) readily restored imatinib cytotoxicity in these cells. Cyclosporine 40-43 ATP binding cassette subfamily B member 1 Homo sapiens 18-21 14662772-5 2004 We now show that MDR1 inhibitors, cyclosporin A or ketoconazole, inhibit neutral glycosphingolipid biosynthesis in 11 of 12 cell lines tested. Cyclosporine 34-47 ATP binding cassette subfamily B member 1 Homo sapiens 17-21 14662772-7 2004 Microsomal lactosyl ceramide and globotriaosyl ceramide synthesis from endogenous or exogenously added liposomal glucosyl ceramide was inhibited by cyclosporin A, consistent with a direct role for MDR1/glucosyl ceramide translocase activity in their synthesis. Cyclosporine 148-161 ATP binding cassette subfamily B member 1 Homo sapiens 197-201 15217301-6 2004 With regard to the variability, polymorphisms of the MDR1 gene have recently been reported to be associated with alterations in disposition kinetics and interaction profiles of clinically useful drugs, including digoxin, fexofenadine, ciclosporin and talinolol. Cyclosporine 235-246 ATP binding cassette subfamily B member 1 Homo sapiens 53-57 15084935-0 2004 Whole-blood cultures from renal-transplant patients stimulated ex vivo show that the effects of cyclosporine on lymphocyte proliferation are related to P-glycoprotein expression. Cyclosporine 96-108 ATP binding cassette subfamily B member 1 Homo sapiens 152-166 15084935-1 2004 BACKGROUND: Cyclosporine (CsA) is a substrate for the MDR-1 gene product P-glycoprotein (P-gp). Cyclosporine 12-24 ATP binding cassette subfamily B member 1 Homo sapiens 54-59 15084935-1 2004 BACKGROUND: Cyclosporine (CsA) is a substrate for the MDR-1 gene product P-glycoprotein (P-gp). Cyclosporine 12-24 ATP binding cassette subfamily B member 1 Homo sapiens 73-87 15084935-1 2004 BACKGROUND: Cyclosporine (CsA) is a substrate for the MDR-1 gene product P-glycoprotein (P-gp). Cyclosporine 12-24 ATP binding cassette subfamily B member 1 Homo sapiens 89-93 15167702-0 2004 The effect of CYP3A5 and MDR1 (ABCB1) polymorphisms on cyclosporine and tacrolimus dose requirements and trough blood levels in stable renal transplant patients. Cyclosporine 55-67 ATP binding cassette subfamily B member 1 Homo sapiens 31-36 15167702-4 2004 The objective of this study was to investigate the effect of CYP3A5 and MDR1 (ABCB1) polymorphisms on cyclosporine and tacrolimus dose requirements and trough blood concentrations in stable transplant patients. Cyclosporine 102-114 ATP binding cassette subfamily B member 1 Homo sapiens 72-76 15167702-4 2004 The objective of this study was to investigate the effect of CYP3A5 and MDR1 (ABCB1) polymorphisms on cyclosporine and tacrolimus dose requirements and trough blood concentrations in stable transplant patients. Cyclosporine 102-114 ATP binding cassette subfamily B member 1 Homo sapiens 78-83 14653942-4 2003 The effects of a P-glycoprotein (P-gp) inhibitor-cyclosporin A, some surfactants, and lower pH on the transepithelial transport of CPU-86017 were also observed. Cyclosporine 49-62 ATP binding cassette subfamily B member 1 Homo sapiens 33-37 14713364-12 2003 The current study suggests that TET enhances the cytotoxicity of anticancer drugs in the P-gp expressing MDR cell line by modulating P-gp in a different manner to the well-known P-gp inhibitor CsA. Cyclosporine 193-196 ATP binding cassette subfamily B member 1 Homo sapiens 89-93 14564197-9 2003 Two polymorphisms (C3435T and G2677[A/T]) of the MDR-1 gene have been shown to influence the bioavailability and toxicity of tacrolimus and cyclosporin. Cyclosporine 140-151 ATP binding cassette subfamily B member 1 Homo sapiens 49-54 14705863-4 2003 Increased expression of MDR1 reduces the bioavailability of MDR1 substrates such as digoxin, cyclosporin, and taxol. Cyclosporine 93-104 ATP binding cassette subfamily B member 1 Homo sapiens 24-28 14705863-4 2003 Increased expression of MDR1 reduces the bioavailability of MDR1 substrates such as digoxin, cyclosporin, and taxol. Cyclosporine 93-104 ATP binding cassette subfamily B member 1 Homo sapiens 60-64 12975485-4 2003 A P-gp modulator, cyclosporin A, inhibited the basal-to-apical transport in L-MDR1 cells. Cyclosporine 18-31 ATP binding cassette subfamily B member 1 Homo sapiens 2-6 12975485-7 2003 The Ki values for the inhibition of P-gp function by cyclosporin A and imatinib mesilate were estimated to be 6.1 and 18.3 muM, respectively, using a calcein-AM efflux assay. Cyclosporine 53-66 ATP binding cassette subfamily B member 1 Homo sapiens 36-40 12817518-0 2003 The effect of CYP3A5 and MDR1 polymorphic expression on cyclosporine oral disposition in renal transplant patients. Cyclosporine 56-68 ATP binding cassette subfamily B member 1 Homo sapiens 25-29 14526408-0 2003 Enhanced expression of enterocyte P-glycoprotein depresses cyclosporine bioavailability in a recipient of living donor liver transplantation. Cyclosporine 59-71 ATP binding cassette subfamily B member 1 Homo sapiens 34-48 12848778-1 2003 AIMS: To investigate the frequency of the single nucleotide polymorphism C3435T in exon 26 of the MDR1 gene in Asians and to determine the functional significance of this SNP with the clinical pharmacokinetics of oral cyclosporin (Neoral) in 10 stable heart transplant patients. Cyclosporine 218-229 ATP binding cassette subfamily B member 1 Homo sapiens 98-102 12966368-0 2003 Genetic polymorphisms of the CYP3A4, CYP3A5, and MDR-1 genes and pharmacokinetics of the calcineurin inhibitors cyclosporine and tacrolimus. Cyclosporine 112-124 ATP binding cassette subfamily B member 1 Homo sapiens 49-54 12966368-3 2003 OBJECTIVE: Our objective was to determine the role of genetic polymorphisms in CYP3A4, CYP3A5, and MDR-1 with respect to interindividual variability in cyclosporine and tacrolimus pharmacokinetics. Cyclosporine 152-164 ATP binding cassette subfamily B member 1 Homo sapiens 99-104 12948013-5 2003 RESULTS: In situ experimental results revealed that the extent to which the intestinal absorption is affected by P-gp was in the following order: quinidine > ritonavir > loperamide, verapamil, daunomycin > digoxin, cyclosporin A > dexamethasone, and vinblastine. Cyclosporine 224-237 ATP binding cassette subfamily B member 1 Homo sapiens 113-117 12817518-1 2003 Variability in CYP3A (CYP3A4/5) and P-glycoprotein (human MDR1 gene product) activity underlies interindividual differences in oral cyclosporine (CsA) bioavailability. Cyclosporine 132-144 ATP binding cassette subfamily B member 1 Homo sapiens 36-50 12817518-1 2003 Variability in CYP3A (CYP3A4/5) and P-glycoprotein (human MDR1 gene product) activity underlies interindividual differences in oral cyclosporine (CsA) bioavailability. Cyclosporine 132-144 ATP binding cassette subfamily B member 1 Homo sapiens 58-62 12817518-1 2003 Variability in CYP3A (CYP3A4/5) and P-glycoprotein (human MDR1 gene product) activity underlies interindividual differences in oral cyclosporine (CsA) bioavailability. Cyclosporine 146-149 ATP binding cassette subfamily B member 1 Homo sapiens 36-50 12817518-1 2003 Variability in CYP3A (CYP3A4/5) and P-glycoprotein (human MDR1 gene product) activity underlies interindividual differences in oral cyclosporine (CsA) bioavailability. Cyclosporine 146-149 ATP binding cassette subfamily B member 1 Homo sapiens 58-62 12817518-3 2003 Our objective was to evaluate the effect of CYP3A5 and MDR1 polymorphic expression on CsA oral disposition. Cyclosporine 86-89 ATP binding cassette subfamily B member 1 Homo sapiens 55-59 12817518-8 2003 MDR1 C3435T genotype was identified as the best predictor of CsA systemic exposure. Cyclosporine 61-64 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 12817518-14 2003 Thus, the MDR1 C3435T genotype offers a potential mechanistic basis to explain interracial differences in CsA oral bioavailability. Cyclosporine 106-109 ATP binding cassette subfamily B member 1 Homo sapiens 10-14 12817895-4 2003 Cyclosporin A (CsA) was used as a model compound for P-gp mediated efflux. Cyclosporine 15-18 ATP binding cassette subfamily B member 1 Homo sapiens 53-57 12642584-6 2003 cis-(Z)-Flupentixol-induced complex formation requires involvement of the Pgp substrate site, because agents that either physically compete (cyclosporin A) for or indirectly occlude (vanadate) the substrate-binding site prevent formation of the complex. Cyclosporine 141-154 ATP binding cassette subfamily B member 1 Homo sapiens 74-77 12751630-7 2003 CONCLUSIONS: The results suggest that the effects of surfactants via micellar solubilization and inhibition of P-gp efflux on CsA transport in Caco-2 cells are significant. Cyclosporine 126-129 ATP binding cassette subfamily B member 1 Homo sapiens 111-115 12531223-1 2003 The cyclosporine analog Valspodar (PSC 833, Novartis Pharma) is a strong inhibitor of the mdr1 gene product p-glycoprotein (pgp). Cyclosporine 4-16 ATP binding cassette subfamily B member 1 Homo sapiens 90-94 12831511-6 2003 The uptake and efflux of Rhodamine123, an MDR1 substrate, in Caco/DX cells were significantly less and greater, respectively, than those in Caco-2 cells, and these transports were affected by the addition of ciclosporin. Cyclosporine 208-219 ATP binding cassette subfamily B member 1 Homo sapiens 42-46 12531223-1 2003 The cyclosporine analog Valspodar (PSC 833, Novartis Pharma) is a strong inhibitor of the mdr1 gene product p-glycoprotein (pgp). Cyclosporine 4-16 ATP binding cassette subfamily B member 1 Homo sapiens 108-122 12531223-1 2003 The cyclosporine analog Valspodar (PSC 833, Novartis Pharma) is a strong inhibitor of the mdr1 gene product p-glycoprotein (pgp). Cyclosporine 4-16 ATP binding cassette subfamily B member 1 Homo sapiens 124-127 12562644-1 2003 BACKGROUND: Pharmacokinetic study has shown that co-administration of cyclosporin A (CsA), which acts as a P-glycoprotein (P-gp) and CYP-3A blocker, resulted in an 8-fold increase in the systemic exposure of oral paclitaxel. Cyclosporine 85-88 ATP binding cassette subfamily B member 1 Homo sapiens 107-121 12562644-1 2003 BACKGROUND: Pharmacokinetic study has shown that co-administration of cyclosporin A (CsA), which acts as a P-glycoprotein (P-gp) and CYP-3A blocker, resulted in an 8-fold increase in the systemic exposure of oral paclitaxel. Cyclosporine 70-83 ATP binding cassette subfamily B member 1 Homo sapiens 107-121 12562644-1 2003 BACKGROUND: Pharmacokinetic study has shown that co-administration of cyclosporin A (CsA), which acts as a P-glycoprotein (P-gp) and CYP-3A blocker, resulted in an 8-fold increase in the systemic exposure of oral paclitaxel. Cyclosporine 85-88 ATP binding cassette subfamily B member 1 Homo sapiens 123-127 12562644-1 2003 BACKGROUND: Pharmacokinetic study has shown that co-administration of cyclosporin A (CsA), which acts as a P-glycoprotein (P-gp) and CYP-3A blocker, resulted in an 8-fold increase in the systemic exposure of oral paclitaxel. Cyclosporine 70-83 ATP binding cassette subfamily B member 1 Homo sapiens 123-127 12176916-6 2002 We conclude that Pgp has prognostic relevance in CML-BP but that the modulation of Pgp function with CsA as applied in this trial is ineffective. Cyclosporine 101-104 ATP binding cassette subfamily B member 1 Homo sapiens 83-86 12563178-0 2003 Genetic polymorphisms in MDR1 and CYP3A4 genes in Asians and the influence of MDR1 haplotypes on cyclosporin disposition in heart transplant recipients. Cyclosporine 97-108 ATP binding cassette subfamily B member 1 Homo sapiens 78-82 12608534-9 2003 In the presence of a Pgp inhibitor such as verapamil, cyclosporine A, or progesterone, the ATP-dependent uptakes of [3H]digoxin and [3H]vinblastine into BBMVs were significantly reduced. Cyclosporine 54-68 ATP binding cassette subfamily B member 1 Homo sapiens 21-24 12434394-6 2002 p-Glycoprotein (p-gp)inhibitors, such as verapamil (100 microM) and cyclosporin A (CsA, 20 microM) significantly (p < 0.05) inhibited P(BA) but significantly (p < 0.05) enhanced P(AB). Cyclosporine 68-81 ATP binding cassette subfamily B member 1 Homo sapiens 0-14 12434394-6 2002 p-Glycoprotein (p-gp)inhibitors, such as verapamil (100 microM) and cyclosporin A (CsA, 20 microM) significantly (p < 0.05) inhibited P(BA) but significantly (p < 0.05) enhanced P(AB). Cyclosporine 83-86 ATP binding cassette subfamily B member 1 Homo sapiens 0-14 12553571-6 2002 A variety of modulators known to interfere with mammalian P-glycoprotein function perturbed resorufin excretion from male adult schistosomes, including cyclosporin A, Ro11-2933, verapamil, or nifedipine. Cyclosporine 152-165 ATP binding cassette subfamily B member 1 Homo sapiens 58-72 12388638-2 2002 Both drugs exhibited greater permeability in the basolateral (BL) to apical (AP) direction than in the AP to BL direction, indicating apically directed secretion; BL to AP transport was inhibited by P-glycoprotein (P-gp) inhibitors verapamil and cyclosporin A. Cyclosporine 246-259 ATP binding cassette subfamily B member 1 Homo sapiens 199-213 12388638-2 2002 Both drugs exhibited greater permeability in the basolateral (BL) to apical (AP) direction than in the AP to BL direction, indicating apically directed secretion; BL to AP transport was inhibited by P-glycoprotein (P-gp) inhibitors verapamil and cyclosporin A. Cyclosporine 246-259 ATP binding cassette subfamily B member 1 Homo sapiens 215-219 12176916-0 2002 Cyclosporine inhibition of P-glycoprotein in chronic myeloid leukemia blast phase. Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 27-41 12387747-11 2002 Vp, CsA, 1,25(OH)(2)D(3) and Dex significantly increased R-123 intracellular retention, indicating the inhibition of Pgp-mediated transport. Cyclosporine 4-7 ATP binding cassette subfamily B member 1 Homo sapiens 117-120 12387747-8 2002 Both MDR-1 Pgp and MDR-1 mRNA were significantly increased in cells cultured in the presence of cyclosporin A (CsA), 1,25(OH)(2)D(3), platelet activating factor, dexamethasone (Dex), or aldosterone. Cyclosporine 111-114 ATP binding cassette subfamily B member 1 Homo sapiens 5-10 12387747-12 2002 Drug-pretreated, Pgp-overexpressing cells showed increased Pgp activity and were less susceptible to toxic concentrations of CsA. Cyclosporine 125-128 ATP binding cassette subfamily B member 1 Homo sapiens 17-20 12387747-8 2002 Both MDR-1 Pgp and MDR-1 mRNA were significantly increased in cells cultured in the presence of cyclosporin A (CsA), 1,25(OH)(2)D(3), platelet activating factor, dexamethasone (Dex), or aldosterone. Cyclosporine 111-114 ATP binding cassette subfamily B member 1 Homo sapiens 11-14 12387747-8 2002 Both MDR-1 Pgp and MDR-1 mRNA were significantly increased in cells cultured in the presence of cyclosporin A (CsA), 1,25(OH)(2)D(3), platelet activating factor, dexamethasone (Dex), or aldosterone. Cyclosporine 111-114 ATP binding cassette subfamily B member 1 Homo sapiens 19-24 12152989-2 2002 There are several potential agents for modulating Pgp-mediated multi-drug resistance, such as cyclosporin A and PSC833, which are currently being evaluated in clinical trials. Cyclosporine 94-107 ATP binding cassette subfamily B member 1 Homo sapiens 50-53 12130727-5 2002 We therefore investigated the influence of piperine on P-glycoprotein-mediated, polarized transport of digoxin and cyclosporine in monolayers of Caco-2 cells. Cyclosporine 115-127 ATP binding cassette subfamily B member 1 Homo sapiens 55-69 12195825-3 2002 Its transport was completely inhibited by two specific P-gp inhibitors, ciclosporin A and GG918, in our experiments. Cyclosporine 72-85 ATP binding cassette subfamily B member 1 Homo sapiens 55-59 12127970-8 2002 Azidopine-binding assay showed that cyclosporin A or verapamil inhibited azidopine binding on Pgp partially but sinensetin did not. Cyclosporine 36-49 ATP binding cassette subfamily B member 1 Homo sapiens 94-97 12071854-3 2002 The increased transport of C6-NBD-PS is mediated by MDR1 Pgp, shown by transport reduction nearly to the level of controls in the presence of MDR1 Pgp inhibitors [PSC 833, cyclosporin A and dexniguldipine hydrochloride (Dex)]. Cyclosporine 172-185 ATP binding cassette subfamily B member 1 Homo sapiens 52-56 12071854-3 2002 The increased transport of C6-NBD-PS is mediated by MDR1 Pgp, shown by transport reduction nearly to the level of controls in the presence of MDR1 Pgp inhibitors [PSC 833, cyclosporin A and dexniguldipine hydrochloride (Dex)]. Cyclosporine 172-185 ATP binding cassette subfamily B member 1 Homo sapiens 142-146 12183111-6 2002 To circumvent this resistant phenotype, several P-gp modulators such as cyclosporin A (CsA) are available. Cyclosporine 72-85 ATP binding cassette subfamily B member 1 Homo sapiens 48-52 12183111-6 2002 To circumvent this resistant phenotype, several P-gp modulators such as cyclosporin A (CsA) are available. Cyclosporine 87-90 ATP binding cassette subfamily B member 1 Homo sapiens 48-52 12021632-1 2002 To determine the relationship between C3435T mutation in exon 26 of the human multidrug resistant 1 (MDR1) gene and cyclosporine pharmacokinetic parameters among healthy volunteers, the oral cyclosporine pharmacokinetic study was performed for 14 healthy subjects. Cyclosporine 116-128 ATP binding cassette subfamily B member 1 Homo sapiens 78-99 12021632-1 2002 To determine the relationship between C3435T mutation in exon 26 of the human multidrug resistant 1 (MDR1) gene and cyclosporine pharmacokinetic parameters among healthy volunteers, the oral cyclosporine pharmacokinetic study was performed for 14 healthy subjects. Cyclosporine 116-128 ATP binding cassette subfamily B member 1 Homo sapiens 101-105 12021632-1 2002 To determine the relationship between C3435T mutation in exon 26 of the human multidrug resistant 1 (MDR1) gene and cyclosporine pharmacokinetic parameters among healthy volunteers, the oral cyclosporine pharmacokinetic study was performed for 14 healthy subjects. Cyclosporine 191-203 ATP binding cassette subfamily B member 1 Homo sapiens 78-99 12021632-1 2002 To determine the relationship between C3435T mutation in exon 26 of the human multidrug resistant 1 (MDR1) gene and cyclosporine pharmacokinetic parameters among healthy volunteers, the oral cyclosporine pharmacokinetic study was performed for 14 healthy subjects. Cyclosporine 191-203 ATP binding cassette subfamily B member 1 Homo sapiens 101-105 11976833-7 2002 The highest MDR was expressed in MOLT-4/DNR cells, which was overcome by the P-gp modulator, cyclosporin A (CsA). Cyclosporine 93-106 ATP binding cassette subfamily B member 1 Homo sapiens 77-81 11976833-7 2002 The highest MDR was expressed in MOLT-4/DNR cells, which was overcome by the P-gp modulator, cyclosporin A (CsA). Cyclosporine 108-111 ATP binding cassette subfamily B member 1 Homo sapiens 77-81 12033380-6 2002 P-gp inhibitors (i.e., GG918, cyclosporine, ketoconazole, vinblastine) decreased the B-->A transport of dicloxacillin and trimethoprim and increased the A-->B transport of trimethoprim while non-P-gp inhibitors (e.g., PAH) had no effect. Cyclosporine 30-42 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 12112526-6 2002 MDR1 gene amplification precedes the emergence of a mutant allele in cells that were coselected with doxorubicin and a cyclosporin inhibitor of P-glycoprotein (P-gp). Cyclosporine 119-130 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 12112526-6 2002 MDR1 gene amplification precedes the emergence of a mutant allele in cells that were coselected with doxorubicin and a cyclosporin inhibitor of P-glycoprotein (P-gp). Cyclosporine 119-130 ATP binding cassette subfamily B member 1 Homo sapiens 144-158 12112526-6 2002 MDR1 gene amplification precedes the emergence of a mutant allele in cells that were coselected with doxorubicin and a cyclosporin inhibitor of P-glycoprotein (P-gp). Cyclosporine 119-130 ATP binding cassette subfamily B member 1 Homo sapiens 160-164 11809535-4 2002 These inhibitory potencies for P-gp were more potent than typical P-gp inhibitors, cyclosporine A and verapamil. Cyclosporine 83-97 ATP binding cassette subfamily B member 1 Homo sapiens 31-35 11877340-7 2002 The accumulation of NBD-octreotide in capillary lumens was inhibited in a concentration-dependent manner by unlabelled octreotide, by verapamil, PSC-833 and cyclosporin A, potent inhibitors of p-glycoprotein, and by leucotriene C(4), a strong modulator of Mrp2. Cyclosporine 157-170 ATP binding cassette subfamily B member 1 Homo sapiens 193-207 11865967-1 2002 Cyclosporine and tacrolimus are substrates and potent inhibitors of the multidrug transporter, P-glycoprotein, in vitro. Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 95-109 12033380-6 2002 P-gp inhibitors (i.e., GG918, cyclosporine, ketoconazole, vinblastine) decreased the B-->A transport of dicloxacillin and trimethoprim and increased the A-->B transport of trimethoprim while non-P-gp inhibitors (e.g., PAH) had no effect. Cyclosporine 30-42 ATP binding cassette subfamily B member 1 Homo sapiens 201-205 11784143-9 2002 Compound 5 has greater potency than verapamil and is equipotent with cyclosporin A, for inhibiting P-glycoprotein function. Cyclosporine 69-82 ATP binding cassette subfamily B member 1 Homo sapiens 99-113 12036392-14 2002 Thus, rhabdomyolysis has occurred following the coadministration of cyclosporin, a potent CYP3A4 and P-glycoprotein inhibitor, and lovastatin. Cyclosporine 68-79 ATP binding cassette subfamily B member 1 Homo sapiens 101-115 11849198-5 2002 As indinavir and cyclosporin are substrates for both CYP3A4 and the multi drug transporter P-glycoprotein we hypothesized that modulation of P-glycoprotein expression and function by SJW may contribute to the development of potentially harmful drug-drug interactions. Cyclosporine 17-28 ATP binding cassette subfamily B member 1 Homo sapiens 91-105 11849198-5 2002 As indinavir and cyclosporin are substrates for both CYP3A4 and the multi drug transporter P-glycoprotein we hypothesized that modulation of P-glycoprotein expression and function by SJW may contribute to the development of potentially harmful drug-drug interactions. Cyclosporine 17-28 ATP binding cassette subfamily B member 1 Homo sapiens 141-155 11990773-4 2002 Drug levels in Pgp-expressing organs may be increased by modulation of this Pgp-facilitated transport with several compounds, such as cyclosporin A. Cyclosporine 134-147 ATP binding cassette subfamily B member 1 Homo sapiens 15-18 11990773-4 2002 Drug levels in Pgp-expressing organs may be increased by modulation of this Pgp-facilitated transport with several compounds, such as cyclosporin A. Cyclosporine 134-147 ATP binding cassette subfamily B member 1 Homo sapiens 76-79 11719356-1 2001 Cyclosporine A (CsA) inhibits P-glycoprotein (Pgp)-mediated cellular export of anthracyclines at clinically achievable concentrations. Cyclosporine 0-14 ATP binding cassette subfamily B member 1 Homo sapiens 30-44 11719356-1 2001 Cyclosporine A (CsA) inhibits P-glycoprotein (Pgp)-mediated cellular export of anthracyclines at clinically achievable concentrations. Cyclosporine 0-14 ATP binding cassette subfamily B member 1 Homo sapiens 46-49 11719356-1 2001 Cyclosporine A (CsA) inhibits P-glycoprotein (Pgp)-mediated cellular export of anthracyclines at clinically achievable concentrations. Cyclosporine 16-19 ATP binding cassette subfamily B member 1 Homo sapiens 30-44 11719356-1 2001 Cyclosporine A (CsA) inhibits P-glycoprotein (Pgp)-mediated cellular export of anthracyclines at clinically achievable concentrations. Cyclosporine 16-19 ATP binding cassette subfamily B member 1 Homo sapiens 46-49 11762554-1 2001 Immunosuppressive agents such as cyclosporine, tacrolimus, sirolimus, and corticosteroids are substrates for the transmembrane multidrug resistance pump P-glycoprotein (P-gp). Cyclosporine 33-45 ATP binding cassette subfamily B member 1 Homo sapiens 153-167 11762554-1 2001 Immunosuppressive agents such as cyclosporine, tacrolimus, sirolimus, and corticosteroids are substrates for the transmembrane multidrug resistance pump P-glycoprotein (P-gp). Cyclosporine 33-45 ATP binding cassette subfamily B member 1 Homo sapiens 169-173 11691790-10 2001 Additionally, in drug-selected MCF7/Adr cells, which constitutively express high levels of Pgp, inhibition of Pgp by cyclosporin A resulted in significantly increased accumulation of TMA-DPH in intracellular membranes but no difference in its accumulation in the extracellular leaflet of the plasma membrane. Cyclosporine 117-130 ATP binding cassette subfamily B member 1 Homo sapiens 91-94 11719356-7 2001 The effect of CsA on survival was greatest in patients with moderate or bright Pgp expression (median 12 months with CsA versus 4 months for controls) compared to patients with absent or low Pgp expression (median 6 months in both arms). Cyclosporine 14-17 ATP binding cassette subfamily B member 1 Homo sapiens 79-82 11691790-10 2001 Additionally, in drug-selected MCF7/Adr cells, which constitutively express high levels of Pgp, inhibition of Pgp by cyclosporin A resulted in significantly increased accumulation of TMA-DPH in intracellular membranes but no difference in its accumulation in the extracellular leaflet of the plasma membrane. Cyclosporine 117-130 ATP binding cassette subfamily B member 1 Homo sapiens 110-113 11676863-1 2001 P-Glycoprotein, which mediates multidrug resistance (MDR) in cancer chemotherapy, is a principal target of cyclosporin A and [3"-keto-Bmt(1)]-[Val(2)]-cyclosporin (valspodar; PSC 833). Cyclosporine 107-120 ATP binding cassette subfamily B member 1 Homo sapiens 0-14 11504821-4 2001 An increase in the rate of accumulation of the MRP1 substrate calcein was observed following treatment with the organic anion/MRP1 inhibitor indomethacin, the Pgp inhibitors cyclosporin A (CsA) and vinblastine, as well as conditions of energy depletion. Cyclosporine 189-192 ATP binding cassette subfamily B member 1 Homo sapiens 159-162 11714218-9 2001 Administration of azithromycin may have caused the increased cyclosporine concentrations in this patient through p-glycoprotein inhibition and/or competition for biliary excretion. Cyclosporine 61-73 ATP binding cassette subfamily B member 1 Homo sapiens 113-127 11493443-2 2001 The MDR phenotype often correlates with expression of P-glycoprotein (Pgp), and Pgp antagonists such as cyclosporine (CSA) have been used as chemosensitizing agents in AML. Cyclosporine 104-116 ATP binding cassette subfamily B member 1 Homo sapiens 80-83 11502320-5 2001 These findings could affect use of drugs that are P-glycoprotein substrates (such as HIV-1 protease inhibitors and ciclosporin) in African populations. Cyclosporine 115-126 ATP binding cassette subfamily B member 1 Homo sapiens 50-64 11676863-1 2001 P-Glycoprotein, which mediates multidrug resistance (MDR) in cancer chemotherapy, is a principal target of cyclosporin A and [3"-keto-Bmt(1)]-[Val(2)]-cyclosporin (valspodar; PSC 833). Cyclosporine 107-118 ATP binding cassette subfamily B member 1 Homo sapiens 0-14 11676863-6 2001 In addition, the intracellular accumulation of valspodar was found to be 3 - 6 fold higher than that of cyclosporin A in four sublines and verapamil, an inhibitor of P-glycoprotein-mediated transport, enhanced the accumulation of cyclosporin A, but not valspodar. Cyclosporine 230-243 ATP binding cassette subfamily B member 1 Homo sapiens 166-180 11422747-13 2001 Increased expression of P-gp in infiltrating leukocytes correlated with the severity of allograft rejection, suggesting that P-gp may decrease the immunosuppressive efficacy of CsA. Cyclosporine 177-180 ATP binding cassette subfamily B member 1 Homo sapiens 125-129 11422747-14 2001 Thus, individual differences in the P-gp induction response of CsA-exposed renal parenchymal cells and/or infiltrating leukocytes may predispose to either CsA nephrotoxicity or rejection, respectively. Cyclosporine 63-66 ATP binding cassette subfamily B member 1 Homo sapiens 36-40 11422747-14 2001 Thus, individual differences in the P-gp induction response of CsA-exposed renal parenchymal cells and/or infiltrating leukocytes may predispose to either CsA nephrotoxicity or rejection, respectively. Cyclosporine 155-158 ATP binding cassette subfamily B member 1 Homo sapiens 36-40 11442496-5 2001 To overcome this drug resistance, we added cyclosporine A (CsA) and these agents to culture media as a P-gp antagonist. Cyclosporine 59-62 ATP binding cassette subfamily B member 1 Homo sapiens 103-107 11422747-1 2001 BACKGROUND: The multidrug resistance (MDR) gene product P-glycoprotein (P-gp) is a transmembrane efflux pump for hydrophobic, potentially toxic compounds, including the immunosuppressant cyclosporine A (CsA). Cyclosporine 203-206 ATP binding cassette subfamily B member 1 Homo sapiens 56-70 11422747-1 2001 BACKGROUND: The multidrug resistance (MDR) gene product P-glycoprotein (P-gp) is a transmembrane efflux pump for hydrophobic, potentially toxic compounds, including the immunosuppressant cyclosporine A (CsA). Cyclosporine 203-206 ATP binding cassette subfamily B member 1 Homo sapiens 72-76 11422747-2 2001 We have previously shown that CsA increases P-gp expression in proximal tubule and endothelial cells in vitro. Cyclosporine 30-33 ATP binding cassette subfamily B member 1 Homo sapiens 44-48 11422747-7 2001 RESULTS: P-gp expression in biopsies with acute tubular necrosis (ATN; N = 10) after CsA treatment was significantly higher in arterial endothelia, proximal tubules, and epithelial cells of Bowman"s capsule (BC), whereas P-gp was sparsely induced in CsA nephrotoxicity (N = 19) compared with controls. Cyclosporine 85-88 ATP binding cassette subfamily B member 1 Homo sapiens 9-13 11422747-7 2001 RESULTS: P-gp expression in biopsies with acute tubular necrosis (ATN; N = 10) after CsA treatment was significantly higher in arterial endothelia, proximal tubules, and epithelial cells of Bowman"s capsule (BC), whereas P-gp was sparsely induced in CsA nephrotoxicity (N = 19) compared with controls. Cyclosporine 85-88 ATP binding cassette subfamily B member 1 Homo sapiens 221-225 11422747-7 2001 RESULTS: P-gp expression in biopsies with acute tubular necrosis (ATN; N = 10) after CsA treatment was significantly higher in arterial endothelia, proximal tubules, and epithelial cells of Bowman"s capsule (BC), whereas P-gp was sparsely induced in CsA nephrotoxicity (N = 19) compared with controls. Cyclosporine 250-253 ATP binding cassette subfamily B member 1 Homo sapiens 9-13 11422747-8 2001 Acute cellular (N = 30) and vascular rejection (N = 10) or chronic allograft nephropathy (N = 10) after CsA was associated with strong P-gp expression in infiltrating leukocytes and increased P-gp expression in arterial endothelia, proximal tubules, and BC. Cyclosporine 104-107 ATP binding cassette subfamily B member 1 Homo sapiens 135-139 11422747-10 2001 Zero biopsies showed a weak, homogeneous, nonpolarized expression of P-gp in tubules and an increased expression of P-gp after CsA therapy in the brush border, arterial endothelia, and BC. Cyclosporine 127-130 ATP binding cassette subfamily B member 1 Homo sapiens 116-120 11422747-11 2001 CONCLUSIONS: CsA treatment was associated with increased P-gp expression in parenchymal cells of kidney transplants with ATN, acute or chronic transplant rejection, but P-gp was not increased in patients with CsA nephrotoxicity. Cyclosporine 13-16 ATP binding cassette subfamily B member 1 Homo sapiens 57-61 11422747-12 2001 This indicates that CsA induces its own detoxification by P-gp and that inadequate up-regulation of P-gp in renal parenchymal cells contributes to CsA nephrotoxicity. Cyclosporine 20-23 ATP binding cassette subfamily B member 1 Homo sapiens 58-62 11422747-12 2001 This indicates that CsA induces its own detoxification by P-gp and that inadequate up-regulation of P-gp in renal parenchymal cells contributes to CsA nephrotoxicity. Cyclosporine 147-150 ATP binding cassette subfamily B member 1 Homo sapiens 100-104 11422747-13 2001 Increased expression of P-gp in infiltrating leukocytes correlated with the severity of allograft rejection, suggesting that P-gp may decrease the immunosuppressive efficacy of CsA. Cyclosporine 177-180 ATP binding cassette subfamily B member 1 Homo sapiens 24-28 11375290-1 2001 BACKGROUND: A substantial proportion of the variability in the absorption and clearance of cyclosporin A (CsA) after oral administration has been attributed to variability in liver cytochrome P-450 3A4 (CYP3A4) activity and intestinal P-glycoprotein (P-gp) concentration. Cyclosporine 106-109 ATP binding cassette subfamily B member 1 Homo sapiens 235-249 11375290-1 2001 BACKGROUND: A substantial proportion of the variability in the absorption and clearance of cyclosporin A (CsA) after oral administration has been attributed to variability in liver cytochrome P-450 3A4 (CYP3A4) activity and intestinal P-glycoprotein (P-gp) concentration. Cyclosporine 106-109 ATP binding cassette subfamily B member 1 Homo sapiens 251-255 11871046-6 2001 St John"s wort may induce cytochrome P-450 3A4 activity and/or P-glycoprotein expression, which are both involved in the metabolism and absorption of cyclosporine. Cyclosporine 150-162 ATP binding cassette subfamily B member 1 Homo sapiens 63-77 11282491-1 2001 Cyclosporin A, a substrate of P-glycoprotein (P-gp), is known to cause cholestasis in humans and in rat experimental models. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 30-44 11282491-1 2001 Cyclosporin A, a substrate of P-glycoprotein (P-gp), is known to cause cholestasis in humans and in rat experimental models. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 46-50 11499549-13 2001 PGP immunoblottable amount was increased when cells were cultured in the presence of either cyclosporin A or dexamethasone. Cyclosporine 92-105 ATP binding cassette subfamily B member 1 Homo sapiens 0-3 11262086-4 2001 Inhibition of membrane Pgp within leukemic cells, characterized by intracellular drug accumulation, was specifically produced by isoprenylated derivatives, with 8-(3,3-dimethylallyl)chrysin being even more efficient than the commonly used cyclosporin A. Cyclosporine 239-252 ATP binding cassette subfamily B member 1 Homo sapiens 23-26 11288109-3 2001 In Calu-3 cells, accumulation of the Pgp substrates rhodamine 123 (Rh123) and calcein acetoxymethyl ester (calcein-AM) was increased in the presence of the specific Pgp inhibitors cyclosporin A (CsA), vinblastine, and taxol. Cyclosporine 195-198 ATP binding cassette subfamily B member 1 Homo sapiens 37-40 11288109-3 2001 In Calu-3 cells, accumulation of the Pgp substrates rhodamine 123 (Rh123) and calcein acetoxymethyl ester (calcein-AM) was increased in the presence of the specific Pgp inhibitors cyclosporin A (CsA), vinblastine, and taxol. Cyclosporine 195-198 ATP binding cassette subfamily B member 1 Homo sapiens 165-168 11288109-10 2001 These results support an energy-dependent Pgp efflux pump pathway that is sensitive to inhibition with CsA in Calu-3 cells. Cyclosporine 103-106 ATP binding cassette subfamily B member 1 Homo sapiens 42-45 11284449-6 2001 Inhibition of P-glycoprotein-mediated transport of these compounds in Caco-2 cells was determined using the cyclosporine analogue PSC-833 (valspodar) as inhibitor of P-glycoprotein. Cyclosporine 108-120 ATP binding cassette subfamily B member 1 Homo sapiens 14-28 11159725-12 2001 In addition, lumenal but not cellular fluorescence intensity was significantly decreased when capillaries were incubated with PSC-833, Cyclosporin A or Verapamil, all inhibitors of p-glycoprotein. Cyclosporine 135-148 ATP binding cassette subfamily B member 1 Homo sapiens 181-195 11213066-7 2001 CONCLUSIONS: Patients taking SJW concomitantly with CSA or other medications whose absorption and metabolism are mediated by cytochrome P-450 and/or P-glycoprotein should require close monitoring. Cyclosporine 52-55 ATP binding cassette subfamily B member 1 Homo sapiens 149-163 11125025-2 2001 The resulting Pgp-stationary phase was used in frontal and zonal chromatographic studies to investigate the binding of vinblastine (VBL), doxorubicin (DOX), verapamil (VER), and cyclosporin A (CsA) to the immobilized Pgp. Cyclosporine 178-191 ATP binding cassette subfamily B member 1 Homo sapiens 14-17 11125025-2 2001 The resulting Pgp-stationary phase was used in frontal and zonal chromatographic studies to investigate the binding of vinblastine (VBL), doxorubicin (DOX), verapamil (VER), and cyclosporin A (CsA) to the immobilized Pgp. Cyclosporine 193-196 ATP binding cassette subfamily B member 1 Homo sapiens 14-17 11139374-10 2000 Experiments have shown that P-gp can be inhibited by different non-chemotherapeutic substrates such as cyclosporin A. Cyclosporine 103-116 ATP binding cassette subfamily B member 1 Homo sapiens 28-32 11498403-6 2000 A wealth of recent experimental data shows that many of the previously tested P-glycoprotein inhibitors, including verapamil, cyclosporin A, and valspodar (SDZ PSC 833), are substrates and/or potent inhibitors of cytochrome P450 3A4 (CYP3A4). Cyclosporine 126-139 ATP binding cassette subfamily B member 1 Homo sapiens 78-92 11205313-1 2000 BACKGROUND: The non-immunosuppressive cyclosporine analog PSC 833 has been shown to reverse multidrug-resistance of neoplastic cells including the MDR-1 gene coded P-glycoprotein (P-gp)-mediated cells resistant to paclitaxel. Cyclosporine 38-50 ATP binding cassette subfamily B member 1 Homo sapiens 147-152 11205313-1 2000 BACKGROUND: The non-immunosuppressive cyclosporine analog PSC 833 has been shown to reverse multidrug-resistance of neoplastic cells including the MDR-1 gene coded P-glycoprotein (P-gp)-mediated cells resistant to paclitaxel. Cyclosporine 38-50 ATP binding cassette subfamily B member 1 Homo sapiens 164-178 11205313-1 2000 BACKGROUND: The non-immunosuppressive cyclosporine analog PSC 833 has been shown to reverse multidrug-resistance of neoplastic cells including the MDR-1 gene coded P-glycoprotein (P-gp)-mediated cells resistant to paclitaxel. Cyclosporine 38-50 ATP binding cassette subfamily B member 1 Homo sapiens 180-184 11408558-8 2001 Incubation of Caco-2 cells with UIC2 in the presence of 1 microM CsA resulted in 50 to 80% inhibition of Pgp-mediated vinblastine efflux, with no significant inhibition observed by UIC2 or CsA alone. Cyclosporine 65-68 ATP binding cassette subfamily B member 1 Homo sapiens 105-108 11408558-9 2001 Inhibition of Pgp in CYP3A4-expressing Caco-2 cells by UIC2 and 1 microM CsA resulted in a significant decrease in the apical secretion of M6, M5, and OH-indinavir and an increase in the amount of the metabolites secreted in the basolateral compartment and retained in the cytosol. Cyclosporine 73-76 ATP binding cassette subfamily B member 1 Homo sapiens 14-17 11181682-3 2001 The purpose of this study was to enhance the systemic exposure to oral docetaxel on coadministration of cyclosporine (CsA), an efficacious inhibitor of P-gp and substrate for CYP 3A4. Cyclosporine 104-116 ATP binding cassette subfamily B member 1 Homo sapiens 152-156 11181682-3 2001 The purpose of this study was to enhance the systemic exposure to oral docetaxel on coadministration of cyclosporine (CsA), an efficacious inhibitor of P-gp and substrate for CYP 3A4. Cyclosporine 118-121 ATP binding cassette subfamily B member 1 Homo sapiens 152-156 11139311-2 2001 We have recently demonstrated that the oral bioavailability of paclitaxel can be increased at least 7-fold by co-administration of the P-gp blocker cyclosporin A (CsA). Cyclosporine 163-166 ATP binding cassette subfamily B member 1 Homo sapiens 135-139 11122104-9 2000 However, P-gp function, measured using cyclosporin modulation of rhodamine 123 (R123) uptake, was not associated with the CDR, demonstrating that there are other properties of P-gp, besides its role in drug efflux, that modulate the responsiveness of AML blasts to chemotherapy. Cyclosporine 39-50 ATP binding cassette subfamily B member 1 Homo sapiens 9-13 11336351-6 2001 The potency of inhibition of P-gp was cyclosporine > tacrolimus > quinidine > verapamil > vinblastine. Cyclosporine 38-50 ATP binding cassette subfamily B member 1 Homo sapiens 29-33 11121733-5 2000 Differing extents of intestinal first-pass metabolic extraction between the two drugs, inhibition of midazolam metabolism by cyclosporine at the level of the intestine, and/or P-glycoprotein-mediated intestinal efflux of cyclosporine (but not midazolam) may account for this poor correlation. Cyclosporine 221-233 ATP binding cassette subfamily B member 1 Homo sapiens 176-190 11202156-8 2000 Furthermore, drug uptake and efflux studies, performed by flow cytometry on isolated nuclei in the presence of the P-glycoprotein inhibitor cyclosporin A, suggested the presence of a functional P-glycoprotein in the nuclear membrane, but not in the nuclear matrix, of drug resistant cells. Cyclosporine 140-153 ATP binding cassette subfamily B member 1 Homo sapiens 115-129 11202156-8 2000 Furthermore, drug uptake and efflux studies, performed by flow cytometry on isolated nuclei in the presence of the P-glycoprotein inhibitor cyclosporin A, suggested the presence of a functional P-glycoprotein in the nuclear membrane, but not in the nuclear matrix, of drug resistant cells. Cyclosporine 140-153 ATP binding cassette subfamily B member 1 Homo sapiens 194-208 10706193-5 2000 Human P-glycoprotein has been shown to transport a wide range of structurally unrelated drugs such as digoxin, quinidine, cyclosporine and HIV-1 protease inhibitors. Cyclosporine 122-134 ATP binding cassette subfamily B member 1 Homo sapiens 6-20 10925353-7 2000 Modulation of P-gp function by cyclosporin A was found to alter DOX accumulation and efflux in LoVo 7 cells, indicating that intracellular P-gp plays a functional role in drug trafficking and suggesting possible implications in determining the intrinsic resistance displayed by this clone. Cyclosporine 31-44 ATP binding cassette subfamily B member 1 Homo sapiens 14-18 10925353-7 2000 Modulation of P-gp function by cyclosporin A was found to alter DOX accumulation and efflux in LoVo 7 cells, indicating that intracellular P-gp plays a functional role in drug trafficking and suggesting possible implications in determining the intrinsic resistance displayed by this clone. Cyclosporine 31-44 ATP binding cassette subfamily B member 1 Homo sapiens 139-143 20950543-21 2000 The reverse effect of CsA for expression of MDR1 requires further clinical study. Cyclosporine 22-25 ATP binding cassette subfamily B member 1 Homo sapiens 44-48 10837354-2 2000 Aldosterone secretion is significantly decreased by the PGP inhibitors verapamil, cyclosporin A (CSA), PSC-833, and vinblastine. Cyclosporine 82-95 ATP binding cassette subfamily B member 1 Homo sapiens 56-59 10837354-2 2000 Aldosterone secretion is significantly decreased by the PGP inhibitors verapamil, cyclosporin A (CSA), PSC-833, and vinblastine. Cyclosporine 97-100 ATP binding cassette subfamily B member 1 Homo sapiens 56-59 10908115-0 2000 The potent immunosuppressive cyclosporin FR901459 inhibits the human P-glycoprotein and formyl peptide receptor functions. Cyclosporine 29-40 ATP binding cassette subfamily B member 1 Homo sapiens 69-83 10783825-1 2000 OBJECTIVE: Increased bioavailability of the P-glycoprotein (Pgp) substrates digoxin and cyclosporin due to erythromycin has been observed in vivo. Cyclosporine 88-99 ATP binding cassette subfamily B member 1 Homo sapiens 44-58 10783825-1 2000 OBJECTIVE: Increased bioavailability of the P-glycoprotein (Pgp) substrates digoxin and cyclosporin due to erythromycin has been observed in vivo. Cyclosporine 88-99 ATP binding cassette subfamily B member 1 Homo sapiens 60-63 10734174-3 2000 An ethyl acetate extract of orange juice did not affect the initial uptake rate of [(3)H]vinblastine but significantly increased the steady-state uptake, as did cyclosporin A (20 microM), an inhibitor of P-gp. Cyclosporine 161-174 ATP binding cassette subfamily B member 1 Homo sapiens 204-208 10727524-0 2000 Loss of cyclosporin and azidopine binding are associated with altered ATPase activity by a mutant P-glycoprotein with deleted phe(335). Cyclosporine 8-19 ATP binding cassette subfamily B member 1 Homo sapiens 98-112 10897619-1 2000 MDR1 gene encodes for a transmembranous glycoprotein, gp-170, which acts as a drug export pump and is also a cyclosporine(CsA)-binding protein. Cyclosporine 109-121 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 10897619-1 2000 MDR1 gene encodes for a transmembranous glycoprotein, gp-170, which acts as a drug export pump and is also a cyclosporine(CsA)-binding protein. Cyclosporine 109-121 ATP binding cassette subfamily B member 1 Homo sapiens 54-60 11775252-9 2000 CsA (3 mg/L) can block the efflux pump function of P-gp shown by the significantly increased accumulation and efflux reduction of Rh123 in K562/MDR cells. Cyclosporine 0-3 ATP binding cassette subfamily B member 1 Homo sapiens 51-55 10737718-12 2000 Preincubation of cells with cyclosporine A, which has high affinity for P-gp, did not diminish the levels of ceramide generated upon exposure to PSC 833. Cyclosporine 28-42 ATP binding cassette subfamily B member 1 Homo sapiens 72-76 10744311-3 2000 Displacement studies using other known PGP ligands, verapamil and cyclosporin A, demonstrated that there was selective binding between vinblastine and the immobilized PGP transporter. Cyclosporine 66-79 ATP binding cassette subfamily B member 1 Homo sapiens 167-170 10744311-6 2000 The Kd values obtained on the PGP-IAM for cyclosporin A and verapamil were 492+/-21 and 172+/-29 microM, respectively. Cyclosporine 42-55 ATP binding cassette subfamily B member 1 Homo sapiens 30-33 10666173-2 2000 Corticosteroids are substrates for P-gp, whose function can be inhibited by cyclosporin. Cyclosporine 76-87 ATP binding cassette subfamily B member 1 Homo sapiens 35-39 10981246-6 2000 DISCUSSION: St. John"s wort is suspected to be a significant inducer of CYP3A4 isoenzyme activity and of P-glycoprotein (P-gp) expression, both of which are important in the metabolism and absorption of cyclosporine. Cyclosporine 203-215 ATP binding cassette subfamily B member 1 Homo sapiens 105-119 10981246-6 2000 DISCUSSION: St. John"s wort is suspected to be a significant inducer of CYP3A4 isoenzyme activity and of P-glycoprotein (P-gp) expression, both of which are important in the metabolism and absorption of cyclosporine. Cyclosporine 203-215 ATP binding cassette subfamily B member 1 Homo sapiens 121-125 10981246-7 2000 Cyclosporine exhibits a relatively small therapeutic window and is sensitive to medications that can modulate the CYP3A4 isoenzyme and P-gp in both the liver and small intestines. Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 135-139 11042226-4 2000 Polarised transport of doxorubicin in the Caco-2 and the LLC-PK1:MDR1 cell lines could be inhibited by the P-gp inhibitors SDZ-PSC 833 (PSC 833), cyclosporin A (CsA), verapamil and quinine, but not by the inhibitors for the organic cation carrier systems cimetidine and tetraethylammonium (TEA). Cyclosporine 146-159 ATP binding cassette subfamily B member 1 Homo sapiens 107-111 11042226-4 2000 Polarised transport of doxorubicin in the Caco-2 and the LLC-PK1:MDR1 cell lines could be inhibited by the P-gp inhibitors SDZ-PSC 833 (PSC 833), cyclosporin A (CsA), verapamil and quinine, but not by the inhibitors for the organic cation carrier systems cimetidine and tetraethylammonium (TEA). Cyclosporine 161-164 ATP binding cassette subfamily B member 1 Homo sapiens 107-111 10938401-3 2000 Derivatives of cyclosporin interact with and reverse the ability of P-gp to act as a drug efflux pump. Cyclosporine 15-26 ATP binding cassette subfamily B member 1 Homo sapiens 68-72 10938401-4 2000 To determine if the Gly185 residue of human P-gp is also important for the interaction of P-gp with closely related cyclosporin derivatives, we examined the effect of PSC-833 and CsA on P-gp in KB3-1 cells transfected with human wild-type P-gp (GSV-2) or with the mutant P-gp (VSV-1) that habored the Gly185-->Val substitution. Cyclosporine 116-127 ATP binding cassette subfamily B member 1 Homo sapiens 44-48 10938401-7 2000 Furthermore, the intracellular accumulation of CsA was low in GSV-2 P-gp-expressing cells, compared with its accumulation in VSV-1 cells and it was found to be as high as in non-P-gp expressing KB3-1 cells. Cyclosporine 47-50 ATP binding cassette subfamily B member 1 Homo sapiens 68-72 10938401-7 2000 Furthermore, the intracellular accumulation of CsA was low in GSV-2 P-gp-expressing cells, compared with its accumulation in VSV-1 cells and it was found to be as high as in non-P-gp expressing KB3-1 cells. Cyclosporine 47-50 ATP binding cassette subfamily B member 1 Homo sapiens 178-182 10938401-8 2000 These results indicated an enhanced sensitivity of Val185-P-gp expressing cells to CsA that correlated with increased intracellular accumulation in these cells. Cyclosporine 83-86 ATP binding cassette subfamily B member 1 Homo sapiens 58-62 10820137-6 2000 Less potent P-glycoprotein inhibitors like valspodar (PSC-833), cyclosporin A, and ketoconazole, as well as quinidine and verapamil, had modest or little effect on brain/plasma ratios but increased plasma nelfinavir concentrations due to inhibition of CYP3A-mediated metabolism. Cyclosporine 64-77 ATP binding cassette subfamily B member 1 Homo sapiens 12-26 11005322-3 2000 Since CsA is an antagonist of cytostatic drugs in P-glycoprotein (Pgp)-mediated transport, increased Pgp expression might contribute to an increased resistance to CsA. Cyclosporine 6-9 ATP binding cassette subfamily B member 1 Homo sapiens 50-64 11005322-3 2000 Since CsA is an antagonist of cytostatic drugs in P-glycoprotein (Pgp)-mediated transport, increased Pgp expression might contribute to an increased resistance to CsA. Cyclosporine 6-9 ATP binding cassette subfamily B member 1 Homo sapiens 66-69 11005322-3 2000 Since CsA is an antagonist of cytostatic drugs in P-glycoprotein (Pgp)-mediated transport, increased Pgp expression might contribute to an increased resistance to CsA. Cyclosporine 163-166 ATP binding cassette subfamily B member 1 Homo sapiens 50-64 11005322-3 2000 Since CsA is an antagonist of cytostatic drugs in P-glycoprotein (Pgp)-mediated transport, increased Pgp expression might contribute to an increased resistance to CsA. Cyclosporine 163-166 ATP binding cassette subfamily B member 1 Homo sapiens 66-69 11005322-3 2000 Since CsA is an antagonist of cytostatic drugs in P-glycoprotein (Pgp)-mediated transport, increased Pgp expression might contribute to an increased resistance to CsA. Cyclosporine 163-166 ATP binding cassette subfamily B member 1 Homo sapiens 101-104 11005322-4 2000 METHODS: The sensitivity of lymphocytes at three different concentrations of CsA was tested in a non-radioactive lymphocyte-transformation test and related to Pgp expression as determined by flow cytometry on mononuclear cells. Cyclosporine 77-80 ATP binding cassette subfamily B member 1 Homo sapiens 159-162 11005322-10 2000 Analysing the relationship between CsA sensitivity and Pgp expression, no significant heterogeneity could be observed between the different groups. Cyclosporine 35-38 ATP binding cassette subfamily B member 1 Homo sapiens 55-58 10772630-5 2000 Known Pgp inhibitors, such as cyclosporin A, nicardipine, verapamil, quinidine, terfenadine, tamoxifen, and vinblastine were demonstrated to inhibit the Pgp-mediated efflux of daunorubicin. Cyclosporine 30-43 ATP binding cassette subfamily B member 1 Homo sapiens 6-9 10772630-5 2000 Known Pgp inhibitors, such as cyclosporin A, nicardipine, verapamil, quinidine, terfenadine, tamoxifen, and vinblastine were demonstrated to inhibit the Pgp-mediated efflux of daunorubicin. Cyclosporine 30-43 ATP binding cassette subfamily B member 1 Homo sapiens 153-156 10838122-3 2000 Results showed that the accumulation of P-gp substrates calcein-AM and vinblastine by BeWo cells or primary cultures of human cytotrophoblasts was significantly enhanced in the presence of a typical P-gp inhibitor, cyclosporin-A, or other inhibitors such as quinidine, verapamil, and dipyridamole. Cyclosporine 215-228 ATP binding cassette subfamily B member 1 Homo sapiens 40-44 10838122-3 2000 Results showed that the accumulation of P-gp substrates calcein-AM and vinblastine by BeWo cells or primary cultures of human cytotrophoblasts was significantly enhanced in the presence of a typical P-gp inhibitor, cyclosporin-A, or other inhibitors such as quinidine, verapamil, and dipyridamole. Cyclosporine 215-228 ATP binding cassette subfamily B member 1 Homo sapiens 199-203 10706193-8 2000 Studies in humans indicate a particular importance of intestinal P-glycoprotein for bioavailability of the immunosuppressant cyclosporine. Cyclosporine 125-137 ATP binding cassette subfamily B member 1 Homo sapiens 65-79 10751037-5 2000 Cyclosporin A (20 microM) was present in the uptake media to block potential P-glycoprotein-mediated atorvastatin efflux. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 77-91 10681718-16 2000 Some, but not all, of these differences in daunorubicin accumulation and efflux as well as in the effect of cyclo-sporin A can be explained by a heterogenous expression of the mdr1-gene. Cyclosporine 108-122 ATP binding cassette subfamily B member 1 Homo sapiens 176-180 10636889-4 2000 When mdr1 inhibitors (PSC833, cyclosporine A, verapamil) were transiently added to cells with mdr1 up-regulation by pretreatment for 72 h with cadmium, cadmium-induced apoptosis increased significantly and to a percentage similar to that obtained in cells with no mdr1 up-regulation (72-h cadmium: 5.2 +/- 0.9% versus 72-h cadmium + 1-h PSC833: 7.2 +/- 1.4%; p < or = 0.001). Cyclosporine 30-44 ATP binding cassette subfamily B member 1 Homo sapiens 5-9 10636889-4 2000 When mdr1 inhibitors (PSC833, cyclosporine A, verapamil) were transiently added to cells with mdr1 up-regulation by pretreatment for 72 h with cadmium, cadmium-induced apoptosis increased significantly and to a percentage similar to that obtained in cells with no mdr1 up-regulation (72-h cadmium: 5.2 +/- 0.9% versus 72-h cadmium + 1-h PSC833: 7.2 +/- 1.4%; p < or = 0.001). Cyclosporine 30-44 ATP binding cassette subfamily B member 1 Homo sapiens 94-98 10636889-4 2000 When mdr1 inhibitors (PSC833, cyclosporine A, verapamil) were transiently added to cells with mdr1 up-regulation by pretreatment for 72 h with cadmium, cadmium-induced apoptosis increased significantly and to a percentage similar to that obtained in cells with no mdr1 up-regulation (72-h cadmium: 5.2 +/- 0.9% versus 72-h cadmium + 1-h PSC833: 7.2 +/- 1.4%; p < or = 0.001). Cyclosporine 30-44 ATP binding cassette subfamily B member 1 Homo sapiens 94-98 10663638-2 2000 We studied the effects of the Pgp inhibitor, cyclosporin A (CsA), on the cerebrospinal fluid (CSF) penetration of the Pgp substrate, doxorubicin, in non-human primates. Cyclosporine 60-63 ATP binding cassette subfamily B member 1 Homo sapiens 30-33 10663638-2 2000 We studied the effects of the Pgp inhibitor, cyclosporin A (CsA), on the cerebrospinal fluid (CSF) penetration of the Pgp substrate, doxorubicin, in non-human primates. Cyclosporine 60-63 ATP binding cassette subfamily B member 1 Homo sapiens 118-121 10755319-0 2000 Effect of high-dose cyclosporine on etoposide pharmacodynamics in a trial to reverse P-glycoprotein (MDR1 gene) mediated drug resistance. Cyclosporine 20-32 ATP binding cassette subfamily B member 1 Homo sapiens 85-99 10755319-0 2000 Effect of high-dose cyclosporine on etoposide pharmacodynamics in a trial to reverse P-glycoprotein (MDR1 gene) mediated drug resistance. Cyclosporine 20-32 ATP binding cassette subfamily B member 1 Homo sapiens 101-105 10755319-1 2000 PURPOSE: The consequences of using cyclosporine (CsA) therapy to modulate P-glycoprotein-mediated multidrug resistance include increased myelosuppression, hyperbilirubinemia, and altered disposition of the cytotoxin. Cyclosporine 35-47 ATP binding cassette subfamily B member 1 Homo sapiens 74-88 10513988-8 1999 Quaternary analogs, which are restricted by a permanent positive charge in transiting the plasma membrane by diffusion, accumulated in Pgp containing I/O vesicles in an ATP-dependent and cyclosporin A-inhibitable manner, which identified them as Pgp substrates. Cyclosporine 187-200 ATP binding cassette subfamily B member 1 Homo sapiens 135-138 10726475-0 1999 [Cyclosporin A reverses steroid-resistance induced by P-glycoprotein in patients with SLE]. Cyclosporine 1-14 ATP binding cassette subfamily B member 1 Homo sapiens 54-68 10513988-8 1999 Quaternary analogs, which are restricted by a permanent positive charge in transiting the plasma membrane by diffusion, accumulated in Pgp containing I/O vesicles in an ATP-dependent and cyclosporin A-inhibitable manner, which identified them as Pgp substrates. Cyclosporine 187-200 ATP binding cassette subfamily B member 1 Homo sapiens 246-249 10516933-4 1999 The objective of this review is to discuss the effects of P-gp modulation on the pharmacokinetics and the pharmacodynamics of immunosuppressive agents such as cyclosporine, tacrolimus, sirolimus, and corticosteroids. Cyclosporine 159-171 ATP binding cassette subfamily B member 1 Homo sapiens 58-62 10334913-3 1999 MDR1 gene expression was associated with the expression of functional P-glycoprotein (gp-170); the function was reversed by verapamil and cyclosporin A. Cyclosporine 138-151 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 10634525-2 2000 Diverse groups of drugs have been identified, including cyclosporine A, which can reverse drug resistance by inhibiting P-glycoprotein transport. Cyclosporine 56-70 ATP binding cassette subfamily B member 1 Homo sapiens 120-134 10503812-4 1999 Additionally, P-glycoprotein (mdr-1) located in the gastrointestinal epithelium can affect affect blood drug concentrations after oral administration of cyclosporin, presumably by counter-transporting the drug from the systemic circulation back into the gastrointestinal lumen. Cyclosporine 153-164 ATP binding cassette subfamily B member 1 Homo sapiens 14-28 10503812-4 1999 Additionally, P-glycoprotein (mdr-1) located in the gastrointestinal epithelium can affect affect blood drug concentrations after oral administration of cyclosporin, presumably by counter-transporting the drug from the systemic circulation back into the gastrointestinal lumen. Cyclosporine 153-164 ATP binding cassette subfamily B member 1 Homo sapiens 30-35 10503812-15 1999 Polypharmacy may have specific relevance for elderly patients treated with cyclosporin since this agent is a substrate of both CYP3A and P-glycoprotein, both of which are important in the elimination of many commonly used drugs. Cyclosporine 75-86 ATP binding cassette subfamily B member 1 Homo sapiens 137-151 10510888-11 1999 One of these strategies is to reverse MDR by using such P-gp inhibitors as verapamil and cyclosporine A. Cyclosporine 89-103 ATP binding cassette subfamily B member 1 Homo sapiens 56-60 10419902-5 1999 MDR1/P-glycoprotein expression, which was highly correlated with cyclosporine-inhibited efflux, was noted in only 35% of these younger AML patients, distinctly lower than the frequency of 71% we previously reported in AML in the elderly (Blood 89:3323, 1997). Cyclosporine 65-77 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 10419902-5 1999 MDR1/P-glycoprotein expression, which was highly correlated with cyclosporine-inhibited efflux, was noted in only 35% of these younger AML patients, distinctly lower than the frequency of 71% we previously reported in AML in the elderly (Blood 89:3323, 1997). Cyclosporine 65-77 ATP binding cassette subfamily B member 1 Homo sapiens 5-19 10419902-11 1999 Only MDR1/P-glycoprotein expression and cyclosporine-inhibited efflux were significantly associated with complete remission (CR) rate (P(MDR1) =.012; P(efflux) =.039) and resistant disease (RD; P(MDR1) =.0007; P(efflux) =.0092). Cyclosporine 40-52 ATP binding cassette subfamily B member 1 Homo sapiens 137-141 10419902-11 1999 Only MDR1/P-glycoprotein expression and cyclosporine-inhibited efflux were significantly associated with complete remission (CR) rate (P(MDR1) =.012; P(efflux) =.039) and resistant disease (RD; P(MDR1) =.0007; P(efflux) =.0092). Cyclosporine 40-52 ATP binding cassette subfamily B member 1 Homo sapiens 137-141 10543726-5 1999 The accumulation of [3H]vinblastine (20 nM), an established P-gp substrate, by the monolayer cells was significantly enhanced in the presence of two P-gp inhibitors (i.e., verapamil and cyclosporin A) and nucleoside transport inhibitors (i.e., dipyridamole and dilazep). Cyclosporine 186-199 ATP binding cassette subfamily B member 1 Homo sapiens 60-64 10543726-5 1999 The accumulation of [3H]vinblastine (20 nM), an established P-gp substrate, by the monolayer cells was significantly enhanced in the presence of two P-gp inhibitors (i.e., verapamil and cyclosporin A) and nucleoside transport inhibitors (i.e., dipyridamole and dilazep). Cyclosporine 186-199 ATP binding cassette subfamily B member 1 Homo sapiens 149-153 10399954-6 1999 Resistance to a P-gp-associated drug, doxorubicin, could be reversed with P-gp circumventing agents such as cyclosporin A and verapamil, but these substances had no effect on resistance to 5-fluorouracil. Cyclosporine 108-121 ATP binding cassette subfamily B member 1 Homo sapiens 16-20 10399954-6 1999 Resistance to a P-gp-associated drug, doxorubicin, could be reversed with P-gp circumventing agents such as cyclosporin A and verapamil, but these substances had no effect on resistance to 5-fluorouracil. Cyclosporine 108-121 ATP binding cassette subfamily B member 1 Homo sapiens 74-78 10334913-3 1999 MDR1 gene expression was associated with the expression of functional P-glycoprotein (gp-170); the function was reversed by verapamil and cyclosporin A. Cyclosporine 138-151 ATP binding cassette subfamily B member 1 Homo sapiens 70-84 10334913-3 1999 MDR1 gene expression was associated with the expression of functional P-glycoprotein (gp-170); the function was reversed by verapamil and cyclosporin A. Cyclosporine 138-151 ATP binding cassette subfamily B member 1 Homo sapiens 86-92 10374882-3 1999 The resistant KG1a and K562 sublines, which expressed high levels of Pgp, responded to low doses of the cyclosporin SDZ PSC 833, the cyclopeptolide SDZ 280-446, and the cyclopropyldibenzosuberane LY335979 with a dose-dependent growth inhibition. Cyclosporine 104-115 ATP binding cassette subfamily B member 1 Homo sapiens 69-72 10378008-6 1999 To study the role of Pgp in the resistance to UVA radiation, two MDR modulators or reversing agents (verapamil and cyclosporin A) capable of blocking Pgp activity were used. Cyclosporine 115-128 ATP binding cassette subfamily B member 1 Homo sapiens 150-153 10344751-3 1999 In vivo pharmacokinetic analysis of P-gp transport might identify the capacity of modulation by P-gp substrate modulators, such as cyclosporin A. Cyclosporine 131-144 ATP binding cassette subfamily B member 1 Homo sapiens 36-40 10344751-3 1999 In vivo pharmacokinetic analysis of P-gp transport might identify the capacity of modulation by P-gp substrate modulators, such as cyclosporin A. Cyclosporine 131-144 ATP binding cassette subfamily B member 1 Homo sapiens 96-100 10344751-8 1999 These levels were increased after modulation with cyclosporin A in GLC4/P-gp. Cyclosporine 50-63 ATP binding cassette subfamily B member 1 Homo sapiens 72-76 9864280-1 1998 PSC 833, a nonimmunosuppressive cyclosporin, is able to inhibit the efflux of antitumor drugs mediated by P-glycoprotein (P-gp). Cyclosporine 32-43 ATP binding cassette subfamily B member 1 Homo sapiens 106-120 9885221-0 1999 P-glycoprotein expression on normal and abnormally expanded natural killer cells and inhibition of P-glycoprotein function by cyclosporin A and its analogue, PSC833. Cyclosporine 126-139 ATP binding cassette subfamily B member 1 Homo sapiens 99-113 10342576-2 1999 Because idarubicin is less vulnerable to MDR1-mediated transport and could thereby represent a better companion to MDR1 inhibitors, we assessed the ability of the anti-MDR1 agent cyclosporin A to modulate this function in multidrug resistant T-lymphoblastic CEM cells challenged in vitro with either daunorubicin or idarubicin. Cyclosporine 179-192 ATP binding cassette subfamily B member 1 Homo sapiens 115-119 10342576-2 1999 Because idarubicin is less vulnerable to MDR1-mediated transport and could thereby represent a better companion to MDR1 inhibitors, we assessed the ability of the anti-MDR1 agent cyclosporin A to modulate this function in multidrug resistant T-lymphoblastic CEM cells challenged in vitro with either daunorubicin or idarubicin. Cyclosporine 179-192 ATP binding cassette subfamily B member 1 Homo sapiens 115-119 10342576-8 1999 Altogether, study results in MDR1+ cells incubated with CsA 1500 ng/ml plus idarubicin+idarubicinol 100+20 ng/ml, that are peak levels achievable in vivo with an idarubicin dose > or = 12 mg/m2 plus cyclosporin A 16 mg/kg/d, were in the range of those obtained with standard-dose daunorubicin in MDR1- cells (p=n.s.). Cyclosporine 56-59 ATP binding cassette subfamily B member 1 Homo sapiens 29-33 10342576-8 1999 Altogether, study results in MDR1+ cells incubated with CsA 1500 ng/ml plus idarubicin+idarubicinol 100+20 ng/ml, that are peak levels achievable in vivo with an idarubicin dose > or = 12 mg/m2 plus cyclosporin A 16 mg/kg/d, were in the range of those obtained with standard-dose daunorubicin in MDR1- cells (p=n.s.). Cyclosporine 56-59 ATP binding cassette subfamily B member 1 Homo sapiens 299-303 10342576-8 1999 Altogether, study results in MDR1+ cells incubated with CsA 1500 ng/ml plus idarubicin+idarubicinol 100+20 ng/ml, that are peak levels achievable in vivo with an idarubicin dose > or = 12 mg/m2 plus cyclosporin A 16 mg/kg/d, were in the range of those obtained with standard-dose daunorubicin in MDR1- cells (p=n.s.). Cyclosporine 202-215 ATP binding cassette subfamily B member 1 Homo sapiens 29-33 10342576-9 1999 In summary, an idarubicin plus short-course cyclosporin A combination could be considered for the management of MDR1+ leukemias, where it may represent a more effective and less toxic option than daunorubicin plus continuous infusion cyclosporin A. Cyclosporine 44-57 ATP binding cassette subfamily B member 1 Homo sapiens 112-116 10198227-3 1999 The initial rates (in percent) for calcein retention by these MDR-1 cells were used to calculate values for the percent initial efflux of calcein-AM through the MDR pump in the presence of the inhibitors PSC833, cyclosporinA, and dexniguldipine. Cyclosporine 212-224 ATP binding cassette subfamily B member 1 Homo sapiens 62-67 10087141-5 1999 Furthermore, glibenclamide is itself a substrate for P-glycoprotein, since the cellular accumulation of [3H]glibenclamide was low and substantially increased by addition of P-glycoprotein substrates (e. g., vinblastine and cyclosporine) only in the P-glycoprotein-expressing cell lines. Cyclosporine 223-235 ATP binding cassette subfamily B member 1 Homo sapiens 53-67 10087141-5 1999 Furthermore, glibenclamide is itself a substrate for P-glycoprotein, since the cellular accumulation of [3H]glibenclamide was low and substantially increased by addition of P-glycoprotein substrates (e. g., vinblastine and cyclosporine) only in the P-glycoprotein-expressing cell lines. Cyclosporine 223-235 ATP binding cassette subfamily B member 1 Homo sapiens 173-187 10087141-5 1999 Furthermore, glibenclamide is itself a substrate for P-glycoprotein, since the cellular accumulation of [3H]glibenclamide was low and substantially increased by addition of P-glycoprotein substrates (e. g., vinblastine and cyclosporine) only in the P-glycoprotein-expressing cell lines. Cyclosporine 223-235 ATP binding cassette subfamily B member 1 Homo sapiens 173-187 10213371-5 1999 Excretion of GS-MF was decreased in presence of the MRP-blocker M K-571.2) Transport experiments with cyclosporin A demonstrated the functional activity of P-gp. Cyclosporine 102-115 ATP binding cassette subfamily B member 1 Homo sapiens 156-160 10500807-4 1999 The apoptotic effect from varying drug type and concentration was compared at 24 hours in CEM-MDR1+ cells, with and without co-incubation with MDR1 functional downregulator cyclosporin A (CSA) used at therapeutic concentration (1500 ng/ml). Cyclosporine 173-186 ATP binding cassette subfamily B member 1 Homo sapiens 143-147 9933132-1 1999 Expression of P-glycoprotein (Pgp), the drug efflux pump which mediates multidrug resistance (MDR), has been widely reported in chronic lymphocytic leukaemia (CLL) and improved accumulation of daunorubicin has been reported using the MDR reversing agent cyclosporin A (CSA). Cyclosporine 269-272 ATP binding cassette subfamily B member 1 Homo sapiens 14-28 9933132-1 1999 Expression of P-glycoprotein (Pgp), the drug efflux pump which mediates multidrug resistance (MDR), has been widely reported in chronic lymphocytic leukaemia (CLL) and improved accumulation of daunorubicin has been reported using the MDR reversing agent cyclosporin A (CSA). Cyclosporine 269-272 ATP binding cassette subfamily B member 1 Homo sapiens 30-33 9864280-1 1998 PSC 833, a nonimmunosuppressive cyclosporin, is able to inhibit the efflux of antitumor drugs mediated by P-glycoprotein (P-gp). Cyclosporine 32-43 ATP binding cassette subfamily B member 1 Homo sapiens 122-126 9677321-5 1998 The measured values of the quenching constant, Kq, for interaction of peptides with P-glycoprotein ranged from 200 nM for cyclosporine A to 138 microM for the tripeptide N-acetyl-leucyl-leucyl-norleucinal. Cyclosporine 122-136 ATP binding cassette subfamily B member 1 Homo sapiens 84-98 9914792-0 1998 Inhibitory effects of a cyclosporin derivative, SDZ PSC 833, on transport of doxorubicin and vinblastine via human P-glycoprotein. Cyclosporine 24-35 ATP binding cassette subfamily B member 1 Homo sapiens 115-129 9914792-1 1998 The inhibitory effects of SDZ PSC 833 (PSC833), a non-immunosuppressive cyclosporin derivative, on the P-glycoprotein (P-gp)-mediated transport of doxorubicin and vinblastine were compared with those of cyclosporin A (Cs-A). Cyclosporine 203-216 ATP binding cassette subfamily B member 1 Homo sapiens 119-123 9914792-1 1998 The inhibitory effects of SDZ PSC 833 (PSC833), a non-immunosuppressive cyclosporin derivative, on the P-glycoprotein (P-gp)-mediated transport of doxorubicin and vinblastine were compared with those of cyclosporin A (Cs-A). Cyclosporine 218-222 ATP binding cassette subfamily B member 1 Homo sapiens 119-123 9914792-3 1998 Both PSC833 and Cs-A inhibited P-gp-mediated transport of doxorubicin and vinblastine in a concentration-dependent manner and increased the intracellular accumulation of doxorubicin and vinblastine in LLC-GA5-COL150 cells. Cyclosporine 16-20 ATP binding cassette subfamily B member 1 Homo sapiens 31-35 9914792-7 1998 These results indicated that the inhibitory effect of PSC833 on P-gp-mediated transport was 5- to 10-fold more potent than that of Cs-A, and this higher inhibitory effect of PSC833 may be related to the absence of PSC833 transport by P-gp and to the higher lipophilicity of PSC833. Cyclosporine 131-135 ATP binding cassette subfamily B member 1 Homo sapiens 64-68 9765504-8 1998 Inhibitors of Pgp, including verapamil and cyclosporin A, were less effective in reversing resistance of the chimeric Pgp compared with wild-type Pgp, for certain drugs. Cyclosporine 43-56 ATP binding cassette subfamily B member 1 Homo sapiens 14-17 9765504-8 1998 Inhibitors of Pgp, including verapamil and cyclosporin A, were less effective in reversing resistance of the chimeric Pgp compared with wild-type Pgp, for certain drugs. Cyclosporine 43-56 ATP binding cassette subfamily B member 1 Homo sapiens 118-121 9765504-8 1998 Inhibitors of Pgp, including verapamil and cyclosporin A, were less effective in reversing resistance of the chimeric Pgp compared with wild-type Pgp, for certain drugs. Cyclosporine 43-56 ATP binding cassette subfamily B member 1 Homo sapiens 118-121 9765504-9 1998 However, [125I]iodoarylazidoprazosin photoaffinity labeling of the chimeric Pgp and its binding competition with cyclosporin A, showed that cyclosporin A competed for the photoaffinity labeling. Cyclosporine 113-126 ATP binding cassette subfamily B member 1 Homo sapiens 76-79 9765504-9 1998 However, [125I]iodoarylazidoprazosin photoaffinity labeling of the chimeric Pgp and its binding competition with cyclosporin A, showed that cyclosporin A competed for the photoaffinity labeling. Cyclosporine 140-153 ATP binding cassette subfamily B member 1 Homo sapiens 76-79 9732409-6 1998 Transport in the basolateral to apical direction was 3-fold greater than apical to basolateral flux for both saquinavir and saquinavir mesylate and was blocked by co-incubation with the established P-gp reversal agents cyclosporine and verapamil. Cyclosporine 219-231 ATP binding cassette subfamily B member 1 Homo sapiens 198-202 9713517-1 1998 The non-immunosuppressive cyclosporine analog SDZ PSC 833 abolished the resistance of human multidrug resistant (MDR-1, P-gp) human promyelocyte leukemia HL-60/VCR cells in vitro to paclitaxel-induced cell cycle- and viability alterations, as well as resistance to paclitaxel-induced radiosensitization. Cyclosporine 26-38 ATP binding cassette subfamily B member 1 Homo sapiens 113-118 9667640-5 1998 In mdr1-negative cells, the median increase in 99Tc(m)-MIBI accumulation with CyA was 30% compared with the mdr1-positive cells with a median increase of 242%, P = 0.009. Cyclosporine 78-81 ATP binding cassette subfamily B member 1 Homo sapiens 3-7 9770112-3 1998 PSC-833 is a non-immunosuppressive cyclosporin derivative that potently and specifically inhibits P-gp. Cyclosporine 35-46 ATP binding cassette subfamily B member 1 Homo sapiens 98-102 9695116-5 1998 Hence, inhibition of intestinal P-glycoprotein, e.g. by a reversal agent like cyclosporin A, may be a promising strategy for improving the oral bioavailability of P-glycoprotein substrate drugs. Cyclosporine 78-91 ATP binding cassette subfamily B member 1 Homo sapiens 32-46 9767529-1 1998 BACKGROUND: The immunosuppressive drugs cyclosporine A (CsA) and tacrolimus (FK506) are extruded from cells by the multidrug resistance P-glycoprotein (P-gp), an efflux pump for drugs and xenobiotics, which may limit their therapeutic effectiveness and/or incidence of toxic side effects. Cyclosporine 56-59 ATP binding cassette subfamily B member 1 Homo sapiens 136-150 9767529-1 1998 BACKGROUND: The immunosuppressive drugs cyclosporine A (CsA) and tacrolimus (FK506) are extruded from cells by the multidrug resistance P-glycoprotein (P-gp), an efflux pump for drugs and xenobiotics, which may limit their therapeutic effectiveness and/or incidence of toxic side effects. Cyclosporine 56-59 ATP binding cassette subfamily B member 1 Homo sapiens 152-156 9767529-2 1998 In the present study, we investigated the effect of therapeutic concentrations of CsA and FK506 on the expression of P-gp in cultured endothelial and proximal tubule cells. Cyclosporine 82-85 ATP binding cassette subfamily B member 1 Homo sapiens 117-121 9767529-4 1998 RESULTS: Following incubation of HAEC with therapeutic concentrations of 0.1 to 1.6 microM CsA up to seven days, P-gp expression increased in a time- and concentration-dependent manner, maximally to 291 +/- 42% of controls with 0.8 microM CsA for seven days. Cyclosporine 91-94 ATP binding cassette subfamily B member 1 Homo sapiens 113-117 9767529-4 1998 RESULTS: Following incubation of HAEC with therapeutic concentrations of 0.1 to 1.6 microM CsA up to seven days, P-gp expression increased in a time- and concentration-dependent manner, maximally to 291 +/- 42% of controls with 0.8 microM CsA for seven days. Cyclosporine 239-242 ATP binding cassette subfamily B member 1 Homo sapiens 113-117 9767529-7 1998 Immunocytochemistry revealed increased P-gp expression in the plasma membrane of HAEC and RPTC treated with 0.8 microM CsA, which was reflected by a decrease of P-gp-mediated accumulation of calcein in both cell types. Cyclosporine 119-122 ATP binding cassette subfamily B member 1 Homo sapiens 39-43 9767529-7 1998 Immunocytochemistry revealed increased P-gp expression in the plasma membrane of HAEC and RPTC treated with 0.8 microM CsA, which was reflected by a decrease of P-gp-mediated accumulation of calcein in both cell types. Cyclosporine 119-122 ATP binding cassette subfamily B member 1 Homo sapiens 161-165 9767529-8 1998 CONCLUSIONS: The data suggest that the induction of P-gp expression in HAEC and RPTC at concentrations of CsA or FK506 above 0.5 microM is part of the protective answer of cells to toxic concentrations of the drugs and could therefore interfere with the therapeutic effectiveness of CsA in vivo. Cyclosporine 106-109 ATP binding cassette subfamily B member 1 Homo sapiens 52-56 9767529-8 1998 CONCLUSIONS: The data suggest that the induction of P-gp expression in HAEC and RPTC at concentrations of CsA or FK506 above 0.5 microM is part of the protective answer of cells to toxic concentrations of the drugs and could therefore interfere with the therapeutic effectiveness of CsA in vivo. Cyclosporine 283-286 ATP binding cassette subfamily B member 1 Homo sapiens 52-56 9695116-5 1998 Hence, inhibition of intestinal P-glycoprotein, e.g. by a reversal agent like cyclosporin A, may be a promising strategy for improving the oral bioavailability of P-glycoprotein substrate drugs. Cyclosporine 78-91 ATP binding cassette subfamily B member 1 Homo sapiens 163-177 9482283-9 1998 When MCS were incubated with verapamil, cyclosporin A, orthovanadate, and quinidine, which are known to reverse P-glycoprotein (Pgp)-mediated multidrug resistance (MDR), Dox accumulated also in deeper cell layers. Cyclosporine 40-53 ATP binding cassette subfamily B member 1 Homo sapiens 112-126 9506530-6 1998 The P-glycoprotein-mediated multidrug resistance (MDR)-reversing agents verapamil, cyclosporin A, quinidine, sodium orthovanadate and tamoxifen significantly increased dox fluorescence at this depth, whereas genistein, indomethacin, probenecid and brefeldin A, which reverse multidrug-resistance-associated protein (MRP) function, exerted no effect. Cyclosporine 83-96 ATP binding cassette subfamily B member 1 Homo sapiens 4-18 9506534-9 1998 P-gp function modulators (verapamil and cyclosporin A) were able to modify DOX intracytoplasmic distribution and to increase drug intracellular concentration and cytotoxic effect in melanoma cells. Cyclosporine 40-53 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 9567214-7 1998 Results from our group and others have suggested that overexpression of P-gp in renal tubular and mesangial cells prevents pharmacological nephrotoxicity by cyclosporin A (CsA). Cyclosporine 172-175 ATP binding cassette subfamily B member 1 Homo sapiens 72-76 9567214-11 1998 This way, the detoxicant function of P-gp against products of the ras catabolism could mediate their accumulation when the "vacuum cleaner" function is blocked by CsA or tacrolimus, contributing to the initial development of fibroblastic activation that leads to interstitial fibrosis associated with nephrotoxicity by these immunosuppressor drugs. Cyclosporine 163-166 ATP binding cassette subfamily B member 1 Homo sapiens 37-41 9697878-2 1998 Cyclosporin A (CsA) is an effective downmodulator of Pgp-related MDR in vitro and has already been tested for that purpose in vivo also. Cyclosporine 15-18 ATP binding cassette subfamily B member 1 Homo sapiens 53-56 9482283-9 1998 When MCS were incubated with verapamil, cyclosporin A, orthovanadate, and quinidine, which are known to reverse P-glycoprotein (Pgp)-mediated multidrug resistance (MDR), Dox accumulated also in deeper cell layers. Cyclosporine 40-53 ATP binding cassette subfamily B member 1 Homo sapiens 128-131 9597807-1 1998 A P-glycoprotein (P-gp) inhibitor, cyclosporin A (CsA) was found to enhance the susceptibility of multidrug resistant (MDR) cancer cells to anti-P-gp antibody-dependent cellular cytolysis (ADCC) by monocytes, but the exact mechanism is unknown. Cyclosporine 50-53 ATP binding cassette subfamily B member 1 Homo sapiens 2-16 9597807-1 1998 A P-glycoprotein (P-gp) inhibitor, cyclosporin A (CsA) was found to enhance the susceptibility of multidrug resistant (MDR) cancer cells to anti-P-gp antibody-dependent cellular cytolysis (ADCC) by monocytes, but the exact mechanism is unknown. Cyclosporine 50-53 ATP binding cassette subfamily B member 1 Homo sapiens 18-22 9597807-1 1998 A P-glycoprotein (P-gp) inhibitor, cyclosporin A (CsA) was found to enhance the susceptibility of multidrug resistant (MDR) cancer cells to anti-P-gp antibody-dependent cellular cytolysis (ADCC) by monocytes, but the exact mechanism is unknown. Cyclosporine 50-53 ATP binding cassette subfamily B member 1 Homo sapiens 145-149 9597807-2 1998 In this study, we examined whether CsA enhanced the susceptibility of MDR cells through its inhibitory effect of P-gp function by using anti-ganglioside GM2 (GM2) monoclonal antibody (Ab), KM966, instead of anti-P-gp Ab, MRK16. Cyclosporine 35-38 ATP binding cassette subfamily B member 1 Homo sapiens 113-117 9597807-2 1998 In this study, we examined whether CsA enhanced the susceptibility of MDR cells through its inhibitory effect of P-gp function by using anti-ganglioside GM2 (GM2) monoclonal antibody (Ab), KM966, instead of anti-P-gp Ab, MRK16. Cyclosporine 35-38 ATP binding cassette subfamily B member 1 Homo sapiens 212-216 9597807-3 1998 Monocyte-ADCC induced by both KM966 and MRK16 against P-gp positive human MDR ovarian cancer cells was significantly augmented by addition of CsA. Cyclosporine 142-145 ATP binding cassette subfamily B member 1 Homo sapiens 54-58 9597807-4 1998 KM966, but not MRK16, induced monocyte-ADCC against P-gp negative human ovarian cancer cells and CsA enhanced this ADCC activity, indicating that suppressive effect of P-gp function by CsA was not essential to the enhancement of ADCC. Cyclosporine 185-188 ATP binding cassette subfamily B member 1 Homo sapiens 168-172 9408959-4 1997 Recently, clinical reversal of MDR by noncytotoxic P-gp modulators such as verapamil, cyclosporin A (CsA), and PSC 833 was explored in acute leukemia and multiple myeloma. Cyclosporine 86-99 ATP binding cassette subfamily B member 1 Homo sapiens 51-55 9465841-1 1998 INTRODUCTION: Sirolimus and cyclosporine (INN, ciclosporin) share the same cytochrome P4503A metabolic pathways, and both drugs are substrates for p-glycoprotein countertransport. Cyclosporine 28-40 ATP binding cassette subfamily B member 1 Homo sapiens 147-161 9465841-1 1998 INTRODUCTION: Sirolimus and cyclosporine (INN, ciclosporin) share the same cytochrome P4503A metabolic pathways, and both drugs are substrates for p-glycoprotein countertransport. Cyclosporine 47-58 ATP binding cassette subfamily B member 1 Homo sapiens 147-161 9370075-4 1997 It has been shown that p-glycoprotein can be circumvented in vitro by noncytotoxic agents such as verapamil and cyclosporin A, which interact pharmacologically with p-glycoprotein-mediated efflux. Cyclosporine 112-125 ATP binding cassette subfamily B member 1 Homo sapiens 23-37 9370075-4 1997 It has been shown that p-glycoprotein can be circumvented in vitro by noncytotoxic agents such as verapamil and cyclosporin A, which interact pharmacologically with p-glycoprotein-mediated efflux. Cyclosporine 112-125 ATP binding cassette subfamily B member 1 Homo sapiens 165-179 9570481-2 1998 A variety of small molecules, such as verapamil and cyclosporin A, bind to P-glycoprotein and inhibit its ability to pump out antitumor drugs. Cyclosporine 52-65 ATP binding cassette subfamily B member 1 Homo sapiens 75-89 9418184-5 1997 The efflux function of P-gP was measured by intracellular accumulation of rhodamine-123 (Rh123; a substrate for P-gP) in the presence or absence of cyclosporin A (which binds to P-gP and inhibits its efflux function). Cyclosporine 148-161 ATP binding cassette subfamily B member 1 Homo sapiens 23-27 9408959-4 1997 Recently, clinical reversal of MDR by noncytotoxic P-gp modulators such as verapamil, cyclosporin A (CsA), and PSC 833 was explored in acute leukemia and multiple myeloma. Cyclosporine 101-104 ATP binding cassette subfamily B member 1 Homo sapiens 51-55 10837558-0 1997 Contributions of hepatic and intestinal metabolism and P-glycoprotein to cyclosporine and tacrolimus oral drug delivery. Cyclosporine 73-85 ATP binding cassette subfamily B member 1 Homo sapiens 55-69 9380680-8 1997 Also, the concentration of vinblastine (Pgp substrate) and cyclosporin A (Pgp modulator) required for 50% inhibition of [125I]IAAP binding to the C-site was increased 5- to 6-fold by cis(Z)-flupentixol without any effect on the N-site. Cyclosporine 59-72 ATP binding cassette subfamily B member 1 Homo sapiens 74-77 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. Cyclosporine 0-12 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. Cyclosporine 130-142 ATP binding cassette subfamily B member 1 Homo sapiens 52-66 10837558-10 1997 However, the quantity of intestinal p-glycoprotein accounts for approximately 17% of the variability in oral cyclosporine pharmacokinetics. Cyclosporine 109-121 ATP binding cassette subfamily B member 1 Homo sapiens 36-50 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. Cyclosporine 131-143 ATP binding cassette subfamily B member 1 Homo sapiens 76-90 9313931-0 1997 Interaction of cyclosporin derivatives with the ATPase activity of human P-glycoprotein. Cyclosporine 15-26 ATP binding cassette subfamily B member 1 Homo sapiens 73-87 9313931-7 1997 While verapamil activated the ATPase, the cyclosporin derivatives inhibited both the substrate-stimulated and the basal P-glycoprotein ATPase. Cyclosporine 42-53 ATP binding cassette subfamily B member 1 Homo sapiens 120-134 9313931-15 1997 The interaction of the cyclosporin derivatives with ATPase of P-glycoprotein might present an alternative and/or additional mechanism of action for the modulation of P-glycoprotein function. Cyclosporine 23-34 ATP binding cassette subfamily B member 1 Homo sapiens 62-76 9313931-15 1997 The interaction of the cyclosporin derivatives with ATPase of P-glycoprotein might present an alternative and/or additional mechanism of action for the modulation of P-glycoprotein function. Cyclosporine 23-34 ATP binding cassette subfamily B member 1 Homo sapiens 166-180 9333100-0 1997 Role of intestinal P-glycoprotein (mdr1) in interpatient variation in the oral bioavailability of cyclosporine. Cyclosporine 98-110 ATP binding cassette subfamily B member 1 Homo sapiens 19-33 9333100-0 1997 Role of intestinal P-glycoprotein (mdr1) in interpatient variation in the oral bioavailability of cyclosporine. Cyclosporine 98-110 ATP binding cassette subfamily B member 1 Homo sapiens 35-39 9333100-2 1997 Recently it has been shown that small bowel also contains CYP3A4, as well as P-glycoprotein, a protein able to transport cyclosporine. Cyclosporine 121-133 ATP binding cassette subfamily B member 1 Homo sapiens 77-91 9333100-7 1997 We conclude that intestinal P-glycoprotein plays a significant role in the first-pass elimination of cyclosporine, presumably by being a rate-limiting step in absorption. Cyclosporine 101-113 ATP binding cassette subfamily B member 1 Homo sapiens 28-42 9333100-8 1997 Drug interactions with cyclosporine previously ascribed to intestinal CYP3A4 may instead be mediated by interactions with intestinal P-glycoprotein. Cyclosporine 23-35 ATP binding cassette subfamily B member 1 Homo sapiens 133-147 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. Cyclosporine 185-197 ATP binding cassette subfamily B member 1 Homo sapiens 123-137 9205009-2 1997 Assessment of P-glycoprotein (P-gp) expression and function by means of immunocytochemistry, DNR accumulation, and modulation of resistance and accumulation by the P-gp inhibitor cyclosporin A (CsA) were selected as parameters for multidrug resistance (MDR). Cyclosporine 194-197 ATP binding cassette subfamily B member 1 Homo sapiens 14-28 9180163-1 1997 Cyclosporin A (CSA) is an effective inhibitor of the P-glycoprotein (P-gp) activity and has been shown to modulate multidrug resistance (MDR) in in vitro experimental models. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 53-67 9639738-1 1997 OBJECTIVE: To study the relationship between multi-drug-resistance (MDR1) gene expression and the drug resistance of ovarian carcinoma and the reversing potency of drug-resistance modifying agent--cyclosporin A (CsA). Cyclosporine 197-210 ATP binding cassette subfamily B member 1 Homo sapiens 68-72 9639738-1 1997 OBJECTIVE: To study the relationship between multi-drug-resistance (MDR1) gene expression and the drug resistance of ovarian carcinoma and the reversing potency of drug-resistance modifying agent--cyclosporin A (CsA). Cyclosporine 212-215 ATP binding cassette subfamily B member 1 Homo sapiens 68-72 9180163-1 1997 Cyclosporin A (CSA) is an effective inhibitor of the P-glycoprotein (P-gp) activity and has been shown to modulate multidrug resistance (MDR) in in vitro experimental models. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 69-73 9086008-0 1997 Regression of established tumors expressing P-glycoprotein by combinations of adriamycin, cyclosporin derivatives, and MRK-16 antibodies. Cyclosporine 90-101 ATP binding cassette subfamily B member 1 Homo sapiens 44-58 9155160-3 1997 Cyclosporine and its analogue, SDZ PSC 833, have demonstrated ability to inhibit P-glycoprotein mediated transport function, restore accumulation defects for anticancer drugs, and reverse resistance in vitro and in vivo. Cyclosporine 0-12 ATP binding cassette subfamily B member 1 Homo sapiens 81-95 9068595-2 1997 SDZ PSC 833 (PSC), a nonimmunosuppressive cyclosporine that potently modulates Pgp, is currently under clinical evaluation in patients with cancer. Cyclosporine 42-54 ATP binding cassette subfamily B member 1 Homo sapiens 79-82 9038218-10 1997 These data suggest that Phe335 is an important binding site on P-glycoprotein for substrates such as dactinomycin and vinblastine and for inhibitors such as cyclosporine and PSC 833. Cyclosporine 157-169 ATP binding cassette subfamily B member 1 Homo sapiens 63-77 9086008-2 1997 Strategies for overcoming this resistance include the use of specific compounds, such as cyclosporin derivatives, that modulate P-glycoprotein function and antibodies that bind to the protein, thereby altering its activity. Cyclosporine 89-100 ATP binding cassette subfamily B member 1 Homo sapiens 128-142 9086008-17 1997 CONCLUSION: Combination treatment with a cyclosporin derivative and an anti-P-glycoprotein antibody can be effective in circumventing P-glycoprotein-mediated drug resistance. Cyclosporine 41-52 ATP binding cassette subfamily B member 1 Homo sapiens 134-148 9123401-0 1997 Multidrug resistance gene MDR1 expression: a gene transfection in vitro model and clinical analysis in cyclosporine-treated patients rejecting their renal grafts. Cyclosporine 103-115 ATP binding cassette subfamily B member 1 Homo sapiens 26-30 9016791-3 1997 In this study, we have demonstrated that C219 inhibits the ATPase activity of P-glycoprotein based on the following findings: 1) the inhibition of total ATPase activity by C219 was selective to P-glycoprotein-positive membranes; 2) the C219-sensitive fraction of ATPase correlated the expression of P-glycoprotein; and 3) modulators of P-glycoprotein ATPase, verapamil and cyclosporin A, affected the C219-sensitive fraction of ATPase. Cyclosporine 373-386 ATP binding cassette subfamily B member 1 Homo sapiens 78-92 9219509-7 1997 Sensitivity to paclitaxel could be modulated by cyclosporin A in unselected cell lines expressing P-glycoprotein and not in P-glycoprotein-negative cell lines. Cyclosporine 48-61 ATP binding cassette subfamily B member 1 Homo sapiens 98-112 9272128-7 1997 Our studies of combinations of high-dose cyclosporin (CsA) or PSC 833 with etoposide, doxorubicin, or paclitaxel have produced data regarding the role of Pgp in the clinical pharmacology of these agents. Cyclosporine 41-52 ATP binding cassette subfamily B member 1 Homo sapiens 154-157 9001418-1 1997 Using cyclosporin A (CsA) to inhibit P-glycoprotein (P-gp) function we showed previously that there was a discordance between the ability of acute myeloid leukemic (AML) blast cells to accumulate daunorubicin and P-gp antigen expression (Xie et al, Leukemia 1995; 9:1882-1887). Cyclosporine 6-19 ATP binding cassette subfamily B member 1 Homo sapiens 37-51 9001418-1 1997 Using cyclosporin A (CsA) to inhibit P-glycoprotein (P-gp) function we showed previously that there was a discordance between the ability of acute myeloid leukemic (AML) blast cells to accumulate daunorubicin and P-gp antigen expression (Xie et al, Leukemia 1995; 9:1882-1887). Cyclosporine 6-19 ATP binding cassette subfamily B member 1 Homo sapiens 53-57 9001418-1 1997 Using cyclosporin A (CsA) to inhibit P-glycoprotein (P-gp) function we showed previously that there was a discordance between the ability of acute myeloid leukemic (AML) blast cells to accumulate daunorubicin and P-gp antigen expression (Xie et al, Leukemia 1995; 9:1882-1887). Cyclosporine 21-24 ATP binding cassette subfamily B member 1 Homo sapiens 37-51 9001418-1 1997 Using cyclosporin A (CsA) to inhibit P-glycoprotein (P-gp) function we showed previously that there was a discordance between the ability of acute myeloid leukemic (AML) blast cells to accumulate daunorubicin and P-gp antigen expression (Xie et al, Leukemia 1995; 9:1882-1887). Cyclosporine 21-24 ATP binding cassette subfamily B member 1 Homo sapiens 53-57 8892677-2 1996 SDZ PSC 833, a non-immunosuppressive cyclosporin analogue reverses multidrug resistance (MDR) in vitro by inhibiting P-glycoprotein (P-gp) mediated drug efflux. Cyclosporine 37-48 ATP binding cassette subfamily B member 1 Homo sapiens 117-131 8980113-6 1996 The resistance to aureobasidin A conferred by the MDR2/Pgp as well as by the MDR1/Pgp was overcome by vinblastine, verapamil, and cyclosporin A, depending on their concentrations, but not by colchicine. Cyclosporine 130-143 ATP binding cassette subfamily B member 1 Homo sapiens 55-58 8980113-6 1996 The resistance to aureobasidin A conferred by the MDR2/Pgp as well as by the MDR1/Pgp was overcome by vinblastine, verapamil, and cyclosporin A, depending on their concentrations, but not by colchicine. Cyclosporine 130-143 ATP binding cassette subfamily B member 1 Homo sapiens 77-81 8980113-6 1996 The resistance to aureobasidin A conferred by the MDR2/Pgp as well as by the MDR1/Pgp was overcome by vinblastine, verapamil, and cyclosporin A, depending on their concentrations, but not by colchicine. Cyclosporine 130-143 ATP binding cassette subfamily B member 1 Homo sapiens 82-85 8892677-2 1996 SDZ PSC 833, a non-immunosuppressive cyclosporin analogue reverses multidrug resistance (MDR) in vitro by inhibiting P-glycoprotein (P-gp) mediated drug efflux. Cyclosporine 37-48 ATP binding cassette subfamily B member 1 Homo sapiens 133-137 9592351-5 1996 Good reversal effect was obtained in refractory patients and MDR1 positive relapsing patients by adding CsA (P < 0.01). Cyclosporine 104-107 ATP binding cassette subfamily B member 1 Homo sapiens 61-65 8893053-2 1996 The function of P-glycoprotein was assessed by the accumulation of rhodamine-123 (Rh123) dye in the presence or absence of cyclosporin A (which inhibits Rh123 efflux). Cyclosporine 123-136 ATP binding cassette subfamily B member 1 Homo sapiens 16-30 8949984-4 1996 After 24 h incubation with 15 microM of the modulators, MDR1 gene expression was slightly but significantly decreased by two of them, quinine and cyclosporine A, whereas verapamil and S-9788 had very little effect on this parameter. Cyclosporine 146-160 ATP binding cassette subfamily B member 1 Homo sapiens 56-60 9816326-2 1996 Cyclosporin blocks P-glycoprotein-induced efflux of vincristine and teniposide in vitro, and possibly modulates responses to carboplatin. Cyclosporine 0-11 ATP binding cassette subfamily B member 1 Homo sapiens 19-33 9055138-3 1997 A variety of nonchemotherapeutic agents have been shown to inhibit P-glycoprotein-dependent drug efflux including cyclosporin. Cyclosporine 114-125 ATP binding cassette subfamily B member 1 Homo sapiens 67-81 8953513-4 1996 Acebutolol uptake by K562/ADM cells was, moreover, markedly enhanced, in a concentration-dependent manner, in the presence of the specific P-glycoprotein inhibitors, MS-209 and cyclosporin. Cyclosporine 177-188 ATP binding cassette subfamily B member 1 Homo sapiens 139-153 8898356-8 1996 This latter observation explains the enhanced potency of cyclosporin A as an inhibitor of the mutant Pgp. Cyclosporine 57-70 ATP binding cassette subfamily B member 1 Homo sapiens 101-104 8898356-10 1996 We conclude that the G185-->V mutation confers pleiotropic alterations on Pgp, including an altered basal ATPase activity and altered interaction with substrates and the inhibitor cyclosporin A. Cyclosporine 183-196 ATP binding cassette subfamily B member 1 Homo sapiens 77-80 8782646-9 1996 Moreover, treatments of MCF-7/Adr cells with P-glycoprotein (P-gp) modulators, cyclosporin A and verapamil increased doxorubicin and vincristine-induced DNA fragmentation about 1.4- and 2.5-fold, indicating that P-gp is involved in the development of resistance to chemotherapy-induced apoptosis in this cell line. Cyclosporine 79-92 ATP binding cassette subfamily B member 1 Homo sapiens 212-216 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. Cyclosporine 0-3 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. Cyclosporine 0-3 ATP binding cassette subfamily B member 1 Homo sapiens 129-132 8842452-0 1996 Relevance of p-glycoprotein for the enteral absorption of cyclosporin A: in vitro-in vivo correlation. Cyclosporine 58-71 ATP binding cassette subfamily B member 1 Homo sapiens 13-27 8842452-2 1996 The interaction of cyclosporin A (CyA) with p-glycoprotein during intestinal uptake was investigated by a combination of in vitro experiments with human Caco-2 cells and an intubation study in healthy volunteers. Cyclosporine 19-32 ATP binding cassette subfamily B member 1 Homo sapiens 44-58 8842452-21 1996 All data provide evidence that CyA is a substrate of p-glycoprotein in the GI-tract, which might explain the local differences and the high variability in cyclosporin absorption found in vivo. Cyclosporine 155-166 ATP binding cassette subfamily B member 1 Homo sapiens 53-67 8831211-13 1996 The addition of Ver or CsA to chemotherapy will be a potential circumvention of P-gp-mediated multidrug resistance of renal cell adenocarcinomas. Cyclosporine 23-26 ATP binding cassette subfamily B member 1 Homo sapiens 80-84 8707421-2 1996 We previously reported that MRK-16, an anti-P-glycoprotein MAb, enhanced MDR reversal activity of cyclosporin A (CsA) through inhibition of P-glycoprotein-mediated CsA transport. Cyclosporine 113-116 ATP binding cassette subfamily B member 1 Homo sapiens 44-58 8707421-2 1996 We previously reported that MRK-16, an anti-P-glycoprotein MAb, enhanced MDR reversal activity of cyclosporin A (CsA) through inhibition of P-glycoprotein-mediated CsA transport. Cyclosporine 113-116 ATP binding cassette subfamily B member 1 Homo sapiens 140-154 8707421-7 1996 P-glycoprotein could not transport PSC833 but could transport CsA. Cyclosporine 62-65 ATP binding cassette subfamily B member 1 Homo sapiens 0-14 8691629-3 1996 For example, verapamil or cyclosporin A may be useful for p-glycoprotein related multidrug resistance, and amphotericin B, docosahexaenoic acid or 8-chloro cAMP can be used for the modification of cisplatin-resistance. Cyclosporine 26-39 ATP binding cassette subfamily B member 1 Homo sapiens 58-72 8792427-3 1996 P-GP efflux function was determined by measuring transmonolayer fluxes of cyclosporin A (CsA) and verapamil, while P-GP expression level was evaluated by Western blot analysis using monoclonal antibody C219. Cyclosporine 74-87 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 8792427-3 1996 P-GP efflux function was determined by measuring transmonolayer fluxes of cyclosporin A (CsA) and verapamil, while P-GP expression level was evaluated by Western blot analysis using monoclonal antibody C219. Cyclosporine 89-92 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 8635866-7 1996 Verapamil and cyclosporin A were only partially effective in blocking P-gp drug efflux in MDR10V compared to Dox40 cells. Cyclosporine 14-27 ATP binding cassette subfamily B member 1 Homo sapiens 70-74 8967446-13 1996 It was found that MDR1 activity and its inhibition by cyclosporine A or flufenamic acid were unaffected by hypotonicity alone or in combination with Cl- channel blockers. Cyclosporine 54-68 ATP binding cassette subfamily B member 1 Homo sapiens 18-22 8791998-0 1996 Detection of P-glycoprotein expression by tumoral cells with NBDL-CsA, a fluorescent derivative of cyclosporin A. Cyclosporine 99-112 ATP binding cassette subfamily B member 1 Homo sapiens 13-27 8791998-2 1996 Though first described as an inhibitor of P-gp function, cyclosporin A (CsA) was more recently shown to behave as a substrate of the P-gp pump. Cyclosporine 57-70 ATP binding cassette subfamily B member 1 Homo sapiens 133-137 8791998-2 1996 Though first described as an inhibitor of P-gp function, cyclosporin A (CsA) was more recently shown to behave as a substrate of the P-gp pump. Cyclosporine 72-75 ATP binding cassette subfamily B member 1 Homo sapiens 133-137 8791998-4 1996 MDR-CEM cell treatment by the P-gp blockers restored the [3H]CsA retention to the control Par-CEM cell levels. Cyclosporine 61-64 ATP binding cassette subfamily B member 1 Homo sapiens 30-34 21544450-0 1996 P-glycoprotein-associated resistance to taxol and taxotere and its reversal by dexniguldipine-HCl, dexverapamil-HCl, or cyclosporin A. Cyclosporine 120-133 ATP binding cassette subfamily B member 1 Homo sapiens 0-14 9816222-0 1996 Cyclosporin A and PSC 833 prevent up-regulation of MDR1 expression by anthracyclines in a human multidrug-resistant cell line. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 51-55 21544450-5 1996 Dexniguldipine-HCl or cyclosporin A, however, both showed a similarly strong modulating activity on the HeLa-MDR1 transfectant in clear contrast to the effects observed using the pyridine B8909-008, or dexverapamil-HCl, respectively, at the same final concentrations. Cyclosporine 22-35 ATP binding cassette subfamily B member 1 Homo sapiens 109-113 8668925-2 1996 Rapamycin was compared to cyclosporine A for its ability to inhibit P-glycoprotein on normal human peripheral blood mononuclear cells (PBMC). Cyclosporine 26-40 ATP binding cassette subfamily B member 1 Homo sapiens 68-82 9816200-3 1996 CsA has been shown to modify the function of a membrane P-glycoprotein (Pgp) whose overexpression is associated with a multidrug-resistant (MDR1) phenotype. Cyclosporine 0-3 ATP binding cassette subfamily B member 1 Homo sapiens 56-70 9816200-3 1996 CsA has been shown to modify the function of a membrane P-glycoprotein (Pgp) whose overexpression is associated with a multidrug-resistant (MDR1) phenotype. Cyclosporine 0-3 ATP binding cassette subfamily B member 1 Homo sapiens 72-75 9816200-3 1996 CsA has been shown to modify the function of a membrane P-glycoprotein (Pgp) whose overexpression is associated with a multidrug-resistant (MDR1) phenotype. Cyclosporine 0-3 ATP binding cassette subfamily B member 1 Homo sapiens 140-144 9816200-7 1996 Pgp expression was assessed further after prolonged (10-day) treatment with CsA. Cyclosporine 76-79 ATP binding cassette subfamily B member 1 Homo sapiens 0-3 9816200-11 1996 Similarly, plasma from patients containing immunosuppressive levels of CsA lowered DOX IC50 of the MDR1(+) Hep G2 cells by up to 4-fold. Cyclosporine 71-74 ATP binding cassette subfamily B member 1 Homo sapiens 99-103 9816200-15 1996 Pharmacological concentrations of cyclosporin analogues, including one nonimmunosuppressive form, enhance DOX cytotoxicity of MDR1(+) HCC cells by modulating drug retention. Cyclosporine 34-45 ATP binding cassette subfamily B member 1 Homo sapiens 126-130 9816200-16 1996 CsA as found in posttransplant patient plasma enhanced DOX cytotoxicity to human MDR1(+) hepatoma cells in vitro, albeit at less than optimal chemosensitizing concentrations. Cyclosporine 0-3 ATP binding cassette subfamily B member 1 Homo sapiens 81-85 9816200-18 1996 These findings support our hypothesis that in vivo immunosuppressive levels of CsA may enhance DOX chemotherapeutic efficacy on MDR1(+) HCC cells. Cyclosporine 79-82 ATP binding cassette subfamily B member 1 Homo sapiens 128-132 8833064-3 1996 P-gp can be competitively inhibited by exposure to antirheumatic drugs including antimalarials and cyclosporin A. Cyclosporine 99-112 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 8833064-9 1996 We hypothesize that antiarthritic effects of the antimalarials and cyclosporine and perhaps glucocorticoids are partially attributable to the inhibition of P-gp function thereby blocking TNF-alpha release by macrophages, TNF-alpha activation of NK cells, and NK cell secretion of cytotoxins in the rheumatoid joint. Cyclosporine 67-79 ATP binding cassette subfamily B member 1 Homo sapiens 156-160 8567666-4 1996 Verapamil, cyclosporin A, and a number of other agents that compete with cytotoxic drugs for binding sites on P-glycoprotein can potently reverse MDR, but this is accompanied by severe toxicity in vivo. Cyclosporine 11-24 ATP binding cassette subfamily B member 1 Homo sapiens 110-124 8944329-11 1996 The data suggest that MPA as well as CsA may be useful as modifying agents in overcoming Pgp-associated multidrug resistance. Cyclosporine 37-40 ATP binding cassette subfamily B member 1 Homo sapiens 89-92 8672855-0 1996 [Expression of the MDR1 gene in five human cell lines of medullary thyroid cancer and reversion of the resistance to doxorubicine by ciclosporin A and verapamil]. Cyclosporine 133-146 ATP binding cassette subfamily B member 1 Homo sapiens 19-23 8548874-8 1996 In contrast, the P-glycoprotein inhibitors verapamil and cyclosporin A did not inhibit THP efflux. Cyclosporine 57-70 ATP binding cassette subfamily B member 1 Homo sapiens 17-31 8884813-0 1996 alpha-(3,4-dimethyoxyphenyl)-3,4-dihydro-6,7-dimethoxy-alpha- [(4-methylphenyl)thio]-2(1H)-isoquinolineheptanenitrile (CL 329,753): a novel chemosensitizing agent for P-glycoprotein-mediated resistance with improved biological properties compared with verapamil and cyclosporine A. Cyclosporine 266-280 ATP binding cassette subfamily B member 1 Homo sapiens 167-181 8533588-1 1995 Cyclosporin A (CyA) overcomes P-glycoprotein (P-gp) associated multidrug resistance (MDR). Cyclosporine 0-11 ATP binding cassette subfamily B member 1 Homo sapiens 30-44 7503774-8 1995 Cremophor El, the vehicle used to administer CsA and PSC intravenously, was also able to inhibit IAAP photolabeling of P-gp. Cyclosporine 45-48 ATP binding cassette subfamily B member 1 Homo sapiens 119-123 7503774-10 1995 Photolabeling of P-gp with this compound was abolished almost completely by CsA and PSC. Cyclosporine 76-79 ATP binding cassette subfamily B member 1 Homo sapiens 17-21 7475279-2 1995 Transport function was assessed by measuring the modulating effect of the Pgp inhibitor cyclosporin A (CsA) on the cellular accumulation of daunorubicin, and Pgp antigen expression by surface immunofluorescence using the MRK-16 antibody. Cyclosporine 88-101 ATP binding cassette subfamily B member 1 Homo sapiens 74-77 7475279-2 1995 Transport function was assessed by measuring the modulating effect of the Pgp inhibitor cyclosporin A (CsA) on the cellular accumulation of daunorubicin, and Pgp antigen expression by surface immunofluorescence using the MRK-16 antibody. Cyclosporine 103-106 ATP binding cassette subfamily B member 1 Homo sapiens 74-77 8944329-8 1996 Incubation with either CsA or MPA plus Adr enhanced Adr toxicity in Pgp+ but not Pgp- cell cultures, whereas TAM had no effect on the sensitivity of any of the cultures. Cyclosporine 23-26 ATP binding cassette subfamily B member 1 Homo sapiens 68-71 8533588-1 1995 Cyclosporin A (CyA) overcomes P-glycoprotein (P-gp) associated multidrug resistance (MDR). Cyclosporine 0-11 ATP binding cassette subfamily B member 1 Homo sapiens 46-50 8845477-3 1995 Such a distribution seems to be responsible for the transcellular transport of Pgp substrates, including cyclosporin A (CsA), from the basal to the apical side. Cyclosporine 120-123 ATP binding cassette subfamily B member 1 Homo sapiens 79-82 7547962-7 1995 P-glycoprotein modulators generally demonstrated significantly greater potency (EC50; microM): SDZ PSC 833, 0.08; cyclosporin A, 1.3; verapamil, 4.1; quinidine, 6.4; prazosin, > 300. Cyclosporine 114-127 ATP binding cassette subfamily B member 1 Homo sapiens 0-14 8845477-5 1995 Nevertheless, the sensitivity of their mitogen-induced proliferation to cytostatics, including doxorubicin and CsA, could be increased by the Pgp blockers. Cyclosporine 111-114 ATP binding cassette subfamily B member 1 Homo sapiens 142-145 8845477-6 1995 Using isotopically-labeled CsA and tumoral lymphoid cell lines, we now show a higher CsA retention in Pgp-lacking parental ("Par") cells than in Pgp-expressing MDR cells. Cyclosporine 85-88 ATP binding cassette subfamily B member 1 Homo sapiens 102-105 8845477-7 1995 The Pgp blockers can restore the CsA retention in the MDR cells to its level in the Par cells. Cyclosporine 33-36 ATP binding cassette subfamily B member 1 Homo sapiens 4-7 7545025-3 1995 Because MDR1 efflux function may be modified by drugs such as cyclosporin A, accurate identification of MDR1+/efflux+ AML cases will be critical to identify patients who may benefit from therapies that contain such MDR1 modulators. Cyclosporine 62-75 ATP binding cassette subfamily B member 1 Homo sapiens 8-12 7545025-3 1995 Because MDR1 efflux function may be modified by drugs such as cyclosporin A, accurate identification of MDR1+/efflux+ AML cases will be critical to identify patients who may benefit from therapies that contain such MDR1 modulators. Cyclosporine 62-75 ATP binding cassette subfamily B member 1 Homo sapiens 104-108 7545025-3 1995 Because MDR1 efflux function may be modified by drugs such as cyclosporin A, accurate identification of MDR1+/efflux+ AML cases will be critical to identify patients who may benefit from therapies that contain such MDR1 modulators. Cyclosporine 62-75 ATP binding cassette subfamily B member 1 Homo sapiens 104-108 7643631-4 1995 Downmodulation of Pgp function in these cell lines could be demonstrated with different substances (verapamil, vinblastine, trifluoperazine, cyclosporin A, progesterone and quinidine) and was proven to be consistently higher in the vinblastine selected cells than in their non-selected drug sensitive counterparts. Cyclosporine 141-154 ATP binding cassette subfamily B member 1 Homo sapiens 18-21 7631829-0 1995 Differential interaction of human renal P-glycoprotein with various metabolites and analogues of cyclosporin A. Cyclosporine 97-110 ATP binding cassette subfamily B member 1 Homo sapiens 40-54 7631829-1 1995 Interactions of P-glycoprotein with several analogues and metabolites of cyclosporin A were studied to gain a better understanding of this immunosuppressant"s mechanism of excretion and nephrotoxicity. Cyclosporine 73-86 ATP binding cassette subfamily B member 1 Homo sapiens 16-30 7631829-4 1995 Cyclosporins A [half-maximal inhibition constant (K0.5) = 20 nM] and G (K0.5 = 40 nM) blocked [3H]azidopine photolabeling of renal P-glycoprotein at very low concentrations, whereas higher concentrations of cyclosporin C (K0.5 = 500 nM) and metabolites 1, 17, and 21 (K0.5 = 200 nM) were required to inhibit photolabeling. Cyclosporine 0-14 ATP binding cassette subfamily B member 1 Homo sapiens 131-145 7559918-0 1995 Inhibition of cell-mediated cytolysis and P-glycoprotein function in natural killer cells by verapamil isomers and cyclosporine A analogs. Cyclosporine 115-129 ATP binding cassette subfamily B member 1 Homo sapiens 42-56 7631829-7 1995 Cyclosporins A, C, and G also enhanced cellular accumulation of [3H]cyclosporin A and several other 3H-labeled compounds known to be transported by P-glycoprotein in multidrug-resistant C5 cells. Cyclosporine 0-14 ATP binding cassette subfamily B member 1 Homo sapiens 148-162 7631829-8 1995 Differential affinities of cyclosporin A metabolites for P-glycoprotein suggest considerable drug-binding site specificity. Cyclosporine 27-40 ATP binding cassette subfamily B member 1 Homo sapiens 57-71 7631829-9 1995 Our current hypothesis is that cyclosporin A may be more nephrotoxic than its metabolites by virtue of its superior ability to bind to and competitively inhibit urinary excretion of an endogenous P-glycoprotein substrate. Cyclosporine 31-44 ATP binding cassette subfamily B member 1 Homo sapiens 196-210 7879232-0 1995 Expression of the multidrug resistance gene MDR-1 in peripheral blood mononuclear cells from cyclosporine-treated renal transplant recipients rejecting their graft. Cyclosporine 93-105 ATP binding cassette subfamily B member 1 Homo sapiens 44-49 7896810-7 1995 Kinetic analyses indicate that cyclosporin A, an inhibitor of Pgp, binds to the verapamil and vinblastine binding/transport site(s) in the Pgp. Cyclosporine 31-44 ATP binding cassette subfamily B member 1 Homo sapiens 62-65 7896810-7 1995 Kinetic analyses indicate that cyclosporin A, an inhibitor of Pgp, binds to the verapamil and vinblastine binding/transport site(s) in the Pgp. Cyclosporine 31-44 ATP binding cassette subfamily B member 1 Homo sapiens 139-142 7896810-8 1995 Taken together, the results presented herein reveal that the verapamil and vinblastine binding/transport site(s) are in close proximity and that the cyclosporin A binding site spans the common region of these two drug binding/transport site(s) in the Pgp molecule. Cyclosporine 149-162 ATP binding cassette subfamily B member 1 Homo sapiens 251-254 7540903-2 1995 The efficacy of verapamil and cyclosporine A as modulators of P-glycoprotein, the multidrug resistance (MDR1) gene product, was studied in leukemic blast cells from 56 patients with de novo acute myeloid leukemia (AML) in vitro. Cyclosporine 30-44 ATP binding cassette subfamily B member 1 Homo sapiens 62-76 7540903-2 1995 The efficacy of verapamil and cyclosporine A as modulators of P-glycoprotein, the multidrug resistance (MDR1) gene product, was studied in leukemic blast cells from 56 patients with de novo acute myeloid leukemia (AML) in vitro. Cyclosporine 30-44 ATP binding cassette subfamily B member 1 Homo sapiens 104-108 7559918-8 1995 Both CsA and PSC maximally inhibited P-gp efflux at 3 microM, but only minimally inhibited cell-mediated cytolysis. Cyclosporine 5-8 ATP binding cassette subfamily B member 1 Homo sapiens 37-41 8704277-7 1995 In this study, the interactions of P-glycoprotein with two cyclosporine derivatives, SDZ PSC 833 and cyclosporine A (CsA, Sandimmune), were analyzed. Cyclosporine 59-71 ATP binding cassette subfamily B member 1 Homo sapiens 35-49 8704277-7 1995 In this study, the interactions of P-glycoprotein with two cyclosporine derivatives, SDZ PSC 833 and cyclosporine A (CsA, Sandimmune), were analyzed. Cyclosporine 101-115 ATP binding cassette subfamily B member 1 Homo sapiens 35-49 8704277-7 1995 In this study, the interactions of P-glycoprotein with two cyclosporine derivatives, SDZ PSC 833 and cyclosporine A (CsA, Sandimmune), were analyzed. Cyclosporine 117-120 ATP binding cassette subfamily B member 1 Homo sapiens 35-49 8704277-9 1995 The two cyclosporine analogs competed with the labeling of P-glycoprotein by a photoactive cyclosporine derivative. Cyclosporine 8-20 ATP binding cassette subfamily B member 1 Homo sapiens 59-73 8704277-9 1995 The two cyclosporine analogs competed with the labeling of P-glycoprotein by a photoactive cyclosporine derivative. Cyclosporine 91-103 ATP binding cassette subfamily B member 1 Homo sapiens 59-73 8704277-11 1995 However, CsA was transported by P-glycoprotein, whereas SDZ PSC 833 was not actively transported. Cyclosporine 9-12 ATP binding cassette subfamily B member 1 Homo sapiens 32-46 8704277-14 1995 In addition, the comparison of the two cyclosporine analogs indicated that limited chemical modifications of MDR reversing agents can affect their potential to inhibit P-glycoprotein function. Cyclosporine 39-51 ATP binding cassette subfamily B member 1 Homo sapiens 168-182 7705462-6 1994 These data suggest that P-glycoprotein possesses at least two allosterically coupled drug acceptor sites; receptor site 1 which binds vinblastine, doxorubucin, etoposide and cyclosporin A, and receptor site 2 which binds dexniguldipine-HCl and other 1,4-dihydropyridines. Cyclosporine 174-187 ATP binding cassette subfamily B member 1 Homo sapiens 24-38 7727860-9 1994 These studies have employed "first generation" antagonists such as verapamil and cyclosporine which were toxic at concentrations needed to block P-glycoprotein. Cyclosporine 81-93 ATP binding cassette subfamily B member 1 Homo sapiens 145-159 21559677-0 1994 Reversion of p-glycoprotein mediated multidrug-resistance to vincristine and adriamycin by psc-833, a cyclosporine derivative in human neuroblastoma cell-lines. Cyclosporine 102-114 ATP binding cassette subfamily B member 1 Homo sapiens 13-27 7964963-8 1994 Verapamil and cyclosporine (CsA) have been used as competitive inhibitors of the multidrug transporter P-gp in early clinical trials. Cyclosporine 14-26 ATP binding cassette subfamily B member 1 Homo sapiens 103-107 7964963-8 1994 Verapamil and cyclosporine (CsA) have been used as competitive inhibitors of the multidrug transporter P-gp in early clinical trials. Cyclosporine 28-31 ATP binding cassette subfamily B member 1 Homo sapiens 103-107 7964963-9 1994 Although these studies show some activity in modulating clinical MDR, both verapamil and CsA manifest considerable toxicities at doses below those required for complete inhibition of P-gp function. Cyclosporine 89-92 ATP binding cassette subfamily B member 1 Homo sapiens 183-187 7808368-4 1994 The existence of drugs (calcium blockers, cyclosporine, tamoxifen, reserpine, quinidine) able to bind themselves to gp170 and to paralyze its activity in vitro is well known. Cyclosporine 42-54 ATP binding cassette subfamily B member 1 Homo sapiens 116-121 7808368-13 1994 Our data suggest a synergy of verapamil and cyclosporine in the inhibition of multidrug resistance induced by gp170, without the occurrence of heavy toxicity. Cyclosporine 44-56 ATP binding cassette subfamily B member 1 Homo sapiens 110-115 7511575-0 1994 Cyclosporin A enhances susceptibility of multi-drug resistant human cancer cells to anti-P-glycoprotein antibody-dependent cytotoxicity of monocytes, but not of lymphocytes. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 89-103 7518859-6 1994 Functional Pgp expression was determined by the effect of CSA on the intracellular accumulation of DXR and VCR. Cyclosporine 58-61 ATP binding cassette subfamily B member 1 Homo sapiens 11-14 7518859-10 1994 CSA, as well as SDZ PSC 833, but not dexamethasone, increased pretreatment intracellular accumulation of DXR and VCR in Pgp+ PC in three of four and six of six patients, respectively. Cyclosporine 0-3 ATP binding cassette subfamily B member 1 Homo sapiens 120-123 7518859-13 1994 CONCLUSION: These data indicate that Pgp overexpression is functional in refractory myeloma and that clinical modulation of MDR by CSA is mediated through an inhibition of Pgp-associated drug efflux. Cyclosporine 131-134 ATP binding cassette subfamily B member 1 Homo sapiens 37-40 7518859-13 1994 CONCLUSION: These data indicate that Pgp overexpression is functional in refractory myeloma and that clinical modulation of MDR by CSA is mediated through an inhibition of Pgp-associated drug efflux. Cyclosporine 131-134 ATP binding cassette subfamily B member 1 Homo sapiens 172-175 7518859-14 1994 Pgp-expressing PC can be eliminated by clinical treatment with VAD/CSA. Cyclosporine 67-70 ATP binding cassette subfamily B member 1 Homo sapiens 0-3 7518390-6 1994 Using experimental conditions in which these ionophores were unable to modify either the intracellular pH, or the transmembrane potential, or to induce an intracellular ATP depletion, we have shown that mobile ionophores as well as cyclosporin inhibit the P-glycoprotein-mediated efflux of 4"-O-tetrahydropyranyl-adriamycin in K562 resistant cells, whereas gramicidin, a channel-forming ionophore, does not. Cyclosporine 232-243 ATP binding cassette subfamily B member 1 Homo sapiens 256-270 7919458-5 1994 In resistant cells, the ether phospholipid effect on DNR accumulation has also been found after blocking the PgP function by verapamil and cyclosporin A. Cyclosporine 139-152 ATP binding cassette subfamily B member 1 Homo sapiens 109-112 7910563-4 1994 There was an inverse relationship between Pgp expression and calcein/AM accumulation, which increased dose-dependently in the presence of cyclosporin A (CsA) and the nonimmunosuppressive analogue SDZ PSC 833 (PSC) in the Pgp-expressing cell lines. Cyclosporine 153-156 ATP binding cassette subfamily B member 1 Homo sapiens 42-45 7915506-5 1994 Whereas the cytotoxic effect of Dox was considerably increased by verapamil, cyclosporin A and its non-immunosuppressive analogue SDZ PSC 833 in the Pgp-expressing Dox-resistant sublines, comparatively small effects on the Dox and Vcr sensitivity were observed in the patient samples, irrespective of their Pgp expression. Cyclosporine 77-90 ATP binding cassette subfamily B member 1 Homo sapiens 149-152 7626853-5 1995 MDR resistance is mediated by GP170, a cell membrane protein, which can be inhibited by several pharmacological agents like verapamil, ciclosporine and S 9788 which are currently being clinically investigated. Cyclosporine 135-147 ATP binding cassette subfamily B member 1 Homo sapiens 30-35 8118035-1 1994 Cremophor (Crem) EL, the vehicle for intravenous delivery of cyclosporin A (CsA), has been reported to counteract multidrug resistance (MDR) in P-glycoprotein (Pgp)-over-expressing cell lines. Cyclosporine 76-79 ATP binding cassette subfamily B member 1 Homo sapiens 144-158 8118035-1 1994 Cremophor (Crem) EL, the vehicle for intravenous delivery of cyclosporin A (CsA), has been reported to counteract multidrug resistance (MDR) in P-glycoprotein (Pgp)-over-expressing cell lines. Cyclosporine 76-79 ATP binding cassette subfamily B member 1 Homo sapiens 160-163 7906507-0 1994 [Enhancement of cellular accumulation of cyclosporine by anti-P-glycoprotein monoclonal antibody MRK-16, and their synergistic modulation of multidrug resistance]. Cyclosporine 41-53 ATP binding cassette subfamily B member 1 Homo sapiens 62-76 7511575-1 1994 Cyclosporin A (CsA) was previously found to bind to P-glycoprotein expressed on multidrug-resistant (MDR) cancer cells. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 52-66 7879670-5 1994 It has been demonstrated, at least in the laboratory, that resistance mediated by P-glycoprotein may be modulated by a wide variety of compounds, including verapamil and cyclosporine A. Cyclosporine 170-184 ATP binding cassette subfamily B member 1 Homo sapiens 82-96 7538609-3 1994 P-glycoprotein also transports MDR modulators such as cyclosporin A, FK506, and calcium channel blockers. Cyclosporine 54-67 ATP binding cassette subfamily B member 1 Homo sapiens 0-14 7910786-0 1994 Inhibition of P-glycoprotein-mediated vinblastine transport across HCT-8 intestinal carcinoma monolayers by verapamil, cyclosporine A and SDZ PSC 833 in dependence on extracellular pH. Cyclosporine 119-133 ATP binding cassette subfamily B member 1 Homo sapiens 14-28 7907333-9 1994 Interestingly, resistance of F4-6RADR-CsA cells remained reversible for the calcium antagonists verapamil and dihydropyridine B859-35 (dexniguldipine-HCl), indicating that CsA and these compounds interfere with the P glycoprotein function by different pharmacodynamic mechanisms. Cyclosporine 38-41 ATP binding cassette subfamily B member 1 Homo sapiens 215-229 7907333-12 1994 Results indicate that increased amounts of the P-glycoprotein--besides other, perhaps more important mechanisms that are as yet unknown--partially mediate CsA resistance in F4-6RADR-CsA cells. Cyclosporine 155-158 ATP binding cassette subfamily B member 1 Homo sapiens 47-61 7907333-12 1994 Results indicate that increased amounts of the P-glycoprotein--besides other, perhaps more important mechanisms that are as yet unknown--partially mediate CsA resistance in F4-6RADR-CsA cells. Cyclosporine 182-185 ATP binding cassette subfamily B member 1 Homo sapiens 47-61 18476229-9 1994 Cyclosporin which is also a strong Ca(2+) chelating agent also inhibits the P-glycoprotein-mediated efflux of anthracycline. Cyclosporine 0-11 ATP binding cassette subfamily B member 1 Homo sapiens 76-90 7911345-11 1993 Reversal compounds specifically inhibiting Pgp were found, such as verapamil, cyclosporin or quinidine. Cyclosporine 78-89 ATP binding cassette subfamily B member 1 Homo sapiens 43-46 7941591-5 1994 Resistance to cytostatic drugs due to the p-glycoprotein coded by the MDR-gene is treated by a combination of cyclosporin-A or verapamil and VAD. Cyclosporine 110-123 ATP binding cassette subfamily B member 1 Homo sapiens 42-56 7693050-10 1993 The functional MDR1-protein against vincristine was also observed, and its function was inhibited by verapamile and Cyclosporin A. Cyclosporine 116-129 ATP binding cassette subfamily B member 1 Homo sapiens 15-19 7690250-6 1993 Transport of P-glycoprotein antagonists in SW620 Ad300 cells was also affected by calphostin C. Cyclosporin A transport decreased, while verapamil transport increased. Cyclosporine 96-109 ATP binding cassette subfamily B member 1 Homo sapiens 13-27 7690250-7 1993 Cyclosporin A in calphostin C-treated cells resulted in additive P-glycoprotein antagonism, while no additive effect could be demonstrated with verapamil, suggesting that the increase in verapamil transport makes it a poorer P-glycoprotein antagonist. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 65-79 7690250-7 1993 Cyclosporin A in calphostin C-treated cells resulted in additive P-glycoprotein antagonism, while no additive effect could be demonstrated with verapamil, suggesting that the increase in verapamil transport makes it a poorer P-glycoprotein antagonist. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 225-239 8099844-5 1993 P-Glycoprotein inhibitors such as quinidine, verapamil, vincristine, and cyclosporine increased the net A-B flux and inhibited the total B-A flux without affecting the nonspecific flux significantly. Cyclosporine 73-85 ATP binding cassette subfamily B member 1 Homo sapiens 0-14 8102639-18 1993 CONCLUSION: High doses of CsA, which achieve blood concentrations capable of reversing P-glycoprotein-mediated anthracycline resistance in vitro, can be incorporated into induction regimens with acceptable nonhematologic toxicity. Cyclosporine 26-29 ATP binding cassette subfamily B member 1 Homo sapiens 87-101 8103797-3 1993 Cyclosporin A inhibited the transepithelial transport of digoxin mediated by human P-glycoprotein; net basal-to-apical transport across the cell monolayer was 22.8, 21.2, 6.61 and 0.91 pmol/mg of protein/3 hr in the presence of 0, 1, 5 and 10 microM cyclosporin A, respectively. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 83-97 8103797-3 1993 Cyclosporin A inhibited the transepithelial transport of digoxin mediated by human P-glycoprotein; net basal-to-apical transport across the cell monolayer was 22.8, 21.2, 6.61 and 0.91 pmol/mg of protein/3 hr in the presence of 0, 1, 5 and 10 microM cyclosporin A, respectively. Cyclosporine 250-263 ATP binding cassette subfamily B member 1 Homo sapiens 83-97 7681059-0 1993 Human P-glycoprotein transports cyclosporin A and FK506. Cyclosporine 32-45 ATP binding cassette subfamily B member 1 Homo sapiens 6-20 7681059-3 1993 Cyclosporin A itself interacts with a common binding site of P-glycoprotein to which Vinca alkaloids and verapamil bind. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 61-75 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. Cyclosporine 40-53 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. Cyclosporine 83-96 ATP binding cassette subfamily B member 1 Homo sapiens 28-42 8397460-15 1993 In summary, the combination of tamoxifen and cyclosporin A at the concentrations normally seen after clinical administration of these modulators showed significant synergism on the sensitivity to doxorubicin in both low and high MDR1 expressor HCC lines. Cyclosporine 45-58 ATP binding cassette subfamily B member 1 Homo sapiens 229-233 8094079-1 1993 We observed increased levels of mdr-1 mRNA and its protein product P-glycoprotein (Pgp) in the human colon carcinoma cell line, LS 180, and its drug-resistant sublines, LS 180-Ad50 and LS 180-Vb2, after treatment with the Pgp antagonists, verapamil, nifedipine, and cyclosporin A. Cyclosporine 266-279 ATP binding cassette subfamily B member 1 Homo sapiens 32-37 8094079-1 1993 We observed increased levels of mdr-1 mRNA and its protein product P-glycoprotein (Pgp) in the human colon carcinoma cell line, LS 180, and its drug-resistant sublines, LS 180-Ad50 and LS 180-Vb2, after treatment with the Pgp antagonists, verapamil, nifedipine, and cyclosporin A. Cyclosporine 266-279 ATP binding cassette subfamily B member 1 Homo sapiens 83-86 1363515-1 1992 Cyclosporin A and verapamil are substrates for P-glycoprotein. Cyclosporine 0-13 ATP binding cassette subfamily B member 1 Homo sapiens 47-61 1363104-5 1992 P-glycoprotein in T cells is a functionally active efflux pump as demonstrated by decreased retention of rhodamine-123 and its increased accumulation by cyclosporin A, an inhibitor of Pgp function. Cyclosporine 153-166 ATP binding cassette subfamily B member 1 Homo sapiens 0-14 1363104-5 1992 P-glycoprotein in T cells is a functionally active efflux pump as demonstrated by decreased retention of rhodamine-123 and its increased accumulation by cyclosporin A, an inhibitor of Pgp function. Cyclosporine 153-166 ATP binding cassette subfamily B member 1 Homo sapiens 184-187 1350249-7 1992 Among the six evaluable cases tested with mitoxantrone and CyA, an increase of 50% in CFU-L sensitivity to mitoxantrone was noted in one (of three) P-gp+ patient. Cyclosporine 59-62 ATP binding cassette subfamily B member 1 Homo sapiens 148-152 1358068-6 1992 It is concluded that P-gp possesses at least two allosterically coupled drug acceptor sites, receptor site-1 that is selective for vinca alkaloids and cyclosporin A, and receptor site-2 that is selective for 1,4-dihydropyridines. Cyclosporine 151-164 ATP binding cassette subfamily B member 1 Homo sapiens 21-25 1685551-0 1991 Increased drug accumulation ex vivo with cyclosporin in chronic lymphatic leukemia and its relationship to epitope masking of P-glycoprotein. Cyclosporine 41-52 ATP binding cassette subfamily B member 1 Homo sapiens 126-140 1679456-4 1991 The binding of 3H-cyclosporine diazirine analogue to P-glycoprotein was competable by excess cyclosporine A and by the nonimmunosuppressive cyclosporine H. Cyclosporine 93-107 ATP binding cassette subfamily B member 1 Homo sapiens 53-67 1671638-6 1991 The MDR modifiers verapamil, Cremophor EL, cyclosporin A and Ro 11-2933/001 had significant effects on DN cytotoxicity, total DN accumulation and efflux, only if P-gp was present. Cyclosporine 43-56 ATP binding cassette subfamily B member 1 Homo sapiens 162-166 1674429-3 1991 By applying the method of immunocytochemical assay, we have demonstrated the appearance of the multidrug-resistant phenotype (P-glycoprotein+ cells, multidrug-resistant cells) in mononuclear cells of the peripheral blood from 32/49 patients receiving triple-drug (azathioprine, steroids, cyclosporine) immunosuppressive therapy after heart transplantation. Cyclosporine 288-300 ATP binding cassette subfamily B member 1 Homo sapiens 126-140 1679456-5 1991 These results suggest that cyclosporine reverses the MDR phenotype by binding directly to P-glycoprotein and that this binding is not dependent on the immunosuppressive potential of the cyclosporine derivative. Cyclosporine 27-39 ATP binding cassette subfamily B member 1 Homo sapiens 90-104 15812356-3 2005 Constant presence of cyclosporin A (CsA) as a P-glycoprotein (Pgp) blocker in some cell cultures simulated prophylactic inhibition of this protein activity for prevention of drug resistance development from the very beginning of treatment. Cyclosporine 21-34 ATP binding cassette subfamily B member 1 Homo sapiens 46-60 2323839-9 1990 Since cyclosporin A is an inhibitor of the mdr1-encoded P-glycoprotein drug pump, these data suggest that in PLL cells mdr3 also codes for a drug efflux pump. Cyclosporine 6-19 ATP binding cassette subfamily B member 1 Homo sapiens 43-47 1968051-0 1990 Overexpression of the mdr1 gene in blast cells from patients with acute myelocytic leukemia is associated with decreased anthracycline accumulation that can be restored by cyclosporin-A. Cyclosporine 172-185 ATP binding cassette subfamily B member 1 Homo sapiens 22-26 1968051-8 1990 The degree of Cy-A-induced increase in drug accumulation in the leukemic cells correlated approximately with the level of overexpression of the mdr1 gene. Cyclosporine 14-18 ATP binding cassette subfamily B member 1 Homo sapiens 144-148 1972761-0 1990 Expression of mdr1 and mdr3 multidrug-resistance genes in human acute and chronic leukemias and association with stimulation of drug accumulation by cyclosporine. Cyclosporine 149-161 ATP binding cassette subfamily B member 1 Homo sapiens 14-18 1972761-4 1990 In vitro drug uptake studies by on-line flow cytometry showed that in leukemia cells expressing either mdr1 or mdr3, the steady-state accumulation of daunorubicin could be significantly increased by addition of cyclosporine and, to a lesser extent, by verapamil. Cyclosporine 211-223 ATP binding cassette subfamily B member 1 Homo sapiens 103-107 1972761-5 1990 Because cyclosporine and verapamil are known as inhibitors of the mdr1-encoded P-glycoprotein drug-efflux pump, and because the mdr1 and mdr3 genes are highly homologous, our data suggest that the mdr3 gene encodes a functional drug pump in B-cell lymphocytic leukemias. Cyclosporine 8-20 ATP binding cassette subfamily B member 1 Homo sapiens 66-70 15812356-3 2005 Constant presence of cyclosporin A (CsA) as a P-glycoprotein (Pgp) blocker in some cell cultures simulated prophylactic inhibition of this protein activity for prevention of drug resistance development from the very beginning of treatment. Cyclosporine 21-34 ATP binding cassette subfamily B member 1 Homo sapiens 62-65 15812356-3 2005 Constant presence of cyclosporin A (CsA) as a P-glycoprotein (Pgp) blocker in some cell cultures simulated prophylactic inhibition of this protein activity for prevention of drug resistance development from the very beginning of treatment. Cyclosporine 36-39 ATP binding cassette subfamily B member 1 Homo sapiens 46-60 15812356-3 2005 Constant presence of cyclosporin A (CsA) as a P-glycoprotein (Pgp) blocker in some cell cultures simulated prophylactic inhibition of this protein activity for prevention of drug resistance development from the very beginning of treatment. Cyclosporine 36-39 ATP binding cassette subfamily B member 1 Homo sapiens 62-65 32682934-10 2020 The saturated binding of ciclosporin to erythrocytes, auto-inhibition induced by the inhibitory effects of ciclosporin on cytochrome P450 3A4/P-glycoprotein may have contributed to the nonlinearity. Cyclosporine 25-36 ATP binding cassette subfamily B member 1 Homo sapiens 142-156 33974505-0 2021 Association of polymorphism of CYP3A4, ABCB1, ABCC2, ABCG2, NFKB1, POR, and PXR with the concentration of cyclosporin a in allogeneic hematopoietic stem cell transplantation recipients. Cyclosporine 106-119 ATP binding cassette subfamily B member 1 Homo sapiens 39-44 33974505-2 2021 In this study, we aimed to identify the association of CYP3A4, ABCB1, ABCC2, ABCG2, NFKB1, POR, and PXR polymorphisms with CsA concentrations in patients with allogeneic hematopoietic cell transplantation (allo-HSCT) based on the route of administration.A total of 40 allo-HSCT recipients receiving CsA were genotyped for CYP3A4, ABCB1, ABCC2, ABCG2, NFKB1, POR, and PXR polymorphisms. Cyclosporine 123-126 ATP binding cassette subfamily B member 1 Homo sapiens 63-68 33974505-2 2021 In this study, we aimed to identify the association of CYP3A4, ABCB1, ABCC2, ABCG2, NFKB1, POR, and PXR polymorphisms with CsA concentrations in patients with allogeneic hematopoietic cell transplantation (allo-HSCT) based on the route of administration.A total of 40 allo-HSCT recipients receiving CsA were genotyped for CYP3A4, ABCB1, ABCC2, ABCG2, NFKB1, POR, and PXR polymorphisms. Cyclosporine 123-126 ATP binding cassette subfamily B member 1 Homo sapiens 330-335 34935100-8 2022 RESULTS: The data showed that drugs which are known P-gp inhibitors, including cyclosporin A, ketoconazole, and verapamil, caused great increases in rhodamine 123 retention, whereas noninhibitors did not affect the intracellular accumulation of the P-gp substrate. Cyclosporine 79-92 ATP binding cassette subfamily B member 1 Homo sapiens 52-56 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. Cyclosporine 111-123 ATP binding cassette subfamily B member 1 Homo sapiens 27-41 35629245-8 2022 ABCB1 homozygous polymorphisms were observed with significantly lower time spent in the therapeutic range with cyclosporine and everolimus/sirolimus. Cyclosporine 111-123 ATP binding cassette subfamily B member 1 Homo sapiens 0-5 32682934-10 2020 The saturated binding of ciclosporin to erythrocytes, auto-inhibition induced by the inhibitory effects of ciclosporin on cytochrome P450 3A4/P-glycoprotein may have contributed to the nonlinearity. Cyclosporine 107-118 ATP binding cassette subfamily B member 1 Homo sapiens 142-156 32222391-13 2020 CONCLUSION: The study results suggest that in KTX metabolic transformations and transport, especially of cyclosporine, dependence on the genetic variability of CYP3A4, UGT1A9, and MDR1 may contribute to kidney damage. Cyclosporine 105-117 ATP binding cassette subfamily B member 1 Homo sapiens 180-184 32094096-5 2020 There was also a significant association between the C/D cyclosporine ratio combined with voriconazole and the ABCB1 2677 G > T > A (rs2032582) genetic polymorphism (P = 0.05). Cyclosporine 57-69 ATP binding cassette subfamily B member 1 Homo sapiens 111-116 32094096-9 2020 Results suggest that the ABCB1 2677 G > T > A genetic polymorphism plays a role in this interaction with cyclosporine related nephrotoxicity. Cyclosporine 105-117 ATP binding cassette subfamily B member 1 Homo sapiens 25-30 31090467-3 2019 To address these challenges, we developed a novel SNEDDS co-loaded with DTX and cyclosporine A (CsA) to achieve effective inhibition of P-gp efflux and P450 enzyme metabolization, improving oral bioavailability of DTX. Cyclosporine 80-94 ATP binding cassette subfamily B member 1 Homo sapiens 136-140 32162881-8 2020 Moreover, frequent TDM monitoring as well as CYP3A4/CYP3A5/MDR1 genotyping were given so as to tailor the oral dosage of cyclosporine individually and prevent the adverse reaction between cyclosporine and posaconazole. Cyclosporine 121-133 ATP binding cassette subfamily B member 1 Homo sapiens 59-63 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). Cyclosporine 72-84 ATP binding cassette subfamily B member 1 Homo sapiens 167-181 31090467-3 2019 To address these challenges, we developed a novel SNEDDS co-loaded with DTX and cyclosporine A (CsA) to achieve effective inhibition of P-gp efflux and P450 enzyme metabolization, improving oral bioavailability of DTX. Cyclosporine 96-99 ATP binding cassette subfamily B member 1 Homo sapiens 136-140