HIV Protease

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研究领域

抑制剂选择性比较

HIV Protease产品

所有产品 HIV Protease抑制剂(14) 新HIV Protease产品

目录号	产品描述	文献引用	实验数据
S1185	Ritonavir Ritonavir是Cytochrome P450 3A和HIV蛋白酶抑制剂，用于治疗HIV感染和AIDS。抑制Cytochrome P450 2D6, P-Glycoprotein，诱导Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6和UDP Glucuronosyltransferases。	Nat Med, 2018, 24(5):604-609 J Med Chem, 2018, 61(9):4189-4202 Front Oncol, 2018, 8:411	(A) KMS11 and (B) L363 cells were plated in 5mM glucose medium with ritonavir or DMSO (D) for 17 hours. Glucose consumption rates are normalized to untreated cells (not shown). (C) KMS11 and (D) L363 cells were treated with ritonavir or DMSO for 72 hours. Relative viable cell numbers were determined by MTS assay and normalized to untreated cells (not shown).
S1380	Lopinavir Lopinavir是一种有效的HIV protease抑制剂，无细胞试验中K_i为1.3 pM。	Cell Mol Life Sci, 2019, 76(6):1169-1183 Anticancer Res, 2019, 39(11):5891-5901 Biochim Biophys Acta, 2017, 1864(3):475-486	Low-micromolar amounts of chloroquine, chlorpromazine, loperamide, and lopinavir inhibit MERS-CoV-induced cytopathology. Huh7 cells in 96-well plates were infected with MERS-CoV isolate EMC/2012 (MOI, 0.005) in the presence of 0 to 20 uM LPV. Cells were incubated for 2 days, and cell viability was monitored using an MTS assay. In addition, the potential toxicity of compound treatment only was monitored in parallel mock-infected Huh7 cell cultures. Graphs show the results (averages and standard deviations [SD]) of a representative experiment that was performed in quadruplicate. All experiments were repeated at least twice. For each compound, the calculated EC50, CC50, and SI values are given.
S1457	Atazanavir Sulfate Atazanavir Sulfate是一种HIV protease抑制剂，无细胞试验中K_i值为2.66 nM。	J Med Chem, 2018, 61(9):4189-4202 Cell Rep, 2017, 20(7):1692-1704 Reprod Toxicol, 2014, 50:122-8	Protease inhibitors induce macroautophagy. JEG3 were seeded on glass chamber slides (1 x 10₄ cell per chamber; 8-well μ slides; Ibidi, Martinsried, Germany), grown for 24 h under cell culture conditions, and treated for 24 h with 0-10 ug/ml of either lopinavir/ritonavir or atazanavir. Cells were then incubated for 30 min with the blue-green fluorescent autophagy marker monodansylcadaverine and viewed under a fluorescence microscope.
S1620	Darunavir Ethanolate Darunavir Ethanolate是一种人类免疫缺陷病毒(HIV)蛋白酶抑制剂。	Drug Metab Dispos, 2015, 44(3):398-408 J Immunol, 2014, 192(8):3496-506	HIV PIs variably alter intracellular HIV epitope stability. (A) HLA-A02–restricted SL9 epitope (SLYNTVATL, aa 77–85 in HIV-1 Gag p17) was degraded in PBMC extracts pretreated with DMSO (control, circles), 5 µM of Nelfinavir (triangles) or 5 µM of Saquinavir (squares). Remaining peptide was quantified by RP-HPLC analysis after 0, 10, 30 and 60 minutes. 100% represents the amount of peptide at time 0 calculated as the surface under the peptide peak detected by RP-HPLC (815.986, 821.569, and 813.118 for DMSO, Saquinavir, and Nelfinavir, respectively). Times at which 50% of the SL9 peptide remained correspond to peptide half-lives (37 min, 52 min and 24 min for Control, Saquinavir and Nelfinavir respectively). (B–F) HLA-A02–SL9, HLA-B57-KF11, HLAB57-ISW9, HLA-B57-TW10 and HLA-A11-ATK9 epitopes (from B to F respectively) were degraded in PBMC extracts pretreated with DMSO, 2 µM or 5 µM PI (Saquinavir, Ritonavir, Nelfinavir, Atazanavir or Darunavir). The cytosolic half-lives in control condition were 33.87, 25.66, 14.83, 119.4 and 37.21 minutes for SL9, KF11, ISW9, TW10 and ATK9 respectively. Fold differences of each epitope half-life upon treatment compared to control are presented in each panel. All data represent the average of 4 different experiments using 4 different PBMC extracts. P < 0.05, P < 0.01, **P < 0.001, 1-way ANOVA with Dunnett’s post-test.
S1639	Amprenavir Amprenavir 是一种人类免疫缺陷病毒(HIV)蛋白酶抑制剂，作用于野生型HIV分离株，IC50为14.6 ng/ml。
S6625^New	Temsavir (BMS-626529) Temsavir (BMS-626529)是一种新型的HIV-1粘附抑制剂。
S6581^New	Fosamprenavir calcium salt Fosamprenavir是amprenavir的前体药物。Amprenavir是蛋白酶体抑制剂和抗逆转录病毒药物。Fosamprenavir可用于治疗HIV-1感染。
S5250	Darunavir Darunavir is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
S9010	Bevirimat Bevirimat, the prototype Human Immunodeficiency Virus type 1 (HIV-1) maturation inhibitor, is highly potent in cell culture and efficacious in HIV-1 infected patients.
S2319	Limonin Limonin又称Limonoate D-ring-lactone 和 Limonoic acid di-delta-lactone，化学上属于Furanolactone类化合物。	Int J Biol Sci, 2019, 15(11):2497-2508 Food Chem Toxicol, 2019, 125:621-628 Onco Targets Ther, 2018, 11:3793-3803
S4662	Atazanavir Atazanavir是一种氮杂肽及HIV-蛋白酶抑制剂，常与其他抗HIV药物结合，用于治疗HIV感染以及获得性免疫缺乏综合征。	Cell Death Dis, 2019, 10(6):419
S9567	Indinavir Sulfate Indinavir sulfate是一种有效的、特异的HIV-1 protease抑制剂，广泛用于艾滋病的治疗。
S4282	Nelfinavir Mesylate Nelfinavir Mesylate 是强效的HIV protease抑制剂，K_i为2 nM。	Leukemia, 2019, 33(1):37-51 Leuk Res, 2019, 78:3-11 Immunity, 2018, 49(5):842-856
S7381	Pepstatin A Pepstatin A 是一种强效的aspartic protease抑制剂, 并可抑制HIV的复制。	Nat Biomed Eng, 2019, 3(4):306-317 Alzheimers Dement, 2019, 15(9):1183-1194 Nat Chem Biol, 2019, 15(1):42-50

目录号	产品描述	文献引用	实验数据
S1185	Ritonavir Ritonavir是Cytochrome P450 3A和HIV蛋白酶抑制剂，用于治疗HIV感染和AIDS。抑制Cytochrome P450 2D6, P-Glycoprotein，诱导Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6和UDP Glucuronosyltransferases。	Nat Med,2018, 24(5):604-609 J Med Chem,2018, 61(9):4189-4202 Front Oncol,2018, 8:411	(A) KMS11 and (B) L363 cells were plated in 5mM glucose medium with ritonavir or DMSO (D) for 17 hours. Glucose consumption rates are normalized to untreated cells (not shown). (C) KMS11 and (D) L363 cells were treated with ritonavir or DMSO for 72 hours. Relative viable cell numbers were determined by MTS assay and normalized to untreated cells (not shown).
S1380	Lopinavir Lopinavir是一种有效的HIV protease抑制剂，无细胞试验中K_i为1.3 pM。	Cell Mol Life Sci,2019, 76(6):1169-1183 Anticancer Res,2019, 39(11):5891-5901 Biochim Biophys Acta,2017, 1864(3):475-486	Low-micromolar amounts of chloroquine, chlorpromazine, loperamide, and lopinavir inhibit MERS-CoV-induced cytopathology. Huh7 cells in 96-well plates were infected with MERS-CoV isolate EMC/2012 (MOI, 0.005) in the presence of 0 to 20 uM LPV. Cells were incubated for 2 days, and cell viability was monitored using an MTS assay. In addition, the potential toxicity of compound treatment only was monitored in parallel mock-infected Huh7 cell cultures. Graphs show the results (averages and standard deviations [SD]) of a representative experiment that was performed in quadruplicate. All experiments were repeated at least twice. For each compound, the calculated EC50, CC50, and SI values are given.
S1457	Atazanavir Sulfate Atazanavir Sulfate是一种HIV protease抑制剂，无细胞试验中K_i值为2.66 nM。	J Med Chem,2018, 61(9):4189-4202 Cell Rep,2017, 20(7):1692-1704 Reprod Toxicol,2014, 50:122-8	Protease inhibitors induce macroautophagy. JEG3 were seeded on glass chamber slides (1 x 10₄ cell per chamber; 8-well μ slides; Ibidi, Martinsried, Germany), grown for 24 h under cell culture conditions, and treated for 24 h with 0-10 ug/ml of either lopinavir/ritonavir or atazanavir. Cells were then incubated for 30 min with the blue-green fluorescent autophagy marker monodansylcadaverine and viewed under a fluorescence microscope.
S1620	Darunavir Ethanolate Darunavir Ethanolate是一种人类免疫缺陷病毒(HIV)蛋白酶抑制剂。	Drug Metab Dispos,2015, 44(3):398-408 J Immunol,2014, 192(8):3496-506	HIV PIs variably alter intracellular HIV epitope stability. (A) HLA-A02–restricted SL9 epitope (SLYNTVATL, aa 77–85 in HIV-1 Gag p17) was degraded in PBMC extracts pretreated with DMSO (control, circles), 5 µM of Nelfinavir (triangles) or 5 µM of Saquinavir (squares). Remaining peptide was quantified by RP-HPLC analysis after 0, 10, 30 and 60 minutes. 100% represents the amount of peptide at time 0 calculated as the surface under the peptide peak detected by RP-HPLC (815.986, 821.569, and 813.118 for DMSO, Saquinavir, and Nelfinavir, respectively). Times at which 50% of the SL9 peptide remained correspond to peptide half-lives (37 min, 52 min and 24 min for Control, Saquinavir and Nelfinavir respectively). (B–F) HLA-A02–SL9, HLA-B57-KF11, HLAB57-ISW9, HLA-B57-TW10 and HLA-A11-ATK9 epitopes (from B to F respectively) were degraded in PBMC extracts pretreated with DMSO, 2 µM or 5 µM PI (Saquinavir, Ritonavir, Nelfinavir, Atazanavir or Darunavir). The cytosolic half-lives in control condition were 33.87, 25.66, 14.83, 119.4 and 37.21 minutes for SL9, KF11, ISW9, TW10 and ATK9 respectively. Fold differences of each epitope half-life upon treatment compared to control are presented in each panel. All data represent the average of 4 different experiments using 4 different PBMC extracts. P < 0.05, P < 0.01, **P < 0.001, 1-way ANOVA with Dunnett’s post-test.
S1639	Amprenavir Amprenavir 是一种人类免疫缺陷病毒(HIV)蛋白酶抑制剂，作用于野生型HIV分离株，IC50为14.6 ng/ml。
S6625^New	Temsavir (BMS-626529) Temsavir (BMS-626529)是一种新型的HIV-1粘附抑制剂。
S6581^New	Fosamprenavir calcium salt Fosamprenavir是amprenavir的前体药物。Amprenavir是蛋白酶体抑制剂和抗逆转录病毒药物。Fosamprenavir可用于治疗HIV-1感染。
S5250	Darunavir Darunavir is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
S9010	Bevirimat Bevirimat, the prototype Human Immunodeficiency Virus type 1 (HIV-1) maturation inhibitor, is highly potent in cell culture and efficacious in HIV-1 infected patients.
S2319	Limonin Limonin又称Limonoate D-ring-lactone 和 Limonoic acid di-delta-lactone，化学上属于Furanolactone类化合物。	Int J Biol Sci,2019, 15(11):2497-2508 Food Chem Toxicol,2019, 125:621-628 Onco Targets Ther,2018, 11:3793-3803
S4662	Atazanavir Atazanavir是一种氮杂肽及HIV-蛋白酶抑制剂，常与其他抗HIV药物结合，用于治疗HIV感染以及获得性免疫缺乏综合征。	Cell Death Dis,2019, 10(6):419
S9567	Indinavir Sulfate Indinavir sulfate是一种有效的、特异的HIV-1 protease抑制剂，广泛用于艾滋病的治疗。
S4282	Nelfinavir Mesylate Nelfinavir Mesylate 是强效的HIV protease抑制剂，K_i为2 nM。	Leukemia,2019, 33(1):37-51 Leuk Res,2019, 78:3-11 Immunity,2018, 49(5):842-856
S7381	Pepstatin A Pepstatin A 是一种强效的aspartic protease抑制剂, 并可抑制HIV的复制。	Nat Biomed Eng,2019, 3(4):306-317 Alzheimers Dement,2019, 15(9):1183-1194 Nat Chem Biol,2019, 15(1):42-50