PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 34017865-6 2021 Methods: Atazanavir, remdesivir, ritonavir, lopinavir and favipiravir were docked to in silico models of the pore domain of hERG, derived from cryo-EM structures of hERG and the closely related EAG channel. Lopinavir 44-53 ETS transcription factor ERG Homo sapiens 124-128 33974624-3 2021 Both, lopinavir and hydroxychloroquine are metabolized by cytochrome P450 (CYP) 3A4. Lopinavir 6-15 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 58-83 33100380-9 2021 Justicia adhatoda alkaloids possessing proper drug-likeness properties and two anti-HIV drugs (lopinavir and darunavir; having binding affinity -7.3 to -7.4 kcal/mol) were docked against SARS CoV-2 Mpro to study their binding properties. Lopinavir 95-104 NEWENTRY Severe acute respiratory syndrome-related coronavirus 198-202 33100380-11 2021 Molecular dynamic simulations (100 ns) revealed that Mpro-anisotine complex is more stable, conformationally less fluctuated; slightly less compact and marginally expanded than Mpro-darunavir/lopinavir complex. Lopinavir 192-201 NEWENTRY Severe acute respiratory syndrome-related coronavirus 53-57 33100380-11 2021 Molecular dynamic simulations (100 ns) revealed that Mpro-anisotine complex is more stable, conformationally less fluctuated; slightly less compact and marginally expanded than Mpro-darunavir/lopinavir complex. Lopinavir 192-201 NEWENTRY Severe acute respiratory syndrome-related coronavirus 177-181 33567992-8 2021 Hepatitis C and use of darunavir and lopinavir were associated with increased AST or ALT. Lopinavir 37-46 solute carrier family 17 member 5 Homo sapiens 78-81 33476691-6 2021 In vivo test showed that QPD prolonged the half-life of lopinavir (a CYP3A substrate-drug) by 1.40-fold and increased the AUC of lopinavir by 2.04-fold, when QPD (6 g/kg) was co-administrated with lopinavir (160 mg/kg) to rats. Lopinavir 56-65 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 69-74 33797130-10 2021 Overall, the present analysis yielded two potential inhibitors (DB02986 and DB08573) that are predicted to bind with the main protease of Covid-19 better than currently used drug molecules such as N3 (co-crystallized native ligand), Lopinavir and Ritonavir. Lopinavir 233-242 n3 None 197-199 33759544-0 2021 Predictive association of ABCB1 C3435T genetic polymorphism with the efficacy or safety of lopinavir and ritonavir in coronavirus disease-2019 patients. Lopinavir 91-100 ATP binding cassette subfamily B member 1 Homo sapiens 26-31 33759544-1 2021 Lopinavir and ritonavir are substrates of permeability glycoprotein encoded by ABCB1. Lopinavir 0-9 ATP binding cassette subfamily B member 1 Homo sapiens 79-84 32807688-2 2021 Lopinavir-interferon alpha2b boosted ribavirin following with lopinavir boosted budesonide might be a potent treatment for viral clearance. Lopinavir 0-9 interferon alpha 2 Homo sapiens 10-28 33531790-12 2021 This finding was of particular importance that other compounds including hydroxychloroquine sulphate, lopinavir and ivermectin could bind with the spike protein only by weak Vander wall bonds and no hydrogen bond formation was noticed. Lopinavir 102-111 surface glycoprotein Severe acute respiratory syndrome coronavirus 2 147-152 33688584-3 2021 Comparing to those under trial/temporarily used antivirus drugs (i.e., umifenovir, lopinavir), ceftriaxone, cefotaxime, and cefuroxime show higher binding affinities to the N-terminal domain of N protein (N-NTD), C-terminal domain of N protein (N-CTD), and receptor-binding domain of S protein (S-RBD). Lopinavir 83-92 nucleocapsid phosphoprotein Severe acute respiratory syndrome coronavirus 2 173-174 33688584-3 2021 Comparing to those under trial/temporarily used antivirus drugs (i.e., umifenovir, lopinavir), ceftriaxone, cefotaxime, and cefuroxime show higher binding affinities to the N-terminal domain of N protein (N-NTD), C-terminal domain of N protein (N-CTD), and receptor-binding domain of S protein (S-RBD). Lopinavir 83-92 nucleocapsid phosphoprotein Severe acute respiratory syndrome coronavirus 2 194-195 33688584-3 2021 Comparing to those under trial/temporarily used antivirus drugs (i.e., umifenovir, lopinavir), ceftriaxone, cefotaxime, and cefuroxime show higher binding affinities to the N-terminal domain of N protein (N-NTD), C-terminal domain of N protein (N-CTD), and receptor-binding domain of S protein (S-RBD). Lopinavir 83-92 nucleocapsid phosphoprotein Severe acute respiratory syndrome coronavirus 2 194-195 33688584-3 2021 Comparing to those under trial/temporarily used antivirus drugs (i.e., umifenovir, lopinavir), ceftriaxone, cefotaxime, and cefuroxime show higher binding affinities to the N-terminal domain of N protein (N-NTD), C-terminal domain of N protein (N-CTD), and receptor-binding domain of S protein (S-RBD). Lopinavir 83-92 surface glycoprotein Severe acute respiratory syndrome coronavirus 2 284-285 33421743-5 2021 The results suggested that by using the combination of Lopinavir, Ritonavir along with Hydroxychloroquine and Vitamin C may turned out to be the effective line of treatment for SARS-CoV-2 as it shows the involvement of PARP-1, MAPK-8, EGFR, PRKCB, PTGS-2, and BCL-2. Lopinavir 55-64 poly(ADP-ribose) polymerase 1 Homo sapiens 219-225 33421743-5 2021 The results suggested that by using the combination of Lopinavir, Ritonavir along with Hydroxychloroquine and Vitamin C may turned out to be the effective line of treatment for SARS-CoV-2 as it shows the involvement of PARP-1, MAPK-8, EGFR, PRKCB, PTGS-2, and BCL-2. Lopinavir 55-64 mitogen-activated protein kinase 8 Homo sapiens 227-233 33421743-5 2021 The results suggested that by using the combination of Lopinavir, Ritonavir along with Hydroxychloroquine and Vitamin C may turned out to be the effective line of treatment for SARS-CoV-2 as it shows the involvement of PARP-1, MAPK-8, EGFR, PRKCB, PTGS-2, and BCL-2. Lopinavir 55-64 epidermal growth factor receptor Homo sapiens 235-239 33421743-5 2021 The results suggested that by using the combination of Lopinavir, Ritonavir along with Hydroxychloroquine and Vitamin C may turned out to be the effective line of treatment for SARS-CoV-2 as it shows the involvement of PARP-1, MAPK-8, EGFR, PRKCB, PTGS-2, and BCL-2. Lopinavir 55-64 protein kinase C beta Homo sapiens 241-246 33421743-5 2021 The results suggested that by using the combination of Lopinavir, Ritonavir along with Hydroxychloroquine and Vitamin C may turned out to be the effective line of treatment for SARS-CoV-2 as it shows the involvement of PARP-1, MAPK-8, EGFR, PRKCB, PTGS-2, and BCL-2. Lopinavir 55-64 prostaglandin-endoperoxide synthase 2 Homo sapiens 248-254 33421743-5 2021 The results suggested that by using the combination of Lopinavir, Ritonavir along with Hydroxychloroquine and Vitamin C may turned out to be the effective line of treatment for SARS-CoV-2 as it shows the involvement of PARP-1, MAPK-8, EGFR, PRKCB, PTGS-2, and BCL-2. Lopinavir 55-64 BCL2 apoptosis regulator Homo sapiens 260-265 33679150-5 2021 In this study, we docked five clinically used drug molecules, favipiravir, hydroxychloroquine, remdesivir, lopinavir, and ritonavir onto three target proteins, the receptor-binding domain of SARS-CoV-2 spike protein, SARS-CoV-2 main protease, and human furin protease. Lopinavir 107-116 surface glycoprotein Severe acute respiratory syndrome coronavirus 2 202-207 32807688-2 2021 Lopinavir-interferon alpha2b boosted ribavirin following with lopinavir boosted budesonide might be a potent treatment for viral clearance. Lopinavir 62-71 interferon alpha 2 Homo sapiens 10-28 33445576-8 2021 LPV also decreased P450SCC and HSD3B1 expression, whereas it increased Mfn2, GRP78 and sXBP1 expression in ST. RTV has no effect on the endocrine placenta. Lopinavir 0-3 cytochrome P450 family 11 subfamily A member 1 Homo sapiens 19-26 33445576-8 2021 LPV also decreased P450SCC and HSD3B1 expression, whereas it increased Mfn2, GRP78 and sXBP1 expression in ST. RTV has no effect on the endocrine placenta. Lopinavir 0-3 hydroxy-delta-5-steroid dehydrogenase, 3 beta- and steroid delta-isomerase 1 Homo sapiens 31-37 33292085-8 2022 Polyphenols that qualified the pharmacological parameters (indigo, sinigrin, hesperetin and daidzein) and two well-known Mpro inhibitors (N3 and lopinavir) were subjected to molecular docking studies. Lopinavir 145-154 NEWENTRY Severe acute respiratory syndrome-related coronavirus 121-125 33292085-11 2022 Molecular dynamics studies further revealed that these two Mpro-polyphenol complexes are more stable and experience less conformational fluctuations than Mpro-N3/lopinavir complex. Lopinavir 162-171 NEWENTRY Severe acute respiratory syndrome-related coronavirus 59-63 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. Lopinavir 164-173 NEWENTRY Severe acute respiratory syndrome-related coronavirus 91-95 33179586-6 2022 We have also performed docking of drugs Lopinavir, Ribavirin, and Azithromycin on SARS-CoV-2 Mpro. Lopinavir 40-49 NEWENTRY Severe acute respiratory syndrome-related coronavirus 93-97 33022569-2 2020 Under this scenario, the combination of two HIV-1 protease inhibitors, lopinavir and ritonavir, has attracted attention since they have been previously employed against the SARS-CoV main proteinase (Mpro) and exhibited some signs of effectiveness. Lopinavir 71-80 NEWENTRY Severe acute respiratory syndrome-related coronavirus 199-203 33022569-6 2020 Our study provides the structural and energetic basis of the inhibitory properties of lopinavir and ritonavir on SARS-CoV Mpro and SARS-CoV2 Mpro, allowing us to identify two FDA-approved drugs that can be used against SARS-CoV2 Mpro. Lopinavir 86-95 NEWENTRY Severe acute respiratory syndrome-related coronavirus 122-126 33022569-6 2020 Our study provides the structural and energetic basis of the inhibitory properties of lopinavir and ritonavir on SARS-CoV Mpro and SARS-CoV2 Mpro, allowing us to identify two FDA-approved drugs that can be used against SARS-CoV2 Mpro. Lopinavir 86-95 NEWENTRY Severe acute respiratory syndrome-related coronavirus 141-145 33022569-6 2020 Our study provides the structural and energetic basis of the inhibitory properties of lopinavir and ritonavir on SARS-CoV Mpro and SARS-CoV2 Mpro, allowing us to identify two FDA-approved drugs that can be used against SARS-CoV2 Mpro. Lopinavir 86-95 NEWENTRY Severe acute respiratory syndrome-related coronavirus 141-145 33200673-2 2022 Using in silico and molecular docking approaches, this study investigated the inhibitory effects of Pradimicin A, Lamivudine, Plerixafor and Lopinavir against SARS-CoV-2 Mpro. Lopinavir 141-150 NEWENTRY Severe acute respiratory syndrome-related coronavirus 170-174 32911432-6 2020 Here, our aim was to investigate small molecules, including lopinavir and ritonavir, alpha-ketoamide 13b, and ebselen, for their ability to interact with the Mpro. Lopinavir 60-69 NEWENTRY Severe acute respiratory syndrome-related coronavirus 158-162 33251975-4 2022 Small molecules such as lopinavir and favipiravir significantly inhibit the activity of Mpro and RdRp in vitro. Lopinavir 24-33 NEWENTRY Severe acute respiratory syndrome-related coronavirus 88-92 33251975-4 2022 Small molecules such as lopinavir and favipiravir significantly inhibit the activity of Mpro and RdRp in vitro. Lopinavir 24-33 ORF1a polyprotein;ORF1ab polyprotein Severe acute respiratory syndrome coronavirus 2 97-101 33251975-5 2022 Studies have shown that structurally modified lopinavir, favipiravir, and other similar compounds can inhibit COVID-19 main protease (Mpro) and RNA-dependent RNA polymerase (RdRp). Lopinavir 46-55 NEWENTRY Severe acute respiratory syndrome-related coronavirus 134-138 33251975-5 2022 Studies have shown that structurally modified lopinavir, favipiravir, and other similar compounds can inhibit COVID-19 main protease (Mpro) and RNA-dependent RNA polymerase (RdRp). Lopinavir 46-55 ORF1a polyprotein;ORF1ab polyprotein Severe acute respiratory syndrome coronavirus 2 174-178 33251975-9 2022 Molecular interaction analyses have displayed that lopinavir and favipiravir analogues interact with the active site residues of Mpro and RdRp, respectively. Lopinavir 51-60 NEWENTRY Severe acute respiratory syndrome-related coronavirus 129-133 33251975-9 2022 Molecular interaction analyses have displayed that lopinavir and favipiravir analogues interact with the active site residues of Mpro and RdRp, respectively. Lopinavir 51-60 ORF1a polyprotein;ORF1ab polyprotein Severe acute respiratory syndrome coronavirus 2 138-142 33251975-11 2022 Subsequently, 50 ns molecular dynamics simulation of the top four docked complexes demonstrated that CID44271905, a lopinavir analogue, forms the most stable complex with the Mpro. Lopinavir 116-125 NEWENTRY Severe acute respiratory syndrome-related coronavirus 175-179 33179586-7 2022 Further, binding of these compounds (Hyaluronic acid, Acarbose, and Lopinavir) is validated by extensive molecular dynamics simulation of 500 ns where these drugs show stable binding with Mpro. Lopinavir 68-77 NEWENTRY Severe acute respiratory syndrome-related coronavirus 188-192 33094701-12 2022 Molecular dynamics studies further revealed that these two Mpro-corticosteroid complexes are more stable, experience less conformational fluctuations and more compact than Mpro-darunavir/lopinavir complexes. Lopinavir 187-196 NEWENTRY Severe acute respiratory syndrome-related coronavirus 59-63 33140695-12 2022 Besides, these complexes experience less conformational fluctuations and more expansion than Mpro-N3 and/or Mpro-lopinavir complex. Lopinavir 113-122 NEWENTRY Severe acute respiratory syndrome-related coronavirus 108-112 33144375-10 2020 A combination of four mutations (S126del, H127del, T122A, and G123E) in the p17 matrix of baseline virus generated a similar 4-fold decrease in susceptibility to LPV but not darunavir. Lopinavir 162-165 family with sequence similarity 72 member B Homo sapiens 76-79 33144375-11 2020 These four amino acid changes were also able to confer LPV resistance to a subtype B Gag-protease backbone. Lopinavir 55-58 Pr55(Gag) Human immunodeficiency virus 1 85-88 33094701-12 2022 Molecular dynamics studies further revealed that these two Mpro-corticosteroid complexes are more stable, experience less conformational fluctuations and more compact than Mpro-darunavir/lopinavir complexes. Lopinavir 187-196 NEWENTRY Severe acute respiratory syndrome-related coronavirus 172-176 33063648-4 2022 The comparative analysis of the MM/GBSA results revealed that the binding affinity (DeltaGbind) of EGCG and K7G for CYP3A4 and ABCB1 are higher than LUT and EGA and fall between the DeltaGbind of the inhibitors of CYP3A4 and ABCB1 (Ritonavir (strong inhibitor) and Lopinavir (moderate inhibitor)). Lopinavir 265-274 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 116-122 33063648-4 2022 The comparative analysis of the MM/GBSA results revealed that the binding affinity (DeltaGbind) of EGCG and K7G for CYP3A4 and ABCB1 are higher than LUT and EGA and fall between the DeltaGbind of the inhibitors of CYP3A4 and ABCB1 (Ritonavir (strong inhibitor) and Lopinavir (moderate inhibitor)). Lopinavir 265-274 ATP binding cassette subfamily B member 1 Homo sapiens 127-132 32878881-6 2020 In silico screening, molecular mechanics and molecular dynamics simulation (MDS) analysis suggest ribavirin, ascorbate, lopinavir and hydroxychloroquine have strong interaction at the RBD-hACE2 interface. Lopinavir 120-129 angiotensin converting enzyme 2 Homo sapiens 188-193 32641296-10 2020 LPV plasma concentrations positively correlated with CRP values (r = 0.37, P < 0.001) and were significantly lower when tocilizumab was preadministered. Lopinavir 0-3 C-reactive protein Homo sapiens 53-56 33312066-8 2020 Based on high alternative allele frequencies in population and the functional effect of the variants, ABCB1 rs1045642 and rs2032582 could be relevant for reduced clearance of azithromycin, lopinavir and ritonavir drugs and UGT1A7 rs17868323 for hyperbilirubinemia in ritonavir treated COVID-19 patients in Serbian population. Lopinavir 189-198 ATP binding cassette subfamily B member 1 Homo sapiens 102-107 33312066-8 2020 Based on high alternative allele frequencies in population and the functional effect of the variants, ABCB1 rs1045642 and rs2032582 could be relevant for reduced clearance of azithromycin, lopinavir and ritonavir drugs and UGT1A7 rs17868323 for hyperbilirubinemia in ritonavir treated COVID-19 patients in Serbian population. Lopinavir 189-198 UDP glucuronosyltransferase family 1 member A7 Homo sapiens 223-229 33312066-9 2020 SLCO1B1 rs4149056 is a potential marker of lopinavir response, especially in Italian population. Lopinavir 43-52 solute carrier organic anion transporter family member 1B1 Homo sapiens 0-7 32590137-8 2020 Osteocalcin (ng/mL) was higher in the LPV/r than efavirenz group both at 8 weeks (88.6 vs. 67.3, p = 0.001) and 2 years (67.6 vs. 49.8, p = 0.001). Lopinavir 38-43 bone gamma-carboxyglutamate protein Homo sapiens 0-11 32590137-10 2020 We did observe higher levels of total osteocalcin in children remaining on LPV/r compared to children switched to efavirenz. Lopinavir 75-80 bone gamma-carboxyglutamate protein Homo sapiens 38-49 33011734-12 2020 Postoperative serum GFAP and IL-6 were lower and IL-10 higher in the LPV group. Lopinavir 69-72 glial fibrillary acidic protein Homo sapiens 20-24 33011734-12 2020 Postoperative serum GFAP and IL-6 were lower and IL-10 higher in the LPV group. Lopinavir 69-72 interleukin 6 Homo sapiens 29-33 33011734-12 2020 Postoperative serum GFAP and IL-6 were lower and IL-10 higher in the LPV group. Lopinavir 69-72 interleukin 10 Homo sapiens 49-54 32759267-3 2020 The major protease (Mpro) of SARS-CoV-2 is considered a promising target, based on previous results from related CoVs with lopinavir (LPV), an HIV protease inhibitor. Lopinavir 123-132 major protease None 4-18 32759267-3 2020 The major protease (Mpro) of SARS-CoV-2 is considered a promising target, based on previous results from related CoVs with lopinavir (LPV), an HIV protease inhibitor. Lopinavir 123-132 NEWENTRY Severe acute respiratory syndrome-related coronavirus 20-24 32759267-3 2020 The major protease (Mpro) of SARS-CoV-2 is considered a promising target, based on previous results from related CoVs with lopinavir (LPV), an HIV protease inhibitor. Lopinavir 134-137 major protease None 4-18 32759267-3 2020 The major protease (Mpro) of SARS-CoV-2 is considered a promising target, based on previous results from related CoVs with lopinavir (LPV), an HIV protease inhibitor. Lopinavir 134-137 NEWENTRY Severe acute respiratory syndrome-related coronavirus 20-24 32759267-6 2020 Our results show that ATV could dock in the active site of SARS-CoV-2 Mpro, with greater strength than LPV, blocking Mpro activity. Lopinavir 103-106 NEWENTRY Severe acute respiratory syndrome-related coronavirus 70-74 32759267-6 2020 Our results show that ATV could dock in the active site of SARS-CoV-2 Mpro, with greater strength than LPV, blocking Mpro activity. Lopinavir 103-106 NEWENTRY Severe acute respiratory syndrome-related coronavirus 117-121 32641296-14 2020 CRP values significantly correlated with LPV but not HCQ plasma concentrations, implying inhibition of cytochrome P450 3A4 (CYP3A4) metabolism by inflammation. Lopinavir 41-44 C-reactive protein Homo sapiens 0-3 32641296-14 2020 CRP values significantly correlated with LPV but not HCQ plasma concentrations, implying inhibition of cytochrome P450 3A4 (CYP3A4) metabolism by inflammation. Lopinavir 41-44 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 103-122 32641296-14 2020 CRP values significantly correlated with LPV but not HCQ plasma concentrations, implying inhibition of cytochrome P450 3A4 (CYP3A4) metabolism by inflammation. Lopinavir 41-44 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 124-130 31633158-10 2020 Lopinavir, but not ritonavir, inhibited CYP17A1 and CYP21A2 activity in H295R cells. Lopinavir 0-9 cytochrome P450 family 17 subfamily A member 1 Homo sapiens 40-47 31633158-10 2020 Lopinavir, but not ritonavir, inhibited CYP17A1 and CYP21A2 activity in H295R cells. Lopinavir 0-9 cytochrome P450 family 21 subfamily A member 2 Homo sapiens 52-59 31633158-12 2020 The impact of long-term exposure and potential clinical consequences require evaluation.Giving lopinavir to infants during their first year of life induces early, asymptomatic adrenal disruption compatible with the combined inhibition of CYP 21 and CYP 17 enzymes. Lopinavir 95-104 cytochrome P450 family 21 subfamily A member 2 Homo sapiens 238-244 31633158-12 2020 The impact of long-term exposure and potential clinical consequences require evaluation.Giving lopinavir to infants during their first year of life induces early, asymptomatic adrenal disruption compatible with the combined inhibition of CYP 21 and CYP 17 enzymes. Lopinavir 95-104 cytochrome P450 family 17 subfamily A member 1 Homo sapiens 249-255 32762411-9 2021 Polyphenols having proper drug-likeness properties and two repurposed drugs (lopinavir and darunavir; having binding affinity -7.3 to -7.4 kcal/mol) were docked against SARS CoV-2 Mpro to study their binding properties. Lopinavir 77-86 NEWENTRY Severe acute respiratory syndrome-related coronavirus 180-184 32762411-11 2021 Molecular dynamic simulations (100 ns) revealed that all Mpro-polyphenol complexes are more stable, conformationally less fluctuated; slightly less compact and marginally expanded than Mpro-darunavir/lopinavir complex. Lopinavir 200-209 NEWENTRY Severe acute respiratory syndrome-related coronavirus 57-61 32762411-12 2021 Even the number of intermolecular H-bond and MM-GBSA analysis suggested that these six polyphenols are more potent Mpro inhibitors than the two repurposed drugs (lopinavir and darunavir) and may serve as promising anti-COVID-19 drugs. Lopinavir 162-171 NEWENTRY Severe acute respiratory syndrome-related coronavirus 115-119 32712670-17 2020 The lopinavir-associated decidualization defects were attributed to a decrease in expression of transcription factor STAT3, known to regulate decidualization. Lopinavir 4-13 signal transducer and activator of transcription 3 Mus musculus 117-122 32476576-8 2021 Furthermore, principal component analysis, free energy landscape and protein-ligand energy calculation studies revealed that these two compounds strongly bind to the catalytic core of the Mpro protein with higher efficacy than lopinavir, a standard antiretroviral of the protease inhibitor class. Lopinavir 227-236 NEWENTRY Severe acute respiratory syndrome-related coronavirus 188-192 32729392-4 2021 Molecular docking on 40 derivatives of standard drugs (Remdesivir, Lopinavir and Theophylline) led to the identification of R10, R2 and L9 as potential inhibitors of 3CLpro, PLpro and Spike protein, respectively. Lopinavir 67-76 ORF1a polyprotein;ORF1ab polyprotein Severe acute respiratory syndrome coronavirus 2 174-179 32729392-4 2021 Molecular docking on 40 derivatives of standard drugs (Remdesivir, Lopinavir and Theophylline) led to the identification of R10, R2 and L9 as potential inhibitors of 3CLpro, PLpro and Spike protein, respectively. Lopinavir 67-76 surface glycoprotein Severe acute respiratory syndrome coronavirus 2 184-189 32022294-0 2020 Influence of SLCO1B1 polymorphisms on lopinavir Ctrough inSerbian HIV/AIDS patients. Lopinavir 38-47 solute carrier organic anion transporter family member 1B1 Homo sapiens 13-20 32022294-3 2020 Since LPV is a substrate for the SLCO1B1 (OATP1B1)-transporter, the aim of this study was to assess the impact of SLCO1B1 polymorphisms (rs11045819, rs4149032 and rs4149056) on LPV trough plasma concentrations (Ctrough ) in Serbian patients. Lopinavir 6-9 solute carrier organic anion transporter family member 1B1 Homo sapiens 33-40 32022294-3 2020 Since LPV is a substrate for the SLCO1B1 (OATP1B1)-transporter, the aim of this study was to assess the impact of SLCO1B1 polymorphisms (rs11045819, rs4149032 and rs4149056) on LPV trough plasma concentrations (Ctrough ) in Serbian patients. Lopinavir 6-9 solute carrier organic anion transporter family member 1B1 Homo sapiens 42-49 32022294-3 2020 Since LPV is a substrate for the SLCO1B1 (OATP1B1)-transporter, the aim of this study was to assess the impact of SLCO1B1 polymorphisms (rs11045819, rs4149032 and rs4149056) on LPV trough plasma concentrations (Ctrough ) in Serbian patients. Lopinavir 6-9 solute carrier organic anion transporter family member 1B1 Homo sapiens 114-121 32022294-12 2020 In multivariate regression analysis, only the SLCO1B1 rs4149056 polymorphism was independently associated with higher LPV Ctrough [beta=2834.5 (1442-4226.9) ng/mL (p=0.001)]. Lopinavir 118-121 solute carrier organic anion transporter family member 1B1 Homo sapiens 46-53 32022294-13 2020 CONCLUSIONS: Our results demonstrate a statistically significant influence of the SLCO1B1 rs4149056 polymorphism on higher LPV Ctrough in Caucasian HIV/AIDS- patients. Lopinavir 123-126 solute carrier organic anion transporter family member 1B1 Homo sapiens 82-89 31924204-11 2020 In contrast, the LPV strategy worsened VIDD by inducing oxidative stress together with the downregulation of PGC-1alpha in the diaphragm. Lopinavir 17-20 PPARG coactivator 1 alpha Rattus norvegicus 109-119 32375574-2 2021 This study demonstrated the putative inhibitory potential of lopinavir, remdesivir, oseltamir, azithromycin, ribavirin, and chloroquine towards V-ATPase, protein kinase A, SARS-CoV spike glycoprotein/ACE-2 complex and viral proteases. Lopinavir 61-70 angiotensin converting enzyme 2 Homo sapiens 200-205 32375574-5 2021 Lopinavir has the highest binding affinities to the pocket site of SARS-CoV spike glycoprotein/ACE-2 complex, cyclic AMP-dependent protein kinase A and 3-Chymotrypsin like protease while redemsivir has the highest binding affinities for vacuolar proton-translocating ATPase (V-ATPase) and papain-like proteins. Lopinavir 0-9 angiotensin converting enzyme 2 Homo sapiens 95-100 32375574-5 2021 Lopinavir has the highest binding affinities to the pocket site of SARS-CoV spike glycoprotein/ACE-2 complex, cyclic AMP-dependent protein kinase A and 3-Chymotrypsin like protease while redemsivir has the highest binding affinities for vacuolar proton-translocating ATPase (V-ATPase) and papain-like proteins. Lopinavir 0-9 cyclic amp-dependent protein kinase a and 3 None 110-153 32375574-6 2021 The amino acids Asp269, Leu370, His374, and His345 were predicted as the key residues for lopinavir binding to human SARS-CoV spike glycoprotein/ACE-2 complex while His378, Tyr515, Leu73, Leu100, Phe32 and Phe40 for remdesivir and Tyr510, Phe504, Met62, Tyr50, and His378 were predicted for azithromycin as the key residues for binding to SARS-CoV spike glycoprotein/ACE-2 complex. Lopinavir 90-99 angiotensin converting enzyme 2 Homo sapiens 145-150 32375574-6 2021 The amino acids Asp269, Leu370, His374, and His345 were predicted as the key residues for lopinavir binding to human SARS-CoV spike glycoprotein/ACE-2 complex while His378, Tyr515, Leu73, Leu100, Phe32 and Phe40 for remdesivir and Tyr510, Phe504, Met62, Tyr50, and His378 were predicted for azithromycin as the key residues for binding to SARS-CoV spike glycoprotein/ACE-2 complex. Lopinavir 90-99 angiotensin converting enzyme 2 Homo sapiens 367-372 32490327-5 2020 Knocking down Rce1 with RNA interference increased ritonavir and lopinavir-induced cell death as well as expression of Golgi stress response markers, TFE3, HSP47 and GCP60, in both primary mouse hepatocytes and mouse liver, and deteriorated alcohol-induced alanine aminotransferase (ALT) and fatty liver injury in mice. Lopinavir 65-74 Ras converting CAAX endopeptidase 1 Mus musculus 14-18 31495591-0 2020 A reconfigurable PID fault tolerant tracking controller design for LPV systems. Lopinavir 67-70 metastasis associated 1 family member 2 Homo sapiens 17-20 32490327-0 2020 Ritonavir and Lopinavir Suppress RCE1 and CAAX Rab Proteins Sensitizing the Liver to Organelle Stress and Injury. Lopinavir 14-23 Ras converting CAAX endopeptidase 1 Homo sapiens 33-37 32490327-2 2020 Here, we found through total RNA sequencing that the transcription of a host protease Ras converting CAAX endopeptidase 1 (RCE1) was altered in HepG2 cells treated with anti-HIV protease inhibitors, ritonavir and lopinavir. Lopinavir 213-222 Ras converting CAAX endopeptidase 1 Homo sapiens 86-121 32490327-2 2020 Here, we found through total RNA sequencing that the transcription of a host protease Ras converting CAAX endopeptidase 1 (RCE1) was altered in HepG2 cells treated with anti-HIV protease inhibitors, ritonavir and lopinavir. Lopinavir 213-222 Ras converting CAAX endopeptidase 1 Homo sapiens 123-127 30753326-0 2019 Gag-protease coevolution shapes the outcome of lopinavir-inclusive treatment regimens in chronically infected HIV-1 subtype C patients. Lopinavir 47-56 Pr55(Gag) Human immunodeficiency virus 1 0-3 31838577-9 2020 Nelfinavir and lopinavir, two clinically approved HIV protease inhibitors, promote eIF2alpha phosphorylation by different mechanisms. Lopinavir 15-24 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. Lopinavir 28-37 natural killer cell cytotoxicity receptor 3 ligand 1 Homo sapiens 60-64 31481446-4 2019 Lopinavir, ritonavir, saquinavir, atazanavir, maraviroc, ledipasvir, and daclatasvir inhibited the efflux of a model ABCB1 substrate, rhodamine 123 (RHD123), in Caco-2 cells and rat-derived PCIS. Lopinavir 0-9 ATP binding cassette subfamily B member 1 Homo sapiens 117-122 31481446-5 2019 Lopinavir, ritonavir, saquinavir, and atazanavir also significantly inhibited RHD123 efflux in human-derived PCIS, while possible interindividual variability was observed in the inhibition of intestinal ABCB1 by maraviroc, ledipasvir, and daclatasvir. Lopinavir 0-9 ATP binding cassette subfamily B member 1 Homo sapiens 203-208 31311649-4 2019 Using a transcription-based assay, we observed that Lopinavir inhibits both parasite-and host-derived SPP activities whereas Atazanavir inhibited only parasite derived SPP activity. Lopinavir 52-61 histocompatibility minor 13 Homo sapiens 102-105 30968368-0 2019 Cost-Effectiveness Analysis of Lopinavir/Ritonavir Monotherapy Versus Standard Combination Antiretroviral Therapy in HIV-1 Infected Patients with Viral Suppression in France (ANRS 140 DREAM). Lopinavir 31-40 potassium voltage-gated channel interacting protein 3 Homo sapiens 184-189 31128760-5 2019 The PIs-IC strip cut-off to detect lopinavir (LPV) concentrations was set at 1,000 ng mL-1. Lopinavir 46-49 L1 cell adhesion molecule Mus musculus 86-90 30958309-7 2019 Substitution of W1201i-Gag with MJ4-Gag resulted in an additional small (twofold), but significant (P<0.01) reduction in susceptibility to lopinavir and atazanavir. Lopinavir 142-151 Pr55(Gag) Human immunodeficiency virus 1 23-26 31028820-10 2019 Herein, Soluplus matrixed extrudate improved the LPV bioavailability through three mechanisms: H-bond with LPV, micelle formation in water and P-gp inhibition in vivo. Lopinavir 49-52 ATP binding cassette subfamily B member 1 Homo sapiens 143-147 31262902-7 2019 Only lopinavir was found to have a high P-gp-inhibitory activity (similar to verapamil). Lopinavir 5-14 ATP binding cassette subfamily B member 1 Homo sapiens 40-44 31133852-0 2019 miRNA-218 Targets Lipin-1 and Glucose Transporter Type 4 Genes in 3T3-L1 Cells Treated With Lopinavir/Ritonavir. Lopinavir 92-101 lipin 1 Mus musculus 18-25 31133852-0 2019 miRNA-218 Targets Lipin-1 and Glucose Transporter Type 4 Genes in 3T3-L1 Cells Treated With Lopinavir/Ritonavir. Lopinavir 92-101 solute carrier family 2 (facilitated glucose transporter), member 4 Mus musculus 30-56 31133852-10 2019 The anti-miR-218 transfection of 3T3-L1 cells significantly ameliorated the adipogenic dysfunction and restored mRNA levels of lipin-1 and GLUT-4 consequent to LPV/RTV treatment. Lopinavir 160-163 microRNA 218 Mus musculus 9-16 31133852-10 2019 The anti-miR-218 transfection of 3T3-L1 cells significantly ameliorated the adipogenic dysfunction and restored mRNA levels of lipin-1 and GLUT-4 consequent to LPV/RTV treatment. Lopinavir 160-163 lipin 1 Mus musculus 127-134 31133852-10 2019 The anti-miR-218 transfection of 3T3-L1 cells significantly ameliorated the adipogenic dysfunction and restored mRNA levels of lipin-1 and GLUT-4 consequent to LPV/RTV treatment. Lopinavir 160-163 solute carrier family 2 (facilitated glucose transporter), member 4 Mus musculus 139-145 30871457-10 2019 Importantly, we found that the LPv approach can distinguish high quality Sirt3 probes. Lopinavir 31-34 sirtuin 3 Mus musculus 73-78 30958309-7 2019 Substitution of W1201i-Gag with MJ4-Gag resulted in an additional small (twofold), but significant (P<0.01) reduction in susceptibility to lopinavir and atazanavir. Lopinavir 142-151 Pr55(Gag) Human immunodeficiency virus 1 36-39 30470150-1 2019 Lopinavir (LPV), an efficient drug for HIV infection treatment, was incorporated into biodegradable PLGA nanocapsules (NCs) embedded in microparticles (MCPs) using the spray-drying technique in an attempt to bypass the P-gp efflux and protect the drug from CYP3A pre-systemic metabolism without ritonavir (RTV). Lopinavir 0-9 phosphoglycolate phosphatase Homo sapiens 219-223 30470150-1 2019 Lopinavir (LPV), an efficient drug for HIV infection treatment, was incorporated into biodegradable PLGA nanocapsules (NCs) embedded in microparticles (MCPs) using the spray-drying technique in an attempt to bypass the P-gp efflux and protect the drug from CYP3A pre-systemic metabolism without ritonavir (RTV). Lopinavir 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 257-262 30470150-4 2019 Results obtained from rat studies showed a two-fold higher bioavailability of LPV following oral administration of the optimal formulation than Kaletra , the marketed drug, showing that when properly entrapped, LPV can be effectively protected from CYP degradation in the gut as well as from the liver following systemic absorption. Lopinavir 211-214 cytochrome P450, family 3, subfamily a, polypeptide 23-polypeptide 1 Rattus norvegicus 249-252 30158154-7 2018 Similarly, treatment with the human immunodeficiency virus protease inhibitors lopinavir and ritonavir reduced the accumulation of Lamin-A at nuclear membranes and preserved nuclear membrane compliance after mechanical ventilation, mimicking the protective phenotype of Zmpste24-/- animals. Lopinavir 79-88 lamin A/C Homo sapiens 131-138 30418350-8 2019 CONCLUSIONS: Our results suggest novel genetic susceptibility to primary LPV associated with specific alleles in genes TRPV1 and NGF and propose the rs222747 "C" allele of TRPV1 as a common genetic predisposition for other pain syndromes. Lopinavir 73-76 transient receptor potential cation channel subfamily V member 1 Homo sapiens 119-124 30418350-8 2019 CONCLUSIONS: Our results suggest novel genetic susceptibility to primary LPV associated with specific alleles in genes TRPV1 and NGF and propose the rs222747 "C" allele of TRPV1 as a common genetic predisposition for other pain syndromes. Lopinavir 73-76 nerve growth factor Homo sapiens 129-132 30418350-8 2019 CONCLUSIONS: Our results suggest novel genetic susceptibility to primary LPV associated with specific alleles in genes TRPV1 and NGF and propose the rs222747 "C" allele of TRPV1 as a common genetic predisposition for other pain syndromes. Lopinavir 73-76 transient receptor potential cation channel subfamily V member 1 Homo sapiens 172-177 30158154-7 2018 Similarly, treatment with the human immunodeficiency virus protease inhibitors lopinavir and ritonavir reduced the accumulation of Lamin-A at nuclear membranes and preserved nuclear membrane compliance after mechanical ventilation, mimicking the protective phenotype of Zmpste24-/- animals. Lopinavir 79-88 zinc metallopeptidase STE24 Homo sapiens 270-278 29661866-8 2018 In human hepatocytes and adipocytes, known target cells of FGF21 action, efavirenz, elvitegravir, and the lopinavir-ritonavir combination exerted inhibitory effects on KLB gene expression. Lopinavir 106-115 klotho beta Homo sapiens 168-171 29470145-7 2018 We demonstrated that liver regeneration triggered by 20% LPV stenosis in the contralateral lobe involves TNF-alpha, IL-6, and inducible nitric oxide synthase 2 by means of STAT3 and hepatocyte growth factor. Lopinavir 57-60 tumor necrosis factor Sus scrofa 105-114 29470145-7 2018 We demonstrated that liver regeneration triggered by 20% LPV stenosis in the contralateral lobe involves TNF-alpha, IL-6, and inducible nitric oxide synthase 2 by means of STAT3 and hepatocyte growth factor. Lopinavir 57-60 interleukin 6 Sus scrofa 116-120 29470145-7 2018 We demonstrated that liver regeneration triggered by 20% LPV stenosis in the contralateral lobe involves TNF-alpha, IL-6, and inducible nitric oxide synthase 2 by means of STAT3 and hepatocyte growth factor. Lopinavir 57-60 signal transducer and activator of transcription 3 Sus scrofa 172-177 29661866-11 2018 Moreover, pharmacological inhibitors of either ER or oxidative stress significantly impaired lopinavir-ritonavir-induced regulation of FGF21, but not KLB. Lopinavir 93-102 fibroblast growth factor 21 Homo sapiens 135-140 29523599-7 2018 In human hepatocytes, lopinavir followed by tipranavir, saquinavir, atazanavir, and darunavir were the most potent inhibitors of MRP2-mediated efflux of CDF. Lopinavir 22-31 ATP binding cassette subfamily C member 2 Homo sapiens 129-133 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. Lopinavir 129-138 ATP binding cassette subfamily B member 1 Homo sapiens 40-45 28861811-5 2018 We found that only lopinavir and elvitegravir were neurotoxic to primary rat neuroglial cultures as determined by the loss of microtubule-associated protein 2 (MAP2). Lopinavir 19-28 microtubule-associated protein 2 Rattus norvegicus 126-158 28861811-5 2018 We found that only lopinavir and elvitegravir were neurotoxic to primary rat neuroglial cultures as determined by the loss of microtubule-associated protein 2 (MAP2). Lopinavir 19-28 microtubule-associated protein 2 Rattus norvegicus 160-164 28861811-7 2018 Furthermore, neurotoxicity of lopinavir was blocked by pharmacological augmentation of the endogenous antioxidant heme oxygenase-1 (HO-1), expanding our previous finding that protease inhibitor-induced neurotoxicity was mediated by oxidative stress. Lopinavir 30-39 heme oxygenase 1 Homo sapiens 114-130 29434718-5 2018 Consistent with previous studies, treatment with lopinavir/ritonavir for 2 weeks decreased body weight, adipose tissue mass, levels of plasma adiponectin and leptin, and increased plasma levels of triglycerides, total cholesterol and insulin. Lopinavir 49-58 adiponectin, C1Q and collagen domain containing Mus musculus 142-153 28676669-0 2018 Carfilzomib resistance due to ABCB1/MDR1 overexpression is overcome by nelfinavir and lopinavir in multiple myeloma. Lopinavir 86-95 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. Lopinavir 86-95 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. Lopinavir 129-138 ATP binding cassette subfamily B member 1 Homo sapiens 180-185 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. Lopinavir 140-143 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. Lopinavir 140-143 ATP binding cassette subfamily B member 1 Homo sapiens 180-185 29135577-4 2018 RESULTS: Among women conceiving on ART, lopinavir/RTV was associated with increased PTD risk in those with CD4 cell count 350 cells/mul or less [odds ratio 1.99 (1.02, 3.85)] and with CD4 cell count more than 350 cells/mul [odds ratio 1.61 (1.07, 2.43)] vs. women on nonnucleoside reverse transcriptase inhibitors-based (mainly efavirenz and nevirapine) regimens in the same CD4 subgroup. Lopinavir 40-49 CD4 molecule Homo sapiens 107-110 29135577-4 2018 RESULTS: Among women conceiving on ART, lopinavir/RTV was associated with increased PTD risk in those with CD4 cell count 350 cells/mul or less [odds ratio 1.99 (1.02, 3.85)] and with CD4 cell count more than 350 cells/mul [odds ratio 1.61 (1.07, 2.43)] vs. women on nonnucleoside reverse transcriptase inhibitors-based (mainly efavirenz and nevirapine) regimens in the same CD4 subgroup. Lopinavir 40-49 CD4 molecule Homo sapiens 184-187 29135577-4 2018 RESULTS: Among women conceiving on ART, lopinavir/RTV was associated with increased PTD risk in those with CD4 cell count 350 cells/mul or less [odds ratio 1.99 (1.02, 3.85)] and with CD4 cell count more than 350 cells/mul [odds ratio 1.61 (1.07, 2.43)] vs. women on nonnucleoside reverse transcriptase inhibitors-based (mainly efavirenz and nevirapine) regimens in the same CD4 subgroup. Lopinavir 40-49 CD4 molecule Homo sapiens 184-187 28569994-6 2017 Darunavir and lopinavir PBPK models that accounted for ritonavir CYP3A inhibition effects (linked PBPK models) were developed. Lopinavir 14-23 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 65-70 28717974-1 2018 Lopinavir is a BCS Class IV drug exhibiting poor bioavailability due to P-gp efflux and limited permeation. Lopinavir 0-9 phosphoglycolate phosphatase Rattus norvegicus 72-76 30227099-2 2017 DDIs with Norvir (ritonavir) and combination products (eg, Kaletra [lopinavir/ritonavir]) containing ritonavir as a PK enhancer are relevant, because these drugs could affect exposures of CYP3A4 substrates. Lopinavir 68-77 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 188-194 29064386-0 2017 The Role of PXR Genotype and Transporter Expression in the Placental Transport of Lopinavir in Mice. Lopinavir 82-91 nuclear receptor subfamily 1, group I, member 2 Mus musculus 12-15 29064386-1 2017 Lopinavir (LPV), an antiretroviral protease inhibitor frequently prescribed in HIV-positive pregnancies, is a substrate of Abcb1 and Abcc2. Lopinavir 0-9 ATP-binding cassette, sub-family B (MDR/TAP), member 1B Mus musculus 123-128 29064386-1 2017 Lopinavir (LPV), an antiretroviral protease inhibitor frequently prescribed in HIV-positive pregnancies, is a substrate of Abcb1 and Abcc2. Lopinavir 0-9 ATP-binding cassette, sub-family C (CFTR/MRP), member 2 Mus musculus 133-138 29064386-1 2017 Lopinavir (LPV), an antiretroviral protease inhibitor frequently prescribed in HIV-positive pregnancies, is a substrate of Abcb1 and Abcc2. Lopinavir 11-14 ATP-binding cassette, sub-family B (MDR/TAP), member 1B Mus musculus 123-128 29064386-1 2017 Lopinavir (LPV), an antiretroviral protease inhibitor frequently prescribed in HIV-positive pregnancies, is a substrate of Abcb1 and Abcc2. Lopinavir 11-14 ATP-binding cassette, sub-family C (CFTR/MRP), member 2 Mus musculus 133-138 29064386-8 2017 Two-fold higher fetal:maternal LPV concentration ratios were also seen in the PXR +/+ as compared to the PXR -/- fetuses (p < 0.05), and this significantly correlated to the placental expression of Abcb1a (r = 0.495; p < 0.005). Lopinavir 31-34 nuclear receptor subfamily 1, group I, member 2 Mus musculus 78-81 29064386-8 2017 Two-fold higher fetal:maternal LPV concentration ratios were also seen in the PXR +/+ as compared to the PXR -/- fetuses (p < 0.05), and this significantly correlated to the placental expression of Abcb1a (r = 0.495; p < 0.005). Lopinavir 31-34 nuclear receptor subfamily 1, group I, member 2 Mus musculus 105-108 29064386-8 2017 Two-fold higher fetal:maternal LPV concentration ratios were also seen in the PXR +/+ as compared to the PXR -/- fetuses (p < 0.05), and this significantly correlated to the placental expression of Abcb1a (r = 0.495; p < 0.005). Lopinavir 31-34 ATP-binding cassette, sub-family B (MDR/TAP), member 1A Mus musculus 201-207 28569994-9 2017 Additional exploratory analyses predicted CYP3A inhibition effects on darunavir or lopinavir exposure in simulated hepatically impaired subjects. Lopinavir 83-92 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 42-47 28569994-11 2017 Exploratory simulations using the linked darunavir or lopinavir PBPK models indicated CYP3A inhibition may further increase darunavir or lopinavir exposure in patients with hepatic impairment. Lopinavir 54-63 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 86-91 28569994-11 2017 Exploratory simulations using the linked darunavir or lopinavir PBPK models indicated CYP3A inhibition may further increase darunavir or lopinavir exposure in patients with hepatic impairment. Lopinavir 137-146 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 86-91 27901085-5 2016 Ten amino acid residues in Gag correlated with lopinavir EC50 (p < 0.01), of which 380 K and 389I showed modest impacts on in vitro drug susceptibility. Lopinavir 47-56 Pr55(Gag) Human immunodeficiency virus 1 27-30 28134057-3 2017 OBJECTIVE: To compare the effect of raltegravir + ritonavir boosted lopinavir (RAL + LPV/r) to efavirenz/tenofovir disoproxil fumarate/emtricitabine (EFV/TDF/FTC) on HIV kinetics and T cell dynamics. Lopinavir 68-77 RAS like proto-oncogene A Homo sapiens 79-82 28038962-2 2017 The antiretrovirals ritonavir-boosted lopinavir (LPV/r) and nevirapine inhibit and induce CYP3A4, respectively. Lopinavir 38-47 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 90-96 28947797-2 2017 Similarly, GRL-09510 efficiently blocked the replication of HIV-1NL4-3 variants, which were capable of propagating at high-concentrations of atazanavir, lopinavir, and amprenavir (APV). Lopinavir 153-162 nuclear receptor subfamily 3 group C member 1 Homo sapiens 11-14 28718515-2 2017 Although primarily metabolized by CYP2B6 and -3A, efavirenz (EFV) and lopinavir/ritonavir (LPV/r) are substrates of P-glycoprotein and the solute carrier organic (SLCO) anion transporter, respectively. Lopinavir 70-79 cytochrome P450 family 2 subfamily B member 6 Homo sapiens 34-40 28592814-9 2017 Furthermore, lopinavir lowered the activin A-induced ERK1/2 phosphorylation. Lopinavir 13-22 mitogen-activated protein kinase 3 Homo sapiens 53-59 28579954-7 2017 The LPV-PC algorithm identified (i) a non-parametric LPV impulse response function (LPV IRF) for intrinsic stiffness and (ii) a LPV-Hammerstein model for reflex stiffness consisting of a LPV static nonlinearity followed by a time-invariant state-space model of reflex dynamics. Lopinavir 4-7 tripartite motif containing 63 Homo sapiens 88-91 26490422-5 2016 At a lopinavir concentration of 1000ng/mL (its suggested minimum effective concentration), a HIV-PRH6 concentration of 6mg/mL and incubation period of 60min were the optimal conditions. Lopinavir 5-14 prolactin releasing hormone Homo sapiens 97-100 27841971-7 2016 Also, the amount of prelamin A accumulation in response to lopinavir (an inhibitor of ZMPSTE24) was similar in wild-type and mutant fibroblasts. Lopinavir 59-68 zinc metallopeptidase STE24 Homo sapiens 86-94 27841971-8 2016 Thus, the LMNA lipodystrophy mutations that we examined did not lead to prelamin A accumulation, nor did they render those cells more susceptible to prelamin A accumulation when ZMPSTE24 was inhibited by lopinavir. Lopinavir 204-213 zinc metallopeptidase STE24 Homo sapiens 178-186 26595451-2 2016 Secretory DMP1 begins with a tripeptide of leucine-proline-valine (LPV) after the endoplasmic reticulum (ER)-entry signal peptide is cleaved. Lopinavir 67-70 dentin matrix protein 1 Mus musculus 10-14 26595451-3 2016 The goal of this study was to determine the role of the LPV motif in the secretion of DMP1. Lopinavir 56-59 dentin matrix protein 1 Mus musculus 86-90 27889708-3 2016 In cultured ECs, miR-34a expression was significantly increased by HIV-Tat protein and by the antiretroviral agents, lopinavir/ritonavir. Lopinavir 117-126 microRNA 34a Mus musculus 17-24 27620483-2 2016 GRL-10413 blocked the infectivity and replication of HIV-1NL4-3 variants selected by use of atazanavir, lopinavir, or amprenavir (APV) at concentrations of up to 5 muM (EC50 = 0.0021 to 0.0023 muM). Lopinavir 104-113 nuclear receptor subfamily 3 group C member 1 Homo sapiens 0-3 27431863-8 2016 RESULTS: We observed significant differences in intracellular concentrations of lopinavir, a PGP substrate, with higher concentrations in M1 cells. Lopinavir 80-89 phosphoglycolate phosphatase Homo sapiens 93-96 27543355-0 2016 Circumvention of P-gp and MRP2 mediated efflux of lopinavir by a histidine based dipeptide prodrug. Lopinavir 50-59 phosphoglycolate phosphatase Homo sapiens 17-21 27543355-0 2016 Circumvention of P-gp and MRP2 mediated efflux of lopinavir by a histidine based dipeptide prodrug. Lopinavir 50-59 ATP binding cassette subfamily C member 2 Homo sapiens 26-30 27543355-1 2016 PURPOSE: This study was aimed to develop a novel Histidine-Leucine-Lopinavir (His-Leu-LPV) dipeptide prodrug and evaluate its potential for circumvention of P-gp and MRP2-mediated efflux of lopinavir (LPV) indicated for HIV-1 infection. Lopinavir 190-199 ATP binding cassette subfamily C member 2 Homo sapiens 166-170 27543355-1 2016 PURPOSE: This study was aimed to develop a novel Histidine-Leucine-Lopinavir (His-Leu-LPV) dipeptide prodrug and evaluate its potential for circumvention of P-gp and MRP2-mediated efflux of lopinavir (LPV) indicated for HIV-1 infection. Lopinavir 86-89 phosphoglycolate phosphatase Homo sapiens 157-161 27543355-1 2016 PURPOSE: This study was aimed to develop a novel Histidine-Leucine-Lopinavir (His-Leu-LPV) dipeptide prodrug and evaluate its potential for circumvention of P-gp and MRP2-mediated efflux of lopinavir (LPV) indicated for HIV-1 infection. Lopinavir 86-89 ATP binding cassette subfamily C member 2 Homo sapiens 166-170 26307135-4 2016 Median intact FGF23 tended to increase with past use of both nonnucleoside reverse-transcriptase inhibitors and protease inhibitors, but tended to decrease with recent use of either tenofovir, efavirenz or lopinavir. Lopinavir 206-215 fibroblast growth factor 23 Homo sapiens 14-19 26968795-4 2016 We found that three distinct PIs, including ritonavir, atazanavir, and lopinavir, stimulated the expression of HO-1 protein and mRNA. Lopinavir 71-80 heme oxygenase 1 Homo sapiens 111-115 26307135-8 2016 Lower levels of intact FGF23 with recent use of tenofovir, efavirenz or lopinavir may reflect their adverse effects on bone and vitamin D metabolism relative to other drugs in their respective drug classes. Lopinavir 72-81 fibroblast growth factor 23 Homo sapiens 23-28 27142945-6 2016 CYP3A4*1B, CYP3A5*3, CYP3A5*6 and ABCC2 c.1249G>A which have been associated with LPV plasma concentration, showed no significant association. Lopinavir 85-88 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 27142945-6 2016 CYP3A4*1B, CYP3A5*3, CYP3A5*6 and ABCC2 c.1249G>A which have been associated with LPV plasma concentration, showed no significant association. Lopinavir 85-88 ATP binding cassette subfamily C member 2 Homo sapiens 34-39 26833162-2 2016 Here we investigated the phenotypic consequences of amino acid changes in Gag and protease on lopinavir (LPV) and ritonavir (RTV) susceptibility among pediatric patients failing PI therapy. Lopinavir 94-103 Pr55(Gag) Human immunodeficiency virus 1 74-77 26833162-2 2016 Here we investigated the phenotypic consequences of amino acid changes in Gag and protease on lopinavir (LPV) and ritonavir (RTV) susceptibility among pediatric patients failing PI therapy. Lopinavir 105-108 Pr55(Gag) Human immunodeficiency virus 1 74-77 26472771-10 2016 Positive correlations were observed for individual CSF antiretroviral activity in different cellular models with CSF concentrations of rilpivirine (P = 0.040 in 373 cells) and lopinavir (P = 0.048 in 373 cells), but not maraviroc. Lopinavir 176-185 colony stimulating factor 2 Homo sapiens 51-54 26818566-3 2016 Artemether and lumefantrine are metabolised by cytochrome P450 isoenzyme CYP3A4, which lopinavir/ritonavir inhibits, potentially causing clinically important drug-drug interactions. Lopinavir 87-96 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 73-79 26558720-6 2016 RESULTS: Excitatory amino-acid transporter-2 (EAAT2) expression was reduced in astrocytes treated with LPV or APV, especially LPV (P < 0.05), which was accompanied by reduced intracellular L-glutamate levels in LPV-treated cells (P < 0.05). Lopinavir 103-106 solute carrier family 1 member 2 Homo sapiens 9-44 26558720-6 2016 RESULTS: Excitatory amino-acid transporter-2 (EAAT2) expression was reduced in astrocytes treated with LPV or APV, especially LPV (P < 0.05), which was accompanied by reduced intracellular L-glutamate levels in LPV-treated cells (P < 0.05). Lopinavir 103-106 solute carrier family 1 member 2 Homo sapiens 46-51 26558720-6 2016 RESULTS: Excitatory amino-acid transporter-2 (EAAT2) expression was reduced in astrocytes treated with LPV or APV, especially LPV (P < 0.05), which was accompanied by reduced intracellular L-glutamate levels in LPV-treated cells (P < 0.05). Lopinavir 126-129 solute carrier family 1 member 2 Homo sapiens 9-44 26558720-6 2016 RESULTS: Excitatory amino-acid transporter-2 (EAAT2) expression was reduced in astrocytes treated with LPV or APV, especially LPV (P < 0.05), which was accompanied by reduced intracellular L-glutamate levels in LPV-treated cells (P < 0.05). Lopinavir 126-129 solute carrier family 1 member 2 Homo sapiens 46-51 26558720-6 2016 RESULTS: Excitatory amino-acid transporter-2 (EAAT2) expression was reduced in astrocytes treated with LPV or APV, especially LPV (P < 0.05), which was accompanied by reduced intracellular L-glutamate levels in LPV-treated cells (P < 0.05). Lopinavir 126-129 solute carrier family 1 member 2 Homo sapiens 9-44 26558720-6 2016 RESULTS: Excitatory amino-acid transporter-2 (EAAT2) expression was reduced in astrocytes treated with LPV or APV, especially LPV (P < 0.05), which was accompanied by reduced intracellular L-glutamate levels in LPV-treated cells (P < 0.05). Lopinavir 126-129 solute carrier family 1 member 2 Homo sapiens 46-51 26741368-11 2016 Finally, CYP3A4 docking with lopinavir and ritonavir in the absence and presence of methamphetamine showed that methamphetamine alters the docking of ritonavir, which is consistent with the results obtained from spectral binding and metabolism studies. Lopinavir 29-38 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 9-15 26463060-9 2016 The discrepancy between the methods was also apparent for conducted trials, e.g., lopinavir/ritonavir was predicted to increased BDQ exposure 22% by NCA and 188% by model-based methods. Lopinavir 82-91 CEA cell adhesion molecule 6 Homo sapiens 149-152 25989422-2 2015 Lopinavir [a substrate of cytochrome P450 3A (CYP3A)] and ritonavir (an inhibitor of CYP3A-mediatd metabolism) were used as a model drug and a model absorption enhancer, respectively. Lopinavir 0-9 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 26-44 26230332-0 2015 Brief Report: Significant Decreases in Both Total and Unbound Lopinavir and Amprenavir Exposures During Coadministration: ACTG Protocol A5143/A5147s Results. Lopinavir 62-71 actin gamma 1 Homo sapiens 122-126 26559816-9 2015 Seventy-eight percent (n = 2772) of patients received a prescription for PEP, consisting of Tenofovir/Emtracitabine (TVD) + Lopinavir/Ritonavir (LPV) in 74% of cases, followed by Zidovudine/Lamivudine (CBV) + LPV (10%) and TVD + Raltegravir (RAL) (8%). Lopinavir 124-133 prolyl endopeptidase Homo sapiens 73-76 26285765-8 2015 Importantly, lopinavir is a potent PMAT inhibitor and exhibited >120 fold selectivity toward PMAT (IC50 = 1.4 +- 0.2 microM) over OCT1 (IC50 = 174 +- 40 microM). Lopinavir 13-22 solute carrier family 29 member 4 Homo sapiens 35-39 26285765-8 2015 Importantly, lopinavir is a potent PMAT inhibitor and exhibited >120 fold selectivity toward PMAT (IC50 = 1.4 +- 0.2 microM) over OCT1 (IC50 = 174 +- 40 microM). Lopinavir 13-22 solute carrier family 29 member 4 Homo sapiens 96-100 26285765-12 2015 Further, we demonstrate that lopinavir can be used as a selective PMAT inhibitor to differentiate PMAT-mediated monoamine and organic cation transport from those mediated by OCT1-3. Lopinavir 29-38 solute carrier family 29 member 4 Homo sapiens 66-70 26285765-12 2015 Further, we demonstrate that lopinavir can be used as a selective PMAT inhibitor to differentiate PMAT-mediated monoamine and organic cation transport from those mediated by OCT1-3. Lopinavir 29-38 solute carrier family 29 member 4 Homo sapiens 98-102 26285765-12 2015 Further, we demonstrate that lopinavir can be used as a selective PMAT inhibitor to differentiate PMAT-mediated monoamine and organic cation transport from those mediated by OCT1-3. Lopinavir 29-38 solute carrier family 22 member 3 Homo sapiens 174-180 25989422-2 2015 Lopinavir [a substrate of cytochrome P450 3A (CYP3A)] and ritonavir (an inhibitor of CYP3A-mediatd metabolism) were used as a model drug and a model absorption enhancer, respectively. Lopinavir 0-9 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 46-51 25261710-0 2014 Dipeptide prodrug approach to evade efflux pumps and CYP3A4 metabolism of lopinavir. Lopinavir 74-83 cytochrome P450 3A12 Canis lupus familiaris 53-59 25831464-7 2015 RESULTS: In the on-treatment analysis, the median (interquartile range) increase in the CD4 count after 48 weeks was +193 (129-349) cells per microliter in the efavirenz arm, +197 (146-238) cells per microliter in the ritonavir-boosted atazanavir arm, and +205 (178-327) cells per microliter in the ritonavir-boosted lopinavir arm (P = 0.73). Lopinavir 317-326 CD4 molecule Homo sapiens 88-91 25407158-12 2015 The trend towards an inverse relationship between the change in the 6betaHF : F ratio and the change in the LPV AUC antepartum vs. postpartum suggests that CYP3A induction may be one mechanism behind altered LPV exposure during pregnancy. Lopinavir 108-111 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 156-161 25545854-0 2015 Anti-HIV drugs, lopinavir/ritonavir and atazanavir, modulate innate immune response triggered by Leishmania in macrophages: the role of NF-kappaB and PPAR-gamma. Lopinavir 16-25 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 136-145 25545854-0 2015 Anti-HIV drugs, lopinavir/ritonavir and atazanavir, modulate innate immune response triggered by Leishmania in macrophages: the role of NF-kappaB and PPAR-gamma. Lopinavir 16-25 peroxisome proliferator activated receptor gamma Mus musculus 150-160 25545854-7 2015 LPV reduced IL-10 and had no effect on IL-12p70, TNF and IL-23 secretion. Lopinavir 0-3 interleukin 10 Mus musculus 12-17 26681533-7 2015 RESULTS: A 48 hours exposure of human erythrocytes to lopinavir significantly increased the percentage of annexin-V-binding cells (>= 10 microg/ml), significantly decreased forward scatter (>=15 microg/ml), significantly increased hemolysis (>= 15 microg/ml), significantly increased Fluo3-fluorescence (20 microg/ml), and significantly increased DCFDA fluorescence (20 microg/ml) but did not significantly modify ceramide abundance. Lopinavir 54-63 annexin A5 Homo sapiens 106-115 26681533-8 2015 The effect of lopinavir on annexin-V-binding was significantly blunted, but not abolished by removal of extracellular Ca2+. Lopinavir 14-23 annexin A5 Homo sapiens 27-36 25391550-1 2015 Cytochrome P450 (CYP) 3A4 has been considered to be the most important enzyme system for metabolism of lopinavir/ritonavir (LPV/r), a widely used HIV protease inhibitor (PI) recommended during pregnancy. Lopinavir 103-112 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-25 25261710-1 2014 Oral absorption of lopinavir (LPV) is limited due to P-glycoprotein (P-gp) and multidrug resistance-associated protein2 (MRP2) mediated efflux by intestinal epithelial cells. Lopinavir 19-28 PGP Canis lupus familiaris 53-67 25261710-1 2014 Oral absorption of lopinavir (LPV) is limited due to P-glycoprotein (P-gp) and multidrug resistance-associated protein2 (MRP2) mediated efflux by intestinal epithelial cells. Lopinavir 19-28 PGP Canis lupus familiaris 69-73 25261710-1 2014 Oral absorption of lopinavir (LPV) is limited due to P-glycoprotein (P-gp) and multidrug resistance-associated protein2 (MRP2) mediated efflux by intestinal epithelial cells. Lopinavir 19-28 ATP binding cassette subfamily C member 2 Canis lupus familiaris 79-119 25261710-1 2014 Oral absorption of lopinavir (LPV) is limited due to P-glycoprotein (P-gp) and multidrug resistance-associated protein2 (MRP2) mediated efflux by intestinal epithelial cells. Lopinavir 19-28 ATP binding cassette subfamily C member 2 Canis lupus familiaris 121-125 25261710-1 2014 Oral absorption of lopinavir (LPV) is limited due to P-glycoprotein (P-gp) and multidrug resistance-associated protein2 (MRP2) mediated efflux by intestinal epithelial cells. Lopinavir 30-33 PGP Canis lupus familiaris 53-67 25261710-1 2014 Oral absorption of lopinavir (LPV) is limited due to P-glycoprotein (P-gp) and multidrug resistance-associated protein2 (MRP2) mediated efflux by intestinal epithelial cells. Lopinavir 30-33 PGP Canis lupus familiaris 69-73 25261710-1 2014 Oral absorption of lopinavir (LPV) is limited due to P-glycoprotein (P-gp) and multidrug resistance-associated protein2 (MRP2) mediated efflux by intestinal epithelial cells. Lopinavir 30-33 ATP binding cassette subfamily C member 2 Canis lupus familiaris 79-119 25261710-1 2014 Oral absorption of lopinavir (LPV) is limited due to P-glycoprotein (P-gp) and multidrug resistance-associated protein2 (MRP2) mediated efflux by intestinal epithelial cells. Lopinavir 30-33 ATP binding cassette subfamily C member 2 Canis lupus familiaris 121-125 25261710-2 2014 Moreover, LPV is extensively metabolized by CYP3A4 enzymes. Lopinavir 10-13 cytochrome P450 3A12 Canis lupus familiaris 44-50 25261710-3 2014 In the present study, dipeptide prodrug approach was employed to circumvent efflux pumps (P-gp and MRP2) and CYP3A4 mediated metabolism of LPV. Lopinavir 139-142 PGP Canis lupus familiaris 90-94 25261710-3 2014 In the present study, dipeptide prodrug approach was employed to circumvent efflux pumps (P-gp and MRP2) and CYP3A4 mediated metabolism of LPV. Lopinavir 139-142 ATP binding cassette subfamily C member 2 Canis lupus familiaris 99-103 25261710-3 2014 In the present study, dipeptide prodrug approach was employed to circumvent efflux pumps (P-gp and MRP2) and CYP3A4 mediated metabolism of LPV. Lopinavir 139-142 cytochrome P450 3A12 Canis lupus familiaris 109-115 25261710-5 2014 The extent of LPV and Val-Ile-LPV interactions with P-gp and MRP2 was studied by uptake and transport studies across MDCK-MDR1 and MDCK-MRP2 cells. Lopinavir 14-17 ATP binding cassette subfamily C member 2 Canis lupus familiaris 61-65 25461911-5 2014 However, markedly elevated XBP1 splicing was found in the placentas of three individuals on combined antiviral therapy, all receiving lopinavir or atazanavir. Lopinavir 134-143 X-box binding protein 1 Homo sapiens 27-31 25120613-5 2014 Translocation of glucose transporter 4 (GLUT4) following treatment with lopinavir or darunavir was observed using immunofluorescence. Lopinavir 72-81 solute carrier family 2 member 4 Homo sapiens 17-38 25397528-0 2014 Gag drug resistance mutations in HIV-1 subtype C patients, failing a protease inhibitor inclusive treatment regimen, with detectable lopinavir levels. Lopinavir 133-142 Pr55(Gag) Human immunodeficiency virus 1 0-3 25394093-1 2014 INTRODUCTION: Plasma trough concentrations of lopinavir (LPV) given as LPV/r 800/200 mg once daily (OD) are reduced in comparison with 400/100 mg twice daily (BID). Lopinavir 46-55 BH3 interacting domain death agonist Homo sapiens 159-162 25394094-0 2014 Potential implications of CYP3A4, CYP3A5 and MDR-1 genetic variants on the efficacy of Lopinavir/Ritonavir (LPV/r) monotherapy in HIV-1 patients. Lopinavir 87-96 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 26-32 25120613-0 2014 Lopinavir inhibits insulin signaling by promoting protein tyrosine phosphatase 1B expression. Lopinavir 0-9 insulin Homo sapiens 19-26 25120613-2 2014 The aim of the present study was to investigate the mechanism of the dysregulation of insulin signaling by two PIs, lopinavir and darunavir, by analyzing changes in the expression or activity of proteins associated with insulin signaling. Lopinavir 116-125 insulin Homo sapiens 86-93 25120613-5 2014 Translocation of glucose transporter 4 (GLUT4) following treatment with lopinavir or darunavir was observed using immunofluorescence. Lopinavir 72-81 solute carrier family 2 member 4 Homo sapiens 40-45 25120613-6 2014 While GLUT4 was recruited to the cellular membrane in control adipocytes following insulin stimulation, it was diffusely distributed in the cytosol in lopinavir-treated adipocytes. Lopinavir 151-160 solute carrier family 2 member 4 Homo sapiens 6-11 25120613-9 2014 Tyrosine phosphorylation of IRS1 was inhibited in lopinavir-treated adipocytes. Lopinavir 50-59 insulin receptor substrate 1 Homo sapiens 28-32 25120613-10 2014 The expression of PTP1B was upregulated in adipocytes pretreated with the PIs, particularly lopinavir, compared with those pretreated with a vehicle control. Lopinavir 92-101 protein tyrosine phosphatase non-receptor type 1 Homo sapiens 18-23 25120613-11 2014 The degree of regulation in insulin signaling differs between lopinavir and darunavir. Lopinavir 62-71 insulin Homo sapiens 28-35 25120613-12 2014 One mechanism by which lopinavir regulates insulin signaling is by the promotion of PTP1B expression. Lopinavir 23-32 insulin Homo sapiens 43-50 25120613-12 2014 One mechanism by which lopinavir regulates insulin signaling is by the promotion of PTP1B expression. Lopinavir 23-32 protein tyrosine phosphatase non-receptor type 1 Homo sapiens 84-89 24950369-0 2014 CYP3A4*22 (c.522-191 C>T; rs35599367) is associated with lopinavir pharmacokinetics in HIV-positive adults. Lopinavir 60-69 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 24950369-2 2014 We investigated the association of CYP3A4*22 with the pharmacokinetics of lopinavir through a population pharmacokinetic approach. Lopinavir 74-83 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 35-41 24950369-7 2014 We observed a 2.3-fold higher lopinavir trough concentration (Ctrough) in individuals with CYP3A4*22/*22, a 1.8-fold higher Ctrough with SLCO1B1 521CC and a 9.7-fold higher Ctrough in individuals homozygous for both single nucleotide polymorphisms, compared with noncarriers. Lopinavir 30-39 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 91-97 24950369-8 2014 A simulated dose-reduction scenario showed that 200/100 mg lopinavir/ritonavir was adequate to achieve therapeutic concentration in individuals with CYP3A4*22/*22 alone or in combination with SLCO1B1 521CC. Lopinavir 59-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 149-155 24950369-8 2014 A simulated dose-reduction scenario showed that 200/100 mg lopinavir/ritonavir was adequate to achieve therapeutic concentration in individuals with CYP3A4*22/*22 alone or in combination with SLCO1B1 521CC. Lopinavir 59-68 solute carrier organic anion transporter family member 1B1 Homo sapiens 192-199 24370933-5 2014 The lopinavir group was characterized by higher rates of HIV diagnosis in pregnancy and treatment indication for maternal health, lower CD4 counts, higher HIV RNA levels, less frequent antiretroviral treatment at conception and shorter duration of drug exposure during pregnancy. Lopinavir 4-13 CD4 molecule Homo sapiens 136-139 24075526-9 2014 Lopinavir/ritonavir, etravirine, and lamivudine administered through a jejunostomy resulted effective in decreasing HIV viral load and increasing CD4 lymphocyte count in a HIV patient who could not receive treatment orally. Lopinavir 0-9 CD4 molecule Homo sapiens 146-149 24380397-1 2014 CD4(+) count increase has been reported to be different with lopinavir/r (LPV/r) and efavirenz (EFV)-containing regimens. Lopinavir 61-70 CD4 molecule Homo sapiens 0-3 24986243-2 2014 In particular, CYP3A4 and CYP3A5 (interacting with more than 60% of licensed drugs) exhibit the most individual variations of gene expression, mostly caused by single nucleotide polymorphisms (SNPs) within the regulatory region of the CYP3A4 and CYP3A5 genes which might affect the level of enzyme production.In this study, we sought to improve the performance of sensitive screening for CYP3A polymorphism detection in twenty HIV-1 infected patients undergoing lopinavir/ritonavir (LPV/r) monotherapy. Lopinavir 462-471 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 15-21 24986243-2 2014 In particular, CYP3A4 and CYP3A5 (interacting with more than 60% of licensed drugs) exhibit the most individual variations of gene expression, mostly caused by single nucleotide polymorphisms (SNPs) within the regulatory region of the CYP3A4 and CYP3A5 genes which might affect the level of enzyme production.In this study, we sought to improve the performance of sensitive screening for CYP3A polymorphism detection in twenty HIV-1 infected patients undergoing lopinavir/ritonavir (LPV/r) monotherapy. Lopinavir 462-471 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 26-32 24986243-2 2014 In particular, CYP3A4 and CYP3A5 (interacting with more than 60% of licensed drugs) exhibit the most individual variations of gene expression, mostly caused by single nucleotide polymorphisms (SNPs) within the regulatory region of the CYP3A4 and CYP3A5 genes which might affect the level of enzyme production.In this study, we sought to improve the performance of sensitive screening for CYP3A polymorphism detection in twenty HIV-1 infected patients undergoing lopinavir/ritonavir (LPV/r) monotherapy. Lopinavir 462-471 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 235-241 24986243-2 2014 In particular, CYP3A4 and CYP3A5 (interacting with more than 60% of licensed drugs) exhibit the most individual variations of gene expression, mostly caused by single nucleotide polymorphisms (SNPs) within the regulatory region of the CYP3A4 and CYP3A5 genes which might affect the level of enzyme production.In this study, we sought to improve the performance of sensitive screening for CYP3A polymorphism detection in twenty HIV-1 infected patients undergoing lopinavir/ritonavir (LPV/r) monotherapy. Lopinavir 462-471 cytochrome P450 family 3 subfamily A member 5 Homo sapiens 246-252 24986243-2 2014 In particular, CYP3A4 and CYP3A5 (interacting with more than 60% of licensed drugs) exhibit the most individual variations of gene expression, mostly caused by single nucleotide polymorphisms (SNPs) within the regulatory region of the CYP3A4 and CYP3A5 genes which might affect the level of enzyme production.In this study, we sought to improve the performance of sensitive screening for CYP3A polymorphism detection in twenty HIV-1 infected patients undergoing lopinavir/ritonavir (LPV/r) monotherapy. Lopinavir 462-471 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 15-20 24413339-1 2014 Recently, it has been reported that anti-viral drugs, such as indinavir and lopinavir (originally targeted for HIV), also inhibit E6-mediated proteasomal degradation of mutant p53 in E6-transfected C33A cells. Lopinavir 76-85 tumor protein p53 Homo sapiens 176-179 24753704-7 2014 NF-kappaB activity was increased in the VILI group compared with the LPS and LPV groups (P < 0.05), and significantly decreased in the Cyst+VILI group compared to the VILI group (P = 0.029). Lopinavir 77-80 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 0-9 24259240-0 2014 Insulin resistance and lipid profiles in HIV-infected Thai children receiving lopinavir/ritonavir-based highly active antiretroviral therapy. Lopinavir 78-87 insulin Homo sapiens 0-7 24259240-1 2014 BACKGROUND: Lopinavir/ritonavir (LPV/r) is associated with insulin resistance (IR). Lopinavir 12-21 insulin Homo sapiens 59-66 24727459-1 2014 Poor systemic concentrations of lopinavir (LPV) following oral administration occur due to high cellular efflux by P-glycoprotein (P-gp) and multidrug resistance-associated proteins (MRPs) and extensive metabolism by CYP3A4 enzymes. Lopinavir 32-41 ATP binding cassette subfamily B member 1 Homo sapiens 115-129 24727459-1 2014 Poor systemic concentrations of lopinavir (LPV) following oral administration occur due to high cellular efflux by P-glycoprotein (P-gp) and multidrug resistance-associated proteins (MRPs) and extensive metabolism by CYP3A4 enzymes. Lopinavir 32-41 ATP binding cassette subfamily B member 1 Homo sapiens 131-135 24727459-1 2014 Poor systemic concentrations of lopinavir (LPV) following oral administration occur due to high cellular efflux by P-glycoprotein (P-gp) and multidrug resistance-associated proteins (MRPs) and extensive metabolism by CYP3A4 enzymes. Lopinavir 32-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 217-223 24727459-1 2014 Poor systemic concentrations of lopinavir (LPV) following oral administration occur due to high cellular efflux by P-glycoprotein (P-gp) and multidrug resistance-associated proteins (MRPs) and extensive metabolism by CYP3A4 enzymes. Lopinavir 43-46 ATP binding cassette subfamily B member 1 Homo sapiens 115-129 24727459-1 2014 Poor systemic concentrations of lopinavir (LPV) following oral administration occur due to high cellular efflux by P-glycoprotein (P-gp) and multidrug resistance-associated proteins (MRPs) and extensive metabolism by CYP3A4 enzymes. Lopinavir 43-46 ATP binding cassette subfamily B member 1 Homo sapiens 131-135 24727459-1 2014 Poor systemic concentrations of lopinavir (LPV) following oral administration occur due to high cellular efflux by P-glycoprotein (P-gp) and multidrug resistance-associated proteins (MRPs) and extensive metabolism by CYP3A4 enzymes. Lopinavir 43-46 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 217-223 23973637-0 2013 Comparative analysis of ER stress response into HIV protease inhibitors: lopinavir but not darunavir induces potent ER stress response via ROS/JNK pathway. Lopinavir 73-82 mitogen-activated protein kinase 8 Homo sapiens 143-146 24335466-8 2014 Further investigation of the five potent repressors revealed that transcriptional repression of BSEP by lopinavir and troglitazone may occur through their interaction with FXR, whereas others are via FXR-independent yet unidentified pathways. Lopinavir 104-113 ATP binding cassette subfamily B member 11 Homo sapiens 96-100 24335466-8 2014 Further investigation of the five potent repressors revealed that transcriptional repression of BSEP by lopinavir and troglitazone may occur through their interaction with FXR, whereas others are via FXR-independent yet unidentified pathways. Lopinavir 104-113 nuclear receptor subfamily 1 group H member 4 Homo sapiens 172-175 24291501-0 2014 P1 and P1" para-fluoro phenyl groups show enhanced binding and favorable predicted pharmacological properties: structure-based virtual screening of extended lopinavir analogs against multi-drug resistant HIV-1 protease. Lopinavir 157-166 crystallin gamma F, pseudogene Homo sapiens 0-10 24080647-3 2013 GRL-04810 and GRL-05010 also blocked the infectivity and replication of each of the HIV-1NL4-3 variants selected by up to 5 muM lopinavir (EC50s, 0.03 and 0.03 muM, respectively) and atazanavir (EC50s, 0.02 and 0.04 muM, respectively). Lopinavir 128-137 nuclear receptor subfamily 3 group C member 1 Homo sapiens 0-3 24080647-3 2013 GRL-04810 and GRL-05010 also blocked the infectivity and replication of each of the HIV-1NL4-3 variants selected by up to 5 muM lopinavir (EC50s, 0.03 and 0.03 muM, respectively) and atazanavir (EC50s, 0.02 and 0.04 muM, respectively). Lopinavir 128-137 nuclear receptor subfamily 3 group C member 1 Homo sapiens 14-17 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. Lopinavir 27-36 AKT serine/threonine kinase 1 Homo sapiens 130-133 23973637-4 2013 We show here that LPV induces the most potent CHOP expression, ER stress marker, among the 9 Food and Drug Administration (FDA)-approved PIs in human peripheral blood mononuclear cells, several human epithelial cells, and mouse embryonic fibroblasts. Lopinavir 18-21 DNA damage inducible transcript 3 Homo sapiens 46-50 23973637-5 2013 LPV induced the most potent ROS production and JNK activation in 9 PIs. Lopinavir 0-3 mitogen-activated protein kinase 8 Homo sapiens 47-50 23260386-9 2013 Atazanavir/r QD and lopinavir/r BID were found to be <<dominated>> by darunavir/r) and, consequently, were outside the efficiency frontier of PI/r-based first-line treatment. Lopinavir 20-29 BH3 interacting domain death agonist Homo sapiens 32-35 23836171-8 2013 Amprenavir, atazanavir, darunavir, efavirenz, ritonavir, and lopinavir were found to activate hPXR, whereas abacavir, efavirenz, and nevirapine were found to activate hCAR. Lopinavir 61-70 nuclear receptor subfamily 1 group I member 2 Homo sapiens 94-98 23836171-8 2013 Amprenavir, atazanavir, darunavir, efavirenz, ritonavir, and lopinavir were found to activate hPXR, whereas abacavir, efavirenz, and nevirapine were found to activate hCAR. Lopinavir 61-70 CXADR Ig-like cell adhesion molecule Homo sapiens 167-171 26251758-0 2013 Lopinavir/Ritonavir Impairs Physical Strength in Association with Reduced Igf1 Expression in Skeletal Muscle of Older Mice. Lopinavir 0-9 insulin-like growth factor 1 Mus musculus 74-78 23221983-7 2013 During pregnancy, total area under the time concentration (AUC0-12h) for LPV was significantly lower than postpartum (PK1, PK2, or PK3 vs. PK4, P = 0.005). Lopinavir 73-76 prokineticin 2 Homo sapiens 123-126 23528223-0 2013 Influence of MDR1 C1236T polymorphism on lopinavir plasma concentration and virological response in HIV-1-infected children. Lopinavir 41-50 ATP binding cassette subfamily B member 1 Homo sapiens 13-17 23528223-2 2013 We investigated whether polymorphisms in MDR1 (T-129C, C1236T and C3435T) and PXR (C63396T) affect lopinavir plasma concentration and the virological or immunological response to HAART in HIV-1-infected children. Lopinavir 99-108 ATP binding cassette subfamily B member 1 Homo sapiens 41-45 23528223-2 2013 We investigated whether polymorphisms in MDR1 (T-129C, C1236T and C3435T) and PXR (C63396T) affect lopinavir plasma concentration and the virological or immunological response to HAART in HIV-1-infected children. Lopinavir 99-108 nuclear receptor subfamily 1 group I member 2 Homo sapiens 78-81 23528223-11 2013 Heterozygotes 1236CT might have an altered level of P-gp expression/activity in enterocytes and CD4(+) T lymphocytes that limits the absorption of LPV leading to an impaired virological suppression. Lopinavir 147-150 phosphoglycolate phosphatase Homo sapiens 52-56 23403426-2 2013 GRL-0519 blocked the infectivity and replication of HIV-1NL4-3 variants selected by up to a 5 muM concentration of ritonavir, lopinavir, or atazanavir (EC50, 0.0028 to 0.0033 muM). Lopinavir 126-135 nuclear receptor subfamily 3 group C member 1 Homo sapiens 0-3 26393009-3 2013 Here, we describe the situation that arose in a pharmacokinetic study on the use of two different doses of rifabutin in patients with human immunodeficiency virus-associated tuberculosis who initiated antiretroviral therapy (ART) with a lopinavir-ritonavir-based regimen in South Africa and Viet Nam. Lopinavir 237-246 SH3 and cysteine rich domain 3 Homo sapiens 296-299 23503447-1 2013 OBJECTIVE: Among HIV-positive patients prescribed ritonavir-boosted lopinavir, SLCO1B1 521T C (rs4149056) is associated with increased plasma lopinavir exposure. Lopinavir 68-77 solute carrier organic anion transporter family member 1B1 Homo sapiens 79-86 23503447-1 2013 OBJECTIVE: Among HIV-positive patients prescribed ritonavir-boosted lopinavir, SLCO1B1 521T C (rs4149056) is associated with increased plasma lopinavir exposure. Lopinavir 142-151 solute carrier organic anion transporter family member 1B1 Homo sapiens 79-86 23503447-8 2013 Of targeted polymorphisms, SLCO1B1 521T C tended to be associated with higher lopinavir concentrations, with a 1.38-fold increase in the mean per C allele (95% confidence interval, 0.97-1.96; n = 98; P = 0.07). Lopinavir 78-87 solute carrier organic anion transporter family member 1B1 Homo sapiens 27-34 23503447-11 2013 CONCLUSIONS: With ritonavir-boosted PIs, a SLCO1B1 polymorphism that predicts higher lopinavir trough concentrations seems to predict lower amprenavir trough concentrations. Lopinavir 85-94 solute carrier organic anion transporter family member 1B1 Homo sapiens 43-50 23582562-5 2013 Protease inhibitors, particularly indinavir and lopinavir, were commonly associated with hypercholesterolemia, high LDL-c, low HDL-c, and hypertriglyceridemia. Lopinavir 48-57 component of oligomeric golgi complex 2 Homo sapiens 116-121 24110489-3 2013 We aimed to develop a biologically relevant pharmacokinetic model of lopinavir with a description of a CYP3A4-mediated first pass metabolism and enterohepatic circulation (EHC). Lopinavir 69-78 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 103-109 23032410-12 2013 CONCLUSION: Despite full viral load-suppression in blood and CSF, antiretroviral monotherapy with lopinavir/ritonavir can raise CSF levels of S100B, suggesting astrocytic damage. Lopinavir 98-107 S100 calcium binding protein B Homo sapiens 142-147 23559827-8 2013 After extensive and controlled in silico analysis it has been observed that the analogue LOPI1 binds to Nef protein (2NEF) at CD4 interacting site residues giving minimum binding energy of -7.68 Kcal/mole, low Ki value of 2.34 muM, maximum number of hydrogen bonds (8), good absorption, distribution, metabolism and excretion properties, and less toxicity in comparison with the standard Lopinavir against HIV1 protease (1HPV). Lopinavir 388-397 Nef Human immunodeficiency virus 1 104-107 23091188-2 2013 Antiretroviral protease inhibitors lopinavir (LPV) and ritonavir (RTV) are reported BSEP inhibitors. Lopinavir 35-44 ATP binding cassette subfamily B member 11 Rattus norvegicus 84-88 23091188-2 2013 Antiretroviral protease inhibitors lopinavir (LPV) and ritonavir (RTV) are reported BSEP inhibitors. Lopinavir 46-49 ATP binding cassette subfamily B member 11 Rattus norvegicus 84-88 23559827-8 2013 After extensive and controlled in silico analysis it has been observed that the analogue LOPI1 binds to Nef protein (2NEF) at CD4 interacting site residues giving minimum binding energy of -7.68 Kcal/mole, low Ki value of 2.34 muM, maximum number of hydrogen bonds (8), good absorption, distribution, metabolism and excretion properties, and less toxicity in comparison with the standard Lopinavir against HIV1 protease (1HPV). Lopinavir 388-397 Nef Human immunodeficiency virus 1 118-121 23559827-8 2013 After extensive and controlled in silico analysis it has been observed that the analogue LOPI1 binds to Nef protein (2NEF) at CD4 interacting site residues giving minimum binding energy of -7.68 Kcal/mole, low Ki value of 2.34 muM, maximum number of hydrogen bonds (8), good absorption, distribution, metabolism and excretion properties, and less toxicity in comparison with the standard Lopinavir against HIV1 protease (1HPV). Lopinavir 388-397 CD4 molecule Homo sapiens 126-129 23533630-8 2013 We also identified through the use of primary adipocytes of CHOP(-/-) mice that CHOP, the major transcriptional factor of the ER stress signaling pathway, is involved in lopinavir/ritonavir-induced inhibition of cell differentiation in adipocytes. Lopinavir 170-179 DNA-damage inducible transcript 3 Mus musculus 80-84 22308076-1 2012 Lopinavir (LPV), a newer HIV protease inhibitor, has poor bioavailability being a substrate of both cytochrome P450 3A enzyme system (CYP3A) and permeability-glycoprotein (P-gp). Lopinavir 11-14 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 134-139 23533630-8 2013 We also identified through the use of primary adipocytes of CHOP(-/-) mice that CHOP, the major transcriptional factor of the ER stress signaling pathway, is involved in lopinavir/ritonavir-induced inhibition of cell differentiation in adipocytes. Lopinavir 170-179 DNA-damage inducible transcript 3 Mus musculus 60-64 22308076-1 2012 Lopinavir (LPV), a newer HIV protease inhibitor, has poor bioavailability being a substrate of both cytochrome P450 3A enzyme system (CYP3A) and permeability-glycoprotein (P-gp). Lopinavir 0-9 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 134-139 22550269-7 2012 The effect of aminobenzotriazole (a nonspecific cytochrome P450 inhibitor) on lopinavir permeability was comparable with using ritonavir, whereas there was no effect for indinavir and darunavir. Lopinavir 78-87 cytochrome P450, family 21, subfamily a, polypeptide 1 Mus musculus 48-63 21719718-5 2012 The lopinavir/ritonavir dose of 500/125 mg bid administered with efavirenz most closely approximates the pharmacokinetic exposure of lopinavir/ritonavir 400/100 mg bid administered alone. Lopinavir 4-13 BH3 interacting domain death agonist Homo sapiens 43-46 21719718-5 2012 The lopinavir/ritonavir dose of 500/125 mg bid administered with efavirenz most closely approximates the pharmacokinetic exposure of lopinavir/ritonavir 400/100 mg bid administered alone. Lopinavir 4-13 BH3 interacting domain death agonist Homo sapiens 164-167 21719718-5 2012 The lopinavir/ritonavir dose of 500/125 mg bid administered with efavirenz most closely approximates the pharmacokinetic exposure of lopinavir/ritonavir 400/100 mg bid administered alone. Lopinavir 133-142 BH3 interacting domain death agonist Homo sapiens 43-46 21826404-5 2012 Atazanavir, ritonavir, and saquinavir modestly inhibited of Abeta degradation, while lopinavir, nelfinavir, and ritonavir enhanced secretion of undigested Abeta after phagocytosis. Lopinavir 85-94 amyloid beta precursor protein Homo sapiens 155-160 22727648-2 2012 Recent clinical data on efavirenz and nevirapine in naive patients confirms their effectiveness compared to protease inhibitors such as lopinavir/r (ACTG 5142) or atazanavir/r (ACTG 5202) for efavirenz, or such as atazanavir/r (ARTEN trial) for nevirapine. Lopinavir 136-145 actin gamma 1 Homo sapiens 149-153 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. Lopinavir 0-9 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. Lopinavir 0-9 beta-secretase 1 Homo sapiens 210-215 22135137-13 2012 CONCLUSIONS: In this pilot study, the addition of enfuvirtide to a lopinavir-based HAART was shown to be associated with a significantly faster and greater immunological recovery in newly discovered HIV-positive patients with very low CD4+ cell counts. Lopinavir 67-76 CD4 molecule Homo sapiens 235-238 22421793-18 2012 Other known strong inhibitors, such as lopinavir, oltipraz, quercetin, raloxifene, and troglitazone, were among 18 compounds classified as plausible potent inhibitors of CYP3A4. Lopinavir 39-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 170-176 21732894-3 2011 In the CASTLE study, patients with the most advanced HIV disease (CD4 cell count <50 cells/mm(3)) showed that 78% (45/58) vs. 58% (28/48) of the patients achieved HIV RNA <50 copies/mL in the intent-to-treat analysis at week 96 for atazanavir/ritonavir and lopinavir/ritonavir, respectively. Lopinavir 263-272 CD4 molecule Homo sapiens 66-69 22293506-11 2012 Lopinavir/ritonavir adversely affected differentiation and lipid content, mitochondrial function, ROS production and insulin sensitivity, and the effect of atazanavir/ritonavir was intermediate. Lopinavir 0-9 insulin Homo sapiens 117-124 22477766-0 2012 Estimation of the effect of SLCO1B1 polymorphisms on lopinavir plasma concentration in HIV-infected adults. Lopinavir 53-62 solute carrier organic anion transporter family member 1B1 Homo sapiens 28-35 22477766-2 2012 The SLCO1B1 521T>C (rs4149056) single nucleotide polymorphism (SNP) has been consistently associated with reduced transport activity in vivo, and we previously showed an association of this polymorphism with lopinavir plasma concentrations. Lopinavir 211-220 solute carrier organic anion transporter family member 1B1 Homo sapiens 4-11 22477766-10 2012 CONCLUSIONS: These data show an association between SLCO1B1 521T>C and lopinavir clearance. Lopinavir 74-83 solute carrier organic anion transporter family member 1B1 Homo sapiens 52-59 22814125-0 2012 Lopinavir/ritonavir monotherapy after 24 weeks of second-line antiretroviral therapy in Africa: a randomized controlled trial (SARA). Lopinavir 0-9 zinc finger FYVE-type containing 9 Homo sapiens 127-131 21953914-0 2012 CYP3A4-mediated lopinavir bioactivation and its inhibition by ritonavir. Lopinavir 16-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 22027652-8 2011 RESULTS: At a comparable expression level, the ABCC2 4544A clone showed higher accumulation of LPV, calcein and carboxyfluorescein diacetate as well as reduced ABCC2-mediated efflux of LPV compared with the ABCC2 4544G clone. Lopinavir 95-98 ATP binding cassette subfamily C member 2 Homo sapiens 47-52 22027652-8 2011 RESULTS: At a comparable expression level, the ABCC2 4544A clone showed higher accumulation of LPV, calcein and carboxyfluorescein diacetate as well as reduced ABCC2-mediated efflux of LPV compared with the ABCC2 4544G clone. Lopinavir 185-188 ATP binding cassette subfamily C member 2 Homo sapiens 47-52 22027652-8 2011 RESULTS: At a comparable expression level, the ABCC2 4544A clone showed higher accumulation of LPV, calcein and carboxyfluorescein diacetate as well as reduced ABCC2-mediated efflux of LPV compared with the ABCC2 4544G clone. Lopinavir 185-188 ATP binding cassette subfamily C member 2 Homo sapiens 160-165 22027652-8 2011 RESULTS: At a comparable expression level, the ABCC2 4544A clone showed higher accumulation of LPV, calcein and carboxyfluorescein diacetate as well as reduced ABCC2-mediated efflux of LPV compared with the ABCC2 4544G clone. Lopinavir 185-188 ATP binding cassette subfamily C member 2 Homo sapiens 160-165 21732894-6 2011 Also in this CD4 cell count stratum, grades 2-4 treatment-related adverse events occurred in 25% in the atazanavir/ritonavir group and in 43% of lopinavir/ritonavir group, and the rate was also higher than in the higher CD4 cell count strata within the lopinavir/ritonavir treatment group (range: 29-34%). Lopinavir 145-154 CD4 molecule Homo sapiens 13-16 21732894-6 2011 Also in this CD4 cell count stratum, grades 2-4 treatment-related adverse events occurred in 25% in the atazanavir/ritonavir group and in 43% of lopinavir/ritonavir group, and the rate was also higher than in the higher CD4 cell count strata within the lopinavir/ritonavir treatment group (range: 29-34%). Lopinavir 253-262 CD4 molecule Homo sapiens 13-16 21742899-7 2011 Expression of relevant transporters, such as Multidrug resistance protein 1 (Mdr1), and cytochrome P450 3a2 (Cyp3a2), which metabolizes LPV in rodents, was measured in maternal liver via quantitative reverse transcriptase polymerase chain reaction and Western blot analysis. Lopinavir 136-139 cytochrome P450, family 3, subfamily a, polypeptide 2 Rattus norvegicus 88-107 21742899-7 2011 Expression of relevant transporters, such as Multidrug resistance protein 1 (Mdr1), and cytochrome P450 3a2 (Cyp3a2), which metabolizes LPV in rodents, was measured in maternal liver via quantitative reverse transcriptase polymerase chain reaction and Western blot analysis. Lopinavir 136-139 cytochrome P450, family 3, subfamily a, polypeptide 2 Rattus norvegicus 109-115 21491455-4 2011 Using nonlinear mixed-effects modeling, we could separately quantify the effects of intestinal CYP3A4 expression, hepatic CYP3A4 expression, and the presence of ritonavir on both the absorption and elimination of lopinavir, which was previously not possible using noncompartmental methods. Lopinavir 213-222 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 95-101 21743379-0 2011 CYP3A5, ABCB1, and SLCO1B1 polymorphisms and pharmacokinetics and virologic outcome of lopinavir/ritonavir in HIV-infected children. Lopinavir 87-96 solute carrier organic anion transporter family member 1B1 Homo sapiens 19-26 21491455-0 2011 An integrated pharmacokinetic model for the influence of CYP3A4 expression on the in vivo disposition of lopinavir and its modulation by ritonavir. Lopinavir 105-114 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 57-63 21491455-4 2011 Using nonlinear mixed-effects modeling, we could separately quantify the effects of intestinal CYP3A4 expression, hepatic CYP3A4 expression, and the presence of ritonavir on both the absorption and elimination of lopinavir, which was previously not possible using noncompartmental methods. Lopinavir 213-222 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 122-128 21491455-2 2011 Our aim was to separately quantify the role of intestinal and hepatic cytochrome P450 3A (CYP3A4) expression on lopinavir disposition in a novel mouse model. Lopinavir 112-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 90-96 21491455-5 2011 Intestinal, but not hepatic, CYP3A4-related first-pass metabolism was the major barrier for systemic entry of lopinavir. Lopinavir 110-119 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 29-35 21491455-3 2011 Lopinavir and ritonavir were administered to mice selectively expressing human CYP3A4 in the intestine and/or liver. Lopinavir 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 79-85 21491455-6 2011 Relative oral bioavailability of lopinavir in mice expressing both hepatic and intestinal CYP3A4 was only 1.3% when compared with mice that were CYP3A deficient. Lopinavir 33-42 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 90-96 21491455-6 2011 Relative oral bioavailability of lopinavir in mice expressing both hepatic and intestinal CYP3A4 was only 1.3% when compared with mice that were CYP3A deficient. Lopinavir 33-42 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 90-95 21491455-8 2011 Hepatic CYP3A4 related systemic clearance was inversely related to ritonavir exposure and not only hepatic but also intestinal CYP3A4 expression contributed to systemic clearance of lopinavir. Lopinavir 182-191 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 8-14 21491455-8 2011 Hepatic CYP3A4 related systemic clearance was inversely related to ritonavir exposure and not only hepatic but also intestinal CYP3A4 expression contributed to systemic clearance of lopinavir. Lopinavir 182-191 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 127-133 21239995-0 2011 Low lopinavir plasma or hair concentrations explain second-line protease inhibitor failures in a resource-limited setting. Lopinavir 4-13 serpin family A member 13, pseudogene Homo sapiens 64-82 21819807-1 2011 The HIV protease inhibitor lopinavir presents a wide inter-individual variability related to liver and intestinal metabolism involving CYP3A. Lopinavir 27-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 135-140 27393203-1 2011 The HIV protease inhibitor lopinavir presents a wide inter-individual variability related to liver and intestinal metabolism involving CYP3A. Lopinavir 27-36 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 135-140 21172791-9 2011 Lopinavir pharmacokinetic parameters were significantly lower for Regimens 2 and 3: GMR (90% CI) AUC(0-12), 0.74 (0.65-0.84) and 0.45 (0.40-0.51); C(max), 0.75 (0.66-0.85) and 0.54 (0.40-0.60); and C(trough), 0.74 (0.62-0.89) and 0.30 (0.25-0.36), respectively. Lopinavir 0-9 colony stimulating factor 2 receptor subunit alpha Homo sapiens 84-87 20722750-5 2011 Further, immunohistochemical analysis of raft cultures was performed to assess the effect of lopinavir/ritonavir on the expression of key differentiation and proliferation markers including cytokeratins, proliferating cell nuclear antigen (PCNA) and cyclin A. Lopinavir 93-102 proliferating cell nuclear antigen Homo sapiens 204-245 21148235-6 2011 Mean change in CD4 cell count from baseline to week 96 was 265 cells/mm(3) for women and 269 cells/mm(3) for men on atazanavir/ritonavir and 298 cells/mm(3) for women and 286 cells/mm(3) for men on lopinavir/ritonavir. Lopinavir 198-207 CD4 molecule Homo sapiens 15-18 20878151-2 2011 Lopinavir is extensively metabolized by the hepatic cytochrome P450 3A4, and the pharmacokinetics of this protease inhibitor (PI) could be influenced by liver impairment. Lopinavir 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 52-71 22155905-8 2011 Saquinavir and lopinavir, HIV protease inhibitors, reduced MMP-9 activity in THP-1 and LX-2 cells, respectively. Lopinavir 15-24 matrix metallopeptidase 9 Homo sapiens 59-64 20596751-0 2011 Lopinavir inhibits meningioma cell proliferation by Akt independent mechanism. Lopinavir 0-9 AKT serine/threonine kinase 1 Homo sapiens 52-55 20596751-5 2011 Lopinavir effects on basal and PDGF-stimulated phosphorylation of the Akt-mTOR, MEK1/2-MAPK and STAT3 pathways, phosphorylation of Rb, Caspase 3 activation and reductions in survivin were assessed by Western blots. Lopinavir 0-9 AKT serine/threonine kinase 1 Homo sapiens 70-73 20596751-5 2011 Lopinavir effects on basal and PDGF-stimulated phosphorylation of the Akt-mTOR, MEK1/2-MAPK and STAT3 pathways, phosphorylation of Rb, Caspase 3 activation and reductions in survivin were assessed by Western blots. Lopinavir 0-9 mechanistic target of rapamycin kinase Homo sapiens 74-78 20596751-5 2011 Lopinavir effects on basal and PDGF-stimulated phosphorylation of the Akt-mTOR, MEK1/2-MAPK and STAT3 pathways, phosphorylation of Rb, Caspase 3 activation and reductions in survivin were assessed by Western blots. Lopinavir 0-9 mitogen-activated protein kinase kinase 1 Homo sapiens 80-86 20596751-5 2011 Lopinavir effects on basal and PDGF-stimulated phosphorylation of the Akt-mTOR, MEK1/2-MAPK and STAT3 pathways, phosphorylation of Rb, Caspase 3 activation and reductions in survivin were assessed by Western blots. Lopinavir 0-9 signal transducer and activator of transcription 3 Homo sapiens 96-101 21685539-0 2011 Lopinavir up-regulates expression of the antiviral protein ribonuclease L in human papillomavirus-positive cervical carcinoma cells. Lopinavir 0-9 ribonuclease L Homo sapiens 59-73 21685539-7 2011 Ribonuclease L (RNASEL) protein was shown to be up-regulated in lopinavir-treated SiHa cells, which was confirmed by PCR and western blot. Lopinavir 64-73 ribonuclease L Homo sapiens 0-14 21685539-7 2011 Ribonuclease L (RNASEL) protein was shown to be up-regulated in lopinavir-treated SiHa cells, which was confirmed by PCR and western blot. Lopinavir 64-73 ribonuclease L Homo sapiens 16-22 21685539-8 2011 Targeted silencing of RNASEL reduced the sensitivity of SiHa cells to lopinavir. Lopinavir 70-79 ribonuclease L Homo sapiens 22-28 22155905-8 2011 Saquinavir and lopinavir, HIV protease inhibitors, reduced MMP-9 activity in THP-1 and LX-2 cells, respectively. Lopinavir 15-24 GLI family zinc finger 2 Homo sapiens 77-82 21685539-10 2011 CONCLUSIONS: These data are consistent with the toxicity of lopinavir against HPV-positive cervical carcinoma cells being related to its ability to block viral proteasome activation and induce an up-regulation of the antiviral protein RNASEL. Lopinavir 60-69 ribonuclease L Homo sapiens 235-241 21685539-11 2011 This is supported by the drug"s selective toxicity and up-regulation of RNASEL in E6/E7 immortalised keratinocytes combined with the increased resistance to lopinavir observed in SiHa cells following silencing of RNASEL gene expression. Lopinavir 157-166 ribonuclease L Homo sapiens 213-219 21949754-0 2011 Polymorphism in Gag gene cleavage sites of HIV-1 non-B subtype and virological outcome of a first-line lopinavir/ritonavir single drug regimen. Lopinavir 103-112 Pr55(Gag) Human immunodeficiency virus 1 16-19 21212519-0 2011 Evidence for time-dependent interactions between ritonavir and lopinavir/ritonavir plasma levels following P-glycoprotein inhibition in Sprague-Dawley rats. Lopinavir 63-72 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 107-121 22312553-2 2011 We aimed to assess cardiac conduction safety of coadministration of the CYP3A4 inhibitor lopinavir/ritonavir (LPV/r) and the CYP3A4 substrate artemether-lumefantrine (AL) in HIV-positive Ugandans. Lopinavir 89-98 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-78 20595906-5 2010 CONCLUSIONS: A single boosting dose of ritonavir does not alter insulin sensitivity, suggesting lopinavir is likely responsible for the induction of insulin resistance demonstrated in prior short-term studies of lopinavir/ritonavir. Lopinavir 96-105 insulin Homo sapiens 149-156 20861742-7 2010 Some PXR variants displayed lower fosamprenavir- and lopinavir-induced CYP3A4 promoter activity than the PXR reference sequence, whereas efavirenz and nelfinavir induction was unchanged. Lopinavir 53-62 nuclear receptor subfamily 1 group I member 2 Homo sapiens 5-8 20861742-7 2010 Some PXR variants displayed lower fosamprenavir- and lopinavir-induced CYP3A4 promoter activity than the PXR reference sequence, whereas efavirenz and nelfinavir induction was unchanged. Lopinavir 53-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 71-77 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. Lopinavir 26-35 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. Lopinavir 26-35 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. Lopinavir 26-35 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. Lopinavir 26-35 nuclear receptor subfamily 1 group I member 2 Homo sapiens 200-203 20595906-1 2010 BACKGROUND: Some HIV protease inhibitors (PIs), including full-dose ritonavir (800 mg) and ritonavir-boosted lopinavir, acutely induce insulin resistance in the absence of HIV infection and changes in body composition. Lopinavir 109-118 insulin Homo sapiens 135-142 20841991-2 2010 Lopinavir, the most potent inducer of interleukin (IL)-8 expression, also inhibited dsRNA-induced monocyte chemotactic protein 1 expression. Lopinavir 0-9 C-X-C motif chemokine ligand 8 Homo sapiens 38-56 20841991-2 2010 Lopinavir, the most potent inducer of interleukin (IL)-8 expression, also inhibited dsRNA-induced monocyte chemotactic protein 1 expression. Lopinavir 0-9 C-C motif chemokine ligand 2 Homo sapiens 98-128 20841991-3 2010 Further analyses demonstrated that nuclear factor-kappaB is required for lopinavir"s induction of IL-8. Lopinavir 73-82 C-X-C motif chemokine ligand 8 Homo sapiens 98-102 20375850-0 2010 Association between lipodystrophy and leptin in human immunodeficiency virus-1-infected children receiving lopinavir/ritonavir-based therapy. Lopinavir 107-116 leptin Homo sapiens 38-44 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). Lopinavir 173-182 solute carrier organic anion transporter family member 2B1 Homo sapiens 31-38 20551216-0 2010 Protease inhibitors atazanavir, lopinavir and ritonavir are potent blockers, but poor substrates, of ABC transporters in a broad panel of ABC transporter-overexpressing cell lines. Lopinavir 32-41 ATP binding cassette subfamily B member 6 (Langereis blood group) Homo sapiens 101-104 20551216-0 2010 Protease inhibitors atazanavir, lopinavir and ritonavir are potent blockers, but poor substrates, of ABC transporters in a broad panel of ABC transporter-overexpressing cell lines. Lopinavir 32-41 ATP binding cassette subfamily B member 6 (Langereis blood group) Homo sapiens 138-141 20551216-5 2010 RESULTS: Atazanavir, lopinavir and ritonavir were highly effective in reversing resistance against established substrates in cells overexpressing MDR1 P-gp and MRP1, and, to a lesser extent, BCRP. Lopinavir 21-30 ATP binding cassette subfamily B member 1 Homo sapiens 146-150 20551216-5 2010 RESULTS: Atazanavir, lopinavir and ritonavir were highly effective in reversing resistance against established substrates in cells overexpressing MDR1 P-gp and MRP1, and, to a lesser extent, BCRP. Lopinavir 21-30 phosphoglycolate phosphatase Homo sapiens 151-155 20551216-5 2010 RESULTS: Atazanavir, lopinavir and ritonavir were highly effective in reversing resistance against established substrates in cells overexpressing MDR1 P-gp and MRP1, and, to a lesser extent, BCRP. Lopinavir 21-30 ATP binding cassette subfamily B member 1 Homo sapiens 160-164 20551216-5 2010 RESULTS: Atazanavir, lopinavir and ritonavir were highly effective in reversing resistance against established substrates in cells overexpressing MDR1 P-gp and MRP1, and, to a lesser extent, BCRP. Lopinavir 21-30 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 191-195 20551216-8 2010 Cells overexpressing MDR1 P-gp, MRP3, MRP4 and MRP5 displayed low levels of resistance to atazanavir (RF: 1.3-1.7); MRP7- and MRP9-overexpressing cells to lopinavir (RF: 1.4-1.5); and MRP9-overexpressing cells to ritonavir (RF: 1.4). Lopinavir 155-164 ATP binding cassette subfamily B member 1 Homo sapiens 21-25 20551216-8 2010 Cells overexpressing MDR1 P-gp, MRP3, MRP4 and MRP5 displayed low levels of resistance to atazanavir (RF: 1.3-1.7); MRP7- and MRP9-overexpressing cells to lopinavir (RF: 1.4-1.5); and MRP9-overexpressing cells to ritonavir (RF: 1.4). Lopinavir 155-164 ATP binding cassette subfamily C member 3 Homo sapiens 32-36 20551216-8 2010 Cells overexpressing MDR1 P-gp, MRP3, MRP4 and MRP5 displayed low levels of resistance to atazanavir (RF: 1.3-1.7); MRP7- and MRP9-overexpressing cells to lopinavir (RF: 1.4-1.5); and MRP9-overexpressing cells to ritonavir (RF: 1.4). Lopinavir 155-164 ATP binding cassette subfamily C member 5 Homo sapiens 47-51 20551216-8 2010 Cells overexpressing MDR1 P-gp, MRP3, MRP4 and MRP5 displayed low levels of resistance to atazanavir (RF: 1.3-1.7); MRP7- and MRP9-overexpressing cells to lopinavir (RF: 1.4-1.5); and MRP9-overexpressing cells to ritonavir (RF: 1.4). Lopinavir 155-164 ATP binding cassette subfamily C member 12 Homo sapiens 126-130 20051929-0 2010 HIV protease inhibitors are substrates for OATP1A2, OATP1B1 and OATP1B3 and lopinavir plasma concentrations are influenced by SLCO1B1 polymorphisms. Lopinavir 76-85 solute carrier organic anion transporter family member 1B1 Homo sapiens 126-133 20597164-6 2010 RESULTS: In some cases, use of protease sequences without the cognate gag overestimated susceptibility to protease inhibitors, in particular to lopinavir. Lopinavir 144-153 Pr55(Gag) Human immunodeficiency virus 1 70-73 20597164-7 2010 We provide evidence that gag sequences from wild-type viruses can contribute as much as 14-fold reduction in susceptibility to lopinavir, and that cognate protease can balance this by partially restoring susceptibility. Lopinavir 127-136 Pr55(Gag) Human immunodeficiency virus 1 25-28 20590614-0 2010 Effects of cytochrome P450 3A (CYP3A) and the drug transporters P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) on the pharmacokinetics of lopinavir. Lopinavir 136-145 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 11-29 19835489-2 2010 Voriconazole induction, including the utilization of voriconazole therapeutic drug monitoring in both serum and CSF, with transition to voriconazole plus interferon-gamma (IFN-gamma) was successfully used in a patient receiving antiretroviral therapy with abacavir/lamivudine and lopinavir/ritonavir. Lopinavir 280-289 interferon gamma Homo sapiens 172-181 19898246-5 2010 RESULTS: Insulin-stimulated peripheral glucose disposal decreased by 25% after 3 months in patients on zidovudine/lamivudine/lopinavir/ritonavir (ZDV/3TC/LPV/r) (P < 0.001) and this decreased rate persisted thereafter, followed by a transient decrease in insulin-mediated inhibition of lipolysis. Lopinavir 125-134 insulin Homo sapiens 9-16 20590614-0 2010 Effects of cytochrome P450 3A (CYP3A) and the drug transporters P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) on the pharmacokinetics of lopinavir. Lopinavir 136-145 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 31-36 20590614-0 2010 Effects of cytochrome P450 3A (CYP3A) and the drug transporters P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) on the pharmacokinetics of lopinavir. Lopinavir 136-145 ATP-binding cassette, sub-family B (MDR/TAP), member 1B Mus musculus 80-84 20590614-0 2010 Effects of cytochrome P450 3A (CYP3A) and the drug transporters P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) on the pharmacokinetics of lopinavir. Lopinavir 136-145 ATP-binding cassette, sub-family B (MDR/TAP), member 1B Mus musculus 85-90 20590614-0 2010 Effects of cytochrome P450 3A (CYP3A) and the drug transporters P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) on the pharmacokinetics of lopinavir. Lopinavir 136-145 ATP-binding cassette, sub-family C (CFTR/MRP), member 2 Mus musculus 96-100 20590614-0 2010 Effects of cytochrome P450 3A (CYP3A) and the drug transporters P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) on the pharmacokinetics of lopinavir. Lopinavir 136-145 ATP-binding cassette, sub-family C (CFTR/MRP), member 2 Mus musculus 102-107 20590614-1 2010 BACKGROUND AND PURPOSE: Lopinavir is extensively metabolized by cytochrome P450 3A (CYP3A) and is considered to be a substrate for the drug transporters ABCB1 (P-glycoprotein) and ABCC2 (MRP2). Lopinavir 24-33 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 64-82 20590614-1 2010 BACKGROUND AND PURPOSE: Lopinavir is extensively metabolized by cytochrome P450 3A (CYP3A) and is considered to be a substrate for the drug transporters ABCB1 (P-glycoprotein) and ABCC2 (MRP2). Lopinavir 24-33 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 84-89 20590614-1 2010 BACKGROUND AND PURPOSE: Lopinavir is extensively metabolized by cytochrome P450 3A (CYP3A) and is considered to be a substrate for the drug transporters ABCB1 (P-glycoprotein) and ABCC2 (MRP2). Lopinavir 24-33 ATP-binding cassette, sub-family B (MDR/TAP), member 1B Mus musculus 153-158 20590614-1 2010 BACKGROUND AND PURPOSE: Lopinavir is extensively metabolized by cytochrome P450 3A (CYP3A) and is considered to be a substrate for the drug transporters ABCB1 (P-glycoprotein) and ABCC2 (MRP2). Lopinavir 24-33 ATP-binding cassette, sub-family C (CFTR/MRP), member 2 Mus musculus 180-185 20590614-1 2010 BACKGROUND AND PURPOSE: Lopinavir is extensively metabolized by cytochrome P450 3A (CYP3A) and is considered to be a substrate for the drug transporters ABCB1 (P-glycoprotein) and ABCC2 (MRP2). Lopinavir 24-33 ATP-binding cassette, sub-family C (CFTR/MRP), member 2 Mus musculus 187-191 20590614-2 2010 Here, we have assessed the individual and combined effects of CYP3A, ABCB1 and ABCC2 on the pharmacokinetics of lopinavir and the relative importance of intestinal and hepatic metabolism. Lopinavir 112-121 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 62-67 20590614-2 2010 Here, we have assessed the individual and combined effects of CYP3A, ABCB1 and ABCC2 on the pharmacokinetics of lopinavir and the relative importance of intestinal and hepatic metabolism. Lopinavir 112-121 ATP-binding cassette, sub-family B (MDR/TAP), member 1B Mus musculus 69-74 20590614-2 2010 Here, we have assessed the individual and combined effects of CYP3A, ABCB1 and ABCC2 on the pharmacokinetics of lopinavir and the relative importance of intestinal and hepatic metabolism. Lopinavir 112-121 ATP-binding cassette, sub-family C (CFTR/MRP), member 2 Mus musculus 79-84 20590614-4 2010 EXPERIMENTAL APPROACH: Lopinavir transport was measured in Madin-Darby canine kidney cells expressing ABCB1 or ABCC2. Lopinavir 23-32 ATP binding cassette subfamily B member 1 Canis lupus familiaris 102-107 20590614-4 2010 EXPERIMENTAL APPROACH: Lopinavir transport was measured in Madin-Darby canine kidney cells expressing ABCB1 or ABCC2. Lopinavir 23-32 ATP binding cassette subfamily C member 2 Canis lupus familiaris 111-116 20590614-6 2010 KEY RESULTS: Lopinavir was transported by ABCB1 but not by ABCC2 in vitro. Lopinavir 13-22 ATP-binding cassette, sub-family B (MDR/TAP), member 1B Mus musculus 42-47 20590614-7 2010 Lopinavir area under the plasma concentration - time curve (AUC)(oral) was increased in Abcb1a/b(-/-) mice (approximately ninefold vs. wild-type) but not in Abcc2(-/-) mice. Lopinavir 0-9 ATP-binding cassette, sub-family B (MDR/TAP), member 1A Mus musculus 88-94 20590614-8 2010 Increased lopinavir AUC(oral) (>2000-fold) was observed in cytochrome P450 3A knockout (Cyp3a(-/-)) mice compared with wild-type mice. Lopinavir 10-19 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 62-80 20590614-8 2010 Increased lopinavir AUC(oral) (>2000-fold) was observed in cytochrome P450 3A knockout (Cyp3a(-/-)) mice compared with wild-type mice. Lopinavir 10-19 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 91-96 20590614-10 2010 CYP3A4 activity in intestine or liver, separately, reduced lopinavir AUC(oral) (>100-fold), compared with Cyp3a(-/-) mice. Lopinavir 59-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 20590614-12 2010 CONCLUSIONS AND IMPLICATIONS: CYP3A was the major determinant of lopinavir pharmacokinetics, far more than Abcb1a/b. Lopinavir 65-74 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 30-35 20590614-13 2010 Both intestinal and hepatic CYP3A activity contributed importantly to low oral bioavailability of lopinavir. Lopinavir 98-107 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 28-33 20590614-14 2010 Ritonavir increased lopinavir bioavailability primarily by inhibiting CYP3A. Lopinavir 20-29 cytochrome P450, family 3, subfamily a, polypeptide 11 Mus musculus 70-75 20192725-10 2010 Lopinavir trough plasma concentrations were higher with BID dosing. Lopinavir 0-9 BH3 interacting domain death agonist Homo sapiens 56-59 20051929-9 2010 The 521T>C polymorphism in SLCO1B1 was significantly associated with higher lopinavir plasma concentrations. Lopinavir 79-88 solute carrier organic anion transporter family member 1B1 Homo sapiens 30-37 20051929-12 2010 Further studies are now required to confirm the association of SLCO1B1 521T>C with lopinavir plasma concentrations and to assess the influence of other polymorphisms in the SLCO family. Lopinavir 86-95 solute carrier organic anion transporter family member 1B1 Homo sapiens 63-70 19890203-3 2010 We studied the effects of the protease inhibitor combination lopinavir and ritonavir on insulin secretion, insulin sensitivity, and lipid metabolism in HIV-negative persons. Lopinavir 61-70 insulin Homo sapiens 88-95 19890203-10 2010 CONCLUSION: Although administration of lopinavir/ritonavir to healthy, HIV-seronegative volunteers for 4 weeks resulted in increased triglyceride and decreased high-density lipoprotein cholesterol levels, there was no change in first-phase insulin secretion during the hyperglycemic clamp. Lopinavir 39-48 insulin Homo sapiens 240-247 19732776-8 2010 CHOP silencing by specific small hairpin RNA prevented lopinavir- and ritonavir-induced barrier dysfunction in cultured intestinal epithelial cells, whereas CHOP(-)/(-) mice exhibited decreased mucosal injury after exposure to lopinavir and ritonavir. Lopinavir 55-64 DNA-damage inducible transcript 3 Mus musculus 0-4 19936726-0 2010 Pharmacogenomic adaptation of antiretroviral therapy: overcoming the failure of lopinavir in an African infant with CYP2D6 ultrarapid metabolism. Lopinavir 80-89 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 116-122 21149919-0 2010 Effect of boosted fosamprenavir or lopinavir-based combinations on whole-body insulin sensitivity and lipids in treatment-naive HIV-type-1-positive men. Lopinavir 35-44 insulin Homo sapiens 78-85 19732776-8 2010 CHOP silencing by specific small hairpin RNA prevented lopinavir- and ritonavir-induced barrier dysfunction in cultured intestinal epithelial cells, whereas CHOP(-)/(-) mice exhibited decreased mucosal injury after exposure to lopinavir and ritonavir. Lopinavir 227-236 DNA-damage inducible transcript 3 Mus musculus 0-4 21182349-2 2010 Furthermore, in the phase III TITAN trial (TMC114-C214), DRV/r 600/100 mg bid-based HAART generated a superior 48-week virological response rate compared with standard-of-care lopinavir/ritonavir (LPV/r; 400/100 mg bid)-based therapy in treatment-experienced, lopinavir-naive patients, and in particular those with one or more International AIDS Society - USA (IAS-USA) primary PI resistance-associated mutations at baseline. Lopinavir 260-269 BH3 interacting domain death agonist Homo sapiens 74-77 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. Lopinavir 72-81 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 169-175 21182349-16 2010 CONCLUSION: From the perspective of Belgian, Italian, Swedish and UK payers, DRV/r 600/100 mg bid-based HAART is predicted to be cost effective compared with LPV/r 400/100 mg bid-based therapy, when used to manage treatment experienced, lopinavir-naive, PI-resistant, HIV-infected adults with a broad range of previous PI use/failure. Lopinavir 237-246 BH3 interacting domain death agonist Homo sapiens 94-97 19757141-10 2009 Lopinavir is also a P-gp inhibitor. Lopinavir 0-9 phosphoglycolate phosphatase Homo sapiens 20-24 19934383-2 2009 Data on lopinavir cerebrospinal fluid (CSF) trough concentration (C(trough)) values have yet to be reported. Lopinavir 8-17 colony stimulating factor 2 Homo sapiens 39-42 19934383-3 2009 OBJECTIVE: To describe lopinavir CSF C(trough) values and compare them with a measure of HIV susceptibility. Lopinavir 23-32 colony stimulating factor 2 Homo sapiens 33-36 19934383-11 2009 Lopinavir CSF C(trough) was above the median 50% inhibitory concentration (IC(50)) for wild-type HIV-1 (wtHIV-1) (1900 pg/mL) in all subjects. Lopinavir 0-9 colony stimulating factor 2 Homo sapiens 10-13 19934383-12 2009 Lopinavir plasma AUC(0-12) (r(2) = 0.65; p = 0.009) and CSF protein (r(2) = 0.26; p = 0.006) were associated with lopinavir CSF concentration, while CSF protein (r(2) = 0.66; p = 0.008) was associated with CSF to plasma concentration ratio. Lopinavir 0-9 colony stimulating factor 2 Homo sapiens 124-127 19934383-12 2009 Lopinavir plasma AUC(0-12) (r(2) = 0.65; p = 0.009) and CSF protein (r(2) = 0.26; p = 0.006) were associated with lopinavir CSF concentration, while CSF protein (r(2) = 0.66; p = 0.008) was associated with CSF to plasma concentration ratio. Lopinavir 0-9 colony stimulating factor 2 Homo sapiens 124-127 19934383-12 2009 Lopinavir plasma AUC(0-12) (r(2) = 0.65; p = 0.009) and CSF protein (r(2) = 0.26; p = 0.006) were associated with lopinavir CSF concentration, while CSF protein (r(2) = 0.66; p = 0.008) was associated with CSF to plasma concentration ratio. Lopinavir 0-9 colony stimulating factor 2 Homo sapiens 124-127 19934383-12 2009 Lopinavir plasma AUC(0-12) (r(2) = 0.65; p = 0.009) and CSF protein (r(2) = 0.26; p = 0.006) were associated with lopinavir CSF concentration, while CSF protein (r(2) = 0.66; p = 0.008) was associated with CSF to plasma concentration ratio. Lopinavir 114-123 colony stimulating factor 2 Homo sapiens 56-59 19934383-12 2009 Lopinavir plasma AUC(0-12) (r(2) = 0.65; p = 0.009) and CSF protein (r(2) = 0.26; p = 0.006) were associated with lopinavir CSF concentration, while CSF protein (r(2) = 0.66; p = 0.008) was associated with CSF to plasma concentration ratio. Lopinavir 114-123 colony stimulating factor 2 Homo sapiens 124-127 19934383-12 2009 Lopinavir plasma AUC(0-12) (r(2) = 0.65; p = 0.009) and CSF protein (r(2) = 0.26; p = 0.006) were associated with lopinavir CSF concentration, while CSF protein (r(2) = 0.66; p = 0.008) was associated with CSF to plasma concentration ratio. Lopinavir 114-123 colony stimulating factor 2 Homo sapiens 124-127 19934383-12 2009 Lopinavir plasma AUC(0-12) (r(2) = 0.65; p = 0.009) and CSF protein (r(2) = 0.26; p = 0.006) were associated with lopinavir CSF concentration, while CSF protein (r(2) = 0.66; p = 0.008) was associated with CSF to plasma concentration ratio. Lopinavir 114-123 colony stimulating factor 2 Homo sapiens 124-127 19934383-13 2009 CONCLUSIONS: Lopinavir CSF C(trough) was above the median IC(50) for wtHIV-1 replication in all patients receiving lopinavir/ritonavir 400/100-mg soft-gel capsules twice daily. Lopinavir 13-22 colony stimulating factor 2 Homo sapiens 23-26 19934383-13 2009 CONCLUSIONS: Lopinavir CSF C(trough) was above the median IC(50) for wtHIV-1 replication in all patients receiving lopinavir/ritonavir 400/100-mg soft-gel capsules twice daily. Lopinavir 115-124 colony stimulating factor 2 Homo sapiens 23-26 19439488-0 2009 Binding of lopinavir to human alpha1-acid glycoprotein and serum albumin. Lopinavir 11-20 albumin Homo sapiens 59-72 19790146-5 2009 In period 2, the addition of lopinavir/ritonavir to the immunosuppressant regimen enabled a reduction in the dose of immunosuppressants required to maintain trough concentrations within the therapeutic range (to 0.3 mg/day for tacrolimus and 75 mg/day for cyclosporine). Lopinavir 29-38 period circadian regulator 2 Homo sapiens 3-11 19842932-0 2009 Association between ABCC2 polymorphism and lopinavir accumulation in peripheral blood mononuclear cells of HIV-infected patients. Lopinavir 43-52 ATP binding cassette subfamily C member 2 Homo sapiens 20-25 19842932-7 2009 RESULTS & CONCLUSION: The 4544G>A (rs8187710)polymorphism in ABCC2 was associated with a higher accumulation of LPV in peripheral blood mononuclear cells of HIV-treated patients. Lopinavir 119-122 ATP binding cassette subfamily C member 2 Homo sapiens 68-73 19194313-1 2009 BACKGROUND: Preliminary studies suggest that the new film-coated tablet formulation of lopinavir/ritonavir (LPV/r-fct) could cut down the rate of adverse gastrointestinal symptoms of the conventional lopinavir/ritonavir soft gelatine capsules (LPV/r-sgc). Lopinavir 87-96 sarcoglycan beta Homo sapiens 250-253 19501568-0 2009 Lopinavir co-induces insulin resistance and ER stress in human adipocytes. Lopinavir 0-9 insulin Homo sapiens 21-28 19501568-3 2009 We report here that lopinavir, one of the most prescribed PI, dose-dependently co-induced insulin resistance and ER stress in human adipocytes obtained from differentiation of precursor cells. Lopinavir 20-29 insulin Homo sapiens 90-97 19451297-10 2009 Major PI resistance-associated mutations were detected in 5 (6%) of 83 patients treated with LPV/r monotherapy, suggesting that LPV/r monotherapy is an inappropriate first option. Lopinavir 93-96 serpin family A member 13, pseudogene Homo sapiens 6-8 19447225-0 2009 HIV protease inhibitor lopinavir-induced TNF-alpha and IL-6 expression is coupled to the unfolded protein response and ERK signaling pathways in macrophages. Lopinavir 23-32 tumor necrosis factor Mus musculus 41-50 19447225-0 2009 HIV protease inhibitor lopinavir-induced TNF-alpha and IL-6 expression is coupled to the unfolded protein response and ERK signaling pathways in macrophages. Lopinavir 23-32 interleukin 6 Mus musculus 55-59 19447225-0 2009 HIV protease inhibitor lopinavir-induced TNF-alpha and IL-6 expression is coupled to the unfolded protein response and ERK signaling pathways in macrophages. Lopinavir 23-32 mitogen-activated protein kinase 1 Mus musculus 119-122 19447225-5 2009 We show here that the HIV PI lopinavir significantly activated the extracellular-signal regulated protein kinase (ERK), but not c-Jun N-terminal kinase (JNK) and p38 MAPK. Lopinavir 29-38 mitogen-activated protein kinase 1 Mus musculus 67-112 19447225-5 2009 We show here that the HIV PI lopinavir significantly activated the extracellular-signal regulated protein kinase (ERK), but not c-Jun N-terminal kinase (JNK) and p38 MAPK. Lopinavir 29-38 mitogen-activated protein kinase 1 Mus musculus 114-117 19447225-5 2009 We show here that the HIV PI lopinavir significantly activated the extracellular-signal regulated protein kinase (ERK), but not c-Jun N-terminal kinase (JNK) and p38 MAPK. Lopinavir 29-38 mitogen-activated protein kinase 8 Mus musculus 128-151 19447225-5 2009 We show here that the HIV PI lopinavir significantly activated the extracellular-signal regulated protein kinase (ERK), but not c-Jun N-terminal kinase (JNK) and p38 MAPK. Lopinavir 29-38 mitogen-activated protein kinase 14 Mus musculus 162-170 19447225-6 2009 Lopinavir-induced cytosolic translocation of HuR and TNF-alpha and IL-6 synthesis was attenuated by specific chemical inhibitor of MEK (PD98058) or over-expression of dominant negative mutant of MEK1. Lopinavir 0-9 ELAV (embryonic lethal, abnormal vision)-like 1 (Hu antigen R) Mus musculus 45-48 19447225-6 2009 Lopinavir-induced cytosolic translocation of HuR and TNF-alpha and IL-6 synthesis was attenuated by specific chemical inhibitor of MEK (PD98058) or over-expression of dominant negative mutant of MEK1. Lopinavir 0-9 tumor necrosis factor Mus musculus 53-62 19447225-6 2009 Lopinavir-induced cytosolic translocation of HuR and TNF-alpha and IL-6 synthesis was attenuated by specific chemical inhibitor of MEK (PD98058) or over-expression of dominant negative mutant of MEK1. Lopinavir 0-9 interleukin 6 Mus musculus 67-71 19447225-6 2009 Lopinavir-induced cytosolic translocation of HuR and TNF-alpha and IL-6 synthesis was attenuated by specific chemical inhibitor of MEK (PD98058) or over-expression of dominant negative mutant of MEK1. Lopinavir 0-9 midkine Mus musculus 131-134 19447225-6 2009 Lopinavir-induced cytosolic translocation of HuR and TNF-alpha and IL-6 synthesis was attenuated by specific chemical inhibitor of MEK (PD98058) or over-expression of dominant negative mutant of MEK1. Lopinavir 0-9 mitogen-activated protein kinase kinase 1 Mus musculus 195-199 19447225-7 2009 In addition, we demonstrated that lopinavir-induced ERK activation and TNF-alpha and IL-6 expression were completely inhibited in macrophages from CHOP null mice. Lopinavir 34-43 mitogen-activated protein kinase 1 Mus musculus 52-55 19447225-7 2009 In addition, we demonstrated that lopinavir-induced ERK activation and TNF-alpha and IL-6 expression were completely inhibited in macrophages from CHOP null mice. Lopinavir 34-43 tumor necrosis factor Mus musculus 71-80 19447225-7 2009 In addition, we demonstrated that lopinavir-induced ERK activation and TNF-alpha and IL-6 expression were completely inhibited in macrophages from CHOP null mice. Lopinavir 34-43 interleukin 6 Mus musculus 85-89 19447225-7 2009 In addition, we demonstrated that lopinavir-induced ERK activation and TNF-alpha and IL-6 expression were completely inhibited in macrophages from CHOP null mice. Lopinavir 34-43 DNA-damage inducible transcript 3 Mus musculus 147-151 19349850-1 2009 In 29 antiretroviral-naive HIV-2-infected patients starting lopinavir/ritonavir-containing regimen, the median CD4 cell count change from baseline (142 cells/microl) was +71 cells/microl at week 24 and +132 cells/microl at week 96. Lopinavir 60-69 CD4 molecule Homo sapiens 111-114 19349850-3 2009 This sustained elevation of CD4 cell count in the first 2 years of combination antiretroviral therapy shows the potential for lopinavir/ritonavir regimens as first-line therapy in HIV-2 infection. Lopinavir 126-135 CD4 molecule Homo sapiens 28-31 19292590-6 2009 By the Cox proportional hazards model, higher reported adherence levels and higher baseline CD4(+) T cell counts were associated with a greater likelihood of maintaining virologic suppression while receiving lopinavir/ritonavir monotherapy. Lopinavir 208-217 CD4 molecule Homo sapiens 92-95 19292590-8 2009 This analysis suggests that adherence and higher baseline CD4(+) T cell counts may help to predict who will sustain virologic suppression with lopinavir/ritonavir monotherapy. Lopinavir 143-152 CD4 molecule Homo sapiens 58-61 19960055-0 2009 Functional role of p-glycoprotein and binding protein effect on the placental transfer of lopinavir/ritonavir in the ex vivo human perfusion model. Lopinavir 90-99 ATP binding cassette subfamily B member 1 Homo sapiens 19-33 19918096-1 2009 BACKGROUND: Lopinavir is a potent protease inhibitor (PI) used for the treatment of HIV infection. Lopinavir 12-21 serpin family A member 13, pseudogene Homo sapiens 34-52 19918096-1 2009 BACKGROUND: Lopinavir is a potent protease inhibitor (PI) used for the treatment of HIV infection. Lopinavir 12-21 serpin family A member 13, pseudogene Homo sapiens 54-56 19918096-10 2009 CONCLUSIONS: These results support lopinavir therapeutic drug monitoring and the use of higher lopinavir doses for PI-pretreated patients. Lopinavir 95-104 serpin family A member 13, pseudogene Homo sapiens 115-117 19960055-11 2009 Even at high albumin concentrations, inhibition of placental P-glycoprotein increased placental transfer of lopinavir, suggesting that this efflux pump actively reduces placental transfer of the drug. Lopinavir 108-117 ATP binding cassette subfamily B member 1 Homo sapiens 61-75 19207033-3 2009 We investigated the impact of three common exonic ABCB1 polymorphisms on the concentrations of lopinavir and ritonavir in blood, semen and saliva of HIV-infected men under stable HAART containing ritonavir-boosted lopinavir. Lopinavir 95-104 ATP binding cassette subfamily B member 1 Homo sapiens 50-55 19960055-2 2009 To study the influence of P-glycoprotein (P-glycoprotein, ABCB1, MDR1) function on placental transfer of lopinavir with ritonavir at different albumin concentrations. Lopinavir 105-114 ATP binding cassette subfamily B member 1 Homo sapiens 26-40 18692133-4 2008 Moreover, we have reported the impact of FTC combined with protease inhibitors (PIs) (ritonavir, atazanavir, lopinavir) on Pgp and MRP1 expression and function, and on PI accumulation. Lopinavir 109-118 phosphoglycolate phosphatase Homo sapiens 123-126 18692133-4 2008 Moreover, we have reported the impact of FTC combined with protease inhibitors (PIs) (ritonavir, atazanavir, lopinavir) on Pgp and MRP1 expression and function, and on PI accumulation. Lopinavir 109-118 ATP binding cassette subfamily C member 1 Homo sapiens 131-135 19002102-11 2008 CONCLUSIONS AND IMPLICATIONS: Human OATPs, MRP, P-gp and lipophilicity determine the cellular uptake and retention of saquinavir and lopinavir. Lopinavir 133-142 phosphoglycolate phosphatase Homo sapiens 48-52 18455890-1 2008 Lopinavir (LVR) is extensively metabolized by CYP3A4 and is prevented from entering the cells by membrane efflux pumps such as P-gp and MRP2. Lopinavir 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 46-52 19002102-2 2008 Here, we studied the expression of one influx transporter system, human organic anion-transporting polypeptide (hOATP), in some T-cell lines (CEM, CEM(VBL), CEM(E1000)) and in peripheral blood mononuclear cells (PBMCs) and examined the effects of manipulation of influx/efflux transporters on the uptake of saquinavir and lopinavir. Lopinavir 322-331 solute carrier organic anion transporter family member 1A2 Homo sapiens 112-117 19086422-5 2008 TDF taken together with lopinavir may increase the plasma concentration of TDF or other medications that could worsen renal function. Lopinavir 24-33 sex determining region Y Homo sapiens 75-78 18455890-1 2008 Lopinavir (LVR) is extensively metabolized by CYP3A4 and is prevented from entering the cells by membrane efflux pumps such as P-gp and MRP2. Lopinavir 11-14 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 46-52 18712774-0 2008 Lopinavir impairs protein synthesis and induces eEF2 phosphorylation via the activation of AMP-activated protein kinase. Lopinavir 0-9 eukaryotic translation elongation factor 2 Homo sapiens 48-52 18712774-8 2008 To verify this connection, myocytes were treated with the AMPK inhibitor compound C. Compound C blocked eEF2K and eEF2 phosphorylation, demonstrating that LPV affects eEF2 activity via an AMPK-eEF2K dependent pathway. Lopinavir 155-158 eukaryotic elongation factor 2 kinase Homo sapiens 104-109 18712774-8 2008 To verify this connection, myocytes were treated with the AMPK inhibitor compound C. Compound C blocked eEF2K and eEF2 phosphorylation, demonstrating that LPV affects eEF2 activity via an AMPK-eEF2K dependent pathway. Lopinavir 155-158 eukaryotic translation elongation factor 2 Homo sapiens 104-108 18712774-8 2008 To verify this connection, myocytes were treated with the AMPK inhibitor compound C. Compound C blocked eEF2K and eEF2 phosphorylation, demonstrating that LPV affects eEF2 activity via an AMPK-eEF2K dependent pathway. Lopinavir 155-158 eukaryotic translation elongation factor 2 Homo sapiens 114-118 18712774-8 2008 To verify this connection, myocytes were treated with the AMPK inhibitor compound C. Compound C blocked eEF2K and eEF2 phosphorylation, demonstrating that LPV affects eEF2 activity via an AMPK-eEF2K dependent pathway. Lopinavir 155-158 eukaryotic elongation factor 2 kinase Homo sapiens 193-198 18639527-4 2008 Here, we purified Ste24p, the yeast ortholog of ZMPSTE24, and showed that its enzymatic activity was blocked by three HIV-PIs (lopinavir, ritonavir, and tipranavir). Lopinavir 127-136 zinc metalloprotease Saccharomyces cerevisiae S288C 18-24 18599597-3 2008 Superfusion with the GJ blockers 18-alpha-glycyrrhetinic acid (AGA; 75 microM) or 18-beta-glycyrrhetinic acid (50 microM) abolished the TNF-alpha-induced increase in LAV and LPV; carbenoxolone (75 microM) or oleamide (100 microM) reduced LAV by 50 and 75%, respectively, and LPV to a lesser extent. Lopinavir 174-177 tumor necrosis factor Mus musculus 136-145 18599597-3 2008 Superfusion with the GJ blockers 18-alpha-glycyrrhetinic acid (AGA; 75 microM) or 18-beta-glycyrrhetinic acid (50 microM) abolished the TNF-alpha-induced increase in LAV and LPV; carbenoxolone (75 microM) or oleamide (100 microM) reduced LAV by 50 and 75%, respectively, and LPV to a lesser extent. Lopinavir 275-278 tumor necrosis factor Mus musculus 136-145 18455890-1 2008 Lopinavir (LVR) is extensively metabolized by CYP3A4 and is prevented from entering the cells by membrane efflux pumps such as P-gp and MRP2. Lopinavir 11-14 phosphoglycolate phosphatase Homo sapiens 127-131 18455890-1 2008 Lopinavir (LVR) is extensively metabolized by CYP3A4 and is prevented from entering the cells by membrane efflux pumps such as P-gp and MRP2. Lopinavir 11-14 ATP binding cassette subfamily C member 2 Homo sapiens 136-140 18455890-1 2008 Lopinavir (LVR) is extensively metabolized by CYP3A4 and is prevented from entering the cells by membrane efflux pumps such as P-gp and MRP2. Lopinavir 0-9 phosphoglycolate phosphatase Homo sapiens 127-131 18455890-1 2008 Lopinavir (LVR) is extensively metabolized by CYP3A4 and is prevented from entering the cells by membrane efflux pumps such as P-gp and MRP2. Lopinavir 0-9 ATP binding cassette subfamily C member 2 Homo sapiens 136-140 18230615-2 2008 We recently demonstrated that a commonly used HIV-PI, lopinavir, inhibits ZMPSTE24, thereby blocking lamin A biogenesis and leading to an accumulation of prelamin A. Lopinavir 54-63 zinc metallopeptidase STE24 Homo sapiens 74-82 18183034-1 2008 This study aimed to quantify the inhibition of cytochrome P450 (CYP3A), CYP2D6, and P-glycoprotein in human immunodeficiency virus (HIV)-infected patients receiving an antiretroviral therapy (ART) containing ritonavir boosted lopinavir, and to identify factors influencing ritonavir and lopinavir pharmacokinetics. Lopinavir 287-296 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 64-69 18183034-8 2008 In conclusion, CYP3A, CYP2D6, and P-glycoprotein are profoundly inhibited in patients receiving ritonavir boosted lopinavir. Lopinavir 114-123 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 15-20 18183034-8 2008 In conclusion, CYP3A, CYP2D6, and P-glycoprotein are profoundly inhibited in patients receiving ritonavir boosted lopinavir. Lopinavir 114-123 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 22-28 18183034-8 2008 In conclusion, CYP3A, CYP2D6, and P-glycoprotein are profoundly inhibited in patients receiving ritonavir boosted lopinavir. Lopinavir 114-123 ATP binding cassette subfamily B member 1 Homo sapiens 34-48 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. Lopinavir 154-163 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 144-150 18356150-7 2008 At baseline, patients starting lopinavir/ritonavir had higher HIV-1 RNA and lower CD4+ cell counts. Lopinavir 31-40 CD4 molecule Homo sapiens 82-85 18183034-0 2008 Effect of an antiretroviral regimen containing ritonavir boosted lopinavir on intestinal and hepatic CYP3A, CYP2D6 and P-glycoprotein in HIV-infected patients. Lopinavir 65-74 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 101-106 18183034-0 2008 Effect of an antiretroviral regimen containing ritonavir boosted lopinavir on intestinal and hepatic CYP3A, CYP2D6 and P-glycoprotein in HIV-infected patients. Lopinavir 65-74 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 108-114 18183034-0 2008 Effect of an antiretroviral regimen containing ritonavir boosted lopinavir on intestinal and hepatic CYP3A, CYP2D6 and P-glycoprotein in HIV-infected patients. Lopinavir 65-74 ATP binding cassette subfamily B member 1 Homo sapiens 119-133 18183034-1 2008 This study aimed to quantify the inhibition of cytochrome P450 (CYP3A), CYP2D6, and P-glycoprotein in human immunodeficiency virus (HIV)-infected patients receiving an antiretroviral therapy (ART) containing ritonavir boosted lopinavir, and to identify factors influencing ritonavir and lopinavir pharmacokinetics. Lopinavir 226-235 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 64-69 18230615-10 2008 Ritonavir, like lopinavir, inhibits ZMPSTE24 and leads to an accumulation of prelamin A. Lopinavir 16-25 zinc metallopeptidase STE24 Homo sapiens 36-44 17713471-5 2008 The LPV/RTV treatment also inhibited the formation of SN38 glucuronide (SN38G), as shown by the 36% decrease in the SN38G/SN38 AUCs ratio (5.9+/-1.6 vs 9.2+/-2.6, P=0.002) consistent with UGT1A1 inhibition by LPV/RTV. Lopinavir 4-7 UDP glucuronosyltransferase family 1 member A1 Homo sapiens 188-194 18090297-0 2007 Effects of atazanavir/ritonavir and lopinavir/ritonavir on glucose uptake and insulin sensitivity. Lopinavir 36-45 insulin Homo sapiens 78-85 18718025-9 2008 NF-kappaB activity was increased in the VILI group as compared with the sham and LPV groups (P < 0.05) and was decreased in the PJ34+VILI group as compared with the VILI group (P = 0.009). Lopinavir 81-84 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 0-9 18090045-4 2007 CONCLUSION: Compared to previously performed studies of identical design using single doses of indinavir and lopinavir/ritonavir, a hierarchy of insulin resistance was observed with the greatest effect seen with indinavir followed by ritonavir and lopinavir/ritonavir, with little effect of amprenavir. Lopinavir 109-118 insulin Homo sapiens 145-152 17890284-0 2007 Inhibition of P-glycoprotein and multidrug resistance-associated proteins modulates the intracellular concentration of lopinavir in cultured CD4 T cells and primary human lymphocytes. Lopinavir 119-128 ATP binding cassette subfamily B member 1 Homo sapiens 14-28 17890284-10 2007 CONCLUSIONS: We provide evidence that lopinavir is a substrate of P-gp, MRP1 and MRP2. Lopinavir 38-47 ATP binding cassette subfamily B member 1 Homo sapiens 66-70 17890284-10 2007 CONCLUSIONS: We provide evidence that lopinavir is a substrate of P-gp, MRP1 and MRP2. Lopinavir 38-47 ATP binding cassette subfamily C member 1 Homo sapiens 72-76 17890284-10 2007 CONCLUSIONS: We provide evidence that lopinavir is a substrate of P-gp, MRP1 and MRP2. Lopinavir 38-47 ATP binding cassette subfamily C member 2 Homo sapiens 81-85 18090045-4 2007 CONCLUSION: Compared to previously performed studies of identical design using single doses of indinavir and lopinavir/ritonavir, a hierarchy of insulin resistance was observed with the greatest effect seen with indinavir followed by ritonavir and lopinavir/ritonavir, with little effect of amprenavir. Lopinavir 248-257 insulin Homo sapiens 145-152 17664327-8 2007 Pgp inhibition constants ranged from 10.3 microM (lopinavir) to >100 microM (amprenavir, indinavir, and darunavir). Lopinavir 50-59 PGP Canis lupus familiaris 0-3 17361129-6 2007 Considering drugs likely to be coadministered with AQ, the antiretroviral drugs efavirenz, saquinavir, lopinavir, and tipranavir were potent CYP2C8 inhibitors at clinically relevant concentrations. Lopinavir 103-112 cytochrome P450 family 2 subfamily C member 8 Homo sapiens 141-147 17451894-0 2007 Both P-gp and MRP2 mediate transport of Lopinavir, a protease inhibitor. Lopinavir 40-49 PGP Canis lupus familiaris 5-9 17451894-0 2007 Both P-gp and MRP2 mediate transport of Lopinavir, a protease inhibitor. Lopinavir 40-49 ATP binding cassette subfamily C member 2 Canis lupus familiaris 14-18 17451894-3 2007 Lopinavir efflux was directional and was completely inhibited by MK-571, a selective MRP family inhibitor in the MDCKII-MRP2 cell line. Lopinavir 0-9 ATP binding cassette subfamily C member 2 Canis lupus familiaris 120-124 17683706-0 2007 [Insulin resistance in HIV-infected patients receiving long-term therapy with efavirenz, lopinavir/ritonavir and atazanavir]. Lopinavir 89-98 insulin Homo sapiens 1-8 17683706-7 2007 Insulin resistance was found in 5 (10.6%) patients, 4 among those receiving lopinavir/ritonavir, one among those treated with efavirenz and none among subjects receiving atazanavir (p = 0.065). Lopinavir 76-85 insulin Homo sapiens 0-7 17503669-5 2007 hOAT3 was more sensitive to Pls with ritonavir (RTV) and lopinavir being the most potent inhibitors of TFV transport (62% and 37% inhibition, respectively, at their Cmax). Lopinavir 57-66 solute carrier family 22 member 8 Homo sapiens 0-5 17324111-0 2007 Multidrug resistance 1 polymorphisms and trough concentrations of atazanavir and lopinavir in patients with HIV. Lopinavir 81-90 ATP binding cassette subfamily B member 1 Homo sapiens 0-22 17668557-10 2007 Lopinavir, nelfinavir, zidovudine and stavudine markedly increased ROS production and release of IL-1 beta and tumour necrosis factor-alpha. Lopinavir 0-9 interleukin 1 beta Homo sapiens 97-139 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. Lopinavir 84-93 ATP binding cassette subfamily G member 2 (Junior blood group) Homo sapiens 64-68 17591027-7 2007 CONCLUSIONS: We hypothesize that differences between the PIs in intracellular protein-binding behaviour or inhibition of drug transporters (P glycoprotein, MDR1 and MDR2) could result in intracellular levels of saquinavir being increased by co-administration with lopinavir or atazanavir. Lopinavir 264-273 ATP binding cassette subfamily B member 1 Homo sapiens 140-154 16954722-0 2006 Effects of atazanavir/ritonavir and lopinavir/ritonavir on glucose uptake and insulin sensitivity: demonstrable differences in vitro and clinically. Lopinavir 36-45 insulin Homo sapiens 78-85 17591027-7 2007 CONCLUSIONS: We hypothesize that differences between the PIs in intracellular protein-binding behaviour or inhibition of drug transporters (P glycoprotein, MDR1 and MDR2) could result in intracellular levels of saquinavir being increased by co-administration with lopinavir or atazanavir. Lopinavir 264-273 ATP binding cassette subfamily B member 1 Homo sapiens 156-160 17591027-7 2007 CONCLUSIONS: We hypothesize that differences between the PIs in intracellular protein-binding behaviour or inhibition of drug transporters (P glycoprotein, MDR1 and MDR2) could result in intracellular levels of saquinavir being increased by co-administration with lopinavir or atazanavir. Lopinavir 264-273 ATP binding cassette subfamily B member 4 Homo sapiens 165-169 16954722-8 2006 During OGTT, the HOMA insulin resistance index significantly increased from baseline at 120 min with atazanavir/ritonavir and at 150 min with lopinavir/ritonavir. Lopinavir 142-151 insulin Homo sapiens 22-29 16954722-1 2006 BACKGROUND: The HIV protease inhibitor (PI) atazanavir does not impair insulin sensitivity acutely but ritonavir and lopinavir induce insulin resistance at therapeutic concentrations. Lopinavir 117-126 insulin Homo sapiens 134-141 16954722-7 2006 During euglycemic clamp, there was no significant change from baseline insulin sensitivity with atazanavir/ritonavir (P = 0.132), while insulin sensitivity significantly decreased with lopinavir/ritonavir from the baseline (-25%; P < 0.001) and from that seen with atazanavir/ritonavir (-18%; P = 0.023). Lopinavir 185-194 insulin Homo sapiens 136-143 16639344-0 2006 Lopinavir/ritonavir induces the hepatic activity of cytochrome P450 enzymes CYP2C9, CYP2C19, and CYP1A2 but inhibits the hepatic and intestinal activity of CYP3A as measured by a phenotyping drug cocktail in healthy volunteers. Lopinavir 0-9 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 76-82 16934050-0 2006 The effects of ritonavir and lopinavir/ritonavir on the pharmacokinetics of a novel CCR5 antagonist, aplaviroc, in healthy subjects. Lopinavir 29-38 C-C motif chemokine receptor 5 Homo sapiens 84-88 16910829-5 2006 Multivariate analysis showed that coadministration of boosted lopinavir (LPV) and patients" body weight were associated with U-beta 2MG levels in TDF+ patients. Lopinavir 62-71 sex determining region Y Homo sapiens 146-149 16910829-5 2006 Multivariate analysis showed that coadministration of boosted lopinavir (LPV) and patients" body weight were associated with U-beta 2MG levels in TDF+ patients. Lopinavir 73-76 sex determining region Y Homo sapiens 146-149 16639344-0 2006 Lopinavir/ritonavir induces the hepatic activity of cytochrome P450 enzymes CYP2C9, CYP2C19, and CYP1A2 but inhibits the hepatic and intestinal activity of CYP3A as measured by a phenotyping drug cocktail in healthy volunteers. Lopinavir 0-9 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 84-91 16639344-0 2006 Lopinavir/ritonavir induces the hepatic activity of cytochrome P450 enzymes CYP2C9, CYP2C19, and CYP1A2 but inhibits the hepatic and intestinal activity of CYP3A as measured by a phenotyping drug cocktail in healthy volunteers. Lopinavir 0-9 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 97-103 16639344-0 2006 Lopinavir/ritonavir induces the hepatic activity of cytochrome P450 enzymes CYP2C9, CYP2C19, and CYP1A2 but inhibits the hepatic and intestinal activity of CYP3A as measured by a phenotyping drug cocktail in healthy volunteers. Lopinavir 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 156-161 17310826-4 2006 After 4 h exposure of HPV16+ve SiHa cells to 15 microM lopinavir, a transient increase in wild-type p53 expression was observed associated with a 7% reduction in the chymotryptic activity of the 205 proteasome and apoptosis after 24h. Lopinavir 55-64 tumor protein p53 Homo sapiens 100-103 17310826-6 2006 In conclusion, these data show that specific HIV PIs such as lopinavir and possibly indinavir, can induce selective toxicity of HPV-transformed cervical carcinoma cells expressing wild-type p53 and may form the basis of a topically applied alternative to surgery for the treatment of HPV-related premalignant lesions of the cervix. Lopinavir 61-70 tumor protein p53 Homo sapiens 190-193 16388722-11 2005 Lopinavir/ritonavir-treated children displayed higher CD4+ T-lymphocyte counts than saquinavir-treated children since the first month of therapy (week 4: P=0.042; week 24: P= 0.029) while nelfinavir-treated children took 24 weeks to reach such an outcome (P=0.034). Lopinavir 0-9 CD4 molecule Homo sapiens 54-57 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. Lopinavir 163-172 glutamic pyruvic transaminase, soluble Mus musculus 9-12 16388722-12 2005 Since lopinavir/ritonavir-based regimen controls viral replication more efficiently and restores CD4+ T-lymphocyte count more quickly than saquinavir- or nelfinavir-based HAART, it may be considered when a salvage therapy or a rapid increase in CD4+ T-lymphocytes is necessary. Lopinavir 6-15 CD4 molecule Homo sapiens 97-100 16388722-12 2005 Since lopinavir/ritonavir-based regimen controls viral replication more efficiently and restores CD4+ T-lymphocyte count more quickly than saquinavir- or nelfinavir-based HAART, it may be considered when a salvage therapy or a rapid increase in CD4+ T-lymphocytes is necessary. Lopinavir 6-15 CD4 molecule Homo sapiens 245-248 15983895-0 2005 Pilot study of saquinavir and lopinavir/ritonavir twice daily in protease inhibitor-naive HIV-positive patients. Lopinavir 30-39 serpin family A member 13, pseudogene Homo sapiens 65-83 16143711-10 2005 CONCLUSIONS: Elevated lopinavir concentrations are associated with raised GGT. Lopinavir 22-31 gamma-glutamyltransferase light chain 5 pseudogene Homo sapiens 74-77 15983895-13 2005 CONCLUSION: Our study demonstrates that saquinavir/lopinavir/ritonavir 1000/400/100 mg bid with tenofovir intensification is a potent nucleoside-sparing regimen for PI-naive patients, associated with durable HIV suppression and improved CD4 cell counts. Lopinavir 51-60 CD4 molecule Homo sapiens 237-240 15668539-0 2005 Combining fosamprenavir with lopinavir/ritonavir substantially reduces amprenavir and lopinavir exposure: ACTG protocol A5143 results. Lopinavir 29-38 actin gamma 1 Homo sapiens 106-110 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. Lopinavir 138-147 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. Lopinavir 138-147 potassium voltage-gated channel subfamily H member 2 Homo sapiens 218-222 15222662-8 2004 Patients in the lopinavir-ritonavir group were more likely to have received highly active antiretroviral therapy and azithromycin than patients receiving nelfinavir, and they had lower baseline CD4+ cell counts (p < or = 0.01 for each comparison). Lopinavir 16-25 CD4 molecule Homo sapiens 194-197 15577646-0 2004 The effects of HIV protease inhibitors atazanavir and lopinavir/ritonavir on insulin sensitivity in HIV-seronegative healthy adults. Lopinavir 54-63 insulin Homo sapiens 77-84 15577646-3 2004 METHODS: Randomized, double-blind, crossover study of the effect of 5 days of administering ATV, lopinavir/ritonavir (LPV/r) or placebo on insulin-stimulated glucose disposal in 30 healthy HIV-negative subjects. Lopinavir 97-106 insulin Homo sapiens 139-146 15577646-3 2004 METHODS: Randomized, double-blind, crossover study of the effect of 5 days of administering ATV, lopinavir/ritonavir (LPV/r) or placebo on insulin-stimulated glucose disposal in 30 healthy HIV-negative subjects. Lopinavir 118-121 insulin Homo sapiens 139-146 15247556-12 2004 Phenytoin appears to increase LPV clearance via CYP3A4 induction, which is not offset by the presence of low-dose RTV. Lopinavir 30-33 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 48-54 15577646-5 2004 RESULTS: The mean insulin-stimulated glucose disposal (mg/min per kg body weight) per unit insulin (microU/ml) (M/I) was 9.88, 9.80 and 7.52 for placebo, ATV and LPV/r, respectively (SEM, 0.84 for all). Lopinavir 162-165 insulin Homo sapiens 18-25 15247556-0 2004 Coadministration of lopinavir/ritonavir and phenytoin results in two-way drug interaction through cytochrome P-450 induction. Lopinavir 20-29 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 98-114 15247556-1 2004 Lopinavir/ritonavir (LPV/RTV) is a CYP3A4 inhibitor and substrate; it also may induce cytochrome P-450 (CYP) isozymes. Lopinavir 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 35-41 15247556-1 2004 Lopinavir/ritonavir (LPV/RTV) is a CYP3A4 inhibitor and substrate; it also may induce cytochrome P-450 (CYP) isozymes. Lopinavir 0-9 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 86-102 15247556-1 2004 Lopinavir/ritonavir (LPV/RTV) is a CYP3A4 inhibitor and substrate; it also may induce cytochrome P-450 (CYP) isozymes. Lopinavir 0-9 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 35-38 15254024-0 2004 Lopinavir/ritonavir combined with twice-daily 400 mg indinavir: pharmacokinetics and pharmacodynamics in blood, CSF and semen. Lopinavir 0-9 colony stimulating factor 2 Homo sapiens 112-115 15254024-6 2004 Median lopinavir trough concentrations (n=5) in CSF and SP were below the limit of detection (BLD) (i.e. <10 ng/mL) and 248 ng/mL (range 96-2777), respectively. Lopinavir 7-16 colony stimulating factor 2 Homo sapiens 48-51 15254024-8 2004 In two of four men lopinavir concentrations in CSF were detectable at 27 and 29 ng/mL. Lopinavir 19-28 colony stimulating factor 2 Homo sapiens 47-50 14731164-1 2004 In a controlled, prospective study, the efficacy of ritonavir 200 mg twice daily (bid) in inhibiting the decrease of amprenavir plasma concentrations caused by co-administration of lopinavir was assessed. Lopinavir 181-190 BH3 interacting domain death agonist Homo sapiens 82-85 15090838-0 2004 Resistance to amprenavir before and after treatment with lopinavir/ritonavir in highly protease inhibitor-experienced HIV patients. Lopinavir 57-66 serpin family A member 13, pseudogene Homo sapiens 87-105 14731164-5 2004 Co-administration of lopinavir was found to decrease the amprenavir concentration, determined as the median area under the curve over 12 h (AUC12), by 25% (AUC12 24.9 microg/h/mL vs. 18.5 microg/h/mL; P<0.01), despite the presence of ritonavir 200 mg bid. Lopinavir 21-30 BH3 interacting domain death agonist Homo sapiens 254-257 15764168-10 2004 We found that antiretroviral combination therapy including lopinavir/ritonavir substantially decreases the viral load, both in CSF and plasma, as well as the intrathecal immunoactivation, measured by beta2-microglobulin and neopterin. Lopinavir 59-68 beta-2-microglobulin Homo sapiens 200-219 12700464-0 2003 Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein. Lopinavir 0-9 ATP binding cassette subfamily B member 1 Homo sapiens 35-49 14711599-1 2003 BACKGROUND: In a retrospective study of HIV patients under antiretroviral therapy, we investigated the influence of the MDR1 genotype (C3435T) on plasma levels of lopinavir (LPV) and efavirenz (EFV). Lopinavir 163-172 ATP binding cassette subfamily B member 1 Homo sapiens 120-124 14711599-2 2003 METHODS: The MDR1 genotype was analysed from 67 patients who were treated with LPV (n = 32; mean treatment period 53 weeks) and/or EFV (n = 43, mean treatment period 105 weeks) between 1999 and 2003. Lopinavir 79-82 ATP binding cassette subfamily B member 1 Homo sapiens 13-17 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. Lopinavir 85-92 low density lipoprotein receptor Homo sapiens 199-203 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). Lopinavir 142-151 endogenous retrovirus group K member 25 Homo sapiens 96-106 14525542-1 2003 OBJECTIVES: To examine the relationship between levels of the T-cell regulatory cytokine interleukin-7 (IL-7) and CD4 cell counts during immune reconstitution and to assess its prognostic value in advanced HIV-1-infected patients receiving lopinavir/ritonavir-based therapy. Lopinavir 240-249 interleukin 7 Homo sapiens 104-108 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. Lopinavir 36-45 ATP binding cassette subfamily B member 1 Homo sapiens 128-132 12700464-0 2003 Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein. Lopinavir 0-9 ATP binding cassette subfamily B member 1 Homo sapiens 77-91 12700464-1 2003 The effect of lopinavir on P-glycoprotein-mediated rhodamine 123 efflux was studied in Caco-2 monolayer cells. Lopinavir 14-23 ATP binding cassette subfamily B member 1 Homo sapiens 27-41 12700464-4 2003 In LS 180V cells, lopinavir induced P-glycoprotein immunoreactive protein (up to threefold) and messenger RNA levels in a concentration-dependent fashion. Lopinavir 18-27 ATP binding cassette subfamily B member 1 Homo sapiens 36-50 12719666-10 2003 However, the treatment with LPV/RTV was not interrupted for these patients, because in the follow-up they showed an increase in CD4+ values. Lopinavir 28-31 CD4 molecule Homo sapiens 128-131 10421617-2 1999 In the present study, the effect of ritonavir, a potent inhibitor of cytochrome P-450 (CYP) 3A, on the in vitro metabolism of ABT-378 was examined. Lopinavir 126-133 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-94 12662125-40 2003 Coadministration of lopinavir/ritonavir is contraindicated with certain drugs (i.e. flecainide, propafenone, astemizole, terfenadine, ergot derivatives, cisapride, pimozide, midazolam and triazolam) that are highly dependent on CYP3A or CYP2D6 for clearance and for which elevated plasma concentrations are associated with serious and/or life-threatening events. Lopinavir 20-29 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 237-243 12086554-8 2002 Lopinavir, the active component of this combination, is extensively metabolized by CYP3A4 and produces low systemic concentrations when used alone. Lopinavir 0-9 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 83-89 12724045-0 2003 Apparent mechanism-based inhibition of human CYP3A in-vitro by lopinavir. Lopinavir 63-72 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 45-50 12724045-3 2003 Lopinavir produced negligible or weak inhibition of human CYP1A2, 2B6, 2C9, 2C19 and 2D6. Lopinavir 0-9 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 58-64 12724045-4 2003 However, lopinavir was an inhibitor of CYP3A. Lopinavir 9-18 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 39-44 12724045-7 2003 This is consistent with mechanism-based inhibition of human CYP3A by lopinavir. Lopinavir 69-78 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 60-65 12724045-8 2003 Although lopinavir is less potent than ritonavir as an inhibitor of CYP3A, lopinavir is nonetheless likely to contribute to net CYP3A inhibition in-vivo during treatment with the lopinavir-ritonavir combination. Lopinavir 75-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 128-133 12724045-8 2003 Although lopinavir is less potent than ritonavir as an inhibitor of CYP3A, lopinavir is nonetheless likely to contribute to net CYP3A inhibition in-vivo during treatment with the lopinavir-ritonavir combination. Lopinavir 75-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 128-133 12458138-8 2002 The CD4 count increased 48% with SQV, 45% with IDV and 37% with LPV. Lopinavir 64-67 CD4 molecule Homo sapiens 4-7 12372511-1 2002 The HIV protease inhibitor Lopinavir has a pseudosymmetric core unit incorporating benzyl groups at both P-1, P-1" positions. Lopinavir 27-36 crystallin gamma F, pseudogene Homo sapiens 105-113 11596909-3 2001 Ritonavir reduces the metabolization of lopinavir by the cytochrome P450 3A4 isoenzyme which leads to markedly increased plasma levels of lopinavir(4). Lopinavir 40-49 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 57-76 11596909-3 2001 Ritonavir reduces the metabolization of lopinavir by the cytochrome P450 3A4 isoenzyme which leads to markedly increased plasma levels of lopinavir(4). Lopinavir 138-147 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 57-76 33032513-3 2021 The antiretroviral drug lopinavir, a protease inhibitor, is a substrate of the drug efflux transporters P-glycoprotein and multi-drug resistance-associated protein 1. Lopinavir 24-33 ATP binding cassette subfamily B member 1 Homo sapiens 104-118 33821626-0 2021 Inhibition of CYP3A7 DHEA-S Oxidation by Lopinavir and Ritonavir: An Alternative Mechanism for Adrenal Impairment in HIV Antiretroviral-Treated Neonates. Lopinavir 41-50 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 14-20 33821626-4 2021 In order to determine if CYP3A7 inhibition could lead to the adverse outcomes associated with Kaletra therapy, we conducted in vitro metabolic studies to determine the extent and mechanism of CYP3A7 inhibition by both ritonavir and lopinavir and the relative intrinsic clearance of lopinavir with and without ritonavir in both neonatal and adult human liver microsomes (HLMs). Lopinavir 232-241 cytochrome P450 family 3 subfamily A member 7 Homo sapiens 192-198 33032513-3 2021 The antiretroviral drug lopinavir, a protease inhibitor, is a substrate of the drug efflux transporters P-glycoprotein and multi-drug resistance-associated protein 1. Lopinavir 24-33 ATP binding cassette subfamily C member 1 Homo sapiens 123-165 33032513-12 2021 MK571, a MRP1 inhibitor, and IKK-16 significantly increased intracellular LPV concentration with or without ethanol treatment. Lopinavir 74-77 ATP binding cassette subfamily C member 1 Homo sapiens 9-13 34885967-6 2021 Our results revealed that LPV, RTV, and NFV have higher binding affinities with Mpro, and they all interact with catalytic residues His41 and the other two key amino acids Met49 and Met165. Lopinavir 26-29 NEWENTRY Severe acute respiratory syndrome-related coronavirus 80-84 34175754-3 2021 Worldwide Conference on Harmonization approval rules were taken after to completely approve the strategy, and linearity was gotten for the two drugs over the extend of 0.4-2.4 microg mL-1 for Lopinavir and 0.1-0.6 microg mL-1 for ritonavir. Lopinavir 192-201 L1 cell adhesion molecule Mus musculus 183-187 34175754-5 2021 As the detection limits were down to 0.133 and 0.022 microg mL-1 and quantitation limits were 0.395 and 0.068 microg mL-1 for lopinavir and ritonavir, individually; the in vivo assurance of lopinavir and ritonavir in spiked plasma tests was pertinent. Lopinavir 126-135 L1 cell adhesion molecule Mus musculus 117-121 34426410-4 2021 Here, we used in vitro transport studies in Transwell , in combination with our m-f PBPK model, to predict fetal Kp,uu of drugs that are effluxed by placental P-glycoprotein (P-gp), namely dexamethasone, betamethasone, darunavir and lopinavir. Lopinavir 233-242 ATP binding cassette subfamily B member 1 Homo sapiens 159-173 34741481-7 2022 Our in silico analysis revealed that the three drugs Lopinavir, Ritonavir, and Remdesivir showed interaction with the active site residues of Mpro. Lopinavir 53-62 NEWENTRY Severe acute respiratory syndrome-related coronavirus 142-146 34790115-10 2021 The analysis showed reduced glucose disposal rates and hence reduced insulin sensitivity with lopinavir (heterogeneity chi-squared = 0.68, I-squared (variation in SMD attributable to heterogeneity) = 0.0%, p = 0.031). Lopinavir 94-103 insulin Homo sapiens 69-76 34130375-9 2021 The best hit compounds on the human ACE2 were the lopinavir (-10.1 kcal/mol), ritonavir (-8.9 kcal/mol), and nafamostat (-8.7 kcal/mol). Lopinavir 50-59 angiotensin converting enzyme 2 Homo sapiens 36-40 34397829-13 2021 CONCLUSION: Limited evidence suggests that lopinavir, ritonavir, atazanavir, and saquinavir could cause PR prolongation, QRS widening, and QT prolongation. Lopinavir 43-52 transmembrane protein 37 Homo sapiens 104-106 34183756-6 2022 In vivo tests showed that HEJG significantly increased the plasma exposure of lopinavir (a CYP3A-substrate drug) by 2.43-fold and strongly prolonged its half-life by 1.91-fold when HEJG (3 g/kg) was co-administered with lopinavir to rats. Lopinavir 78-87 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 91-96 34183756-6 2022 In vivo tests showed that HEJG significantly increased the plasma exposure of lopinavir (a CYP3A-substrate drug) by 2.43-fold and strongly prolonged its half-life by 1.91-fold when HEJG (3 g/kg) was co-administered with lopinavir to rats. Lopinavir 220-229 cytochrome P450, family 3, subfamily a, polypeptide 62 Rattus norvegicus 91-96 34130375-3 2021 Thus, in this current computational study we carried out molecular docking experiments to assess the bridging potentials of some commercial drugs such as chloroquine, hydroxychloroquine, lopinavir, ritonavir, nafamostat, camostat, famotidine, umifenovir, nitazoxanide, ivermectin, and fluvoxamine at the interface between human ACE2 and the coronavirus spike glycoprotein complex. Lopinavir 187-196 angiotensin converting enzyme 2 Homo sapiens 328-332 34497279-5 2021 Lopinavir and ritonavir in low micromolar concentrations inhibited BSEP and MATE1 exporters, as well as OATP1B1/1B3 uptake transporters. Lopinavir 0-9 ATP binding cassette subfamily B member 11 Homo sapiens 67-71 34497279-5 2021 Lopinavir and ritonavir in low micromolar concentrations inhibited BSEP and MATE1 exporters, as well as OATP1B1/1B3 uptake transporters. Lopinavir 0-9 solute carrier family 47 member 1 Homo sapiens 76-81 34497279-5 2021 Lopinavir and ritonavir in low micromolar concentrations inhibited BSEP and MATE1 exporters, as well as OATP1B1/1B3 uptake transporters. Lopinavir 0-9 solute carrier organic anion transporter family member 1B1 Homo sapiens 104-115 34312587-10 2021 whereas Lopinavir (- 7.7 kcal/mol) exhibited the strongest affinity for RdRp. Lopinavir 8-17 ORF1a polyprotein;ORF1ab polyprotein Severe acute respiratory syndrome coronavirus 2 72-76 34253143-3 2021 To understand the co-evolutionary molecular mechanisms of resistance in the HIV-1 PR and Gag, we performed 100 ns molecular dynamic simulations on multidrug resistant PR"s when bound to LPV, DRV or a mutated A431V NC p1 Gag cleavage site (CS). Lopinavir 186-189 transmembrane protein 37 Homo sapiens 82-84 34253143-3 2021 To understand the co-evolutionary molecular mechanisms of resistance in the HIV-1 PR and Gag, we performed 100 ns molecular dynamic simulations on multidrug resistant PR"s when bound to LPV, DRV or a mutated A431V NC p1 Gag cleavage site (CS). Lopinavir 186-189 transmembrane protein 37 Homo sapiens 167-169 34253143-3 2021 To understand the co-evolutionary molecular mechanisms of resistance in the HIV-1 PR and Gag, we performed 100 ns molecular dynamic simulations on multidrug resistant PR"s when bound to LPV, DRV or a mutated A431V NC p1 Gag cleavage site (CS). Lopinavir 186-189 citrate synthase Homo sapiens 239-241 34253143-4 2021 Here we showed that distinct changes in PR"s active site, flap and elbow regions due to several PR resistance mutations (L10F, M46I, I54V, L76V, V82A) were found to alter LPV and DRV drug binding. Lopinavir 171-174 transmembrane protein 37 Homo sapiens 40-42 34253143-4 2021 Here we showed that distinct changes in PR"s active site, flap and elbow regions due to several PR resistance mutations (L10F, M46I, I54V, L76V, V82A) were found to alter LPV and DRV drug binding. Lopinavir 171-174 transmembrane protein 37 Homo sapiens 96-98 34184163-7 2021 Lopinavir (LPV) and ritonavir (RTV), available as FDA-approved fixed-dose combination products, were chosen as model ART drugs, and the formulation and processing parameters of spray-dried cyclodextrin (CD)-based LPV and RTV complexes were studied. Lopinavir 213-216 cyclodextrin None 189-201 35461087-0 2022 Exposure of human immune cells, to the antiretrovirals efavirenz and lopinavir, leads to lower glucose uptake and altered bioenergetic cell profiles through interactions with SLC2A1. Lopinavir 69-78 solute carrier family 2 member 1 Homo sapiens 175-181 35401674-4 2022 Three drug candidates (i.e., anidulafungin, lopinavir, and indinavir) were selected, which show high binding affinity toward the ACE2 receptor. Lopinavir 44-53 angiotensin converting enzyme 2 Homo sapiens 129-133 35401674-9 2022 Altogether, anidulafungin and lopinavir are ranked the most effective among all the tested drugs against ACE2 receptor-S glycoprotein interaction. Lopinavir 30-39 angiotensin converting enzyme 2 Homo sapiens 105-109 35328720-5 2022 Both LPV and LPVI restored the reduced transcript of IGF-1 while decreasing the transcript of insulin-like growth factor binding protein 1 (IGFBP1) in the liver. Lopinavir 5-8 insulin like growth factor 1 Sus scrofa 53-58 35328720-5 2022 Both LPV and LPVI restored the reduced transcript of IGF-1 while decreasing the transcript of insulin-like growth factor binding protein 1 (IGFBP1) in the liver. Lopinavir 5-8 insulin like growth factor binding protein 1 Sus scrofa 94-138 35328720-5 2022 Both LPV and LPVI restored the reduced transcript of IGF-1 while decreasing the transcript of insulin-like growth factor binding protein 1 (IGFBP1) in the liver. Lopinavir 5-8 insulin like growth factor binding protein 1 Sus scrofa 140-146 35328720-6 2022 LPV and LPVI recovered the reduced plasma Val, glycine, and leucine concentrations, which were positively correlated with improved gut morphology and the hepatic IGF-1 gene expression and negatively correlated with hepatic IGFBP1 mRNA abundance. Lopinavir 0-3 insulin like growth factor 1 Sus scrofa 162-167 34071195-3 2021 To confirm this hypothesis, molecular docking assays revealed that lopinavir bound to the Sap2 catalytic site of C. albicans as well as inhibited the Sap hydrolytic activity in a typically dose-dependent manner. Lopinavir 67-76 SH2 domain containing 1A Mus musculus 150-153 34071195-6 2021 Furthermore, our results revealed that lopinavir was able to (i) arrest the yeasts-into-hyphae transformation, (ii) disturb the synthesis of neutral lipids, including ergosterol, (iii) modulate the surface-located molecules, such as Saps and mannose-, sialic acid- and N-acetylglucosamine-containing glycoconjugates, (iv) diminish the secretion of hydrolytic enzymes, such as Saps and esterase, (v) negatively influence the biofilm formation on polystyrene surface, (vi) block the in vitro adhesion to epithelial cells, (vii) contain the in vivo infection in both immunocompetent and immunosuppressed mice and (viii) reduce the Sap production by yeasts recovered from kidneys of infected animals. Lopinavir 39-48 SH2 domain containing 1A Mus musculus 628-631 35628472-7 2022 Favipiravir, hydroxychloroquine, lopinavir, and the combination of lopinavir with ritonavir were found to inhibit pannexin1 channel activity without affecting pannexin1 protein or mRNA levels. Lopinavir 33-42 pannexin 1 Homo sapiens 114-123 35628472-7 2022 Favipiravir, hydroxychloroquine, lopinavir, and the combination of lopinavir with ritonavir were found to inhibit pannexin1 channel activity without affecting pannexin1 protein or mRNA levels. Lopinavir 67-76 pannexin 1 Homo sapiens 114-123