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(16)

目录号	产品描述	文献引用	实验数据
S1030	Panobinostat (LBH589) Panobinostat (LBH589)是一种新型的，广谱HDAC抑制剂，无细胞试验中IC50为5 nM。Panobinostat (LBH589) 可诱导自噬和凋亡。Panobinostat 可以有效地破坏体内 HIV 的潜伏期。Phase 3。	Nat Biotechnol, 2020, 10.1038/s41587-019-0388-4 Nat Commun, 2020, 11(1):583 Genome Med, 2020, 18;12(1):17	LSD1 and HDAC inhibitors exhibit synergistic growth inhibition. Cells were simultaneously treated with pargyline or HDAC inhibitors for 48 h.
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。	bioRxiv, 2020, 2020/9/20.4.7.30734 J Nat Prod, 2019, 82(6):1694-1703 Anticancer Res, 2019, 39(7):3757-3765	(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。	Antimicrob Agents Chemother, 2020, 4 pii: AAC bioRxiv, 2020, 2020/9/20.4.7.30734 Cell Mol Life Sci, 2019, 76(6):1169-1183	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.
S3013	Plerixafor 8HCl (AMD3100 8HCl) Plerixafor 8HCl (AMD3100 8HCl)是Plerixafor的盐酸盐，是CXCR4趋化因子受体拮抗剂，作用于CXCR4和CXCL12介导调节的趋化性，IC50分别为44 nM和5.7 nM。Plerixafor 可应用为抗HIV的药物。	Mol Oncol, 2020, 14(4):779-794 Biol Reprod, 2019, 101(1):102-111 Gastroenterology, 2018, 155(3):880-891.e8	BLI of NSG mice engrafted with BV173, treated with no therapy (control), plerixafor: 1 mg/kg IP daily, ESKM 100 ug twice weekly, and a combination of ESKM and plerixafor. (A) Logarithmic plot of BLI of leukemia growth measured weekly. Error bars are 5-95% confidence intervals. There was a small but not significant difference between ESKM and combination treated group. (B) End of therapy (day 34) BLI.
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。	Cancer Cell Int, 2020, 19;20:58 J Virol, 2019, 93(9) J Med Chem, 2018, 61(9):4189-4202	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.
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。
S1620	Darunavir Ethanolate Darunavir Ethanolate是一种人类免疫缺陷病毒(HIV)蛋白酶抑制剂。	J Virol, 2019, 93(9) JCI Insight, 2019, 4(12) mBio, 2018, 9(6)	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。
S5250	Darunavir Darunavir is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.	Anticancer Res, 2019, 39(7):3757-3765 Sci Rep, 2017, 7(1):7456
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 Biomed Pharmacother, 2019, 118:109366
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 Anticancer Res, 2019, 39(7):3757-3765
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。	Mol Metab, 2020, 29;101027
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 Anticancer Res, 2019, 39(7):3757-3765
S7381	Pepstatin A Pepstatin A 是一种强效的aspartic protease抑制剂, 并可抑制HIV的复制。	Hum Exp Toxicol, 2020, 39(2):194-211 Nat Biomed Eng, 2019, 3(4):306-317 Alzheimers Dement, 2019, 15(9):1183-1194

目录号	产品描述	文献引用	实验数据
S1030	Panobinostat (LBH589) Panobinostat (LBH589)是一种新型的，广谱HDAC抑制剂，无细胞试验中IC50为5 nM。Panobinostat (LBH589) 可诱导自噬和凋亡。Panobinostat 可以有效地破坏体内 HIV 的潜伏期。Phase 3。	Nat Biotechnol,2020, 10.1038/s41587-019-0388-4 Nat Commun,2020, 11(1):583 Genome Med,2020, 18;12(1):17	LSD1 and HDAC inhibitors exhibit synergistic growth inhibition. Cells were simultaneously treated with pargyline or HDAC inhibitors for 48 h.
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。	bioRxiv,2020, 2020/9/20.4.7.30734 J Nat Prod,2019, 82(6):1694-1703 Anticancer Res,2019, 39(7):3757-3765	(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。	Antimicrob Agents Chemother,2020, 4 pii: AAC bioRxiv,2020, 2020/9/20.4.7.30734 Cell Mol Life Sci,2019, 76(6):1169-1183	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.
S3013	Plerixafor 8HCl (AMD3100 8HCl) Plerixafor 8HCl (AMD3100 8HCl)是Plerixafor的盐酸盐，是CXCR4趋化因子受体拮抗剂，作用于CXCR4和CXCL12介导调节的趋化性，IC50分别为44 nM和5.7 nM。Plerixafor 可应用为抗HIV的药物。	Mol Oncol,2020, 14(4):779-794 Biol Reprod,2019, 101(1):102-111 Gastroenterology,2018, 155(3):880-891.e8	BLI of NSG mice engrafted with BV173, treated with no therapy (control), plerixafor: 1 mg/kg IP daily, ESKM 100 ug twice weekly, and a combination of ESKM and plerixafor. (A) Logarithmic plot of BLI of leukemia growth measured weekly. Error bars are 5-95% confidence intervals. There was a small but not significant difference between ESKM and combination treated group. (B) End of therapy (day 34) BLI.
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。	Cancer Cell Int,2020, 19;20:58 J Virol,2019, 93(9) J Med Chem,2018, 61(9):4189-4202	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.
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。
S1620	Darunavir Ethanolate Darunavir Ethanolate是一种人类免疫缺陷病毒(HIV)蛋白酶抑制剂。	J Virol,2019, 93(9) JCI Insight,2019, 4(12) mBio,2018, 9(6)	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。
S5250	Darunavir Darunavir is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.	Anticancer Res,2019, 39(7):3757-3765 Sci Rep,2017, 7(1):7456
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 Biomed Pharmacother,2019, 118:109366
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 Anticancer Res,2019, 39(7):3757-3765
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。	Mol Metab,2020, 29;101027
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 Anticancer Res,2019, 39(7):3757-3765
S7381	Pepstatin A Pepstatin A 是一种强效的aspartic protease抑制剂, 并可抑制HIV的复制。	Hum Exp Toxicol,2020, 39(2):194-211 Nat Biomed Eng,2019, 3(4):306-317 Alzheimers Dement,2019, 15(9):1183-1194