PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 10954886-4 2000 Twelve additional children chose to receive stavudine plus lamivudine plus nelfinavir, with nelfinavir given bid, rather than tid as for the main regimens. Nelfinavir 92-102 BH3 interacting domain death agonist Homo sapiens 109-112 10954886-8 2000 At Week 24 64% (7/11, 95% CI 31-89%) of the children on the bid nelfinavir combination regimen were still on initial therapy with an HIV RNA response as compared with 46% (23/50; 95% CI 32-61%) on the corresponding tid nelfinavir combination regimen. Nelfinavir 64-74 BH3 interacting domain death agonist Homo sapiens 60-63 10996400-4 2000 In these cells the PIs, nelfinavir, saquinavir, and ritonavir, reduced triglyceride accumulation, lipogenesis, and expression of the adipose markers, aP2 and LPL. Nelfinavir 24-34 transcription factor AP-2, alpha Mus musculus 150-153 10996400-4 2000 In these cells the PIs, nelfinavir, saquinavir, and ritonavir, reduced triglyceride accumulation, lipogenesis, and expression of the adipose markers, aP2 and LPL. Nelfinavir 24-34 lipoprotein lipase Mus musculus 158-161 10939550-1 2000 STUDY OBJECTIVES: To evaluate hepatic cytochrome P450 (CYP) 3A4 activity in patients infected with the human immunodeficiency virus (HIV) using the erythromycin breath test (ERMBT), and to examine the relationship of the ERMBT to plasma concentrations of indinavir and nelfinavir. Nelfinavir 269-279 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-63 10926350-13 2000 The HIV protease inhibitors amprenavir, indinavir, nelfinavir, ritonavir and saquinavir inhibit CYP3A4. Nelfinavir 51-61 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 96-102 10820137-3 2000 Intravenous administration of the novel and potent P-glycoprotein inhibitor LY-335979 to mice (1-50 mg/kg) increased brain and testes concentration of [(14)C]nelfinavir, up to 37- and 4-fold, respectively, in a dose-dependent fashion. Nelfinavir 158-168 ATP binding cassette subfamily B member 1 Homo sapiens 51-65 10776836-16 2000 CONCLUSION: Nelfinavir, in combination with reverse transcriptase inhibitors and/or other protease inhibitors, is effective in limiting HIV replication and increasing CD4+ cell counts in HIV-infected adults and children. Nelfinavir 12-22 CD4 molecule Homo sapiens 167-170 10597780-1 1999 OBJECTIVES: (i) To investigate whether protease inhibitor (PI) (nelfinavir)-containing highly active antiretroviral therapy (HAART) affects body composition differently in HIV-infected and AIDS patients without wasting syndrome. Nelfinavir 64-74 serpin family A member 13, pseudogene Homo sapiens 39-57 10651392-4 1999 In numerous clinical trials, pronounced and sustained decreases in plasma HIV RNA levels and increases in CD4+ cell counts occurred in previously untreated or antiretroviral therapy-experienced patients treated with didanosine in combination with at least 1 other antiretroviral drug; zidovudine, stavudine, lamivudine, nevirapine, nelfinavir and hydroxyurea (hydroxycarbamide) are among the drugs that have been given in combination with didanosine. Nelfinavir 332-342 CD4 molecule Homo sapiens 106-109 10509562-1 1999 OBJECTIVES: To determine the effect of the protease inhibitors ritonavir, nelfinavir and indinavir on the P-glycoprotein (P-gp)-mediated transport of saquinavir in Caco-2 cell monolayers. Nelfinavir 74-84 ATP binding cassette subfamily B member 1 Homo sapiens 106-120 10509562-1 1999 OBJECTIVES: To determine the effect of the protease inhibitors ritonavir, nelfinavir and indinavir on the P-glycoprotein (P-gp)-mediated transport of saquinavir in Caco-2 cell monolayers. Nelfinavir 74-84 ATP binding cassette subfamily B member 1 Homo sapiens 122-126 10509562-2 1999 To study the modulation of P-gp function in human lymphocytes by saquinavir, ritonavir, nelfinavir and indinavir. Nelfinavir 88-98 ATP binding cassette subfamily B member 1 Homo sapiens 27-31 10509562-14 1999 CONCLUSIONS: We have demonstrated that saquinavir is a substrate for P-gp and that ritonavir, nelfinavir and indinavir modulate P-gp function in both human lymphocytes and Caco-2 cells. Nelfinavir 94-104 ATP binding cassette subfamily B member 1 Homo sapiens 128-132 10381636-5 1999 Therapy with nelfinavir plus saquinavir in combination with two nucleoside analogue inhibitors of reverse transcriptase dramatically reduces plasma viremia and increases CD4 T cell counts. Nelfinavir 13-23 CD4 molecule Homo sapiens 170-173 10452644-5 1999 Children who began taking at least one new reverse transcriptase inhibitor near the time when nelfinavir mesylate was started, and those with a > or = 24% proportion of CD4 lymphocytes, had a greater chance of achieving and maintaining a decline in plasma HIV-1 RNA to < 400 copies/mL. Nelfinavir 94-113 CD4 molecule Homo sapiens 172-175 10049256-4 1999 The combination of K-12 and the protease inhibitor nelfinavir (NFV) also synergistically inhibited HIV-1, whereas the synergism of this combination was weaker than that of the combinations with the RT inhibitors. Nelfinavir 63-66 keratin 12 Homo sapiens 19-23 10066640-11 1999 - In patients refractory to standard triple therapy the combination of nelfinavir and saquinavir showed significant elevation of CD4-count, but only short term virological efficacy in a minority of patients. Nelfinavir 71-81 CD4 molecule Homo sapiens 129-132 9835508-1 1998 The human immunodeficiency virus type 1 (HIV-1) protease inhibitors (PIs)-saquinavir, ritonavir, nelfinavir, and indinavir-interact with the ABC-type multidrug transporter proteins MDR1 and MRP1 in CEM T-lymphocytic cell lines. Nelfinavir 97-107 ATP binding cassette subfamily B member 1 Homo sapiens 181-185 9835508-1 1998 The human immunodeficiency virus type 1 (HIV-1) protease inhibitors (PIs)-saquinavir, ritonavir, nelfinavir, and indinavir-interact with the ABC-type multidrug transporter proteins MDR1 and MRP1 in CEM T-lymphocytic cell lines. Nelfinavir 97-107 ATP binding cassette subfamily C member 1 Homo sapiens 190-194 9878993-7 1998 Once-daily efavirenz in combination with zidovudine plus lamivudine or indinavir or nelfinavir increased CD4+ cell counts and reduced HIV RNA plasma levels to below quantifiable levels (< 400 copies/ml) in HIV-infected patients. Nelfinavir 84-94 CD4 molecule Homo sapiens 105-108 9803961-6 1998 Saquinavir, ritonavir and nelfinavir significantly inhibited the efflux of [3H]paclitaxel and [3H]vinblastine in P-gp-positive cells, resulting in an increase in intracellular accumulation of these drugs. Nelfinavir 26-36 ATP binding cassette subfamily B member 1 Homo sapiens 113-117 9803961-9 1998 These data suggest that saquinavir, ritonavir, and nelfinavir are inhibitors and possibly substrates of P-gp. Nelfinavir 51-61 ATP binding cassette subfamily B member 1 Homo sapiens 104-108 9660842-2 1998 At therapeutic concentrations (steady-state plasma concentrations approximately 4 microM), nelfinavir was found to be a competitive inhibitor of only testosterone 6beta-hydroxylase (CYP3A4) with a Ki concentration of 4. Nelfinavir 91-101 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 182-188 9660842-4 1998 At supratherapeutic concentrations, nelfinavir competitively inhibited dextromethorphan O-demethylase (CYP2D6), S-mephenytoin 4-hydroxylase (CYP2C19), and phenacetin O-deethylase (CYP1A2) with Ki concentrations of 68, 126, and 190 microM, respectively. Nelfinavir 36-46 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 103-109 9660842-4 1998 At supratherapeutic concentrations, nelfinavir competitively inhibited dextromethorphan O-demethylase (CYP2D6), S-mephenytoin 4-hydroxylase (CYP2C19), and phenacetin O-deethylase (CYP1A2) with Ki concentrations of 68, 126, and 190 microM, respectively. Nelfinavir 36-46 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 112-139 9660842-4 1998 At supratherapeutic concentrations, nelfinavir competitively inhibited dextromethorphan O-demethylase (CYP2D6), S-mephenytoin 4-hydroxylase (CYP2C19), and phenacetin O-deethylase (CYP1A2) with Ki concentrations of 68, 126, and 190 microM, respectively. Nelfinavir 36-46 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 141-148 9660842-4 1998 At supratherapeutic concentrations, nelfinavir competitively inhibited dextromethorphan O-demethylase (CYP2D6), S-mephenytoin 4-hydroxylase (CYP2C19), and phenacetin O-deethylase (CYP1A2) with Ki concentrations of 68, 126, and 190 microM, respectively. Nelfinavir 36-46 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 180-186 9660842-6 1998 The inhibitory potency of nelfinavir toward CYP3A4 suggested the possibility of in vivo inhibition of this isoform, whereas in vivo inhibition of other P450s was considered unlikely. Nelfinavir 26-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 44-50 9660842-7 1998 In a one-sequence crossover study in 12 healthy volunteers, nelfinavir inhibited the elimination of the CYP3A substrate terfenadine and the carboxylate metabolite of terfenadine. Nelfinavir 60-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 104-109 9660842-8 1998 The 24-hr urinary recoveries of 6beta-hydroxycortisol were reduced by an average of 27% during nelfinavir treatment, consistent with CYP3A inhibition by nelfinavir. Nelfinavir 153-163 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 133-138 9660842-9 1998 Inhibition of CYP3A4 by nelfinavir in vitro was NADPH-dependent requiring the catalytic formation of a metabolite or a metabolic intermediate. Nelfinavir 24-34 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-20 9660842-12 1998 Although incubations with nelfinavir showed a time- and concentration-dependent loss of CYP3A4 activity, the partial or complete recovery of enzyme activity upon dialysis indicated that inhibition was reversible. Nelfinavir 26-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-94 9660842-15 1998 Collectively, these results suggest that the probable mechanism for CYP3A4 inhibition by nelfinavir is a transient metabolic intermediate or stable metabolite that coordinates tightly but reversibly to the heme moiety of the P450. Nelfinavir 89-99 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-74 9649346-8 1998 Amprenavir, nelfinavir, and indinavir appear to inhibit CYP3A4 to a moderate extent, suggesting a selected number of coadministration restrictions. Nelfinavir 12-22 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-62 9617598-5 1998 Combination therapy comprising amprenavir and other antiretroviral agents (abacavir, zidovudine, lamivudine, indinavir, saquinavir or nelfinavir) decreased viral load and increased CD4+ cell counts in patients with HIV infection. Nelfinavir 134-144 CD4 molecule Homo sapiens 181-184 9211082-5 1997 Combination therapy with nelfinavir and stavudine produced greater reductions in plasma HIV RNA levels that stavudine monotherapy in patients who had not previously received stavudine treatment; mean increases in CD4+ cell counts were also greater in the combination treatment group than in monotherapy recipients. Nelfinavir 25-35 CD4 molecule Homo sapiens 213-216 9056009-2 1997 In rat and human liver microsomes, ritonavir potently inhibited the cytochrome P450 (CYP)-mediated metabolism of saquinavir, indinavir, nelfinavir, and VX-478. Nelfinavir 136-146 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 68-83 9056009-2 1997 In rat and human liver microsomes, ritonavir potently inhibited the cytochrome P450 (CYP)-mediated metabolism of saquinavir, indinavir, nelfinavir, and VX-478. Nelfinavir 136-146 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 85-88 34986429-8 2022 Glecaprevir and nelfinavir (DeltaGbind = -95.4 kJ/mol) appear to be the most effective antiviral drugs against Mpro. Nelfinavir 16-26 NEWENTRY Severe acute respiratory syndrome-related coronavirus 111-115 34815424-6 2021 We find that the eEF2K agonist nelfinavir abolishes p-bodies in sensory neurons and impairs translation. Nelfinavir 31-41 eukaryotic elongation factor 2 kinase Homo sapiens 17-22 34158378-6 2021 Nelfinavir affected the fluidity and composition of lipid-rich membranes, disrupted mitochondrial respiration, blocked vesicular transport, and affected the function of membrane-embedded drug efflux transporter ABCB1, triggering the integrated stress response. Nelfinavir 0-10 ATP binding cassette subfamily B member 1 Homo sapiens 211-216 34158378-7 2021 Sensitivity to nelfinavir was dependent on ADIPOR2, which maintains membrane fluidity by promoting fatty acid desaturation and incorporation into phospholipids. Nelfinavir 15-25 adiponectin receptor 2 Homo sapiens 43-50 34903997-7 2021 Our MM-PBSA computation illustrates that ZINC31157475 is more potent (-88.03 kcal mol-1) than nelfinavir (-19.54 kcal mol-1) against COVID-19 3CLp. Nelfinavir 94-104 calmodulin like 3 Homo sapiens 143-146 34136086-5 2021 The IU-TAB-1 cell line was noted to be resistant to everolimus (mTORC1 inhibitor) and sensitive to nelfinavir (AKT1 inhibitor) across the endpoints measured. Nelfinavir 99-109 AKT serine/threonine kinase 1 Homo sapiens 111-115 34136086-6 2021 Sensitivity to nelfinavir was due to the IU-TAB-1 cell line"s gain-of function (GOF) mutation in PIK3CA and amplification of genes observed from array comparative genomic hybridization (aCGH), including AURKA, ERBB2, KIT, PDGFRA and PDGFB, that are known upregulate AKT, while resistance to everolimus was primarily driven by upregulation of downstream signaling of KIT, PDGFRA and PDGFB in the presence of mTORC1 inhibition. Nelfinavir 15-25 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha Homo sapiens 97-103 34136086-6 2021 Sensitivity to nelfinavir was due to the IU-TAB-1 cell line"s gain-of function (GOF) mutation in PIK3CA and amplification of genes observed from array comparative genomic hybridization (aCGH), including AURKA, ERBB2, KIT, PDGFRA and PDGFB, that are known upregulate AKT, while resistance to everolimus was primarily driven by upregulation of downstream signaling of KIT, PDGFRA and PDGFB in the presence of mTORC1 inhibition. Nelfinavir 15-25 aurora kinase A Homo sapiens 203-208 34136086-6 2021 Sensitivity to nelfinavir was due to the IU-TAB-1 cell line"s gain-of function (GOF) mutation in PIK3CA and amplification of genes observed from array comparative genomic hybridization (aCGH), including AURKA, ERBB2, KIT, PDGFRA and PDGFB, that are known upregulate AKT, while resistance to everolimus was primarily driven by upregulation of downstream signaling of KIT, PDGFRA and PDGFB in the presence of mTORC1 inhibition. Nelfinavir 15-25 erb-b2 receptor tyrosine kinase 2 Homo sapiens 210-215 34136086-6 2021 Sensitivity to nelfinavir was due to the IU-TAB-1 cell line"s gain-of function (GOF) mutation in PIK3CA and amplification of genes observed from array comparative genomic hybridization (aCGH), including AURKA, ERBB2, KIT, PDGFRA and PDGFB, that are known upregulate AKT, while resistance to everolimus was primarily driven by upregulation of downstream signaling of KIT, PDGFRA and PDGFB in the presence of mTORC1 inhibition. Nelfinavir 15-25 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 217-220 34136086-6 2021 Sensitivity to nelfinavir was due to the IU-TAB-1 cell line"s gain-of function (GOF) mutation in PIK3CA and amplification of genes observed from array comparative genomic hybridization (aCGH), including AURKA, ERBB2, KIT, PDGFRA and PDGFB, that are known upregulate AKT, while resistance to everolimus was primarily driven by upregulation of downstream signaling of KIT, PDGFRA and PDGFB in the presence of mTORC1 inhibition. Nelfinavir 15-25 platelet derived growth factor receptor alpha Homo sapiens 222-228 34136086-6 2021 Sensitivity to nelfinavir was due to the IU-TAB-1 cell line"s gain-of function (GOF) mutation in PIK3CA and amplification of genes observed from array comparative genomic hybridization (aCGH), including AURKA, ERBB2, KIT, PDGFRA and PDGFB, that are known upregulate AKT, while resistance to everolimus was primarily driven by upregulation of downstream signaling of KIT, PDGFRA and PDGFB in the presence of mTORC1 inhibition. Nelfinavir 15-25 platelet derived growth factor subunit B Homo sapiens 233-238 34136086-6 2021 Sensitivity to nelfinavir was due to the IU-TAB-1 cell line"s gain-of function (GOF) mutation in PIK3CA and amplification of genes observed from array comparative genomic hybridization (aCGH), including AURKA, ERBB2, KIT, PDGFRA and PDGFB, that are known upregulate AKT, while resistance to everolimus was primarily driven by upregulation of downstream signaling of KIT, PDGFRA and PDGFB in the presence of mTORC1 inhibition. Nelfinavir 15-25 AKT serine/threonine kinase 1 Homo sapiens 266-269 34136086-6 2021 Sensitivity to nelfinavir was due to the IU-TAB-1 cell line"s gain-of function (GOF) mutation in PIK3CA and amplification of genes observed from array comparative genomic hybridization (aCGH), including AURKA, ERBB2, KIT, PDGFRA and PDGFB, that are known upregulate AKT, while resistance to everolimus was primarily driven by upregulation of downstream signaling of KIT, PDGFRA and PDGFB in the presence of mTORC1 inhibition. Nelfinavir 15-25 KIT proto-oncogene, receptor tyrosine kinase Homo sapiens 366-369 34136086-6 2021 Sensitivity to nelfinavir was due to the IU-TAB-1 cell line"s gain-of function (GOF) mutation in PIK3CA and amplification of genes observed from array comparative genomic hybridization (aCGH), including AURKA, ERBB2, KIT, PDGFRA and PDGFB, that are known upregulate AKT, while resistance to everolimus was primarily driven by upregulation of downstream signaling of KIT, PDGFRA and PDGFB in the presence of mTORC1 inhibition. Nelfinavir 15-25 platelet derived growth factor receptor alpha Homo sapiens 371-377 34136086-6 2021 Sensitivity to nelfinavir was due to the IU-TAB-1 cell line"s gain-of function (GOF) mutation in PIK3CA and amplification of genes observed from array comparative genomic hybridization (aCGH), including AURKA, ERBB2, KIT, PDGFRA and PDGFB, that are known upregulate AKT, while resistance to everolimus was primarily driven by upregulation of downstream signaling of KIT, PDGFRA and PDGFB in the presence of mTORC1 inhibition. Nelfinavir 15-25 platelet derived growth factor subunit B Homo sapiens 382-387 35364308-6 2022 Our obtained result demonstrate that Hesperidin, rutin, diosmin, and apiin are most effective compounds agents against SARS-CoV-2 Mpro as compared to Nelfinavir (positive control). Nelfinavir 150-160 NEWENTRY Severe acute respiratory syndrome-related coronavirus 130-134 35589686-9 2022 Finally, we show that partial inhibition of the DDI2-protease domain with the antiviral drug nelfinavir increased bortezomib susceptibility in treated MM cells. Nelfinavir 93-103 DNA damage inducible 1 homolog 2 Homo sapiens 48-52 35149540-10 2022 Significance Statement The in vivo Kp,uu,fetal of nelfinavir (P-gp substrate), efavirenz (BCRP substrate), and imatinib (P-gp and BCRP substrate) was successfully estimated using m-f- PBPK modeling. Nelfinavir 50-60 phosphoglycolate phosphatase Homo sapiens 62-66 35149540-10 2022 Significance Statement The in vivo Kp,uu,fetal of nelfinavir (P-gp substrate), efavirenz (BCRP substrate), and imatinib (P-gp and BCRP substrate) was successfully estimated using m-f- PBPK modeling. Nelfinavir 50-60 phosphoglycolate phosphatase Homo sapiens 121-125 35358511-7 2022 We show that blocking Ddi2"s endoprotease activity either genetically or with the HIV protease inhibitor nelfinavir increased its binding to ubiquitin conjugates, but decreased its binding to proteasomes, and reduced subsequent protein degradation by proteasomes leading to further accumulation of ubiquitin conjugates. Nelfinavir 105-115 cyanamide hydratase Saccharomyces cerevisiae S288C 22-26 35358511-8 2022 Finally, nelfinavir treatment required Ddi2 to induce the unfolded protein response. Nelfinavir 9-19 cyanamide hydratase Saccharomyces cerevisiae S288C 39-43 35387819-3 2022 This trial will investigate the impact of nelfinavir, a protease inhibitor that targets the protein kinase B (AKT) pathway on disease-free survival (DFS). Nelfinavir 42-52 protein tyrosine kinase 2 beta Homo sapiens 92-108 35387819-3 2022 This trial will investigate the impact of nelfinavir, a protease inhibitor that targets the protein kinase B (AKT) pathway on disease-free survival (DFS). Nelfinavir 42-52 AKT serine/threonine kinase 1 Homo sapiens 110-113 35217718-4 2022 We demonstrate that Sitagliptin and Daclatasvir inhibit PLpro, and MG-101, Lycorine HCl, and Nelfinavir mesylate inhibit Mpro of SARS-CoV-2. Nelfinavir 93-112 NEWENTRY Severe acute respiratory syndrome-related coronavirus 121-125 35204223-8 2022 Furthermore, although activated in cells that survived standalone FUS, pre-sensitization with CDDO-me and/or nelfinavir suppressed both total and activated (phosphorylated) NF-kappaB and Akt protein levels. Nelfinavir 109-119 nuclear factor kappa B subunit 1 Homo sapiens 173-182 35204223-8 2022 Furthermore, although activated in cells that survived standalone FUS, pre-sensitization with CDDO-me and/or nelfinavir suppressed both total and activated (phosphorylated) NF-kappaB and Akt protein levels. Nelfinavir 109-119 AKT serine/threonine kinase 1 Homo sapiens 187-190 33483427-0 2021 Nelfinavir and its active metabolite M8 are partial agonists and competitive antagonists of the human pregnane X receptor. Nelfinavir 0-10 nuclear receptor subfamily 1 group I member 2 Homo sapiens 102-121 33483427-3 2021 The present study addresses the effects of nelfinavir and its major and pharmacologically active metabolite nelfinavir hydroxy-tert-butylamide (M8) on PXR to elucidate the underlying molecular mechanism. Nelfinavir 43-53 nuclear receptor subfamily 1 group I member 2 Homo sapiens 151-154 33483427-7 2021 Impaired co-activator recruitment by nelfinavir, as compared to the full agonist rifampin, proved to be the underlying mechanism of both effects on PXR. Nelfinavir 37-47 nuclear receptor subfamily 1 group I member 2 Homo sapiens 148-151 33483427-8 2021 Physiological relevance of nelfinavir-dependent modulation of PXR activity was investigated in respectively treated primary human hepatocytes, which showed differential induction of PXR target genes and antagonism of rifampin-induced ABCB1 and CYP3A4 gene expression. Nelfinavir 27-37 nuclear receptor subfamily 1 group I member 2 Homo sapiens 62-65 33483427-8 2021 Physiological relevance of nelfinavir-dependent modulation of PXR activity was investigated in respectively treated primary human hepatocytes, which showed differential induction of PXR target genes and antagonism of rifampin-induced ABCB1 and CYP3A4 gene expression. Nelfinavir 27-37 nuclear receptor subfamily 1 group I member 2 Homo sapiens 182-185 33483427-8 2021 Physiological relevance of nelfinavir-dependent modulation of PXR activity was investigated in respectively treated primary human hepatocytes, which showed differential induction of PXR target genes and antagonism of rifampin-induced ABCB1 and CYP3A4 gene expression. Nelfinavir 27-37 ATP binding cassette subfamily B member 1 Homo sapiens 234-239 33483427-8 2021 Physiological relevance of nelfinavir-dependent modulation of PXR activity was investigated in respectively treated primary human hepatocytes, which showed differential induction of PXR target genes and antagonism of rifampin-induced ABCB1 and CYP3A4 gene expression. Nelfinavir 27-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 244-250 33483427-9 2021 In conclusion, we elucidated here the molecular mechanism of nelfinavir interaction with PXR. Nelfinavir 61-71 nuclear receptor subfamily 1 group I member 2 Homo sapiens 89-92 33483427-10 2021 It is hypothesized that modulation of PXR activity may impact on the anticancer effects of nelfinavir. Nelfinavir 91-101 nuclear receptor subfamily 1 group I member 2 Homo sapiens 38-41 33483427-13 2021 Nelfinavir anticancer activity may partially rely on modulation of PXR, which itself is discussed as a therapeutic target in cancer therapy and for the reversal of chemoresistance. Nelfinavir 0-10 nuclear receptor subfamily 1 group I member 2 Homo sapiens 67-70 32737681-5 2021 From the screening of approved drug library, three antiviral agents ritonavir, nelfinavir and saquinavir were predicted to be the most potent Mpro inhibitors. Nelfinavir 79-89 NEWENTRY Severe acute respiratory syndrome-related coronavirus 142-146 33414432-4 2021 Conversely, two inhibitors of eIF2alpha dephosphorylation, nelfinavir and salubrinal, enhanced the induction of such autophagic puncta. Nelfinavir 59-69 eukaryotic translation initiation factor 2A Mus musculus 30-39 33419802-5 2021 RESULTS: Nelfinavir inhibited SCLC cell proliferation and induced cell death in vitro, which was caused by induction of the unfolded protein response (UPR), inhibition of mammalian/mechanistic target of rapamycin (mTOR) activation, and reduction in the expression of SCLC-related molecules such as achaete-scute homolog 1 (ASCL1). Nelfinavir 9-19 mechanistic target of rapamycin kinase Homo sapiens 171-212 33419802-5 2021 RESULTS: Nelfinavir inhibited SCLC cell proliferation and induced cell death in vitro, which was caused by induction of the unfolded protein response (UPR), inhibition of mammalian/mechanistic target of rapamycin (mTOR) activation, and reduction in the expression of SCLC-related molecules such as achaete-scute homolog 1 (ASCL1). Nelfinavir 9-19 mechanistic target of rapamycin kinase Homo sapiens 214-218 33419802-5 2021 RESULTS: Nelfinavir inhibited SCLC cell proliferation and induced cell death in vitro, which was caused by induction of the unfolded protein response (UPR), inhibition of mammalian/mechanistic target of rapamycin (mTOR) activation, and reduction in the expression of SCLC-related molecules such as achaete-scute homolog 1 (ASCL1). Nelfinavir 9-19 achaete-scute family bHLH transcription factor 1 Homo sapiens 298-321 33419802-5 2021 RESULTS: Nelfinavir inhibited SCLC cell proliferation and induced cell death in vitro, which was caused by induction of the unfolded protein response (UPR), inhibition of mammalian/mechanistic target of rapamycin (mTOR) activation, and reduction in the expression of SCLC-related molecules such as achaete-scute homolog 1 (ASCL1). Nelfinavir 9-19 achaete-scute family bHLH transcription factor 1 Homo sapiens 323-328 33419802-6 2021 In vivo, nelfinavir inhibited the growth of SCLC PDX tumors, which correlated with the induction of UPR and reduced expression of ASCL1. Nelfinavir 9-19 achaete-scute family bHLH transcription factor 1 Homo sapiens 130-135 33425427-7 2020 The results showed that hesperidin, nabiximols, pectolinarin, epigallocatechin gallate, and rhoifolin had better poses than nelfinavir, chloroquine, and hydroxychloroquine sulfate as spike glycoprotein inhibitors. Nelfinavir 124-134 surface glycoprotein Severe acute respiratory syndrome coronavirus 2 183-188 33022567-3 2020 We report these two compounds (ZINC000621278586 and ZINC000621285995) as potent SARS-CoV-2 Mpro inhibitors with high affinity (<-9 kCal/mol) and less toxicity than Lopinavir and Nelfinavir positive controls. Nelfinavir 178-188 NEWENTRY Severe acute respiratory syndrome-related coronavirus 91-95 32916277-0 2020 Nelfinavir inhibits human DDI2 and potentiates cytotoxicity of proteasome inhibitors. Nelfinavir 0-10 DNA damage inducible 1 homolog 2 Homo sapiens 26-30 32916277-5 2020 Here, we report that Nelfinavir (NFV), an HIV protease inhibitor, can inhibit DDI2 activity directly. Nelfinavir 21-31 DNA damage inducible 1 homolog 2 Homo sapiens 78-82 32916277-5 2020 Here, we report that Nelfinavir (NFV), an HIV protease inhibitor, can inhibit DDI2 activity directly. Nelfinavir 33-36 DNA damage inducible 1 homolog 2 Homo sapiens 78-82 33193684-8 2020 All the eight compounds can effectively interfere with the binding of ACE2 and Spike protein, especially Nelfinavir, providing drug candidates for the treatment and prevention of SARS-CoV-2, suggesting further assessment of the anti-SARS-CoV-2 activity of these compounds in cell culture. Nelfinavir 105-115 angiotensin converting enzyme 2 Homo sapiens 70-74 33193684-8 2020 All the eight compounds can effectively interfere with the binding of ACE2 and Spike protein, especially Nelfinavir, providing drug candidates for the treatment and prevention of SARS-CoV-2, suggesting further assessment of the anti-SARS-CoV-2 activity of these compounds in cell culture. Nelfinavir 105-115 surface glycoprotein Severe acute respiratory syndrome coronavirus 2 79-84 32406687-6 2020 Along with the highly potent drugs and/or molecules (such as nelfinavir) revealed in this study, the newly discovered binding mechanism paves the way for further optimizations and designs of Mpro"s inhibitors with a high binding affinity. Nelfinavir 61-71 NEWENTRY Severe acute respiratory syndrome-related coronavirus 191-195 32344880-0 2020 Nelfinavir Inhibits the TCF11/Nrf1-Mediated Proteasome Recovery Pathway in Multiple Myeloma. Nelfinavir 0-10 NFE2 like bZIP transcription factor 1 Homo sapiens 24-29 32344880-0 2020 Nelfinavir Inhibits the TCF11/Nrf1-Mediated Proteasome Recovery Pathway in Multiple Myeloma. Nelfinavir 0-10 nuclear respiratory factor 1 Homo sapiens 30-34 32344880-8 2020 Here, we describe how nelfinavir inhibits the TCF11/Nrf1-driven recovery pathway by a dual mode of action. Nelfinavir 22-32 NFE2 like bZIP transcription factor 1 Homo sapiens 46-51 32344880-8 2020 Here, we describe how nelfinavir inhibits the TCF11/Nrf1-driven recovery pathway by a dual mode of action. Nelfinavir 22-32 nuclear respiratory factor 1 Homo sapiens 52-56 32344880-9 2020 Nelfinavir decreases the total protein level of TCF11/Nrf1 and inhibits TCF11/Nrf1 proteolytic processing, likely by interfering with the DDI2 protease, and therefore reduces the TCF11/Nrf1 protein level in the nucleus. Nelfinavir 0-10 NFE2 like bZIP transcription factor 1 Homo sapiens 48-53 32344880-9 2020 Nelfinavir decreases the total protein level of TCF11/Nrf1 and inhibits TCF11/Nrf1 proteolytic processing, likely by interfering with the DDI2 protease, and therefore reduces the TCF11/Nrf1 protein level in the nucleus. Nelfinavir 0-10 nuclear respiratory factor 1 Homo sapiens 54-58 32344880-9 2020 Nelfinavir decreases the total protein level of TCF11/Nrf1 and inhibits TCF11/Nrf1 proteolytic processing, likely by interfering with the DDI2 protease, and therefore reduces the TCF11/Nrf1 protein level in the nucleus. Nelfinavir 0-10 NFE2 like bZIP transcription factor 1 Homo sapiens 72-77 32344880-9 2020 Nelfinavir decreases the total protein level of TCF11/Nrf1 and inhibits TCF11/Nrf1 proteolytic processing, likely by interfering with the DDI2 protease, and therefore reduces the TCF11/Nrf1 protein level in the nucleus. Nelfinavir 0-10 nuclear respiratory factor 1 Homo sapiens 78-82 32344880-9 2020 Nelfinavir decreases the total protein level of TCF11/Nrf1 and inhibits TCF11/Nrf1 proteolytic processing, likely by interfering with the DDI2 protease, and therefore reduces the TCF11/Nrf1 protein level in the nucleus. Nelfinavir 0-10 DNA damage inducible 1 homolog 2 Homo sapiens 138-142 32344880-9 2020 Nelfinavir decreases the total protein level of TCF11/Nrf1 and inhibits TCF11/Nrf1 proteolytic processing, likely by interfering with the DDI2 protease, and therefore reduces the TCF11/Nrf1 protein level in the nucleus. Nelfinavir 0-10 NFE2 like bZIP transcription factor 1 Homo sapiens 72-77 32344880-9 2020 Nelfinavir decreases the total protein level of TCF11/Nrf1 and inhibits TCF11/Nrf1 proteolytic processing, likely by interfering with the DDI2 protease, and therefore reduces the TCF11/Nrf1 protein level in the nucleus. Nelfinavir 0-10 nuclear respiratory factor 1 Homo sapiens 78-82 31838577-9 2020 Nelfinavir and lopinavir, two clinically approved HIV protease inhibitors, promote eIF2alpha phosphorylation by different mechanisms. Nelfinavir 0-10 eukaryotic translation initiation factor 2A Homo sapiens 83-92 31838577-10 2020 We show that nelfinavir and lopinavir sustainably instigate B7H6 expression at their pharmacologically relevant concentrations. Nelfinavir 13-23 natural killer cell cytotoxicity receptor 3 ligand 1 Homo sapiens 60-64 31838577-15 2020 Exposure of tumor cells to the HIV protease inhibitor nelfinavir improves the recognition by B7H6-directed CAR-T. Nelfinavir 54-64 natural killer cell cytotoxicity receptor 3 ligand 1 Homo sapiens 93-97 31262902-11 2019 In particular, the sensitizing effect of co-treatment with nelfinavir on antimitotic drug-resistant cancer cells was found to be strong and independent of P-gp-inhibitory activity. Nelfinavir 59-69 ATP binding cassette subfamily B member 1 Homo sapiens 155-159 31262902-12 2019 As P-gp inhibition can be toxic to normal cells, selecting nelfinavir may be safer for normal cells in patients with drug-resistant cancer. Nelfinavir 59-69 ATP binding cassette subfamily B member 1 Homo sapiens 3-7 31059280-7 2019 Treatments of these foam cells with ritonavir, nelfinavir, and saquinavir at least doubled cholestryl ester accumulation ( P=0.02, 0.0009, and 0.02, respectively), whereas RNA silencing of the AR-RGN top key driver, PQBP1 (polyglutamine binding protein 1), significantly curbed cholestryl ester accumulation following treatment with any of these ART drugs by >37% ( P<0.05). Nelfinavir 47-57 polyglutamine binding protein 1 Homo sapiens 216-221 31059280-7 2019 Treatments of these foam cells with ritonavir, nelfinavir, and saquinavir at least doubled cholestryl ester accumulation ( P=0.02, 0.0009, and 0.02, respectively), whereas RNA silencing of the AR-RGN top key driver, PQBP1 (polyglutamine binding protein 1), significantly curbed cholestryl ester accumulation following treatment with any of these ART drugs by >37% ( P<0.05). Nelfinavir 47-57 polyglutamine binding protein 1 Homo sapiens 223-254 30695683-0 2019 Metformin combined with nelfinavir induces SIRT3/mROS-dependent autophagy in human cervical cancer cells and xenograft in nude mice. Nelfinavir 24-34 sirtuin 3 Homo sapiens 43-48 30695683-10 2019 Therefore, it can be concluded that metformin, in combination with nelfinavir, can induce SIRT3/mROS-dependent autophagy and sensitize NK cell-mediated lysis in human cervical cancer cells and cervical cancer cell xenografts in nude mice. Nelfinavir 67-77 sirtuin 3 Homo sapiens 90-95 30823453-7 2019 ELISA for HIV-1 p24 indicated that CyO2 enhances the antiviral efficacy of both SQV and nelfinavir. Nelfinavir 88-98 transmembrane p24 trafficking protein 2 Homo sapiens 16-19 30308940-2 2018 We show that nelfinavir and mefloquine synergize to selectively evoke a cytotoxic response in TSC2-deficient cell lines with mTORC1 hyperactivity. Nelfinavir 13-23 CREB regulated transcription coactivator 1 Mus musculus 125-131 30308940-3 2018 We optimize the concentrations of nelfinavir and mefloquine to a clinically viable range that kill cells that lack TSC2, while wild-type cells tolerate treatment. Nelfinavir 34-44 TSC complex subunit 2 Homo sapiens 115-119 30308940-8 2018 This work underpins a critical vulnerability with cancer cells with aberrant signaling through the TSC2-mTORC1 pathway that lack flexibility in homeostatic pathways, which could be exploited with combined nelfinavir and mefloquine treatment. Nelfinavir 205-215 TSC complex subunit 2 Homo sapiens 99-103 30308940-8 2018 This work underpins a critical vulnerability with cancer cells with aberrant signaling through the TSC2-mTORC1 pathway that lack flexibility in homeostatic pathways, which could be exploited with combined nelfinavir and mefloquine treatment. Nelfinavir 205-215 CREB regulated transcription coactivator 1 Mus musculus 104-110 30275179-7 2018 Nelfinavir was also found to increase the expression of the mammalian target of rapamycin (mTOR) inhibitor AMP-activated protein kinase (AMPK) and inhibited the panobinostat-activated mTOR pathway. Nelfinavir 0-10 mechanistic target of rapamycin kinase Homo sapiens 60-89 30275179-7 2018 Nelfinavir was also found to increase the expression of the mammalian target of rapamycin (mTOR) inhibitor AMP-activated protein kinase (AMPK) and inhibited the panobinostat-activated mTOR pathway. Nelfinavir 0-10 mechanistic target of rapamycin kinase Homo sapiens 91-95 30275179-7 2018 Nelfinavir was also found to increase the expression of the mammalian target of rapamycin (mTOR) inhibitor AMP-activated protein kinase (AMPK) and inhibited the panobinostat-activated mTOR pathway. Nelfinavir 0-10 mechanistic target of rapamycin kinase Homo sapiens 184-188 30061216-0 2018 Nelfinavir Induces Endoplasmic Reticulum Stress and Sensitizes Renal Cancer Cells to TRAIL. Nelfinavir 0-10 TNF superfamily member 10 Homo sapiens 85-90 30061216-3 2018 MATERIALS AND METHODS: Using renal cancer cells (769-P, 786-O, Caki-2), the ability of nelfinavir to induce ER stress and sensitize them to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) was tested. Nelfinavir 87-97 TNF superfamily member 10 Homo sapiens 140-195 30061216-3 2018 MATERIALS AND METHODS: Using renal cancer cells (769-P, 786-O, Caki-2), the ability of nelfinavir to induce ER stress and sensitize them to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) was tested. Nelfinavir 87-97 TNF superfamily member 10 Homo sapiens 197-202 30061216-6 2018 Nelfinavir induced ER stress and increased the expression of TRAIL death receptor (DR) 4 and DR5, sensitizing the cancer cells to TRAIL. Nelfinavir 0-10 TNF superfamily member 10 Homo sapiens 61-66 30061216-6 2018 Nelfinavir induced ER stress and increased the expression of TRAIL death receptor (DR) 4 and DR5, sensitizing the cancer cells to TRAIL. Nelfinavir 0-10 TNF receptor superfamily member 10b Homo sapiens 93-96 30061216-6 2018 Nelfinavir induced ER stress and increased the expression of TRAIL death receptor (DR) 4 and DR5, sensitizing the cancer cells to TRAIL. Nelfinavir 0-10 TNF superfamily member 10 Homo sapiens 130-135 30061216-8 2018 CONCLUSION: Nelfinavir induces ER stress in renal cancer cells and sensitizes them to TRAIL. Nelfinavir 12-22 TNF superfamily member 10 Homo sapiens 86-91 28676669-0 2018 Carfilzomib resistance due to ABCB1/MDR1 overexpression is overcome by nelfinavir and lopinavir in multiple myeloma. Nelfinavir 71-81 ATP binding cassette subfamily B member 1 Homo sapiens 30-35 28676669-0 2018 Carfilzomib resistance due to ABCB1/MDR1 overexpression is overcome by nelfinavir and lopinavir in multiple myeloma. Nelfinavir 71-81 ATP binding cassette subfamily B member 1 Homo sapiens 36-40 28676669-8 2018 In search for potential drugs targeting ABCB1 in clinical trials, we identified the HIV protease inhibitors nelfinavir (NFV) and lopinavir (LPV) as potent functional modulators of ABCB1-mediated drug export, most likely via modulation of mitochondria permeability transition pore. Nelfinavir 108-118 ATP binding cassette subfamily B member 1 Homo sapiens 40-45 28676669-8 2018 In search for potential drugs targeting ABCB1 in clinical trials, we identified the HIV protease inhibitors nelfinavir (NFV) and lopinavir (LPV) as potent functional modulators of ABCB1-mediated drug export, most likely via modulation of mitochondria permeability transition pore. Nelfinavir 108-118 ATP binding cassette subfamily B member 1 Homo sapiens 180-185 30497065-0 2018 Targeting P-Glycoprotein: Nelfinavir Reverses Adriamycin Resistance in K562/ADR Cells. Nelfinavir 26-36 ATP binding cassette subfamily B member 1 Homo sapiens 10-24 28951049-8 2017 To prove the applicability of the procedure, the effect of amprenavir, indinavir, nelfinavir, ritonavir, and saquinavir on the hBCRP ATPase activity was tested. Nelfinavir 82-92 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 127-132 28951049-9 2017 Nelfinavir, ritonavir, and saquinavir were identified as hBCRP ATPase inhibitors and none of the five HIV protease inhibitors turned out to be an hBCRP substrate. Nelfinavir 0-10 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 57-62 28415776-0 2017 Targeting protein homeostasis with nelfinavir/salinomycin dual therapy effectively induces death of mTORC1 hyperactive cells. Nelfinavir 35-45 CREB regulated transcription coactivator 1 Mus musculus 100-106 28415776-4 2017 We found a nelfinavir and salinomycin combination specifically killed TSC2-deficient, mTORC1 hyperactive cells. Nelfinavir 11-21 CREB regulated transcription coactivator 1 Mus musculus 86-92 28415776-9 2017 Sporadic cancer cell lines with hyperactive mTORC1 signalling were also susceptible to this nelfinavir/salinomycin drug combination. Nelfinavir 92-102 CREB regulated transcription coactivator 1 Mus musculus 44-50 28137980-1 2017 The HIV protease inhibitor Nelfinavir (NFV) inhibits PI3K/AKT and MAPK/ERK signaling pathways, emerging targets in thyroid cancers. Nelfinavir 27-37 AKT serine/threonine kinase 1 Homo sapiens 58-61 28137980-9 2017 Treatment with NFV (20 microM) resulted in caspase-3 cleavage in all examined cells. Nelfinavir 15-18 caspase 3 Homo sapiens 43-52 28137980-10 2017 NFV (20 microM) decreased the levels of total and p-AKT in PTEN-deficient FTC133 cells. Nelfinavir 0-3 AKT serine/threonine kinase 1 Homo sapiens 52-55 28137980-10 2017 NFV (20 microM) decreased the levels of total and p-AKT in PTEN-deficient FTC133 cells. Nelfinavir 0-3 phosphatase and tensin homolog Homo sapiens 59-63 29657993-0 2017 The HIV protease and PI3K/Akt inhibitor nelfinavir does not improve the curative effect of fractionated irradiation in PC-3 prostate cancer in vitro and in vivo. Nelfinavir 40-50 thymoma viral proto-oncogene 1 Mus musculus 26-29 29657993-6 2017 Methods: The in vitro effect of nelfinavir on radioresponse of PC-3 was tested by colony formation assay with 10 muM nelfinavir. Nelfinavir 32-42 chromobox 8 Mus musculus 63-67 29657993-6 2017 Methods: The in vitro effect of nelfinavir on radioresponse of PC-3 was tested by colony formation assay with 10 muM nelfinavir. Nelfinavir 117-127 chromobox 8 Mus musculus 63-67 29657993-10 2017 Results: Nelfinavir inhibited Akt phosphorylation at Ser473 and showed a minor but significant effect on clonogenic cell survival in vitro with slightly higher cell survival rates after combined treatment. Nelfinavir 9-19 thymoma viral proto-oncogene 1 Mus musculus 30-33 29657993-11 2017 The treatment of PC-3 xenografts with nelfinavir alone led to no significant increase of tumour growth time and no improvement of local tumour control. Nelfinavir 38-48 chromobox 8 Mus musculus 17-21 27572820-3 2016 Here we show that inhibitors of the HIV aspartyl protease (HIV-PIs), nelfinavir in particular, trigger a robust activation of eEF2K leading to the phosphorylation of eEF2. Nelfinavir 69-79 eukaryotic elongation factor 2 kinase Homo sapiens 126-131 27572820-3 2016 Here we show that inhibitors of the HIV aspartyl protease (HIV-PIs), nelfinavir in particular, trigger a robust activation of eEF2K leading to the phosphorylation of eEF2. Nelfinavir 69-79 eukaryotic translation elongation factor 2 Homo sapiens 126-130 27572820-5 2016 We show that nelfinavir-resistant cells specifically evade eEF2 inhibition. Nelfinavir 13-23 eukaryotic translation elongation factor 2 Homo sapiens 59-63 27572820-6 2016 Decreased cell viability induced by nelfinavir is impaired in cells lacking eEF2K. Nelfinavir 36-46 eukaryotic elongation factor 2 kinase Homo sapiens 76-81 27572820-7 2016 Moreover, nelfinavir-mediated anti-tumoral activity is severely compromised in eEF2K-deficient engrafted tumors in vivo Our findings imply that exacerbated activation of eEF2K is detrimental for tumor survival and describe a mechanism explaining the anti-tumoral properties of HIV-PIs. Nelfinavir 10-20 eukaryotic elongation factor 2 kinase Homo sapiens 79-84 27462105-4 2016 We found that Nelfinavir impaired the maturation of lamin A, a structural component of the nuclear envelope, thereby promoting the release of DNA in the cytosol. Nelfinavir 14-24 lamin A Mus musculus 52-59 27462105-5 2016 Moreover, deficiency of the cytosolic DNA-sensor AIM2 impaired Nelfinavir-mediated inflammasome activation. Nelfinavir 63-73 absent in melanoma 2 Mus musculus 49-53 27280849-2 2016 Although the molecular mechanism by which nelfinavir exerts antitumor activity is still unknown, its effects have been related to Akt inhibition. Nelfinavir 42-52 AKT serine/threonine kinase 1 Homo sapiens 130-133 27280849-7 2016 Nelfinavir treated tumor cells also displayed a downregulation of the Akt pathway due to disruption of the Akt-HSP90 complex, and subsequent degradation of Akt. Nelfinavir 0-10 AKT serine/threonine kinase 1 Homo sapiens 70-73 27280849-7 2016 Nelfinavir treated tumor cells also displayed a downregulation of the Akt pathway due to disruption of the Akt-HSP90 complex, and subsequent degradation of Akt. Nelfinavir 0-10 AKT serine/threonine kinase 1 Homo sapiens 107-110 27280849-7 2016 Nelfinavir treated tumor cells also displayed a downregulation of the Akt pathway due to disruption of the Akt-HSP90 complex, and subsequent degradation of Akt. Nelfinavir 0-10 AKT serine/threonine kinase 1 Homo sapiens 107-110 27376043-9 2016 Verapamil reduces the expressions of P-glycoprotein in HepG2 and Huh-7; nelfinavir reduces the expression of OATP1B1 in HepG2 and Huh-7; while quinidine reduces the OCT1 gene expressions in HepG2, but not in Huh-7 cells. Nelfinavir 72-82 solute carrier organic anion transporter family member 1B1 Homo sapiens 109-116 27376043-9 2016 Verapamil reduces the expressions of P-glycoprotein in HepG2 and Huh-7; nelfinavir reduces the expression of OATP1B1 in HepG2 and Huh-7; while quinidine reduces the OCT1 gene expressions in HepG2, but not in Huh-7 cells. Nelfinavir 72-82 MIR7-3 host gene Homo sapiens 130-135 27376043-9 2016 Verapamil reduces the expressions of P-glycoprotein in HepG2 and Huh-7; nelfinavir reduces the expression of OATP1B1 in HepG2 and Huh-7; while quinidine reduces the OCT1 gene expressions in HepG2, but not in Huh-7 cells. Nelfinavir 72-82 solute carrier family 22 member 1 Homo sapiens 165-169 27376043-9 2016 Verapamil reduces the expressions of P-glycoprotein in HepG2 and Huh-7; nelfinavir reduces the expression of OATP1B1 in HepG2 and Huh-7; while quinidine reduces the OCT1 gene expressions in HepG2, but not in Huh-7 cells. Nelfinavir 72-82 MIR7-3 host gene Homo sapiens 130-135 27247056-10 2016 In vitro, nelfinavir sensitized Panc-1 and PSN-1 under normoxic and hypoxic conditions. Nelfinavir 10-20 5'-nucleotidase, cytosolic IIIA Homo sapiens 43-48 26977874-3 2016 (2016) report that nelfinavir suppresses MITF expression induced by MAPK pathway inhibition in melanoma cells and sensitizes melanoma cells with NRAS or BRAF plus NRAS mutations to MEK inhibitors. Nelfinavir 19-29 melanocyte inducing transcription factor Homo sapiens 41-45 26977874-3 2016 (2016) report that nelfinavir suppresses MITF expression induced by MAPK pathway inhibition in melanoma cells and sensitizes melanoma cells with NRAS or BRAF plus NRAS mutations to MEK inhibitors. Nelfinavir 19-29 NRAS proto-oncogene, GTPase Homo sapiens 145-149 26977874-3 2016 (2016) report that nelfinavir suppresses MITF expression induced by MAPK pathway inhibition in melanoma cells and sensitizes melanoma cells with NRAS or BRAF plus NRAS mutations to MEK inhibitors. Nelfinavir 19-29 mitogen-activated protein kinase kinase 7 Homo sapiens 181-184 26977879-3 2016 A drug-repositioning screen identified the HIV1-protease inhibitor nelfinavir as potent suppressor of PAX3 and MITF expression. Nelfinavir 67-77 paired box 3 Homo sapiens 102-106 26977879-3 2016 A drug-repositioning screen identified the HIV1-protease inhibitor nelfinavir as potent suppressor of PAX3 and MITF expression. Nelfinavir 67-77 melanocyte inducing transcription factor Homo sapiens 111-115 26977879-4 2016 Nelfinavir profoundly sensitizes BRAF and NRAS mutant melanoma cells to MAPK-pathway inhibitors. Nelfinavir 0-10 B-Raf proto-oncogene, serine/threonine kinase Homo sapiens 33-37 26977879-4 2016 Nelfinavir profoundly sensitizes BRAF and NRAS mutant melanoma cells to MAPK-pathway inhibitors. Nelfinavir 0-10 NRAS proto-oncogene, GTPase Homo sapiens 42-46 26977879-5 2016 Moreover, nelfinavir is effective in BRAF and NRAS mutant melanoma cells isolated from patients progressed on MAPK inhibitor (MAPKi) therapy and in BRAF/NRAS/PTEN mutant tumors. Nelfinavir 10-20 B-Raf proto-oncogene, serine/threonine kinase Homo sapiens 37-41 26977879-5 2016 Moreover, nelfinavir is effective in BRAF and NRAS mutant melanoma cells isolated from patients progressed on MAPK inhibitor (MAPKi) therapy and in BRAF/NRAS/PTEN mutant tumors. Nelfinavir 10-20 NRAS proto-oncogene, GTPase Homo sapiens 46-50 26977879-5 2016 Moreover, nelfinavir is effective in BRAF and NRAS mutant melanoma cells isolated from patients progressed on MAPK inhibitor (MAPKi) therapy and in BRAF/NRAS/PTEN mutant tumors. Nelfinavir 10-20 B-Raf proto-oncogene, serine/threonine kinase Homo sapiens 148-152 26977879-5 2016 Moreover, nelfinavir is effective in BRAF and NRAS mutant melanoma cells isolated from patients progressed on MAPK inhibitor (MAPKi) therapy and in BRAF/NRAS/PTEN mutant tumors. Nelfinavir 10-20 NRAS proto-oncogene, GTPase Homo sapiens 153-157 26977879-5 2016 Moreover, nelfinavir is effective in BRAF and NRAS mutant melanoma cells isolated from patients progressed on MAPK inhibitor (MAPKi) therapy and in BRAF/NRAS/PTEN mutant tumors. Nelfinavir 10-20 phosphatase and tensin homolog Homo sapiens 158-162 27121513-8 2016 This review describes the mechanisms by which PI3-K/AKT pathway causes radioresistance and the role of HIV protease inhibitors especially nelfinavir as a potential candidate drug to target the AKT pathway for overcoming radioresistance and its use in various clinical trials for different malignancies. Nelfinavir 138-148 AKT serine/threonine kinase 1 Rattus norvegicus 193-196 26715744-5 2016 Mice treated with Nelfinavir display hallmarks of this stress response in the liver, including alpha subunit of translation initiation factor 2 (eIF2alpha) phosphorylation, activating transcription factor-4 (ATF4) induction, and increased expression of known downstream targets. Nelfinavir 18-28 eukaryotic translation initiation factor 2A Mus musculus 145-154 26715744-5 2016 Mice treated with Nelfinavir display hallmarks of this stress response in the liver, including alpha subunit of translation initiation factor 2 (eIF2alpha) phosphorylation, activating transcription factor-4 (ATF4) induction, and increased expression of known downstream targets. Nelfinavir 18-28 activating transcription factor 4 Mus musculus 173-206 26715744-5 2016 Mice treated with Nelfinavir display hallmarks of this stress response in the liver, including alpha subunit of translation initiation factor 2 (eIF2alpha) phosphorylation, activating transcription factor-4 (ATF4) induction, and increased expression of known downstream targets. Nelfinavir 18-28 activating transcription factor 4 Mus musculus 208-212 26715744-6 2016 Mechanistically, Nelfinavir-mediated ISR bypassed direct activation of the eIF2alpha stress kinases and instead relied on the inhibition of the constitutive eIF2alpha dephosphorylation and down-regulation of the phophatase cofactor CReP (Constitutive Repressor of eIF2alpha Phosphorylation; also known as PPP1R15B). Nelfinavir 17-27 eukaryotic translation initiation factor 2A Homo sapiens 75-84 26715744-6 2016 Mechanistically, Nelfinavir-mediated ISR bypassed direct activation of the eIF2alpha stress kinases and instead relied on the inhibition of the constitutive eIF2alpha dephosphorylation and down-regulation of the phophatase cofactor CReP (Constitutive Repressor of eIF2alpha Phosphorylation; also known as PPP1R15B). Nelfinavir 17-27 eukaryotic translation initiation factor 2A Homo sapiens 157-166 26715744-6 2016 Mechanistically, Nelfinavir-mediated ISR bypassed direct activation of the eIF2alpha stress kinases and instead relied on the inhibition of the constitutive eIF2alpha dephosphorylation and down-regulation of the phophatase cofactor CReP (Constitutive Repressor of eIF2alpha Phosphorylation; also known as PPP1R15B). Nelfinavir 17-27 protein phosphatase 1 regulatory subunit 15B Homo sapiens 232-236 26715744-6 2016 Mechanistically, Nelfinavir-mediated ISR bypassed direct activation of the eIF2alpha stress kinases and instead relied on the inhibition of the constitutive eIF2alpha dephosphorylation and down-regulation of the phophatase cofactor CReP (Constitutive Repressor of eIF2alpha Phosphorylation; also known as PPP1R15B). Nelfinavir 17-27 protein phosphatase 1 regulatory subunit 15B Homo sapiens 238-289 26715744-6 2016 Mechanistically, Nelfinavir-mediated ISR bypassed direct activation of the eIF2alpha stress kinases and instead relied on the inhibition of the constitutive eIF2alpha dephosphorylation and down-regulation of the phophatase cofactor CReP (Constitutive Repressor of eIF2alpha Phosphorylation; also known as PPP1R15B). Nelfinavir 17-27 protein phosphatase 1 regulatory subunit 15B Homo sapiens 305-313 25752914-0 2015 Impact of CYP2C19 polymorphism on the pharmacokinetics of nelfinavir in patients with pancreatic cancer. Nelfinavir 58-68 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 10-17 25752914-1 2015 AIM: This study evaluated the influence of CYP2C19 polymorphisms on the pharmacokinetics of nelfinavir and its metabolite M8 in patients with pancreatic cancer. Nelfinavir 92-102 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 43-50 25752914-6 2015 The mean Cmax of nelfinavir in CYP2C19*1/*1 patients was 3.89 +- 0.40 (n = 3) and 5.12 +- 0.41 (n = 30) microg ml(-1) , while that of CYP2C19*1/*2 patients was 3.60 (n = 1) and 6.14 +- 0.31 (n = 5) microg ml(-1) at the doses of 625 and 1250 mg nelfinavir twice daily, respectively. Nelfinavir 17-27 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 31-38 25752914-6 2015 The mean Cmax of nelfinavir in CYP2C19*1/*1 patients was 3.89 +- 0.40 (n = 3) and 5.12 +- 0.41 (n = 30) microg ml(-1) , while that of CYP2C19*1/*2 patients was 3.60 (n = 1) and 6.14 +- 0.31 (n = 5) microg ml(-1) at the doses of 625 and 1250 mg nelfinavir twice daily, respectively. Nelfinavir 17-27 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 134-141 25752914-7 2015 For the M8 metabolite, the mean Cmax of CYP2C19*1/*1 patients was 1.06 +- 0.06 (n = 3) and 1.58 +- 0.27 (n = 30) microg ml(-1) , while those of CYP2C19*1/*2 patients were 1.01 (n = 1) and 1.23 +- 0.15 (n = 5) microg ml(-1) at the doses of 625 and 1250 mg nelfinavir twice daily, respectively. Nelfinavir 255-265 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 40-47 25752914-9 2015 The Cmax of nelfinavir was significantly higher (P <0.05) in CYP2C19*1/*2 patients but there was no statistical difference in AUC(0,12 h). Nelfinavir 12-22 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 64-71 25752914-10 2015 CONCLUSION: CYP2C19*1/*2 genotype modestly affected the pharmacokinetic profiles of nelfinavir and M8 in patients with locally advanced pancreatic cancer. Nelfinavir 84-94 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 12-19 25937300-7 2015 We further showed that Nelfinavir increased mitochondrial ROS production by decreasing manganese superoxide dismutase (MnSOD) protein levels. Nelfinavir 23-33 superoxide dismutase 2 Homo sapiens 87-117 25937300-7 2015 We further showed that Nelfinavir increased mitochondrial ROS production by decreasing manganese superoxide dismutase (MnSOD) protein levels. Nelfinavir 23-33 superoxide dismutase 2 Homo sapiens 119-124 26008229-7 2015 A 48 h treatment of human erythrocytes with nelfinavir significantly increased the percentage of annexin-V-binding cells (>=5microg/mL), significantly decreased forward scatter (>=2.5microg/mL), significantly increased ROS abundance (10 microg/mL), and significantly increased [Ca2+]i (>=5 microg/mL). Nelfinavir 44-54 annexin A5 Homo sapiens 97-106 26008229-8 2015 The up-regulation of annexin-V-binding following nelfinavir treatment was significantly blunted, but not abolished by either addition of the antioxidant N-acetylcysteine (1 mM) or removal of extracellular Ca2+. Nelfinavir 49-59 annexin A5 Homo sapiens 21-30 25880275-0 2015 Nelfinavir and nelfinavir analogs block site-2 protease cleavage to inhibit castration-resistant prostate cancer. Nelfinavir 0-10 membrane bound transcription factor peptidase, site 2 Homo sapiens 40-55 25880275-0 2015 Nelfinavir and nelfinavir analogs block site-2 protease cleavage to inhibit castration-resistant prostate cancer. Nelfinavir 15-25 membrane bound transcription factor peptidase, site 2 Homo sapiens 40-55 25880275-1 2015 Nelfinavir and its analogs inhibit proliferation and induce apoptosis of castration-resistant prostate cancer through inhibition of site-2 protease (S2P) activity, which leads to suppression of regulated intramembrane proteolysis. Nelfinavir 0-10 membrane bound transcription factor peptidase, site 2 Homo sapiens 132-147 25880275-1 2015 Nelfinavir and its analogs inhibit proliferation and induce apoptosis of castration-resistant prostate cancer through inhibition of site-2 protease (S2P) activity, which leads to suppression of regulated intramembrane proteolysis. Nelfinavir 0-10 membrane bound transcription factor peptidase, site 2 Homo sapiens 149-152 25880275-2 2015 Western blotting in nelfinavir and its analog treated cells confirms accumulation of precursor SREBP-1 and ATF6. Nelfinavir 20-30 sterol regulatory element binding transcription factor 1 Homo sapiens 95-102 25880275-2 2015 Western blotting in nelfinavir and its analog treated cells confirms accumulation of precursor SREBP-1 and ATF6. Nelfinavir 20-30 activating transcription factor 6 Homo sapiens 107-111 25880275-3 2015 Nelfinavir and its analogs inhibit human homolog M. jannaschii S2P cleavage of an artificial protein substrate CED-9 in an in vitro proteolysis assay in a dose-dependent manner. Nelfinavir 0-10 membrane bound transcription factor peptidase, site 2 Homo sapiens 63-66 25880275-4 2015 Nelfinavir and its analogs are more potent inhibitors of S2P cleavage activity than 1,10-phenanthroline, a metalloprotease-specific inhibitor. Nelfinavir 0-10 membrane bound transcription factor peptidase, site 2 Homo sapiens 57-60 25880275-6 2015 These results show nelfinavir and its analogs inhibit castration-resistant prostate cancer proliferation by blocking regulated intramembrane proteolysis through suppression of S2P cleavage activity. Nelfinavir 19-29 membrane bound transcription factor peptidase, site 2 Homo sapiens 176-179 25498902-0 2015 Endoplasmic reticulum stress and cell death in mTORC1-overactive cells is induced by nelfinavir and enhanced by chloroquine. Nelfinavir 85-95 CREB regulated transcription coactivator 1 Mus musculus 47-53 25498902-3 2015 This study utilised drug-induced ER stress through nelfinavir in order to examine ER stress tolerance in cell lines with hyper-active mTORC1 signalling. Nelfinavir 51-61 CREB regulated transcription coactivator 1 Mus musculus 134-140 25498902-4 2015 Our initial findings in wild type cells showed nelfinavir inhibited mTORC1 signalling and upregulated autophagy, as determined by decreased rpS6 and S6K1 phosphorylation, and SQTSM1 protein expression, respectively. Nelfinavir 47-57 CREB regulated transcription coactivator 1 Mus musculus 68-74 25498902-4 2015 Our initial findings in wild type cells showed nelfinavir inhibited mTORC1 signalling and upregulated autophagy, as determined by decreased rpS6 and S6K1 phosphorylation, and SQTSM1 protein expression, respectively. Nelfinavir 47-57 ribosomal protein S6 Homo sapiens 140-144 25498902-4 2015 Our initial findings in wild type cells showed nelfinavir inhibited mTORC1 signalling and upregulated autophagy, as determined by decreased rpS6 and S6K1 phosphorylation, and SQTSM1 protein expression, respectively. Nelfinavir 47-57 ribosomal protein S6 kinase B1 Homo sapiens 149-153 25498902-5 2015 Contrastingly, cells with hyper-active mTORC1 displayed basally elevated levels of ER stress which was greatly exaggerated following nelfinavir treatment, seen through increased CHOP mRNA and XBP1 splicing. Nelfinavir 133-143 CREB regulated transcription coactivator 1 Mus musculus 39-45 25498902-5 2015 Contrastingly, cells with hyper-active mTORC1 displayed basally elevated levels of ER stress which was greatly exaggerated following nelfinavir treatment, seen through increased CHOP mRNA and XBP1 splicing. Nelfinavir 133-143 DNA damage inducible transcript 3 Homo sapiens 178-182 25498902-5 2015 Contrastingly, cells with hyper-active mTORC1 displayed basally elevated levels of ER stress which was greatly exaggerated following nelfinavir treatment, seen through increased CHOP mRNA and XBP1 splicing. Nelfinavir 133-143 X-box binding protein 1 Homo sapiens 192-196 25498902-7 2015 Combination of nelfinavir and chloroquine significantly increased ER stress and caused selective cell death in multiple cell line models with hyper-active mTORC1, whilst control cells with normalised mTORC1 signalling tolerated treatment. Nelfinavir 15-25 CREB regulated transcription coactivator 1 Mus musculus 155-161 25498902-7 2015 Combination of nelfinavir and chloroquine significantly increased ER stress and caused selective cell death in multiple cell line models with hyper-active mTORC1, whilst control cells with normalised mTORC1 signalling tolerated treatment. Nelfinavir 15-25 CREB regulated transcription coactivator 1 Mus musculus 200-206 25498902-9 2015 Our research demonstrates that combination of nelfinavir and chloroquine has therapeutic potential for treatment of mTORC1-driven tumours. Nelfinavir 46-56 CREB regulated transcription coactivator 1 Mus musculus 116-122 25327558-12 2014 In peripheral blood mononuclear cells, Nelfinavir inhibited AKT and induced markers of ER stress. Nelfinavir 39-49 AKT serine/threonine kinase 1 Homo sapiens 60-63 24483157-0 2014 The HIV protease inhibitor nelfinavir down-regulates RET signaling and induces apoptosis in medullary thyroid cancer cells. Nelfinavir 27-37 ret proto-oncogene Homo sapiens 53-56 24483157-3 2014 HSP90 is a molecular target for the HIV protease inhibitor nelfinavir (NFV). Nelfinavir 59-69 heat shock protein 90 alpha family class A member 1 Homo sapiens 0-5 24418752-6 2014 Saquinavir, nelfinavir and lopinavir were likewise cytotoxic against primary AML cells, triggered PS-induced apoptosis, inhibited AKT-phosphorylation and showed synergistic cytotoxicity with bortezomib and carfilzomib at low micromolar concentrations. Nelfinavir 12-22 AKT serine/threonine kinase 1 Homo sapiens 130-133 24418752-7 2014 Exclusively nelfinavir inhibited intracellular proteasome activity, including the beta2 proteasome activity that is not targeted by bortezomib/carfilzomib. Nelfinavir 12-22 potassium calcium-activated channel subfamily M regulatory beta subunit 2 Homo sapiens 82-87 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). Nelfinavir 237-247 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%. Nelfinavir 204-214 ATP binding cassette subfamily B member 1 Homo sapiens 86-90 25571293-3 2014 Nelfinavir, a protease inhibitor, and its major metabolite (M8) are known to be potent CYP3A4 inhibitors. Nelfinavir 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 87-93 24194293-11 2014 NFV (1,250 mg bid) concurrent with temozolomide and radiotherapy is tolerated in most patients with glioblastoma. Nelfinavir 0-3 BH3 interacting domain death agonist Homo sapiens 14-17 23916134-0 2013 Nelfinavir and bortezomib inhibit mTOR activity via ATF4-mediated sestrin-2 regulation. Nelfinavir 0-10 mechanistic target of rapamycin kinase Homo sapiens 34-38 23916134-0 2013 Nelfinavir and bortezomib inhibit mTOR activity via ATF4-mediated sestrin-2 regulation. Nelfinavir 0-10 activating transcription factor 4 Homo sapiens 52-56 23916134-0 2013 Nelfinavir and bortezomib inhibit mTOR activity via ATF4-mediated sestrin-2 regulation. Nelfinavir 0-10 sestrin 2 Homo sapiens 66-75 23916134-4 2013 In this study, the treatment of cancer cells with ER stress-inducing drug nelfinavir resulted in the expression of endogenous mTOR inhibitor sestrin-2 (SESN2). Nelfinavir 74-84 mechanistic target of rapamycin kinase Homo sapiens 126-130 23916134-4 2013 In this study, the treatment of cancer cells with ER stress-inducing drug nelfinavir resulted in the expression of endogenous mTOR inhibitor sestrin-2 (SESN2). Nelfinavir 74-84 sestrin 2 Homo sapiens 141-150 23916134-4 2013 In this study, the treatment of cancer cells with ER stress-inducing drug nelfinavir resulted in the expression of endogenous mTOR inhibitor sestrin-2 (SESN2). Nelfinavir 74-84 sestrin 2 Homo sapiens 152-157 23916134-9 2013 Accordingly, cancer cells treated with the ER stress-inducing agent nelfinavir showed reduced mTOR activity and associated increases in the expression levels of ATF4 and SESN2. Nelfinavir 68-78 mechanistic target of rapamycin kinase Homo sapiens 94-98 23916134-9 2013 Accordingly, cancer cells treated with the ER stress-inducing agent nelfinavir showed reduced mTOR activity and associated increases in the expression levels of ATF4 and SESN2. Nelfinavir 68-78 activating transcription factor 4 Homo sapiens 161-165 23916134-9 2013 Accordingly, cancer cells treated with the ER stress-inducing agent nelfinavir showed reduced mTOR activity and associated increases in the expression levels of ATF4 and SESN2. Nelfinavir 68-78 sestrin 2 Homo sapiens 170-175 23916134-11 2013 mTOR inhibition by nelfinavir, which is currently in clinical trials for cancer patients, may also explain its observed ability to induce autophagy, growth arrest, and radiosensitization in cancer cells. Nelfinavir 19-29 mechanistic target of rapamycin kinase Homo sapiens 0-4 24052619-0 2013 Re: selective inhibition of Her2-positive breast cancer cells by the HIV protease inhibitor nelfinavir. Nelfinavir 92-102 erb-b2 receptor tyrosine kinase 2 Homo sapiens 28-32 23775562-4 2013 Among the PIs evaluated (nelfinavir, ritonavir, amprenavir, saquinavir, and indinavir), only nelfinavir both effectively stimulated MRP4 ATPase activity and inhibited substrate-stimulated ATPase activity. Nelfinavir 93-103 ATP binding cassette subfamily C member 4 Homo sapiens 132-136 23775562-6 2013 MRP4 expression reduced intracellular accumulation of nelfinavir and consequently conferred survival advantage to nelfinavir cytotoxicity. Nelfinavir 54-64 ATP binding cassette subfamily C member 4 Homo sapiens 0-4 23775562-6 2013 MRP4 expression reduced intracellular accumulation of nelfinavir and consequently conferred survival advantage to nelfinavir cytotoxicity. Nelfinavir 114-124 ATP binding cassette subfamily C member 4 Homo sapiens 0-4 23775562-7 2013 Nelfinavir blocked Mrp4-mediated export, which is consistent with its ability to increase the sensitivity of MRP4-expressing cells to methotrexate. Nelfinavir 0-10 ATP binding cassette subfamily C member 4 Homo sapiens 19-23 23775562-7 2013 Nelfinavir blocked Mrp4-mediated export, which is consistent with its ability to increase the sensitivity of MRP4-expressing cells to methotrexate. Nelfinavir 0-10 ATP binding cassette subfamily C member 4 Homo sapiens 109-113 23775562-8 2013 In contrast, targeted inactivation of Abcc4/Mrp4 in mouse cells specifically enhanced nelfinavir and 9-(2-phosphonylmethoxyethyl) adenine cytotoxicity. Nelfinavir 86-96 ATP-binding cassette, sub-family C (CFTR/MRP), member 4 Mus musculus 38-43 23775562-8 2013 In contrast, targeted inactivation of Abcc4/Mrp4 in mouse cells specifically enhanced nelfinavir and 9-(2-phosphonylmethoxyethyl) adenine cytotoxicity. Nelfinavir 86-96 ATP-binding cassette, sub-family C (CFTR/MRP), member 4 Mus musculus 44-48 23775562-9 2013 These results suggest that nelfinavir is both an inhibitor and substrate of MRP4. Nelfinavir 27-37 ATP binding cassette subfamily C member 4 Homo sapiens 76-80 23775562-10 2013 Because nelfinavir is a new MRP4/ABCC4 substrate, we developed a MRP4/ABCC4 pharmacophore model, which showed that the nelfinavir binding site is shared with chemotherapeutic substrates such as adefovir and methotrexate. Nelfinavir 8-18 ATP binding cassette subfamily C member 4 Homo sapiens 28-32 23775562-10 2013 Because nelfinavir is a new MRP4/ABCC4 substrate, we developed a MRP4/ABCC4 pharmacophore model, which showed that the nelfinavir binding site is shared with chemotherapeutic substrates such as adefovir and methotrexate. Nelfinavir 8-18 ATP binding cassette subfamily C member 4 Homo sapiens 33-38 23775562-10 2013 Because nelfinavir is a new MRP4/ABCC4 substrate, we developed a MRP4/ABCC4 pharmacophore model, which showed that the nelfinavir binding site is shared with chemotherapeutic substrates such as adefovir and methotrexate. Nelfinavir 8-18 ATP binding cassette subfamily C member 4 Homo sapiens 65-69 23775562-10 2013 Because nelfinavir is a new MRP4/ABCC4 substrate, we developed a MRP4/ABCC4 pharmacophore model, which showed that the nelfinavir binding site is shared with chemotherapeutic substrates such as adefovir and methotrexate. Nelfinavir 8-18 ATP binding cassette subfamily C member 4 Homo sapiens 70-75 23775562-10 2013 Because nelfinavir is a new MRP4/ABCC4 substrate, we developed a MRP4/ABCC4 pharmacophore model, which showed that the nelfinavir binding site is shared with chemotherapeutic substrates such as adefovir and methotrexate. Nelfinavir 119-129 ATP binding cassette subfamily C member 4 Homo sapiens 28-32 23775562-10 2013 Because nelfinavir is a new MRP4/ABCC4 substrate, we developed a MRP4/ABCC4 pharmacophore model, which showed that the nelfinavir binding site is shared with chemotherapeutic substrates such as adefovir and methotrexate. Nelfinavir 119-129 ATP binding cassette subfamily C member 4 Homo sapiens 33-38 23775562-10 2013 Because nelfinavir is a new MRP4/ABCC4 substrate, we developed a MRP4/ABCC4 pharmacophore model, which showed that the nelfinavir binding site is shared with chemotherapeutic substrates such as adefovir and methotrexate. Nelfinavir 119-129 ATP binding cassette subfamily C member 4 Homo sapiens 65-69 23775562-10 2013 Because nelfinavir is a new MRP4/ABCC4 substrate, we developed a MRP4/ABCC4 pharmacophore model, which showed that the nelfinavir binding site is shared with chemotherapeutic substrates such as adefovir and methotrexate. Nelfinavir 119-129 ATP binding cassette subfamily C member 4 Homo sapiens 70-75 23775562-11 2013 Our studies reveal, for the first time, that nelfinavir, a potent and cytotoxic PI, is both a substrate and inhibitor of MRP4. Nelfinavir 45-55 ATP binding cassette subfamily C member 4 Homo sapiens 121-125 23775562-12 2013 These findings suggest that HIV-infected cancer patients receiving nelfinavir might experience both enhanced antitumor efficacy and unexpected adverse toxicity given the role of MRP4/ABCC4 in exporting nucleoside-based antiretroviral medications and cancer chemotherapeutics. Nelfinavir 67-77 ATP binding cassette subfamily C member 4 Homo sapiens 178-182 23775562-12 2013 These findings suggest that HIV-infected cancer patients receiving nelfinavir might experience both enhanced antitumor efficacy and unexpected adverse toxicity given the role of MRP4/ABCC4 in exporting nucleoside-based antiretroviral medications and cancer chemotherapeutics. Nelfinavir 67-77 ATP binding cassette subfamily C member 4 Homo sapiens 183-188 23386514-0 2013 Indinavir and nelfinavir inhibit proximal insulin receptor signaling and salicylate abrogates inhibition: potential role of the NFkappa B pathway. Nelfinavir 14-24 insulin receptor Cricetulus griseus 42-58 23386514-3 2013 Indinavir and nelfinavir induced a significant decrease in tyrosine phosphorylation of the insulin receptor beta-subunit. Nelfinavir 14-24 insulin receptor Cricetulus griseus 91-107 23647753-0 2013 Phase I trial of the combination of the Akt inhibitor nelfinavir and chemoradiation for locally advanced rectal cancer. Nelfinavir 54-64 AKT serine/threonine kinase 1 Homo sapiens 40-43 23647753-12 2013 CONCLUSIONS: Nelfinavir 750 mg BID was defined as the recommended phase II dose in combination with capecitabine and 50.4 Gy pre-operative radiotherapy in rectal cancer. Nelfinavir 13-23 BH3 interacting domain death agonist Homo sapiens 31-34 23454896-5 2013 Nelfinavir is the HIV-PI with highest cytotoxic activity against primary myeloma cells and with an IC50 near therapeutic drug blood levels (8-14 muM), irrespective of bortezomib sensitivity. Nelfinavir 0-10 latexin Homo sapiens 145-148 23454896-6 2013 Only nelfinavir inhibited intracellular proteasome activity in situ at drug concentrations <40 muM. Nelfinavir 5-15 latexin Homo sapiens 98-101 23454896-11 2013 Nelfinavir has unique proteasome inhibiting activity in particular on the bortezomib/carfilzomib-insensitive tryptic (beta2) proteasome activity in intact myeloma cells, and is active against bortezomib/carfilzomib-resistant myeloma cells in vitro. Nelfinavir 0-10 potassium calcium-activated channel subfamily M regulatory beta subunit 2 Homo sapiens 118-123 23042933-0 2012 Selective inhibition of HER2-positive breast cancer cells by the HIV protease inhibitor nelfinavir. Nelfinavir 88-98 erb-b2 receptor tyrosine kinase 2 Homo sapiens 24-28 23042933-4 2012 To identify molecular targets of nelfinavir, identified in the screen as a selective inhibitor of HER2-positive cells, we conducted a genome-wide screen of a haploinsufficiency yeast mutant collection. Nelfinavir 33-43 erb-b2 receptor tyrosine kinase 2 Homo sapiens 98-102 23042933-7 2012 RESULTS: Pharmacological profiling showed that nelfinavir, an anti-HIV drug, selectively inhibited the growth of HER2-positive breast cancer cells in vitro. Nelfinavir 47-57 erb-b2 receptor tyrosine kinase 2 Homo sapiens 113-117 23042933-8 2012 A genome-wide screening of haploinsufficiency yeast mutants revealed that nelfinavir inhibited heat shock protein 90 (HSP90) function. Nelfinavir 74-84 Hsp90 family chaperone HSP82 Saccharomyces cerevisiae S288C 95-116 23042933-8 2012 A genome-wide screening of haploinsufficiency yeast mutants revealed that nelfinavir inhibited heat shock protein 90 (HSP90) function. Nelfinavir 74-84 Hsp90 family chaperone HSP82 Saccharomyces cerevisiae S288C 118-123 23042933-9 2012 Further characterization using proteolytic footprinting experiments indicated that nelfinavir inhibited HSP90 in breast cancer cells through a novel mechanism. Nelfinavir 83-93 heat shock protein 90 alpha family class A member 1 Homo sapiens 104-109 23042933-11 2012 Moreover, nelfinavir inhibited the growth of trastuzumab- and/or lapatinib-resistant, HER2-positive breast cancer cells in vitro at clinically achievable concentrations. Nelfinavir 10-20 erb-b2 receptor tyrosine kinase 2 Homo sapiens 86-90 23042933-12 2012 CONCLUSION: Nelfinavir was found to be a new class of HSP90 inhibitor and can be brought to HER2-breast cancer treatment trials with the same dosage regimen as that used among HIV patients. Nelfinavir 12-22 heat shock protein 90 alpha family class A member 1 Homo sapiens 54-59 22786868-0 2012 The HIV-1 protease inhibitor nelfinavir activates PP2 and inhibits MAPK signaling in macrophages: a pathway to reduce inflammation. Nelfinavir 29-39 neuropeptide Y receptor Y6 (pseudogene) Homo sapiens 50-53 22540830-0 2012 Nelfinavir inhibits regulated intramembrane proteolysis of sterol regulatory element binding protein-1 and activating transcription factor 6 in castration-resistant prostate cancer. Nelfinavir 0-10 sterol regulatory element binding transcription factor 1 Homo sapiens 59-102 22540830-0 2012 Nelfinavir inhibits regulated intramembrane proteolysis of sterol regulatory element binding protein-1 and activating transcription factor 6 in castration-resistant prostate cancer. Nelfinavir 0-10 activating transcription factor 6 Homo sapiens 107-140 22540830-1 2012 Nelfinavir induces apoptosis in liposarcoma by inhibiting site-2 protease (S2P) activity, which leads to suppression of regulated intramembrane proteolysis. Nelfinavir 0-10 membrane bound transcription factor peptidase, site 2 Homo sapiens 58-73 22540830-1 2012 Nelfinavir induces apoptosis in liposarcoma by inhibiting site-2 protease (S2P) activity, which leads to suppression of regulated intramembrane proteolysis. Nelfinavir 0-10 membrane bound transcription factor peptidase, site 2 Homo sapiens 75-78 22540830-3 2012 Nelfinavir inhibited androgen receptor activation in androgen-sensitive prostate cancer and the nuclear translocation of the fusion proteins sterol regulatory element binding protein-1 (SREBP-1)-enhanced green fluorescence protein (EGFP) and activating transcription factor 6 (ATF6)-EGFP in castration-resistant prostate cancer cells, viewed under confocal microscopy. Nelfinavir 0-10 androgen receptor Homo sapiens 21-38 22540830-3 2012 Nelfinavir inhibited androgen receptor activation in androgen-sensitive prostate cancer and the nuclear translocation of the fusion proteins sterol regulatory element binding protein-1 (SREBP-1)-enhanced green fluorescence protein (EGFP) and activating transcription factor 6 (ATF6)-EGFP in castration-resistant prostate cancer cells, viewed under confocal microscopy. Nelfinavir 0-10 sterol regulatory element binding transcription factor 1 Homo sapiens 141-184 22540830-3 2012 Nelfinavir inhibited androgen receptor activation in androgen-sensitive prostate cancer and the nuclear translocation of the fusion proteins sterol regulatory element binding protein-1 (SREBP-1)-enhanced green fluorescence protein (EGFP) and activating transcription factor 6 (ATF6)-EGFP in castration-resistant prostate cancer cells, viewed under confocal microscopy. Nelfinavir 0-10 sterol regulatory element binding transcription factor 1 Homo sapiens 186-193 22540830-3 2012 Nelfinavir inhibited androgen receptor activation in androgen-sensitive prostate cancer and the nuclear translocation of the fusion proteins sterol regulatory element binding protein-1 (SREBP-1)-enhanced green fluorescence protein (EGFP) and activating transcription factor 6 (ATF6)-EGFP in castration-resistant prostate cancer cells, viewed under confocal microscopy. Nelfinavir 0-10 activating transcription factor 6 Homo sapiens 242-275 22540830-3 2012 Nelfinavir inhibited androgen receptor activation in androgen-sensitive prostate cancer and the nuclear translocation of the fusion proteins sterol regulatory element binding protein-1 (SREBP-1)-enhanced green fluorescence protein (EGFP) and activating transcription factor 6 (ATF6)-EGFP in castration-resistant prostate cancer cells, viewed under confocal microscopy. Nelfinavir 0-10 activating transcription factor 6 Homo sapiens 277-281 22540830-6 2012 Western blotting of S1P and S2P siRNA knockdown and/or nelfinavir-treated cells confirmed the accumulation of precursor SREBP-1 and ATF6. Nelfinavir 55-65 sterol regulatory element binding transcription factor 1 Homo sapiens 120-127 22540830-6 2012 Western blotting of S1P and S2P siRNA knockdown and/or nelfinavir-treated cells confirmed the accumulation of precursor SREBP-1 and ATF6. Nelfinavir 55-65 activating transcription factor 6 Homo sapiens 132-136 22540830-8 2012 In contrast, 1,10-phenanthroline, an S2P inhibitor, reproduced the nelfinavir-treated molecular and biological phenotype. Nelfinavir 67-77 membrane bound transcription factor peptidase, site 2 Homo sapiens 37-40 22540830-9 2012 Nelfinavir-mediated inhibition of regulated intramembrane proteolysis led to the accumulation of unprocessed SREBP-1 and ATF6. Nelfinavir 0-10 sterol regulatory element binding transcription factor 1 Homo sapiens 109-116 22540830-9 2012 Nelfinavir-mediated inhibition of regulated intramembrane proteolysis led to the accumulation of unprocessed SREBP-1 and ATF6. Nelfinavir 0-10 activating transcription factor 6 Homo sapiens 121-125 22271897-10 2012 Cell death triggered by nelfinavir treatment correlated with decreased phosphorylation of AKT, STAT3 and ERK1/2. Nelfinavir 24-34 AKT serine/threonine kinase 1 Homo sapiens 90-93 22271897-10 2012 Cell death triggered by nelfinavir treatment correlated with decreased phosphorylation of AKT, STAT3 and ERK1/2. Nelfinavir 24-34 signal transducer and activator of transcription 3 Homo sapiens 95-100 22271897-10 2012 Cell death triggered by nelfinavir treatment correlated with decreased phosphorylation of AKT, STAT3 and ERK1/2. Nelfinavir 24-34 mitogen-activated protein kinase 3 Homo sapiens 105-111 22759761-4 2012 Nelfinavir induced apoptosis in both cell lines, although the extent as indicated by Annexin V staining varied. Nelfinavir 0-10 annexin A5 Homo sapiens 85-94 21826404-5 2012 Atazanavir, ritonavir, and saquinavir modestly inhibited of Abeta degradation, while lopinavir, nelfinavir, and ritonavir enhanced secretion of undigested Abeta after phagocytosis. Nelfinavir 96-106 amyloid beta precursor protein Homo sapiens 155-160 21826404-6 2012 Lopinavir, nelfinavir, ritonavir, and saquinavir inhibited endogenous Abeta40 production from primary cultured human cortical neurons, which were associated with reduction in Beta-site APP Converting Enzyme 1 (BACE1) and gamma-secretase enzyme activities. Nelfinavir 11-21 beta-secretase 1 Homo sapiens 175-208 21826404-6 2012 Lopinavir, nelfinavir, ritonavir, and saquinavir inhibited endogenous Abeta40 production from primary cultured human cortical neurons, which were associated with reduction in Beta-site APP Converting Enzyme 1 (BACE1) and gamma-secretase enzyme activities. Nelfinavir 11-21 beta-secretase 1 Homo sapiens 210-215 22338016-0 2012 Akt inhibitors MK-2206 and nelfinavir overcome mTOR inhibitor resistance in diffuse large B-cell lymphoma. Nelfinavir 27-37 AKT serine/threonine kinase 1 Homo sapiens 0-3 22338016-0 2012 Akt inhibitors MK-2206 and nelfinavir overcome mTOR inhibitor resistance in diffuse large B-cell lymphoma. Nelfinavir 27-37 mechanistic target of rapamycin kinase Homo sapiens 47-51 22338016-10 2012 Nelfinavir and MK-2206, chosen for their Akt-inhibitory properties, yielded synergistic inhibition of cell viability in combination with rapamycin in DLBCL cell lines, and potently inhibited phosphorylation of Akt and downstream targets of activated mTOR. Nelfinavir 0-10 AKT serine/threonine kinase 1 Homo sapiens 41-44 22338016-10 2012 Nelfinavir and MK-2206, chosen for their Akt-inhibitory properties, yielded synergistic inhibition of cell viability in combination with rapamycin in DLBCL cell lines, and potently inhibited phosphorylation of Akt and downstream targets of activated mTOR. Nelfinavir 0-10 AKT serine/threonine kinase 1 Homo sapiens 210-213 22338016-10 2012 Nelfinavir and MK-2206, chosen for their Akt-inhibitory properties, yielded synergistic inhibition of cell viability in combination with rapamycin in DLBCL cell lines, and potently inhibited phosphorylation of Akt and downstream targets of activated mTOR. Nelfinavir 0-10 mechanistic target of rapamycin kinase Homo sapiens 250-254 22564423-0 2012 Matrix metalloproteinase-2 and -9 in glioblastoma: a trio of old drugs-captopril, disulfiram and nelfinavir-are inhibitors with potential as adjunctive treatments in glioblastoma. Nelfinavir 97-107 matrix metallopeptidase 2 Homo sapiens 0-33 22161308-1 2012 PURPOSE: To predict and determine whether the protease inhibitors (PIs) nelfinavir, amprenavir, atazanavir, ritonavir, and saquinavir could serve as metabolic inhibitors of the human CES1 (hCES1) using both molecular modeling techniques and in vitro inhibition assays. Nelfinavir 72-82 carboxylesterase 1 Homo sapiens 183-187 22161308-4 2012 RESULTS: Pharmacophore and 2D-QSAR modeling predicted that nelfinavir would serve as a potent hCES1 inhibitor. Nelfinavir 59-69 carboxylesterase 1 Homo sapiens 94-99 22161308-8 2012 DDIs could occur when nelfinavir is co-administered with drugs metabolized by hCES1. Nelfinavir 22-32 carboxylesterase 1 Homo sapiens 78-83 22568101-15 2012 Our data indicate that AIF could contribute to photoreceptor apoptosis in retinal detachment, and that an AIF inhibitor, Nelfinavir, could prevent apoptotic change. Nelfinavir 121-131 apoptosis inducing factor mitochondria associated 1 Homo sapiens 106-109 22017299-6 2012 The stimulation of the GSH export from viable astrocytes by indinavir or nelfinavir was completely prevented by the application of MK571, an inhibitor of the multidrug resistance protein 1. Nelfinavir 73-83 ATP binding cassette subfamily B member 1 Homo sapiens 158-188 22017299-7 2012 These data demonstrate that indinavir and nelfinavir stimulate multidrug resistance protein 1-mediated GSH export from viable astrocytes and suggest that treatment of patients with such inhibitors may affect the GSH homeostasis in brain. Nelfinavir 42-52 ATP binding cassette subfamily B member 1 Homo sapiens 63-93 23082557-2 2012 A previous study showed that ABCB-1 C3435T polymorphism affects plasma efavirenz and nelfinavir concentrations and rate of CD4+ T cell recovery after starting antiretroviral treatment (ART). Nelfinavir 85-95 ATP binding cassette subfamily B member 1 Homo sapiens 29-35 21682753-3 2011 However, CYP3A4-ethanol physical interaction and its impact on drug binding, inhibition, or metabolism is not known, except that we have recently shown that ethanol facilitates the binding of a protease inhibitor (PI), nelfinavir, with CYP3A4. Nelfinavir 219-229 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 9-15 21682753-3 2011 However, CYP3A4-ethanol physical interaction and its impact on drug binding, inhibition, or metabolism is not known, except that we have recently shown that ethanol facilitates the binding of a protease inhibitor (PI), nelfinavir, with CYP3A4. Nelfinavir 219-229 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 236-242 21930825-0 2011 Complex drug interactions of HIV protease inhibitors 2: in vivo induction and in vitro to in vivo correlation of induction of cytochrome P450 1A2, 2B6, and 2C9 by ritonavir or nelfinavir. Nelfinavir 176-186 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 126-150 21930825-3 2011 Statistically significant induction of CYP1A2 (2.1-, 2.9-, and 2.2-fold), CYP2B6 (1.8-, 2.4-, and 4-fold), and CYP2C9 (1.3-, 1.8-, and 2.6-fold) was observed after NFV, RTV, or RIF treatment, respectively (as expected, CYP2D6 was not induced). Nelfinavir 164-167 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 39-45 21930825-3 2011 Statistically significant induction of CYP1A2 (2.1-, 2.9-, and 2.2-fold), CYP2B6 (1.8-, 2.4-, and 4-fold), and CYP2C9 (1.3-, 1.8-, and 2.6-fold) was observed after NFV, RTV, or RIF treatment, respectively (as expected, CYP2D6 was not induced). Nelfinavir 164-167 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 74-80 21930825-3 2011 Statistically significant induction of CYP1A2 (2.1-, 2.9-, and 2.2-fold), CYP2B6 (1.8-, 2.4-, and 4-fold), and CYP2C9 (1.3-, 1.8-, and 2.6-fold) was observed after NFV, RTV, or RIF treatment, respectively (as expected, CYP2D6 was not induced). Nelfinavir 164-167 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 111-117 21811091-5 2011 We evaluated tumor growth delay and confirmed nelfinavir"s effect on the PI3K-AKT-mTOR pathway in a hind-flank model. Nelfinavir 46-56 mechanistic target of rapamycin kinase Homo sapiens 82-86 21811091-10 2011 Decreased phospho-S6 on Western blotting in vitro and immunohistochemistry in vivo demonstrated nelfinavir inhibition of the PI3K-AKT-mTOR pathway. Nelfinavir 96-106 mechanistic target of rapamycin kinase Homo sapiens 134-138 21697087-0 2011 Modulation of CCAAT/enhancer binding protein homologous protein (CHOP)-dependent DR5 expression by nelfinavir sensitizes glioblastoma multiforme cells to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL). Nelfinavir 99-109 DNA damage inducible transcript 3 Homo sapiens 14-63 21697087-0 2011 Modulation of CCAAT/enhancer binding protein homologous protein (CHOP)-dependent DR5 expression by nelfinavir sensitizes glioblastoma multiforme cells to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL). Nelfinavir 99-109 DNA damage inducible transcript 3 Homo sapiens 65-69 21697087-0 2011 Modulation of CCAAT/enhancer binding protein homologous protein (CHOP)-dependent DR5 expression by nelfinavir sensitizes glioblastoma multiforme cells to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL). Nelfinavir 99-109 TNF receptor superfamily member 10b Homo sapiens 81-84 21697087-0 2011 Modulation of CCAAT/enhancer binding protein homologous protein (CHOP)-dependent DR5 expression by nelfinavir sensitizes glioblastoma multiforme cells to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL). Nelfinavir 99-109 TNF superfamily member 10 Homo sapiens 154-209 21697087-0 2011 Modulation of CCAAT/enhancer binding protein homologous protein (CHOP)-dependent DR5 expression by nelfinavir sensitizes glioblastoma multiforme cells to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL). Nelfinavir 99-109 TNF superfamily member 10 Homo sapiens 211-216 21697087-5 2011 We found that Nelfinavir treatment led to ER stress-induced up-regulation of the DR5 receptor. Nelfinavir 14-24 TNF receptor superfamily member 10b Homo sapiens 81-84 21697087-9 2011 Combining Nelfinavir with TRAIL led to a significantly enhanced level of apoptosis that was abrogated by siRNA silencing of DR5. Nelfinavir 10-20 TNF receptor superfamily member 10b Homo sapiens 124-127 21697087-10 2011 We provide evidence that Nelfinavir-induced ER stress modulates DR5 expression in human glioblastoma multiforme cells and can enhance TRAIL efficacy. Nelfinavir 25-35 TNF receptor superfamily member 10b Homo sapiens 64-67 21697087-10 2011 We provide evidence that Nelfinavir-induced ER stress modulates DR5 expression in human glioblastoma multiforme cells and can enhance TRAIL efficacy. Nelfinavir 25-35 TNF superfamily member 10 Homo sapiens 134-139 21266539-7 2011 Dose responses allowed calculation of IC(50) values; e.g., for nelfinavir, of 3.4 muM (human Ddi1) and 0.44 muM (Leishmania Ddi1). Nelfinavir 63-73 latexin Homo sapiens 82-85 21266539-7 2011 Dose responses allowed calculation of IC(50) values; e.g., for nelfinavir, of 3.4 muM (human Ddi1) and 0.44 muM (Leishmania Ddi1). Nelfinavir 63-73 DNA damage inducible 1 homolog 1 Homo sapiens 93-97 21355074-0 2011 Nelfinavir induces liposarcoma apoptosis through inhibition of regulated intramembrane proteolysis of SREBP-1 and ATF6. Nelfinavir 0-10 sterol regulatory element binding transcription factor 1 Homo sapiens 102-109 21355074-0 2011 Nelfinavir induces liposarcoma apoptosis through inhibition of regulated intramembrane proteolysis of SREBP-1 and ATF6. Nelfinavir 0-10 activating transcription factor 6 Homo sapiens 114-118 21355074-1 2011 PURPOSE: We previously reported that nelfinavir (NFV) induces G(1) cell-cycle block and apoptosis selectively in liposarcoma cell lines due to increased SREBP-1 (sterol regulatory element binding protein-1) expression in the absence of increased transcription. Nelfinavir 37-47 sterol regulatory element binding transcription factor 1 Homo sapiens 153-160 21355074-1 2011 PURPOSE: We previously reported that nelfinavir (NFV) induces G(1) cell-cycle block and apoptosis selectively in liposarcoma cell lines due to increased SREBP-1 (sterol regulatory element binding protein-1) expression in the absence of increased transcription. Nelfinavir 37-47 sterol regulatory element binding transcription factor 1 Homo sapiens 162-205 21329798-6 2011 Among the several methods presented, the analysis of an unconventional XBP1 splicing, caused by the ER stress sensor IRE1, is shown to present the most sensitive and most specific marker for nelfinavir-induced ER stress. Nelfinavir 191-201 X-box binding protein 1 Homo sapiens 71-75 21329798-6 2011 Among the several methods presented, the analysis of an unconventional XBP1 splicing, caused by the ER stress sensor IRE1, is shown to present the most sensitive and most specific marker for nelfinavir-induced ER stress. Nelfinavir 191-201 endoplasmic reticulum to nucleus signaling 1 Homo sapiens 117-121 21329798-8 2011 Such a PCR-based XBP1 splicing analysis might not only be suitable to monitor nelfinavir-induced ER stress, but could also be applied in drug screening programs to test for other ER stress-inducing agents with similar activities or synergistic activities with nelfinavir. Nelfinavir 78-88 X-box binding protein 1 Homo sapiens 17-21 21329798-8 2011 Such a PCR-based XBP1 splicing analysis might not only be suitable to monitor nelfinavir-induced ER stress, but could also be applied in drug screening programs to test for other ER stress-inducing agents with similar activities or synergistic activities with nelfinavir. Nelfinavir 260-270 X-box binding protein 1 Homo sapiens 17-21 20861742-5 2010 Darunavir, fosamprenavir, lopinavir, nelfinavir, tipranavir, efavirenz, and abacavir increased CYP3A4 and/or CYP2B6 promoter activity, some through constitutive androstane receptor but mainly through PXR. Nelfinavir 37-47 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 95-101 20861742-5 2010 Darunavir, fosamprenavir, lopinavir, nelfinavir, tipranavir, efavirenz, and abacavir increased CYP3A4 and/or CYP2B6 promoter activity, some through constitutive androstane receptor but mainly through PXR. Nelfinavir 37-47 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 109-115 20861742-5 2010 Darunavir, fosamprenavir, lopinavir, nelfinavir, tipranavir, efavirenz, and abacavir increased CYP3A4 and/or CYP2B6 promoter activity, some through constitutive androstane receptor but mainly through PXR. Nelfinavir 37-47 nuclear receptor subfamily 1 group I member 3 Homo sapiens 148-180 20861742-5 2010 Darunavir, fosamprenavir, lopinavir, nelfinavir, tipranavir, efavirenz, and abacavir increased CYP3A4 and/or CYP2B6 promoter activity, some through constitutive androstane receptor but mainly through PXR. Nelfinavir 37-47 nuclear receptor subfamily 1 group I member 2 Homo sapiens 200-203 20937259-0 2010 Effect of ethanol on spectral binding, inhibition, and activity of CYP3A4 with an antiretroviral drug nelfinavir. Nelfinavir 102-112 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 67-73 20937259-8 2010 These results suggest that ethanol facilitates binding of nelfinavir with CYP3A4. Nelfinavir 58-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 74-80 19554262-0 2010 Nelfinavir induces mitochondria protection by ERK1/2-mediated mcl-1 stabilization that can be overcome by sorafenib. Nelfinavir 0-10 mitogen-activated protein kinase 3 Homo sapiens 46-52 19554262-0 2010 Nelfinavir induces mitochondria protection by ERK1/2-mediated mcl-1 stabilization that can be overcome by sorafenib. Nelfinavir 0-10 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 62-67 19554262-3 2010 In contrast to the pro-apoptotic effect of nelfinavir on human cancer cells, we noticed a significant upregulation of the anti-apoptotic mitochondrial membrane protein mcl-1 by nelfinavir, resulting in a mitochondria-independent induction of apoptosis. Nelfinavir 177-187 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 168-173 19554262-6 2010 The combination of nelfinavir with sorafenib, a clinically applied inhibitor of the RAS/RAF/ERK1/2 pathway, inhibited nelfinavir-induced ERK1/2 activation and mcl-1 protein upregulation. Nelfinavir 19-29 zinc fingers and homeoboxes 2 Homo sapiens 88-91 19554262-6 2010 The combination of nelfinavir with sorafenib, a clinically applied inhibitor of the RAS/RAF/ERK1/2 pathway, inhibited nelfinavir-induced ERK1/2 activation and mcl-1 protein upregulation. Nelfinavir 19-29 mitogen-activated protein kinase 3 Homo sapiens 92-98 19554262-6 2010 The combination of nelfinavir with sorafenib, a clinically applied inhibitor of the RAS/RAF/ERK1/2 pathway, inhibited nelfinavir-induced ERK1/2 activation and mcl-1 protein upregulation. Nelfinavir 19-29 mitogen-activated protein kinase 3 Homo sapiens 137-143 19554262-6 2010 The combination of nelfinavir with sorafenib, a clinically applied inhibitor of the RAS/RAF/ERK1/2 pathway, inhibited nelfinavir-induced ERK1/2 activation and mcl-1 protein upregulation. Nelfinavir 19-29 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 159-164 19554262-6 2010 The combination of nelfinavir with sorafenib, a clinically applied inhibitor of the RAS/RAF/ERK1/2 pathway, inhibited nelfinavir-induced ERK1/2 activation and mcl-1 protein upregulation. Nelfinavir 118-128 zinc fingers and homeoboxes 2 Homo sapiens 88-91 19554262-6 2010 The combination of nelfinavir with sorafenib, a clinically applied inhibitor of the RAS/RAF/ERK1/2 pathway, inhibited nelfinavir-induced ERK1/2 activation and mcl-1 protein upregulation. Nelfinavir 118-128 mitogen-activated protein kinase 3 Homo sapiens 92-98 19554262-6 2010 The combination of nelfinavir with sorafenib, a clinically applied inhibitor of the RAS/RAF/ERK1/2 pathway, inhibited nelfinavir-induced ERK1/2 activation and mcl-1 protein upregulation. Nelfinavir 118-128 mitogen-activated protein kinase 3 Homo sapiens 137-143 20591557-3 2010 STUDY DESIGN: The effects of saquinavir and nelfinavir were evaluated on human trophoblast functions and integrity by investigating their effect on human chorionic gonadotropin (hCG) secretion and on P-gp expression and functionality. Nelfinavir 44-54 hypertrichosis 2 (generalised, congenital) Homo sapiens 178-181 20591557-3 2010 STUDY DESIGN: The effects of saquinavir and nelfinavir were evaluated on human trophoblast functions and integrity by investigating their effect on human chorionic gonadotropin (hCG) secretion and on P-gp expression and functionality. Nelfinavir 44-54 phosphoglycolate phosphatase Homo sapiens 200-204 20591557-4 2010 RESULTS: Nelfinavir significantly reduced hCG secretion by 30% after a 48-h treatment but it had no effect on syncytia formation. Nelfinavir 9-19 hypertrichosis 2 (generalised, congenital) Homo sapiens 42-45 20507927-7 2010 Several PIs potently inhibited OATP2B1-mediated transport in Caco-2 cells at clinically relevant IC(50) concentrations for ritonavir (0.93 microM), atazanavir (2.2 microM), lopinavir (1.7 microM), tipranavir (0.77 microM), and nelfinavir (2.2 microM). Nelfinavir 227-237 solute carrier organic anion transporter family member 2B1 Homo sapiens 31-38 19890215-0 2010 CYP2C19 genetic variants affect nelfinavir pharmacokinetics and virologic response in HIV-1-infected children receiving highly active antiretroviral therapy. Nelfinavir 32-42 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 0-7 19890215-4 2010 RESULTS: Nelfinavir CL/F and M8 to nelfinavir ratios were significantly associated with the CYP2C19-G681A genotypes (P < 0.001). Nelfinavir 35-45 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 92-99 19890215-7 2010 CONCLUSIONS: CYP2C19 genotypes altered nelfinavir pharmacokinetics and the virologic response to HAART in HIV-1-infected children. Nelfinavir 39-49 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 13-20 19890215-8 2010 These findings suggest that CYP2C19 genotypes are important determinants of nelfinavir pharmacokinetics and virologic response in HIV-1-infected children. Nelfinavir 76-86 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 28-35 20361030-6 2010 We also demonstrate that parasites overexpressing GSH1 (the rate limiting enzyme of glutathione biosynthesis) were more resistant to nelfinavir when compared to untransfected controls. Nelfinavir 133-143 GS homeobox 1 Homo sapiens 50-54 20238377-5 2010 In human hepatocytes, saquinavir, ritonavir and atazanavir were the most efficient inhibitors of ABCC2-mediated biliary excretion of CDF, whereas in rat hepatocytes indinavir, lopinavir and nelfinavir were the most efficient. Nelfinavir 190-200 ATP binding cassette subfamily C member 2 Homo sapiens 97-102 20103665-11 2010 Oral nelfinavir administration to mice bearing mutant K-ras-containing Capan-2 xenografts resulted in a greater than additive increase in radiation-mediated tumor growth delay (synergy assessment ratio of 1.5). Nelfinavir 5-15 Kirsten rat sarcoma viral oncogene homolog Mus musculus 54-59 20105315-0 2010 The mitochondria-independent cytotoxic effect of nelfinavir on leukemia cells can be enhanced by sorafenib-mediated mcl-1 downregulation and mitochondrial membrane destabilization. Nelfinavir 49-59 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 116-121 20105315-6 2010 Nelfinavir-induced death of leukemia cells was accompanied by activation of caspases 3, 7, and 8. Nelfinavir 0-10 caspase 3 Homo sapiens 76-96 20105315-7 2010 Despite caspase activation, the upregulation of the anti-apoptotic bcl-2 family member protein mcl-1 that resulted from nelfinavir treatment stabilized the mitochondrial membrane potential, resulting in primarily mitochondria-independent cell death. Nelfinavir 120-130 BCL2 apoptosis regulator Homo sapiens 67-72 20105315-7 2010 Despite caspase activation, the upregulation of the anti-apoptotic bcl-2 family member protein mcl-1 that resulted from nelfinavir treatment stabilized the mitochondrial membrane potential, resulting in primarily mitochondria-independent cell death. Nelfinavir 120-130 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 95-100 20105315-8 2010 Pharmacological downregulation of mcl-1 expression by treatment with sorafenib (2 microg/ml) significantly enhanced nelfinavir-induced apoptosis even at lower nelfinavir concentrations (5 microg/ml), but did not have additional detrimental effects on non-malignant bone marrow cells. Nelfinavir 116-126 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 34-39 20105315-8 2010 Pharmacological downregulation of mcl-1 expression by treatment with sorafenib (2 microg/ml) significantly enhanced nelfinavir-induced apoptosis even at lower nelfinavir concentrations (5 microg/ml), but did not have additional detrimental effects on non-malignant bone marrow cells. Nelfinavir 159-169 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 34-39 20594311-7 2010 At a concentration of 6 mug/ml, tamoxifen substantially enhanced the endoplasmic reticulum stress reaction in those cell lines that responded to nelfinavir with binding protein (BiP) upregulation (MCF7, T47D), and enhanced autophagy in cell lines that responded to nelfinavir treatment with autophagy marker light chain 3B upregulation (MDA-MB-453). Nelfinavir 145-155 heat shock protein family A (Hsp70) member 5 Homo sapiens 178-181 19931478-9 2010 We have shown that HIV-1 protease drugs such as tipranavir, nelfinavir, lopinavir, and atazanavir differ in their binding modes on each other for metabolic clearance in CYP3A4, whereas ritonavir, amprenavir, indinavir, saquinavir, fosamprenavir, and darunavir share the same binding mode. Nelfinavir 60-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 169-175 19916992-0 2009 Influence of CYP2C19 polymorphism on the pharmacokinetics of nelfinavir and its active metabolite. Nelfinavir 61-71 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 13-20 19916992-8 2009 CONCLUSIONS: Mutation in CYP2C19 increased the systemic exposure of nelfinavir and reduced the exposure of M8. Nelfinavir 68-78 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 25-32 19283769-5 2009 Nelfinavir and saquinavir associated extensively with micelles and equilibrium free fractions were low at P85 concentrations above the CMC, with association constants being in the order nelfinavir > saquinavir >>> abacavir. Nelfinavir 0-10 phosphoinositide-3-kinase regulatory subunit 2 Homo sapiens 106-109 19345476-6 2009 We conclude that the anti-tumor effects of nelfinavir can be enhanced by celecoxib analogs in a COX-2 independent fashion via the aggravation of ER stress, and such drug combinations should be considered as a beneficial adjunct to the treatment of drug-resistant breast cancers. Nelfinavir 43-53 prostaglandin-endoperoxide synthase 2 Homo sapiens 96-101 19500085-8 2009 Both nelfinavir and ritonavir decreased both M1 and M3, consistent with their ability to inhibit CYP3A and 2C8. Nelfinavir 5-15 cholinergic receptor muscarinic 1 Homo sapiens 45-54 19500085-8 2009 Both nelfinavir and ritonavir decreased both M1 and M3, consistent with their ability to inhibit CYP3A and 2C8. Nelfinavir 5-15 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-102 19478134-3 2009 Nelfinavir is cleared from the body predominantly by CYP3A metabolism and P-glycoprotein (P-gp) efflux. Nelfinavir 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-58 19478134-3 2009 Nelfinavir is cleared from the body predominantly by CYP3A metabolism and P-glycoprotein (P-gp) efflux. Nelfinavir 0-10 ATP binding cassette subfamily B member 1 Homo sapiens 74-88 19478134-3 2009 Nelfinavir is cleared from the body predominantly by CYP3A metabolism and P-glycoprotein (P-gp) efflux. Nelfinavir 0-10 ATP binding cassette subfamily B member 1 Homo sapiens 90-94 19480971-4 2009 We are in the process of starting a clinical trial in H&N cancer patients using nelfinavir (NFV) (which inhibits Akt) and it would be important to know the effect of HPV on radiation response +/- NFV. Nelfinavir 84-94 AKT serine/threonine kinase 1 Homo sapiens 117-120 19302339-10 2009 Our results suggest that the direct effects of nelfinavir on the HCV subgenome and its synergism with IFN could improve clinical responses to IFN therapy in HCV/HIV coinfected patients. Nelfinavir 47-57 interferon alpha 1 Homo sapiens 142-145 19179444-0 2009 Postreceptoral adipocyte insulin resistance induced by nelfinavir is caused by insensitivity of PKB/Akt to phosphatidylinositol-3,4,5-trisphosphate. Nelfinavir 55-65 insulin Homo sapiens 25-32 19179444-2 2009 Adipocytes exposed for 18 h to the HIV protease inhibitor nelfinavir manifest insulin resistance characterized by normal insulin-stimulated tyrosine phosphorylation of the insulin receptor and insulin receptor substrate proteins, preserved in vitro phosphatidylinositol 3-kinase (PI 3-kinase) assay activity but impaired activation of PKB/Akt and stimulation of glucose uptake. Nelfinavir 58-68 insulin Homo sapiens 78-85 19179444-2 2009 Adipocytes exposed for 18 h to the HIV protease inhibitor nelfinavir manifest insulin resistance characterized by normal insulin-stimulated tyrosine phosphorylation of the insulin receptor and insulin receptor substrate proteins, preserved in vitro phosphatidylinositol 3-kinase (PI 3-kinase) assay activity but impaired activation of PKB/Akt and stimulation of glucose uptake. Nelfinavir 58-68 insulin Homo sapiens 121-128 19179444-2 2009 Adipocytes exposed for 18 h to the HIV protease inhibitor nelfinavir manifest insulin resistance characterized by normal insulin-stimulated tyrosine phosphorylation of the insulin receptor and insulin receptor substrate proteins, preserved in vitro phosphatidylinositol 3-kinase (PI 3-kinase) assay activity but impaired activation of PKB/Akt and stimulation of glucose uptake. Nelfinavir 58-68 insulin Homo sapiens 121-128 19179444-2 2009 Adipocytes exposed for 18 h to the HIV protease inhibitor nelfinavir manifest insulin resistance characterized by normal insulin-stimulated tyrosine phosphorylation of the insulin receptor and insulin receptor substrate proteins, preserved in vitro phosphatidylinositol 3-kinase (PI 3-kinase) assay activity but impaired activation of PKB/Akt and stimulation of glucose uptake. Nelfinavir 58-68 insulin Homo sapiens 121-128 19179444-3 2009 Here we aimed to assess whether impaired PKB/Akt activation is indeed rate limiting for insulin signaling propagation in response to nelfinavir and the mechanism for defective PKB/Akt activation. Nelfinavir 133-143 insulin Homo sapiens 88-95 19179444-4 2009 Nelfinavir treatment of 3T3-L1 adipocytes impaired the insulin-stimulated translocation and membrane fusion of myc-glucose transporter (GLUT)-4-green fluorescent protein (GFP) reporter. Nelfinavir 0-10 insulin Homo sapiens 55-62 19179444-5 2009 Phosphorylation of PKB/Akt substrates including glycogen synthase kinase-3 and AS160 decreased in response to nelfinavir, and this remained true, even in cells with forced generation of phosphatidylinositol-3,4,5-trisphohphate (PIP(3)) by a membrane-targeted active PI 3-kinase, confirming that impaired PKB/Akt activation was rate limiting for insulin signal propagation. Nelfinavir 110-120 TBC1 domain family member 4 Homo sapiens 79-84 19179444-5 2009 Phosphorylation of PKB/Akt substrates including glycogen synthase kinase-3 and AS160 decreased in response to nelfinavir, and this remained true, even in cells with forced generation of phosphatidylinositol-3,4,5-trisphohphate (PIP(3)) by a membrane-targeted active PI 3-kinase, confirming that impaired PKB/Akt activation was rate limiting for insulin signal propagation. Nelfinavir 110-120 insulin Homo sapiens 345-352 19179444-9 2009 Collectively, nelfinavir uncovers a postreceptor mechanism for insulin resistance, caused by interference with the sensing of PIP(3) by PKB/Akt, leading to impaired GLUT4 translocation and membrane fusion. Nelfinavir 14-24 insulin Homo sapiens 63-70 19179444-9 2009 Collectively, nelfinavir uncovers a postreceptor mechanism for insulin resistance, caused by interference with the sensing of PIP(3) by PKB/Akt, leading to impaired GLUT4 translocation and membrane fusion. Nelfinavir 14-24 solute carrier family 2 member 4 Homo sapiens 165-170 19234050-5 2009 The present study showed that exposure to several different PIs, nelfinavir (5-10 microM), saquinavir (5-10 microM) and atazanavir (8-20 microM), decreases glucose stimulated insulin secretion from rat pancreatic beta-cells (INS-1). Nelfinavir 65-75 insulin 1 Rattus norvegicus 225-230 19234050-6 2009 Nelfinavir significantly increased reactive oxygen species (ROS) generation and suppressed cytosolic, but not mitochondrial superoxide dismutase (SOD) levels. Nelfinavir 0-10 superoxide dismutase 1 Homo sapiens 124-144 19234050-6 2009 Nelfinavir significantly increased reactive oxygen species (ROS) generation and suppressed cytosolic, but not mitochondrial superoxide dismutase (SOD) levels. Nelfinavir 0-10 superoxide dismutase 1 Homo sapiens 146-149 19234050-8 2009 Simultaneous treatment with thymoquinone (TQ) (2.5 microM), an active ingredient of black seed oil, significantly inhibited the effect of nelfinavir on augmented ROS production and suppressed SOD levels. Nelfinavir 138-148 superoxide dismutase 1 Homo sapiens 192-195 19176623-5 2009 In contrast, the five Gag mutations significantly delayed the acquisition of HIV-1 resistance to ritonavir and nelfinavir (NFV). Nelfinavir 111-121 Pr55(Gag) Human immunodeficiency virus 1 22-25 19246729-8 2009 While nelfinavir exposure was higher in poor compared with extensive metabolizers of CYP2C19 isozyme, there were no corresponding significant differences in QTcF change from placebo. Nelfinavir 6-16 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 85-92 19033543-7 2009 As previously reported, nelfinavir inhibited adipogenesis downstream of C/EBPbeta, but similarly in both cell lines. Nelfinavir 24-34 CCAAT enhancer binding protein beta Homo sapiens 72-81 19033543-8 2009 In contrast, nelfinavir"s capacity to diminish insulin signaling, decrease leptin secretion, enhance basal lipolysis, and decrease expression of the lipid droplet-associated protein perilipin occurred more robustly and/or at lower nelfinavir concentrations in the SC line. Nelfinavir 13-23 insulin Homo sapiens 47-54 19106637-4 2009 Nelfinavir significantly changed the morphology of ovarian cancer cells, resulting in formation of large ER-derived vacuoles and induced upregulation of the hsp70 heat shock family member BiP (GRP78) which accumulated within swollen ER membranes. Nelfinavir 0-10 heat shock protein family A (Hsp70) member 4 Homo sapiens 157-162 19106637-4 2009 Nelfinavir significantly changed the morphology of ovarian cancer cells, resulting in formation of large ER-derived vacuoles and induced upregulation of the hsp70 heat shock family member BiP (GRP78) which accumulated within swollen ER membranes. Nelfinavir 0-10 heat shock protein family A (Hsp70) member 5 Homo sapiens 188-191 19106637-4 2009 Nelfinavir significantly changed the morphology of ovarian cancer cells, resulting in formation of large ER-derived vacuoles and induced upregulation of the hsp70 heat shock family member BiP (GRP78) which accumulated within swollen ER membranes. Nelfinavir 0-10 heat shock protein family A (Hsp70) member 5 Homo sapiens 193-198 19106637-6 2009 Correspondingly, we observed downregulation of cell cycle regulatory proteins after nelfinavir treatment, especially that of cyclin D3, and induction of apoptosis as confirmed by annexin binding. Nelfinavir 84-94 cyclin D3 Homo sapiens 125-134 19834271-10 2009 EFV, ritonavir (RTV) and nelfinavir (NFV) inhibited the expression of adiponectin mRNA in mature 3T3-L1 and to a greater extent in pre-mature 3T3-L1. Nelfinavir 25-35 adiponectin, C1Q and collagen domain containing Homo sapiens 70-81 19834271-10 2009 EFV, ritonavir (RTV) and nelfinavir (NFV) inhibited the expression of adiponectin mRNA in mature 3T3-L1 and to a greater extent in pre-mature 3T3-L1. Nelfinavir 37-40 adiponectin, C1Q and collagen domain containing Homo sapiens 70-81 19000651-0 2008 Nelfinavir induces TRAIL receptor upregulation in ovarian cancer cells. Nelfinavir 0-10 TNF superfamily member 10 Homo sapiens 19-24 19000651-4 2008 Nelfinavir sensitized ovarian cancer cells to treatment with an apoptosis-inducing TRAIL receptor antibody due to upregulation of the TRAIL receptor DR5 as shown by RT-PCR and FACScan analysis. Nelfinavir 0-10 TNF superfamily member 10 Homo sapiens 83-88 19000651-4 2008 Nelfinavir sensitized ovarian cancer cells to treatment with an apoptosis-inducing TRAIL receptor antibody due to upregulation of the TRAIL receptor DR5 as shown by RT-PCR and FACScan analysis. Nelfinavir 0-10 TNF superfamily member 10 Homo sapiens 134-139 19000651-4 2008 Nelfinavir sensitized ovarian cancer cells to treatment with an apoptosis-inducing TRAIL receptor antibody due to upregulation of the TRAIL receptor DR5 as shown by RT-PCR and FACScan analysis. Nelfinavir 0-10 TNF receptor superfamily member 10b Homo sapiens 149-152 19000651-5 2008 We conclude that nelfinavir, an already approved drug, is a highly efficient agent against ovarian cancer cells and could sensitize ovarian cancer cells to TRAIL treatment, either therapeutically applied or endogenously produced by cells of the immune system. Nelfinavir 17-27 TNF superfamily member 10 Homo sapiens 156-161 18393290-4 2008 Pluronic P85 inhibited both basal and nelfinavir-stimulated P-gp ATPase activity, while Pluronic F127 had no effect. Nelfinavir 38-48 phosphoglycolate phosphatase Homo sapiens 60-64 18393290-5 2008 In cell accumulation studies, Pluronic P85 restored the accumulation of nelfinavir in MDCKII-MDR1 cells while Pluronic F127 and F88 had no effect. Nelfinavir 72-82 ATP binding cassette subfamily B member 1 Homo sapiens 93-97 18393290-7 2008 In conclusion, this study provides evidence that a block-copolymer, Pluronic P85, effectively inhibits the interaction of P-gp with nelfinavir and saquinavir. Nelfinavir 132-142 phosphoglycolate phosphatase Homo sapiens 122-126 18576910-9 2008 The increased warfarin doses required in these two patients may have been caused by induction of CYP3A4 by nevirapine, CYP2C9 by nelfinavir, or CYP2C9 by lopinavir-ritonavir. Nelfinavir 129-139 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-103 18576910-9 2008 The increased warfarin doses required in these two patients may have been caused by induction of CYP3A4 by nevirapine, CYP2C9 by nelfinavir, or CYP2C9 by lopinavir-ritonavir. Nelfinavir 129-139 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 119-125 18497877-5 2008 Oral administration of the PIs nelfinavir and ritonavir significantly inhibited photoreceptor apoptosis, while preventing the translocation of AIF from mitochondria to the nucleus as well as the activation of caspase-9. Nelfinavir 31-41 apoptosis-inducing factor, mitochondrion-associated 1 Mus musculus 143-146 18497877-5 2008 Oral administration of the PIs nelfinavir and ritonavir significantly inhibited photoreceptor apoptosis, while preventing the translocation of AIF from mitochondria to the nucleus as well as the activation of caspase-9. Nelfinavir 31-41 caspase 9 Mus musculus 209-218 18497877-7 2008 Nelfinavir attenuated apoptosis as well as mitochondrial release of AIF and cytochrome c, and subsequent activation of caspase-9 in vitro, in photoreceptor cultures exposed to starvation or monocyte chemoattractant protein-1-stimulated (MCP-1-stimulated) macrophages. Nelfinavir 0-10 apoptosis-inducing factor, mitochondrion-associated 1 Mus musculus 68-71 18497877-7 2008 Nelfinavir attenuated apoptosis as well as mitochondrial release of AIF and cytochrome c, and subsequent activation of caspase-9 in vitro, in photoreceptor cultures exposed to starvation or monocyte chemoattractant protein-1-stimulated (MCP-1-stimulated) macrophages. Nelfinavir 0-10 caspase 9 Mus musculus 119-128 18497877-7 2008 Nelfinavir attenuated apoptosis as well as mitochondrial release of AIF and cytochrome c, and subsequent activation of caspase-9 in vitro, in photoreceptor cultures exposed to starvation or monocyte chemoattractant protein-1-stimulated (MCP-1-stimulated) macrophages. Nelfinavir 0-10 chemokine (C-C motif) ligand 2 Mus musculus 190-224 18497877-7 2008 Nelfinavir attenuated apoptosis as well as mitochondrial release of AIF and cytochrome c, and subsequent activation of caspase-9 in vitro, in photoreceptor cultures exposed to starvation or monocyte chemoattractant protein-1-stimulated (MCP-1-stimulated) macrophages. Nelfinavir 0-10 chemokine (C-C motif) ligand 2 Mus musculus 237-242 18509182-6 2008 Phospho-Akt downregulation by nelfinavir was monitored by immunoblotting in patient leukocytes. Nelfinavir 30-40 AKT serine/threonine kinase 1 Homo sapiens 8-11 18344876-8 2008 Cells treated with nelfinavir had a lower expression of PPARgamma, LPL, and ap2 and presented disorganization of lamin A/C. Nelfinavir 19-29 peroxisome proliferator activated receptor gamma Homo sapiens 56-65 18344876-8 2008 Cells treated with nelfinavir had a lower expression of PPARgamma, LPL, and ap2 and presented disorganization of lamin A/C. Nelfinavir 19-29 transcription factor AP-2 alpha Homo sapiens 76-79 18344876-8 2008 Cells treated with nelfinavir had a lower expression of PPARgamma, LPL, and ap2 and presented disorganization of lamin A/C. Nelfinavir 19-29 lamin A/C Homo sapiens 113-122 17922881-0 2008 Effect of CYP2C19 polymorphism on nelfinavir to M8 biotransformation in HIV patients. Nelfinavir 34-44 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 10-17 17922881-1 2008 WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT: * Nelfinavir is an HIV protease inhibitor, substrate of the transporter P-glycoprotein and metabolized via CYP2C19, CYP3A4 and CYP3A5 enzymes. Nelfinavir 44-54 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 149-156 17922881-1 2008 WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT: * Nelfinavir is an HIV protease inhibitor, substrate of the transporter P-glycoprotein and metabolized via CYP2C19, CYP3A4 and CYP3A5 enzymes. Nelfinavir 44-54 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 158-164 17922881-1 2008 WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT: * Nelfinavir is an HIV protease inhibitor, substrate of the transporter P-glycoprotein and metabolized via CYP2C19, CYP3A4 and CYP3A5 enzymes. Nelfinavir 44-54 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 169-175 17922881-5 2008 WHAT THIS STUDY ADDS: * Patients with an *1/*2 or *2/*2 genotype for CYP2C19 had a nelfinavir to M8 biotransformation divided by 2 compared with *1/*1 patients. Nelfinavir 83-93 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 69-76 17922881-7 2008 AIMS: To evaluate the effect of CYP2C19 polymorphism on nelfinavir and M8 pharmacokinetic variability in human immunodeficiency virus-infected patients and to study the link between pharmacokinetic exposure and short-term efficacy and toxicity. Nelfinavir 56-66 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 32-39 17922881-18 2008 CONCLUSIONS: The rate of metabolism of nelfinavir to M8 was reduced by 50% in patients with *1/*2 or *2/*2 genotype for CYP2C19 compared with those with *1/*1 genotype. Nelfinavir 39-49 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 120-127 18302767-0 2008 Alterations in the Notch4 pathway in cerebral endothelial cells by the HIV aspartyl protease inhibitor, nelfinavir. Nelfinavir 104-114 notch receptor 4 Homo sapiens 19-25 18302767-2 2008 Recently, PIs, particularly Nelfinavir, were reported to disrupt Notch signaling in the HIV-related endothelial cell neoplasm, Kaposi"s sarcoma. Nelfinavir 28-38 notch receptor 1 Homo sapiens 65-70 18302767-8 2008 On the other hand, only Nelfinavir increased significantly Notch 4 processing, Notch4 intracellular domain nuclear localization and the expression of notch intracellular domain targets NFkappaB and matrix metalloproteinase 2. Nelfinavir 24-34 notch receptor 4 Homo sapiens 59-66 18302767-8 2008 On the other hand, only Nelfinavir increased significantly Notch 4 processing, Notch4 intracellular domain nuclear localization and the expression of notch intracellular domain targets NFkappaB and matrix metalloproteinase 2. Nelfinavir 24-34 notch receptor 4 Homo sapiens 79-85 18302767-8 2008 On the other hand, only Nelfinavir increased significantly Notch 4 processing, Notch4 intracellular domain nuclear localization and the expression of notch intracellular domain targets NFkappaB and matrix metalloproteinase 2. Nelfinavir 24-34 nuclear factor kappa B subunit 1 Homo sapiens 185-193 18302767-8 2008 On the other hand, only Nelfinavir increased significantly Notch 4 processing, Notch4 intracellular domain nuclear localization and the expression of notch intracellular domain targets NFkappaB and matrix metalloproteinase 2. Nelfinavir 24-34 matrix metallopeptidase 2 Homo sapiens 198-224 18302767-9 2008 Pre-treatment with the antioxidant Vitamin E prevented PI-induced reactive oxygen species generation and partially prevented Nelfinavir-induced changes in both Notch 4 processing, and cellular localization patterns. Nelfinavir 125-135 notch receptor 4 Homo sapiens 160-167 18302767-11 2008 CONCLUSION: Nelfinavir affects Notch 4 processing that results in induction of expression of the pro-angiogenic genes NFkappaB and matrix metalloproteinase 2 in cerebral endothelial cells. Nelfinavir 12-22 notch receptor 4 Homo sapiens 31-38 18302767-11 2008 CONCLUSION: Nelfinavir affects Notch 4 processing that results in induction of expression of the pro-angiogenic genes NFkappaB and matrix metalloproteinase 2 in cerebral endothelial cells. Nelfinavir 12-22 nuclear factor kappa B subunit 1 Homo sapiens 118-126 18302767-11 2008 CONCLUSION: Nelfinavir affects Notch 4 processing that results in induction of expression of the pro-angiogenic genes NFkappaB and matrix metalloproteinase 2 in cerebral endothelial cells. Nelfinavir 12-22 matrix metallopeptidase 2 Homo sapiens 131-157 18040268-14 2008 Furthermore, all four protease inhibitors (PIs) used in highly active antiretroviral therapy decreased OPG synthesis by human blood T cells, nelfinavir being the most efficient PI. Nelfinavir 141-151 TNF receptor superfamily member 11b Homo sapiens 103-106 18000394-6 2008 Nelfinavir blocks growth factor receptor activation and decreases growth factor-induced and endogenous Akt signaling. Nelfinavir 0-10 AKT serine/threonine kinase 1 Homo sapiens 103-106 17981652-4 2008 Whereas TREC copies did not change over 3 weeks in untreated controls, TREC copies/copies CCR5 increased following Nelfinavir monotherapy in 8 patients (p < 0.02), and did not change in 7 patients (p = NS). Nelfinavir 115-125 C-C motif chemokine receptor 5 Homo sapiens 90-94 17978814-5 2008 Hoechst 33342 dye efflux from primary human proximal tubule cells was significantly reduced by the BCRP/ABCG2 inhibitors fumitremorgin C and nelfinavir. Nelfinavir 141-151 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 99-103 17978814-5 2008 Hoechst 33342 dye efflux from primary human proximal tubule cells was significantly reduced by the BCRP/ABCG2 inhibitors fumitremorgin C and nelfinavir. Nelfinavir 141-151 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 104-109 17639026-3 2007 At 10 microM, ritonavir and nelfinavir suppressed CYP3A4 activity but induced its transcripts and protein expression (19- and 12- and 12- and 6-fold, respectively; a >2-fold change over control was interpreted as induction). Nelfinavir 28-38 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 50-56 17785575-10 2007 Akt was variably inhibited by HIV protease inhibitors, but nelfinavir caused the greatest inhibition of endogenous and growth factor-induced Akt activation. Nelfinavir 59-69 AKT serine/threonine kinase 1 Homo sapiens 141-144 17591677-7 2007 Our data indicate that nelfinavir has poor penetration into the macaque"s brain and CSF, and P-gp inhibition at the BBB by zosuquidar enhanced the distribution of nelfinavir into the brain by 146-fold. Nelfinavir 163-173 ATP binding cassette subfamily B member 1 Homo sapiens 93-97 17591677-0 2007 Inhibition of P-glycoprotein activity at the primate blood-brain barrier increases the distribution of nelfinavir into the brain but not into the cerebrospinal fluid. Nelfinavir 103-113 ATP binding cassette subfamily B member 1 Homo sapiens 14-28 17591677-9 2007 In conclusion, P-gp inhibition at the nonhuman primate BBB significantly enhanced the distribution of nelfinavir into the brain, and this effect was not observed in the CSF. Nelfinavir 102-112 ATP binding cassette subfamily B member 1 Homo sapiens 15-19 17653450-8 2007 The mean CD4 cell count increase after a 12-month period was also greater in the efavirenz group (195 x 10(6) cells/L) than in the nelfinavir group (119 x 10(6) cells/L; P = 0.002). Nelfinavir 131-141 CD4 molecule Homo sapiens 9-12 17351982-0 2007 Doxorubicin cardiomyopathy via TLR-2 stimulation: potential for prevention using current anti-retroviral inhibitors such as ritonavir and nelfinavir. Nelfinavir 138-148 toll like receptor 2 Homo sapiens 31-36 17483362-0 2007 Phosphatase and tensin homologue deficiency in glioblastoma confers resistance to radiation and temozolomide that is reversed by the protease inhibitor nelfinavir. Nelfinavir 152-162 phosphatase and tensin homolog Homo sapiens 0-32 17483362-3 2007 We examined whether PTEN deficiency leads to radioresistance and whether this can be reversed by nelfinavir, a protease inhibitor that decreases Akt signaling. Nelfinavir 97-107 AKT serine/threonine kinase 1 Homo sapiens 145-148 17483362-4 2007 Nelfinavir decreased Akt phosphorylation and enhanced radiosensitization in U251MG and U87MG glioblastoma cells, both of which are PTEN deficient. Nelfinavir 0-10 AKT serine/threonine kinase 1 Homo sapiens 21-24 17483362-4 2007 Nelfinavir decreased Akt phosphorylation and enhanced radiosensitization in U251MG and U87MG glioblastoma cells, both of which are PTEN deficient. Nelfinavir 0-10 phosphatase and tensin homolog Homo sapiens 131-135 17483362-5 2007 In the derivative line U251MG-PTEN, induction of wild-type PTEN with doxycycline decreased P-Akt expression and increased radiosensitivity to a similar extent as nelfinavir. Nelfinavir 162-172 phosphatase and tensin homolog Homo sapiens 59-63 17483362-7 2007 This epistasis-type analysis suggests that the nelfinavir acts along the Akt pathway to radiosensitize cells. Nelfinavir 47-57 AKT serine/threonine kinase 1 Homo sapiens 73-76 17240460-6 2007 Analysis of gene and protein expression determined a selectively increase of the pro-inflammatory cytokines monocyte chemoattractant protein (MCP)-1 and interleukin-8 (IL-8) following exposure to a pharmacological concentration of NFV and RTV. Nelfinavir 231-234 C-C motif chemokine ligand 2 Homo sapiens 108-148 17240460-6 2007 Analysis of gene and protein expression determined a selectively increase of the pro-inflammatory cytokines monocyte chemoattractant protein (MCP)-1 and interleukin-8 (IL-8) following exposure to a pharmacological concentration of NFV and RTV. Nelfinavir 231-234 C-X-C motif chemokine ligand 8 Homo sapiens 153-166 17240460-6 2007 Analysis of gene and protein expression determined a selectively increase of the pro-inflammatory cytokines monocyte chemoattractant protein (MCP)-1 and interleukin-8 (IL-8) following exposure to a pharmacological concentration of NFV and RTV. Nelfinavir 231-234 C-X-C motif chemokine ligand 8 Homo sapiens 168-172 17460771-0 2007 The HIV protease inhibitor nelfinavir downregulates Akt phosphorylation by inhibiting proteasomal activity and inducing the unfolded protein response. Nelfinavir 27-37 AKT serine/threonine kinase 1 Homo sapiens 52-55 17460771-8 2007 Furthermore, our data indicate that nelfinavir decreases Akt phosphorylation by triggering this response. Nelfinavir 36-46 AKT serine/threonine kinase 1 Homo sapiens 57-60 17460771-9 2007 These findings may have important implications in understanding how nelfinavir may increase radiation sensitivity and also result in downregulation of the PI3K/Akt pathway. Nelfinavir 68-78 AKT serine/threonine kinase 1 Homo sapiens 160-163 17331030-4 2007 Runx-2 mRNA expression, calcium deposition, and alkaline phosphatase (ALP) activity decreased significantly in human osteoblast cultures after exposure to the PIs nelfinavir (NFV) and indinavir (IDV). Nelfinavir 163-173 RUNX family transcription factor 2 Homo sapiens 0-6 17331030-4 2007 Runx-2 mRNA expression, calcium deposition, and alkaline phosphatase (ALP) activity decreased significantly in human osteoblast cultures after exposure to the PIs nelfinavir (NFV) and indinavir (IDV). Nelfinavir 163-173 alkaline phosphatase, placental Homo sapiens 48-68 17331030-4 2007 Runx-2 mRNA expression, calcium deposition, and alkaline phosphatase (ALP) activity decreased significantly in human osteoblast cultures after exposure to the PIs nelfinavir (NFV) and indinavir (IDV). Nelfinavir 163-173 alkaline phosphatase, placental Homo sapiens 70-73 17283158-7 2007 We further show that nelfinavir inhibits CDK2 through proteasome-dependent degradation of Cdc25A phosphatase. Nelfinavir 21-31 cyclin dependent kinase 2 Homo sapiens 41-45 17283158-7 2007 We further show that nelfinavir inhibits CDK2 through proteasome-dependent degradation of Cdc25A phosphatase. Nelfinavir 21-31 cell division cycle 25A Homo sapiens 90-96 17202245-6 2007 RESULTS: According to the IC(50) estimation, the rank order for BCRP inhibition was lopinavir > nelfinavir > delavirdine > efavirenz > saquinavir > atazanavir > amprenavir > abacavir. Nelfinavir 99-109 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 64-68 17668557-10 2007 Lopinavir, nelfinavir, zidovudine and stavudine markedly increased ROS production and release of IL-1 beta and tumour necrosis factor-alpha. Nelfinavir 11-21 interleukin 1 beta Homo sapiens 97-139 17961046-10 2007 Moreover, an increase in the proapoptotic Bax/Bcl-2 protein ratio was demonstrated with the combination of imatinib and nelfinavir. Nelfinavir 120-130 BCL2 associated X, apoptosis regulator Homo sapiens 42-45 17961046-10 2007 Moreover, an increase in the proapoptotic Bax/Bcl-2 protein ratio was demonstrated with the combination of imatinib and nelfinavir. Nelfinavir 120-130 BCL2 apoptosis regulator Homo sapiens 46-51 17133272-0 2006 NFV, an HIV-1 protease inhibitor, induces growth arrest, reduced Akt signalling, apoptosis and docetaxel sensitisation in NSCLC cell lines. Nelfinavir 0-3 AKT serine/threonine kinase 1 Homo sapiens 65-68 17133272-1 2006 HIV-1 protease inhibitor (PI), nelfinavir (NFV) induced growth arrest and apoptosis of NCI-H460 and -H520, A549, EBC-1 and ABC-1 non-small-cell lung cancer (NSCLC) cells in association with upregulation of p21waf1, p27kip1 and p53, and downregulation of Bcl-2 and matrix metalloproteinase (MMP)-2 proteins. Nelfinavir 31-41 cyclin dependent kinase inhibitor 1B Homo sapiens 215-222 17133272-1 2006 HIV-1 protease inhibitor (PI), nelfinavir (NFV) induced growth arrest and apoptosis of NCI-H460 and -H520, A549, EBC-1 and ABC-1 non-small-cell lung cancer (NSCLC) cells in association with upregulation of p21waf1, p27kip1 and p53, and downregulation of Bcl-2 and matrix metalloproteinase (MMP)-2 proteins. Nelfinavir 31-41 tumor protein p53 Homo sapiens 227-230 17133272-1 2006 HIV-1 protease inhibitor (PI), nelfinavir (NFV) induced growth arrest and apoptosis of NCI-H460 and -H520, A549, EBC-1 and ABC-1 non-small-cell lung cancer (NSCLC) cells in association with upregulation of p21waf1, p27kip1 and p53, and downregulation of Bcl-2 and matrix metalloproteinase (MMP)-2 proteins. Nelfinavir 31-41 BCL2 apoptosis regulator Homo sapiens 254-259 17133272-1 2006 HIV-1 protease inhibitor (PI), nelfinavir (NFV) induced growth arrest and apoptosis of NCI-H460 and -H520, A549, EBC-1 and ABC-1 non-small-cell lung cancer (NSCLC) cells in association with upregulation of p21waf1, p27kip1 and p53, and downregulation of Bcl-2 and matrix metalloproteinase (MMP)-2 proteins. Nelfinavir 31-41 matrix metallopeptidase 2 Homo sapiens 264-296 17026490-0 2006 Effect of nelfinavir on insulin metabolism, proteasome activity and protein degradation in HepG2 cells. Nelfinavir 10-20 insulin Homo sapiens 24-31 17026490-4 2006 We examined whether the protease inhibitor nelfinavir inhibited IDE and its effect on protein degradation both in vitro and in whole cells. Nelfinavir 43-53 insulin degrading enzyme Homo sapiens 64-67 17026490-8 2006 Nelfinavir inhibited IDE in a concentration-dependent manner with 50% inhibition at the maximal concentration tested, 100 microm. Nelfinavir 0-10 insulin degrading enzyme Homo sapiens 21-24 17026490-10 2006 The ability of insulin to inhibit the proteasome was abrogated by nelfinavir. Nelfinavir 66-76 insulin Homo sapiens 15-22 17026490-13 2006 Addition of 50 microm nelfinavir inhibited cellular protein degradation by 14% and blunted the effect of insulin. Nelfinavir 22-32 insulin Homo sapiens 105-112 17026490-14 2006 These data show that nelfinavir inhibits IDE, decreases insulin"s ability to inhibit protein degradation via the proteasome and provides another possible mechanism for the insulin resistance seen in protease inhibitor-treated HIV patients. Nelfinavir 21-31 insulin degrading enzyme Homo sapiens 41-44 17026490-14 2006 These data show that nelfinavir inhibits IDE, decreases insulin"s ability to inhibit protein degradation via the proteasome and provides another possible mechanism for the insulin resistance seen in protease inhibitor-treated HIV patients. Nelfinavir 21-31 insulin Homo sapiens 56-63 17026490-14 2006 These data show that nelfinavir inhibits IDE, decreases insulin"s ability to inhibit protein degradation via the proteasome and provides another possible mechanism for the insulin resistance seen in protease inhibitor-treated HIV patients. Nelfinavir 21-31 insulin Homo sapiens 172-179 17132220-4 2006 We examined the effects of two human immunodeficiency virus protease inhibitors, nelfinavir and amprenavir, which inhibit Akt signaling, on VEGF and HIF-1alpha expression and on angiogenesis. Nelfinavir 81-91 vascular endothelial growth factor A Homo sapiens 140-144 17132220-6 2006 Downregulation of P-Akt decreased VEGF secretion in a manner similar to that of nelfinavir, but the combination of the two had no greater effect, consistent with the idea that nelfinavir decreases VEGF through the PI3K/Akt pathway. Nelfinavir 176-186 vascular endothelial growth factor A Homo sapiens 197-201 17132220-6 2006 Downregulation of P-Akt decreased VEGF secretion in a manner similar to that of nelfinavir, but the combination of the two had no greater effect, consistent with the idea that nelfinavir decreases VEGF through the PI3K/Akt pathway. Nelfinavir 176-186 AKT serine/threonine kinase 1 Homo sapiens 219-222 17132220-7 2006 Nelfinavir also decreased the hypoxic induction of VEGF and the hypoxic induction of HIF-1alpha, which regulates VEGF promoter. Nelfinavir 0-10 vascular endothelial growth factor A Homo sapiens 51-55 17132220-7 2006 Nelfinavir also decreased the hypoxic induction of VEGF and the hypoxic induction of HIF-1alpha, which regulates VEGF promoter. Nelfinavir 0-10 hypoxia inducible factor 1 subunit alpha Homo sapiens 85-95 17132220-7 2006 Nelfinavir also decreased the hypoxic induction of VEGF and the hypoxic induction of HIF-1alpha, which regulates VEGF promoter. Nelfinavir 0-10 vascular endothelial growth factor A Homo sapiens 113-117 17132220-8 2006 The effect of nelfinavir on HIF-1alpha was most likely mediated by decreased protein translation. Nelfinavir 14-24 hypoxia inducible factor 1 subunit alpha Homo sapiens 28-38 17047492-10 2006 Among 155 participants who received efavirenz without nelfinavir, virologic failure was associated with a two-locus interaction between ABCB1 2677G>T and CYP2B6 516G>T (65% accuracy, P<0.001). Nelfinavir 54-64 ATP binding cassette subfamily B member 1 Homo sapiens 136-141 16982770-0 2006 Nelfinavir down-regulates hypoxia-inducible factor 1alpha and VEGF expression and increases tumor oxygenation: implications for radiotherapy. Nelfinavir 0-10 hypoxia inducible factor 1, alpha subunit Mus musculus 26-57 16982770-0 2006 Nelfinavir down-regulates hypoxia-inducible factor 1alpha and VEGF expression and increases tumor oxygenation: implications for radiotherapy. Nelfinavir 0-10 vascular endothelial growth factor A Mus musculus 62-66 16982770-2 2006 We examined the effect of nelfinavir, an HIV protease inhibitor that inhibits Akt signaling, on VEGF and HIF-1alpha expression and on angiogenesis, tumor oxygenation, and radiosensitization. Nelfinavir 26-36 vascular endothelial growth factor A Mus musculus 96-100 16982770-3 2006 Nelfinavir decreases VEGF expression under normoxia via the transcription factor Sp1, which regulates the proximal core VEGF promoter. Nelfinavir 0-10 vascular endothelial growth factor A Mus musculus 21-25 16982770-3 2006 Nelfinavir decreases VEGF expression under normoxia via the transcription factor Sp1, which regulates the proximal core VEGF promoter. Nelfinavir 0-10 vascular endothelial growth factor A Mus musculus 120-124 16982770-4 2006 Nelfinavir decreased Sp1 phosphorylation and decreased Sp1 binding to a probe corresponding to the proximal VEGF promoter in a gel shift assay. Nelfinavir 0-10 vascular endothelial growth factor A Mus musculus 108-112 16982770-5 2006 Nelfinavir also decreased the hypoxic induction of HIF-1alpha, which also regulates the VEGF promoter, most likely by decreasing its translation. Nelfinavir 0-10 hypoxia inducible factor 1, alpha subunit Mus musculus 51-61 16982770-5 2006 Nelfinavir also decreased the hypoxic induction of HIF-1alpha, which also regulates the VEGF promoter, most likely by decreasing its translation. Nelfinavir 0-10 vascular endothelial growth factor A Mus musculus 88-92 16982770-6 2006 The effect of nelfinavir on VEGF expression had the functional consequence of decreasing angiogenesis in an in vivo Matrigel plug assay. Nelfinavir 14-24 vascular endothelial growth factor A Mus musculus 28-32 16940799-0 2006 Nelfinavir induces liposarcoma apoptosis and cell cycle arrest by upregulating sterol regulatory element binding protein-1. Nelfinavir 0-10 sterol regulatory element binding transcription factor 1 Homo sapiens 79-122 16940799-9 2006 Nelfinavir induced significant sterol regulatory element binding protein-1 expression in a dose-dependent and time-dependent fashion in sensitive SW872 and LiSa-2 cells, modestly in HT1080 cells, but not in nelfinavir-insensitive FU-DDLS-1 and 293 cells without inducing adipocytic differentiation. Nelfinavir 0-10 sterol regulatory element binding transcription factor 1 Homo sapiens 31-74 16940799-11 2006 Our data indicate that nelfinavir represents a novel class of antiliposarcoma agent that acts by selectively upregulating sterol regulatory element binding protein-1 expression in liposarcomas. Nelfinavir 23-33 sterol regulatory element binding transcription factor 1 Homo sapiens 122-165 16842404-0 2006 The effect of the CYP2C19*2 heterozygote genotype on the pharmacokinetics of nelfinavir. Nelfinavir 77-87 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 18-25 16487604-1 2006 We previously described a clinical human immunodeficiency virus type-1 (HIV-1) isolate, CL-4, which showed nelfinavir (NFV)-dependent enhancement of replication (Matsuoka-Aizawa, S., Sato, H., Hachiya, A., Tsuchiya, K., Takebe, Y., Gatanaga, H., Kimura, S., Oka, S, 2003. Nelfinavir 107-117 endogenous retrovirus group W member 3 Homo sapiens 88-92 16165208-9 2006 This MDR1 overexpression was observed in a similar extent in placentas from pregnant women treated with Zidovudine alone or in combination with Nelfinavir and/or Lamivudine. Nelfinavir 144-154 ATP binding cassette subfamily B member 1 Homo sapiens 5-9 16420257-1 2006 OBJECTIVES: To determine the characteristics of the binding of nelfinavir and active M8 to alpha1-acid glycoprotein (AAG) and human serum albumin (HSA), and to examine the displacement effects of drugs binding extensively to AAG (ritonavir and saquinavir) or to HSA (salicylic acid and valproic acid). Nelfinavir 63-73 albumin Homo sapiens 132-145 17302375-0 2006 Nelfinavir induces adipocyte insulin resistance through the induction of oxidative stress: differential protective effect of antioxidant agents. Nelfinavir 0-10 insulin Homo sapiens 29-36 17302375-2 2006 The HIV protease inhibitor nelfinavir (NFV) impairs insulin signal propagation by inducing similar signalling defects to those induced by exposure to oxidative stress. Nelfinavir 27-37 insulin Homo sapiens 52-59 16408618-6 2005 Compared to controls, gene expression analyses demonstrated an increased expression of glucuronyltransferase (UDPGT) and CYP450 3A1 in nelfinavir-treated rat hepatocytes and liver slices. Nelfinavir 135-145 UDP glucuronosyltransferase family 2 member B15 Rattus norvegicus 110-115 16267764-1 2005 BACKGROUND: Efavirenz and nelfinavir are metabolized by cytochrome P-450 (CYP) 2B6 and CYP2C19, respectively, with some involvement by CYP3A. Nelfinavir 26-36 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 56-82 16267764-1 2005 BACKGROUND: Efavirenz and nelfinavir are metabolized by cytochrome P-450 (CYP) 2B6 and CYP2C19, respectively, with some involvement by CYP3A. Nelfinavir 26-36 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 87-94 16267764-1 2005 BACKGROUND: Efavirenz and nelfinavir are metabolized by cytochrome P-450 (CYP) 2B6 and CYP2C19, respectively, with some involvement by CYP3A. Nelfinavir 26-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 135-140 16267764-2 2005 Nelfinavir is a substrate for P-glycoprotein, which is encoded by MDR1. Nelfinavir 0-10 ATP binding cassette subfamily B member 1 Homo sapiens 30-44 16267764-2 2005 Nelfinavir is a substrate for P-glycoprotein, which is encoded by MDR1. Nelfinavir 0-10 ATP binding cassette subfamily B member 1 Homo sapiens 66-70 16267764-9 2005 Plasma exposure to efavirenz and nelfinavir in each population was significantly associated with the polymorphisms CYP2B6 516G-->T and CYP2C19 681G-->A, respectively. Nelfinavir 33-43 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 115-121 16267764-9 2005 Plasma exposure to efavirenz and nelfinavir in each population was significantly associated with the polymorphisms CYP2B6 516G-->T and CYP2C19 681G-->A, respectively. Nelfinavir 33-43 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 138-145 16267764-11 2005 Among nelfinavir recipients, a trend toward decreased virologic failure was associated with the polymorphism CYP2C19 681G-->A. Nelfinavir 6-16 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 109-116 16163639-9 2005 The mean ALT level increased by 45 U/L at 24 weeks and 18 U/L at 48 weeks in the nelfinavir group but decreased by 18 U/L at 24 weeks and 7 U/L at 48 weeks in the lopinavir-ritonavir group. Nelfinavir 81-91 glutamic pyruvic transaminase, soluble Mus musculus 9-12 16163639-10 2005 Eight patients in the nelfinavir group and 2 patients in the lopinavir-ritonavir group had grade 3 or 4 flares in the ALT level. Nelfinavir 22-32 glutamic pyruvic transaminase, soluble Mus musculus 118-121 16163639-12 2005 A low baseline CD4+ cell count is associated with persistent increases in the HCV RNA load in nelfinavir-treated patients. Nelfinavir 94-104 CD4 molecule Homo sapiens 15-18 16225412-10 2005 The decreased protein synthesis induced by nelfinavir and zidovudine was associated with decreases in the phosphorylation of the S6 ribosomal protein (rpS6) and the repressor binding protein 4EBP1, while the inhibitory effect of nevirapine was mainly associated with a decline in phosphorylated 4EBP1. Nelfinavir 43-53 ribosomal protein S6 Homo sapiens 151-155 16225412-10 2005 The decreased protein synthesis induced by nelfinavir and zidovudine was associated with decreases in the phosphorylation of the S6 ribosomal protein (rpS6) and the repressor binding protein 4EBP1, while the inhibitory effect of nevirapine was mainly associated with a decline in phosphorylated 4EBP1. Nelfinavir 43-53 eukaryotic translation initiation factor 4E binding protein 1 Homo sapiens 191-196 16225412-10 2005 The decreased protein synthesis induced by nelfinavir and zidovudine was associated with decreases in the phosphorylation of the S6 ribosomal protein (rpS6) and the repressor binding protein 4EBP1, while the inhibitory effect of nevirapine was mainly associated with a decline in phosphorylated 4EBP1. Nelfinavir 43-53 eukaryotic translation initiation factor 4E binding protein 1 Homo sapiens 295-300 16166302-4 2005 Five first-generation HPIs were subsequently tested and three of the five (amprenavir, nelfinavir, and saquinavir but not ritonavir or indinavir) inhibited Akt phosphorylation at Ser473 at serum concentrations routinely achieved in HIV patients. Nelfinavir 87-97 AKT serine/threonine kinase 1 Homo sapiens 156-159 16166302-6 2005 In addition, in vivo, doses of amprenavir or nelfinavir comparable with the therapeutic levels achieved in HIV patients were sufficient to down-regulate phosphorylation of Akt in SQ20B and T24 xenografts. Nelfinavir 45-55 AKT serine/threonine kinase 1 Homo sapiens 172-175 15977242-0 2005 Diverse pattern of protease inhibitor resistance mutations in HIV-1 infected patients failing nelfinavir. Nelfinavir 94-104 serpin family A member 13, pseudogene Homo sapiens 19-37 15977242-1 2005 The aim of the study was to describe the pattern of resistance mutations in human immunodeficiency virus type 1 (HIV-1) infected patients experiencing their first protease inhibitor (PI) failure on nelfinavir (NFV)-containing therapy. Nelfinavir 198-208 serpin family A member 13, pseudogene Homo sapiens 163-181 15977242-1 2005 The aim of the study was to describe the pattern of resistance mutations in human immunodeficiency virus type 1 (HIV-1) infected patients experiencing their first protease inhibitor (PI) failure on nelfinavir (NFV)-containing therapy. Nelfinavir 210-213 serpin family A member 13, pseudogene Homo sapiens 163-181 16078135-4 2005 RESULTS: For R123 (P-gp probe), the rank order potency for inhibiting R123 accumulation in the BBMEC was saquinavir=nelfinavir>ritonavir=amprenavir>indinavir. Nelfinavir 116-126 phosphoglycolate phosphatase Homo sapiens 19-23 16078135-6 2005 The rank order potency for MRP-related drug efflux transporters, was nelfinavir>ritonavir>saquinavir>amprenavir>indinavir. Nelfinavir 69-79 ATP binding cassette subfamily C member 1 Homo sapiens 27-30 16170225-5 2005 CYP2C19 polymorphisms predict nelfinavir plasma levels and, possibly, risk of virologic failure on this drug. Nelfinavir 30-40 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 0-7 15858856-0 2005 The impact of pharmacologic and genetic knockout of P-glycoprotein on nelfinavir levels in the brain and other tissues in mice. Nelfinavir 70-80 phosphoglycolate phosphatase Mus musculus 52-66 15858856-2 2005 The efflux transporter mdr1 product P-glycoprotein (P-gp) has been demonstrated to play a role in limiting nelfinavir brain levels. Nelfinavir 107-117 ATP-binding cassette, sub-family B (MDR/TAP), member 1B Mus musculus 23-27 15858856-2 2005 The efflux transporter mdr1 product P-glycoprotein (P-gp) has been demonstrated to play a role in limiting nelfinavir brain levels. Nelfinavir 107-117 phosphoglycolate phosphatase Mus musculus 36-50 15858856-2 2005 The efflux transporter mdr1 product P-glycoprotein (P-gp) has been demonstrated to play a role in limiting nelfinavir brain levels. Nelfinavir 107-117 phosphoglycolate phosphatase Mus musculus 52-56 15858856-4 2005 Intravenous administration with the P-gp inhibitor GF120918 to mdr1a/1b (+/+) mice increased nelfinavir concentrations over a range of 2.3- to 27-fold, whereas nelfinavir distribution in mdr1a/1b (-/-) mice was 2- to 16-fold higher than that in their wild counterparts. Nelfinavir 93-103 phosphoglycolate phosphatase Mus musculus 36-40 15858856-4 2005 Intravenous administration with the P-gp inhibitor GF120918 to mdr1a/1b (+/+) mice increased nelfinavir concentrations over a range of 2.3- to 27-fold, whereas nelfinavir distribution in mdr1a/1b (-/-) mice was 2- to 16-fold higher than that in their wild counterparts. Nelfinavir 160-170 phosphoglycolate phosphatase Mus musculus 36-40 15858856-4 2005 Intravenous administration with the P-gp inhibitor GF120918 to mdr1a/1b (+/+) mice increased nelfinavir concentrations over a range of 2.3- to 27-fold, whereas nelfinavir distribution in mdr1a/1b (-/-) mice was 2- to 16-fold higher than that in their wild counterparts. Nelfinavir 160-170 ATP-binding cassette, sub-family B (MDR/TAP), member 1A Mus musculus 187-192 15858856-6 2005 In contrast, mdr1a/1b knockout mice exhibited higher nelfinavir levels in the brain (16.1-fold vs. 8.9-fold increase) and spleen (4.1-fold vs. 2.3-fold increase) compared to pharmacological inhibition with GF120918 in wild mice. Nelfinavir 53-63 ATP-binding cassette, sub-family B (MDR/TAP), member 1A Mus musculus 13-18 15858856-8 2005 Our results suggest mdr1a/1b-independant mechanisms may also contribute to nelfinavir tissue distribution in mice. Nelfinavir 75-85 ATP-binding cassette, sub-family B (MDR/TAP), member 1A Mus musculus 20-25 15793156-0 2005 Role of P-glycoprotein in distribution of nelfinavir across the blood-mammary tissue barrier and blood-brain barrier. Nelfinavir 42-52 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 8-22 15750390-0 2005 An MDR1-3435 variant is associated with higher plasma nelfinavir levels and more rapid virologic response in HIV-1 infected children. Nelfinavir 54-64 ATP binding cassette subfamily B member 1 Homo sapiens 3-7 15750390-2 2005 This research examined the impact of single nucleotide polymorphisms (SNP) of MDR1 and CYP genes on nelfinavir and efavirenz pharmacokinetics and the response to highly active antiretroviral therapy (HAART) in HIV-1 infected children. Nelfinavir 100-110 ATP binding cassette subfamily B member 1 Homo sapiens 78-82 15750390-2 2005 This research examined the impact of single nucleotide polymorphisms (SNP) of MDR1 and CYP genes on nelfinavir and efavirenz pharmacokinetics and the response to highly active antiretroviral therapy (HAART) in HIV-1 infected children. Nelfinavir 100-110 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 87-90 15750390-10 2005 CONCLUSIONS: HIV-1 infected children with the MDR1-3435-C/T genotype had more rapid virologic responses to HAART at week 8 with higher plasma nelfinavir concentrations compared to those with the C/C genotype. Nelfinavir 142-152 ATP binding cassette subfamily B member 1 Homo sapiens 46-50 15750390-11 2005 These findings suggest that P-gp may play an important role in the pharmacokinetics and virologic response to HAART containing nelfinavir. Nelfinavir 127-137 ATP binding cassette subfamily B member 1 Homo sapiens 28-32 15721475-5 2005 Drug-induced QT prolongation is usually caused by block of human ether-a-go-go-related gene (HERG) potassium channels, and we showed that lopinavir, nelfinavir, ritonavir, and saquinavir caused dose-dependent block of HERG channels heterologously expressed in HEK293 cells in vitro. Nelfinavir 149-159 potassium voltage-gated channel subfamily H member 2 Homo sapiens 93-97 15721475-5 2005 Drug-induced QT prolongation is usually caused by block of human ether-a-go-go-related gene (HERG) potassium channels, and we showed that lopinavir, nelfinavir, ritonavir, and saquinavir caused dose-dependent block of HERG channels heterologously expressed in HEK293 cells in vitro. Nelfinavir 149-159 potassium voltage-gated channel subfamily H member 2 Homo sapiens 218-222 15629151-0 2005 C/EBPalpha reverses the anti-adipogenic effects of the HIV protease inhibitor nelfinavir. Nelfinavir 78-88 CCAAT enhancer binding protein alpha Homo sapiens 0-10 15629151-4 2005 Forced expression of the adipogenic transcription factor C/EBPalpha rescues some of the anti-adipogenic effects of nelfinavir. Nelfinavir 115-125 CCAAT enhancer binding protein alpha Homo sapiens 57-67 15629151-5 2005 These results suggest that nelfinavir may mediate an anti-adipogenic effect by antagonizing expression of C/EBPalpha. Nelfinavir 27-37 CCAAT enhancer binding protein alpha Homo sapiens 106-116 15657782-7 2005 CYP3A activity was lower in the efavirenz + ritonavir group (P = 0.01) and in the ritonavir group (P = 0.04) than in the nelfinavir group, although already strongly inhibited in the latter. Nelfinavir 121-131 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-5 15657782-10 2005 Nelfinavir strongly decreases CYP3A activity, but to a lesser extent than ritonavir. Nelfinavir 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-35 15657782-11 2005 The inhibition of CYP3A by ritonavir or nelfinavir offsets the inductive effects of efavirenz or nevirapine administered concomitantly. Nelfinavir 40-50 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 18-23 15523003-6 2005 For CYP3A5, nelfinavir exhibited the highest k(inact) (0.47 min(-1)), but ritonavir was the most potent (K(I) = 0.12 microM). Nelfinavir 12-22 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 4-10 15654921-3 2005 Acute inhibition of GLUT4-mediated glucose transport, and defective insulin signalling induced by chronic exposure to nelfinavir, are described as cellular mechanisms of insulin resistance. Nelfinavir 118-128 insulin Homo sapiens 68-75 15654921-3 2005 Acute inhibition of GLUT4-mediated glucose transport, and defective insulin signalling induced by chronic exposure to nelfinavir, are described as cellular mechanisms of insulin resistance. Nelfinavir 118-128 insulin Homo sapiens 170-177 15865214-6 2005 RESULTS: Nelfinavir, ritonavir and saquinavir inhibited adipogenesis and up-regulated the expression of TNF-alpha and IL-6, but this effect was not seen with indinavir, zidovudine and stavudine. Nelfinavir 9-19 tumor necrosis factor Mus musculus 104-113 15865214-6 2005 RESULTS: Nelfinavir, ritonavir and saquinavir inhibited adipogenesis and up-regulated the expression of TNF-alpha and IL-6, but this effect was not seen with indinavir, zidovudine and stavudine. Nelfinavir 9-19 interleukin 6 Mus musculus 118-122 15865214-9 2005 CONCLUSIONS: Our data suggest that the PIs nelfinavir, ritonavir and saquinavir have potent effects in inhibiting adipocyte differentiation whilst up-regulating TNF-alpha and IL-6 mRNA levels and decreasing adiponectin levels. Nelfinavir 43-53 tumor necrosis factor Mus musculus 161-170 15865214-9 2005 CONCLUSIONS: Our data suggest that the PIs nelfinavir, ritonavir and saquinavir have potent effects in inhibiting adipocyte differentiation whilst up-regulating TNF-alpha and IL-6 mRNA levels and decreasing adiponectin levels. Nelfinavir 43-53 interleukin 6 Mus musculus 175-179 15865214-9 2005 CONCLUSIONS: Our data suggest that the PIs nelfinavir, ritonavir and saquinavir have potent effects in inhibiting adipocyte differentiation whilst up-regulating TNF-alpha and IL-6 mRNA levels and decreasing adiponectin levels. Nelfinavir 43-53 adiponectin, C1Q and collagen domain containing Mus musculus 207-218 15865230-10 2005 The GMR of the nelfinavir AUC0-12 values was 0.97 (95% CI: 0.80-1.17). Nelfinavir 15-25 colony stimulating factor 2 receptor subunit alpha Homo sapiens 4-7 15651752-0 2004 Influence of single-nucleotide polymorphisms in the multidrug resistance-1 gene on the cellular export of nelfinavir and its clinical implication for highly active antiretroviral therapy. Nelfinavir 106-116 ATP binding cassette subfamily B member 1 Homo sapiens 52-74 15563361-14 2004 The relative bioavailability, expressed as a geometric mean ratio (90% confidence interval) for nelfinavir AUC(0-24 h), C(max) and C(24) of period 2 compared with period 1 was: 1.30 (1.21, 1.40), 1.29 (1.19, 1.40) and 1.48 (1.32, 1.66). Nelfinavir 96-106 period circadian regulator 2 Homo sapiens 140-148 15563361-15 2004 The sum of nelfinavir and M8 C(24) in period 2 was 0.99 mg l(-1), an increase of 19%. Nelfinavir 11-21 period circadian regulator 2 Homo sapiens 38-46 15448116-0 2004 Conversion of the HIV protease inhibitor nelfinavir to a bioactive metabolite by human liver CYP2C19. Nelfinavir 41-51 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 93-100 15448116-6 2004 In reconstituted systems, CYP2C19 catalyzed nelfinavir t-butylamide hydroxylation at a turnover rate of 2.2 min(-1), whereas CYP2C9, CYP2C8, and CYP3A4 were inactive toward nelfinavir. Nelfinavir 44-54 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 26-33 15448116-8 2004 Similarly, the CYP2C19 substrate omeprazole strongly inhibited (75%) hepatic nelfinavir t-butylamide hydroxylation at a concentration of only 12.5 microM. Nelfinavir 77-87 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 15-22 15448116-9 2004 Our study shows that CYP2C19 underlies formation in human liver of M8, a bioactive nelfinavir metabolite. Nelfinavir 83-93 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 21-28 15448116-10 2004 The inducibility of CYP2C19 by agents (e.g., rifampicin) often taken concurrently with nelfinavir, together with this P450"s known polymorphic nature, may thus be important determinants of nelfinavir"s antiviral potency. Nelfinavir 87-97 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 20-27 15448116-10 2004 The inducibility of CYP2C19 by agents (e.g., rifampicin) often taken concurrently with nelfinavir, together with this P450"s known polymorphic nature, may thus be important determinants of nelfinavir"s antiviral potency. Nelfinavir 189-199 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 20-27 15590971-6 2004 The impaired insulin secretion by ritonavir, nelfinavir and saquinavir was associated with decreased insulin-stimulated IRS-2 phosphorylation, and, for nelfinavir and saquinavir, with decreased insulin-stimulated IRS-1 and Thr308-Akt phosphorylation. Nelfinavir 45-55 insulin Homo sapiens 13-20 15590971-6 2004 The impaired insulin secretion by ritonavir, nelfinavir and saquinavir was associated with decreased insulin-stimulated IRS-2 phosphorylation, and, for nelfinavir and saquinavir, with decreased insulin-stimulated IRS-1 and Thr308-Akt phosphorylation. Nelfinavir 45-55 insulin receptor substrate 2 Homo sapiens 120-125 15590971-6 2004 The impaired insulin secretion by ritonavir, nelfinavir and saquinavir was associated with decreased insulin-stimulated IRS-2 phosphorylation, and, for nelfinavir and saquinavir, with decreased insulin-stimulated IRS-1 and Thr308-Akt phosphorylation. Nelfinavir 45-55 insulin Homo sapiens 101-108 15590971-6 2004 The impaired insulin secretion by ritonavir, nelfinavir and saquinavir was associated with decreased insulin-stimulated IRS-2 phosphorylation, and, for nelfinavir and saquinavir, with decreased insulin-stimulated IRS-1 and Thr308-Akt phosphorylation. Nelfinavir 152-162 insulin Homo sapiens 13-20 15590971-8 2004 In conclusion, certain HIV-1 protease inhibitors, such as ritonavir, nelfinavir and saquinavir, not only induce peripheral insulin resistance, but also impair glucose-stimulated insulin secretion from beta cells. Nelfinavir 69-79 insulin Homo sapiens 123-130 15590971-8 2004 In conclusion, certain HIV-1 protease inhibitors, such as ritonavir, nelfinavir and saquinavir, not only induce peripheral insulin resistance, but also impair glucose-stimulated insulin secretion from beta cells. Nelfinavir 69-79 insulin Homo sapiens 178-185 15007102-5 2004 We found that ritonavir, saquinavir, and nelfinavir were effective inhibitors of wild-type BCRP (482R) with IC50 values of 19.5 +/- 0.8 microM, 19.5 +/- 7.6 microM, and 12.5 +/- 4.1 microM, respectively. Nelfinavir 41-51 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 91-95 15269981-0 2004 [Impairment of IRS-2 signaling in rat insulinoma INS-1 cells by nelfinavir]. Nelfinavir 64-74 insulin receptor substrate 2 Rattus norvegicus 15-20 15269981-5 2004 RESULT: Nelfinavir decreased insulin stimulated phosphorylation of IRS-2 and Akt-Thr(308) in a dose-dependent manner; for 10 micromol/L of nelfinavir, the decrease was 52% and 55%, respectively. Nelfinavir 8-18 insulin receptor substrate 2 Rattus norvegicus 67-72 15269981-5 2004 RESULT: Nelfinavir decreased insulin stimulated phosphorylation of IRS-2 and Akt-Thr(308) in a dose-dependent manner; for 10 micromol/L of nelfinavir, the decrease was 52% and 55%, respectively. Nelfinavir 8-18 AKT serine/threonine kinase 1 Rattus norvegicus 77-80 15269981-5 2004 RESULT: Nelfinavir decreased insulin stimulated phosphorylation of IRS-2 and Akt-Thr(308) in a dose-dependent manner; for 10 micromol/L of nelfinavir, the decrease was 52% and 55%, respectively. Nelfinavir 139-149 insulin receptor substrate 2 Rattus norvegicus 67-72 15269981-5 2004 RESULT: Nelfinavir decreased insulin stimulated phosphorylation of IRS-2 and Akt-Thr(308) in a dose-dependent manner; for 10 micromol/L of nelfinavir, the decrease was 52% and 55%, respectively. Nelfinavir 139-149 AKT serine/threonine kinase 1 Rattus norvegicus 77-80 15269981-6 2004 CONCLUSION: Treatment with nelfinavir might impair IRS-2-mediated signaling in pancreatic beta cells. Nelfinavir 27-37 insulin receptor substrate 2 Rattus norvegicus 51-56 15168016-0 2004 Nelfinavir-induced insulin resistance is associated with impaired plasma membrane recruitment of the PI 3-kinase effectors Akt/PKB and PKC-zeta. Nelfinavir 0-10 insulin Homo sapiens 19-26 15168016-0 2004 Nelfinavir-induced insulin resistance is associated with impaired plasma membrane recruitment of the PI 3-kinase effectors Akt/PKB and PKC-zeta. Nelfinavir 0-10 AKT serine/threonine kinase 1 Homo sapiens 123-130 15168016-0 2004 Nelfinavir-induced insulin resistance is associated with impaired plasma membrane recruitment of the PI 3-kinase effectors Akt/PKB and PKC-zeta. Nelfinavir 0-10 protein kinase C zeta Homo sapiens 135-143 15168016-1 2004 AIMS/HYPOTHESIS: Chronic exposure of 3T3-L1 adipocytes to the HIV protease inhibitor nelfinavir induces insulin resistance, recapitulating key metabolic alterations of adipose tissue in the lipodystrophy syndrome induced by these agents. Nelfinavir 85-95 insulin Homo sapiens 104-111 15168016-2 2004 Our goal was to identify the defect in the insulin signal transduction cascade leading to nelfinavir-induced insulin resistance. Nelfinavir 90-100 insulin Homo sapiens 43-50 15168016-2 2004 Our goal was to identify the defect in the insulin signal transduction cascade leading to nelfinavir-induced insulin resistance. Nelfinavir 90-100 insulin Homo sapiens 109-116 15168016-3 2004 METHODS: Fully differentiated 3T3-L1 adipocytes were exposed to 30 micro mol/l nelfinavir for 18 h, after which the amount, the phosphorylation and the localisation of key proteins in the insulin signalling cascade were evaluated. Nelfinavir 79-89 insulin Homo sapiens 188-195 15168016-4 2004 RESULTS: Insulin-induced interaction of phosphatidylinositol 3"-kinase (PI 3-kinase) with IRS proteins was normal in cells treated with nelfinavir, as was IRS-1-associated PI 3-kinase activity. Nelfinavir 136-146 insulin Homo sapiens 9-16 15168016-4 2004 RESULTS: Insulin-induced interaction of phosphatidylinositol 3"-kinase (PI 3-kinase) with IRS proteins was normal in cells treated with nelfinavir, as was IRS-1-associated PI 3-kinase activity. Nelfinavir 136-146 isoleucyl-tRNA synthetase 1 Homo sapiens 90-93 15168016-8 2004 CONCLUSIONS/INTERPRETATION: We therefore conclude that nelfinavir induces a defect in the insulin signalling cascade downstream of the activation of PI 3-kinase. Nelfinavir 55-65 insulin Homo sapiens 90-97 15060514-0 2004 Nelfinavir and felodipine: a cytochrome P450 3A4-mediated drug interaction. Nelfinavir 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 29-48 15078991-2 2004 In this study, we found that protease inhibitors, including ritonavir, saquinavir, and nelfinavir, but not indinavir, induced growth arrest and apoptosis of U266, RPMI8226, and ARH77 human multiple myeloma (MM) cells in association with down-regulation of antiapoptotic protein Mcl-1. Nelfinavir 87-97 low density lipoprotein receptor adaptor protein 1 Homo sapiens 177-180 15078991-2 2004 In this study, we found that protease inhibitors, including ritonavir, saquinavir, and nelfinavir, but not indinavir, induced growth arrest and apoptosis of U266, RPMI8226, and ARH77 human multiple myeloma (MM) cells in association with down-regulation of antiapoptotic protein Mcl-1. Nelfinavir 87-97 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 278-283 15040543-0 2004 Intracellular accumulation of nelfinavir and its relationship to P-glycoprotein expression and function in HIV-infected patients. Nelfinavir 30-40 ATP binding cassette subfamily B member 1 Homo sapiens 65-79 15040543-1 2004 OBJECTIVE: To compare plasma and intracellular nelfinavir pharmacokinetics, and determine their relationship to P-glycoprotein (P-gp) expression and function in lymphocytes of HIV-infected patients. Nelfinavir 47-57 ATP binding cassette subfamily B member 1 Homo sapiens 128-132 15040543-10 2004 In patients chronically treated with nelfinavir mean P-gp expression was 8.85 +/- 1.3 MFI, there was no correlation between P-gp expression and either intracellular AUC(0-12) (r=-0.35; P=0.29) or intracellular C0 values. Nelfinavir 37-47 ATP binding cassette subfamily B member 1 Homo sapiens 53-57 15040543-11 2004 There was a correlation between intracellular nelfinavir concentrations and P-gp function at baseline (r=0.59; P<0.05). Nelfinavir 46-56 ATP binding cassette subfamily B member 1 Homo sapiens 76-80 15040543-15 2004 CONCLUSIONS: Nelfinavir undergoes significant intracellular accumulation within the PBMCs of HIV-infected patients, which may be in part related to its moderate ability to inhibit P-gp-mediated drug efflux. Nelfinavir 13-23 ATP binding cassette subfamily B member 1 Homo sapiens 180-184 15040543-17 2004 Intracellular accumulation of nelfinavir correlated with P-gp function but not P-gp expression, suggesting pump activity is substrate concentration-dependant. Nelfinavir 30-40 ATP binding cassette subfamily B member 1 Homo sapiens 57-61 14592951-4 2004 The steady-state mRNA levels of the adiponectin gene and secretion of this protein from 3T3-L1 adipocytes are significantly decreased after treatment with several PIs (indinavir, nelfinavir, and ritonavir), with ritonavir having the greatest effect. Nelfinavir 179-189 adiponectin, C1Q and collagen domain containing Mus musculus 36-47 15002082-1 2004 PURPOSE: To compare the long-term clinical efficacy and toxicity of initial strategies of nelfinavir (NFV) or ritonavir (RTV) in patients with CD4+ cells below 200/mm3. Nelfinavir 90-100 CD4 molecule Homo sapiens 143-146 15002082-1 2004 PURPOSE: To compare the long-term clinical efficacy and toxicity of initial strategies of nelfinavir (NFV) or ritonavir (RTV) in patients with CD4+ cells below 200/mm3. Nelfinavir 102-105 CD4 molecule Homo sapiens 143-146 12837856-5 2003 In this present study we investigated the effect of several HIV protease inhibitors (ABT-378, Amprenavir, Indinavir, Nelfinavir, Ritonavir, and Saquinavir) on mRNA, protein, and functional levels of LDLR family members. Nelfinavir 117-127 low density lipoprotein receptor Homo sapiens 199-203 12837856-6 2003 Our results demonstrate that one of these drugs, Nelfinavir, significantly decreases LDLR and LDLR-related protein (LRP) mRNA and protein levels, resulting in the reduced functional activity of these two receptors. Nelfinavir 49-59 low density lipoprotein receptor Homo sapiens 85-89 12837856-6 2003 Our results demonstrate that one of these drugs, Nelfinavir, significantly decreases LDLR and LDLR-related protein (LRP) mRNA and protein levels, resulting in the reduced functional activity of these two receptors. Nelfinavir 49-59 LDL receptor related protein 1 Homo sapiens 94-114 12837856-6 2003 Our results demonstrate that one of these drugs, Nelfinavir, significantly decreases LDLR and LDLR-related protein (LRP) mRNA and protein levels, resulting in the reduced functional activity of these two receptors. Nelfinavir 49-59 LDL receptor related protein 1 Homo sapiens 116-119 12837856-7 2003 Nelfinavir exerts its effect by reducing levels of active SREBP1 in the nucleus. Nelfinavir 0-10 sterol regulatory element binding transcription factor 1 Homo sapiens 58-64 12837856-8 2003 The finding that Nelfinavir reduces the levels of two key receptors (LRP and LDLR) involved in lipoprotein catabolism and maintenance of vessel wall integrity identifies a mechanism that causes hypercholesterolemia complications in HIV patients treated with this drug and raises concerns about the atherogenic nature of Nelfinavir. Nelfinavir 17-27 LDL receptor related protein 1 Homo sapiens 69-72 12837856-8 2003 The finding that Nelfinavir reduces the levels of two key receptors (LRP and LDLR) involved in lipoprotein catabolism and maintenance of vessel wall integrity identifies a mechanism that causes hypercholesterolemia complications in HIV patients treated with this drug and raises concerns about the atherogenic nature of Nelfinavir. Nelfinavir 17-27 low density lipoprotein receptor Homo sapiens 77-81 12837856-8 2003 The finding that Nelfinavir reduces the levels of two key receptors (LRP and LDLR) involved in lipoprotein catabolism and maintenance of vessel wall integrity identifies a mechanism that causes hypercholesterolemia complications in HIV patients treated with this drug and raises concerns about the atherogenic nature of Nelfinavir. Nelfinavir 320-330 LDL receptor related protein 1 Homo sapiens 69-72 12837856-8 2003 The finding that Nelfinavir reduces the levels of two key receptors (LRP and LDLR) involved in lipoprotein catabolism and maintenance of vessel wall integrity identifies a mechanism that causes hypercholesterolemia complications in HIV patients treated with this drug and raises concerns about the atherogenic nature of Nelfinavir. Nelfinavir 320-330 low density lipoprotein receptor Homo sapiens 77-81 12917239-7 2003 Nelfinavir, however, increased P-gp expression. Nelfinavir 0-10 ATP binding cassette subfamily B member 1 Homo sapiens 31-35 12917239-9 2003 CONCLUSION: This study suggests that, of the PIs, only nelfinavir increases P-gp expression in vitro, and in vivo the PI class of antiretrovirals do not increase P-gp expression on lymphocytes. Nelfinavir 55-65 ATP binding cassette subfamily B member 1 Homo sapiens 76-80 12949316-11 2003 NFV dosed at 55 mg/kg BID in children who are <30 kg provides comparable exposure to that measured in children who are >25 kg and receiving NFV 30 mg/kg TID. Nelfinavir 0-3 BH3 interacting domain death agonist Homo sapiens 22-25 12902797-6 2003 Significant increases in median P-gp expression were observed following incubation with 10 microM nelfinavir (10.2 versus 6.7% P-gp-positive cells) and efavirenz (10.0 versus 6.7% P-gp-positive cells). Nelfinavir 98-108 ATP binding cassette subfamily B member 1 Homo sapiens 32-36 12902797-6 2003 Significant increases in median P-gp expression were observed following incubation with 10 microM nelfinavir (10.2 versus 6.7% P-gp-positive cells) and efavirenz (10.0 versus 6.7% P-gp-positive cells). Nelfinavir 98-108 ATP binding cassette subfamily B member 1 Homo sapiens 127-131 12902797-6 2003 Significant increases in median P-gp expression were observed following incubation with 10 microM nelfinavir (10.2 versus 6.7% P-gp-positive cells) and efavirenz (10.0 versus 6.7% P-gp-positive cells). Nelfinavir 98-108 ATP binding cassette subfamily B member 1 Homo sapiens 127-131 12902797-9 2003 However, nelfinavir, ritonavir, and lopinavir caused marked toxicity, indicating that at higher concentrations, the increase in P-gp may be at least partially related to a stress response. Nelfinavir 9-19 ATP binding cassette subfamily B member 1 Homo sapiens 128-132 12705974-2 2003 Therefore, a highly specific method is presented, which is capable of quantifying the different proteinase inhibitors (amprenavir, indinavir, lopinavir, nelfinavir, ritonavir, saquinavir) and non-nucleoside reverse transcriptase inhibitors (efavirenz, nelfinavir). Nelfinavir 252-262 endogenous retrovirus group K member 25 Homo sapiens 96-106 12689411-0 2003 Greater reversal of CD4+ cell abnormalities and viral load reduction after initiation of antiretroviral therapy with zidovudine, lamivudine, and nelfinavir before complete HIV type 1 seroconversion. Nelfinavir 145-155 CD4 molecule Homo sapiens 20-23 12478066-3 2003 RESULTS: Prolonged exposure of 3T3-L1 adipocytes to nelfinavir, but not to indinavir or saquinavir, resulted in increased basal lipolysis but decreased insulin-stimulated glucose transport and PKB phosphorylation. Nelfinavir 52-62 insulin Homo sapiens 152-159 12478066-6 2003 In contrast to these unique effects of nelfinavir, the mere presence of any of the agents in the 5 min transport assay inhibited insulin-stimulated glucose-uptake activity. Nelfinavir 39-49 insulin Homo sapiens 129-136 12478066-8 2003 CONCLUSIONS: Independent mechanisms for HPI-induced insulin resistance exist: prolonged exposure to nelfinavir interferes with insulin signaling and alters cellular metabolism of adipocytes and muscle cells, whereas a direct inhibitory effect on insulin-stimulated glucose uptake may occurs through specific interaction of HPI with GLUT4. Nelfinavir 100-110 insulin Homo sapiens 52-59 12478066-8 2003 CONCLUSIONS: Independent mechanisms for HPI-induced insulin resistance exist: prolonged exposure to nelfinavir interferes with insulin signaling and alters cellular metabolism of adipocytes and muscle cells, whereas a direct inhibitory effect on insulin-stimulated glucose uptake may occurs through specific interaction of HPI with GLUT4. Nelfinavir 100-110 insulin Homo sapiens 127-134 12478066-8 2003 CONCLUSIONS: Independent mechanisms for HPI-induced insulin resistance exist: prolonged exposure to nelfinavir interferes with insulin signaling and alters cellular metabolism of adipocytes and muscle cells, whereas a direct inhibitory effect on insulin-stimulated glucose uptake may occurs through specific interaction of HPI with GLUT4. Nelfinavir 100-110 solute carrier family 2 member 4 Homo sapiens 332-337 12545146-3 2003 The 50% P-glycoprotein inhibitory concentrations of purified nelfinavir and M8 were 10.9 micromol/L and 29.5 micromol/L, respectively, for CD4(+) T cells and 19.3 micromol/L and >48 micromol/L, respectively, for CD8(+) T cells. Nelfinavir 61-71 CD4 molecule Homo sapiens 139-142 12545146-3 2003 The 50% P-glycoprotein inhibitory concentrations of purified nelfinavir and M8 were 10.9 micromol/L and 29.5 micromol/L, respectively, for CD4(+) T cells and 19.3 micromol/L and >48 micromol/L, respectively, for CD8(+) T cells. Nelfinavir 61-71 CD8a molecule Homo sapiens 215-218 12545146-5 2003 Plasma nelfinavir concentrations correlated with percent inhibition on CD4(+) (rho = 0.85, P <.0001) and CD8(+) (rho = 0.83, P <.0001) T cells. Nelfinavir 7-17 CD4 molecule Homo sapiens 71-74 12545146-5 2003 Plasma nelfinavir concentrations correlated with percent inhibition on CD4(+) (rho = 0.85, P <.0001) and CD8(+) (rho = 0.83, P <.0001) T cells. Nelfinavir 7-17 CD8a molecule Homo sapiens 108-111 12545146-7 2003 On the basis of our findings in lymphocytes from a healthy volunteer exposed to plasma from human immunodeficiency virus-positive patients, we believe it is likely that CD4(+) and CD8(+) lymphocytes in patients receiving nelfinavir as therapy for human immunodeficiency virus may have P-glycoprotein inhibited by plasma concentrations of nelfinavir. Nelfinavir 221-231 CD4 molecule Homo sapiens 169-172 12545146-7 2003 On the basis of our findings in lymphocytes from a healthy volunteer exposed to plasma from human immunodeficiency virus-positive patients, we believe it is likely that CD4(+) and CD8(+) lymphocytes in patients receiving nelfinavir as therapy for human immunodeficiency virus may have P-glycoprotein inhibited by plasma concentrations of nelfinavir. Nelfinavir 221-231 CD8a molecule Homo sapiens 180-183 12545146-7 2003 On the basis of our findings in lymphocytes from a healthy volunteer exposed to plasma from human immunodeficiency virus-positive patients, we believe it is likely that CD4(+) and CD8(+) lymphocytes in patients receiving nelfinavir as therapy for human immunodeficiency virus may have P-glycoprotein inhibited by plasma concentrations of nelfinavir. Nelfinavir 338-348 CD4 molecule Homo sapiens 169-172 12545146-7 2003 On the basis of our findings in lymphocytes from a healthy volunteer exposed to plasma from human immunodeficiency virus-positive patients, we believe it is likely that CD4(+) and CD8(+) lymphocytes in patients receiving nelfinavir as therapy for human immunodeficiency virus may have P-glycoprotein inhibited by plasma concentrations of nelfinavir. Nelfinavir 338-348 CD8a molecule Homo sapiens 180-183 12949438-6 2003 Serious cases by coadministration of CYP3A inhibitors resulting in acute hepatitis, hypotension, rhabdomyolyis, torsade de pointes, sedation, or ergotism are presented: interactions with azole antifungals (ketoconazole, itraconazole, fluconazole), HIV protease inhibitors (ritonavir, indinavir, saquinavir, nelfinavir), macrolide antibiotics (clarithromycin, erythromycin), and grapefruit juice. Nelfinavir 307-317 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-42 12477837-1 2003 During the use of a phenotypic anti-human immunodeficiency virus type 1 (HIV-1) drug resistance assay in a large set of clinical virus isolates, we found a unique variant (CL-4) that exhibited a high level of nelfinavir (NFV) resistance and rather enhanced replication under subinhibitory concentrations of NFV (0.001 to 0.1 micro M). Nelfinavir 209-219 endogenous retrovirus group W member 3 Homo sapiens 172-176 12435624-5 2002 Nelfinavir 1250 mg BID was well tolerated. Nelfinavir 0-10 BH3 interacting domain death agonist Homo sapiens 19-22 12189360-9 2002 The absolute magnitude of amprenavir intrinsic clearance suggests that CYP3A4 inhibition by nelfinavir and indinavir is balanced by enzymatic induction in the presence of the background drug(s), most likely efavirenz. Nelfinavir 92-102 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 71-77 12176683-1 2002 BACKGROUND: In this retrospective study the effect of antiretroviral triple therapy including the protease-inhibitor nelfinavir (NFV) on CD4-cells and viral load (VL) in heavily pretreated HIV-infected children was evaluated. Nelfinavir 117-127 CD4 molecule Homo sapiens 137-140 12403023-20 2002 The study has therefore demonstrated the significant efficacy and tolerability of (Nelfinavir/Zalcitabine/ Zidovudine combination in suppressing viral replication, increasing the CD4 cell counts and improving the quality of life in Nigeria patients with HIV. Nelfinavir 83-93 CD4 molecule Homo sapiens 179-182 12405866-18 2002 Losartan may have increased effect when coadministered with ritonavir and nelfinavir because of the induction of CYP2C9 and the expected increase in formation of the active metabolite, E-3174. Nelfinavir 74-84 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 113-119 11468419-4 2001 We found that HIV-PIs (i.e., ritonavir, saquinavir, nelfinavir and indinavir) interfere with P-gp function in normal PBLs as demonstrated by the reduced efflux of rhodamine 123 (Rh123). Nelfinavir 52-62 ATP binding cassette subfamily B member 1 Homo sapiens 93-97 11477322-1 2001 Nelfinavir has been recently approved as a twice-daily (BID) dose regimen, but no evaluation of the influence of this regimen change on patients" protease inhibitor exposure has been published. Nelfinavir 0-10 BH3 interacting domain death agonist Homo sapiens 56-59 11375344-0 2001 The HIV protease inhibitor nelfinavir induces insulin resistance and increases basal lipolysis in 3T3-L1 adipocytes. Nelfinavir 27-37 insulin Homo sapiens 46-53 11375344-5 2001 Impaired insulin stimulation of glucose up take occurred at nelfinavir concentrations >10 micromol/l (EC(50) = 20 micromol/l) and could be attributed to impaired GLUT4 translocation. Nelfinavir 60-70 insulin Homo sapiens 9-16 11375344-10 2001 This study demonstrates that nelfinavir induces insulin resistance and activates basal lipolysis in differentiated 3T3-L1 adipocytes, providing potential cellular mechanisms that may contribute to altered adipocyte metabolism in treated HIV patients. Nelfinavir 29-39 insulin Homo sapiens 48-55 11399981-8 2001 Coadministration of CYP2C19 inhibitors, such as omeprazole, decreased the median M8/nelfinavir ratio. Nelfinavir 84-94 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 20-27 11302944-9 2001 Nelfinavir treatment increased expression of intestinal Pgp and hepatic CYP3A levels by 83 and 85%, respectively, but not hepatic Pgp or intestinal CYP3A. Nelfinavir 0-10 ATP binding cassette subfamily B member 1 Homo sapiens 56-59 11302944-9 2001 Nelfinavir treatment increased expression of intestinal Pgp and hepatic CYP3A levels by 83 and 85%, respectively, but not hepatic Pgp or intestinal CYP3A. Nelfinavir 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-77 11590524-6 2001 RESULTS: In both trials, patients receiving nelfinavir had greater CD4 T-cell increases than patients receiving RTI alone. Nelfinavir 44-54 CD4 molecule Homo sapiens 67-70 11590524-10 2001 CONCLUSION: Nelfinavir-containing therapy is associated with enhanced increases in CD4 T-cell number compared to RTI therapy alone with equivalent antiviral effect. Nelfinavir 12-22 CD4 molecule Homo sapiens 83-86 11159797-0 2001 Ritonavir, efavirenz, and nelfinavir inhibit CYP2B6 activity in vitro: potential drug interactions with bupropion. Nelfinavir 26-36 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 45-51 11159797-4 2001 The inhibition of bupropion hydroxylation in vitro by nelfinavir, ritonavir, and efavirenz indicates inhibitory potency versus CYP2B6 and suggests the potential for clinical drug interactions. Nelfinavir 54-64 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 127-133 11116063-4 2000 Moreover, nelfinavir increased mRNA expression of diacylglycerol acyltransferase and fatty acid synthase. Nelfinavir 10-20 fatty acid synthase Mus musculus 85-104 11185676-9 2000 Inhibition of p-glycoprotein by nelfinavir may be responsible for this significant interaction. Nelfinavir 32-42 ATP binding cassette subfamily B member 1 Homo sapiens 14-28 11120614-2 2000 This study investigated whether the inducible levels of RANTES, MIP-1alpha and MIP-1beta produced by cultured whole blood samples related to different rates of progression of HIV infection and to the introduction of Nelfinavir-based highly active anti-retroviral therapy (HAART). Nelfinavir 216-226 C-C motif chemokine ligand 5 Homo sapiens 56-62