HIV Protease
信号通路图
研究领域
抑制剂选择性比较
HIV Protease产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1185 |
RitonavirRitonavir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。 |
(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 |
LopinavirLopinavir是一种有效的HIV protease抑制剂，无细胞试验中Ki为1.3 pM。 |
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 SulfateAtazanavir Sulfate是一种HIV protease抑制剂，无细胞试验中Ki值为2.66 nM。 |
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 EthanolateDarunavir Ethanolate是一种人类免疫缺陷病毒(HIV)蛋白酶抑制剂。 |
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 |
AmprenavirAmprenavir 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。 |
||
| S9567New |
Indinavir SulfateIndinavir 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。 |
||
| S5250 |
DarunavirDarunavir is a nonpeptidic HIV protease inhibitor, used to treat HIV infection. |
||
| S2319 |
LimoninLimonin又称Limonoate D-ring-lactone 和 Limonoic acid di-delta-lactone，化学上属于Furanolactone类化合物。 |
||
| S4662 |
AtazanavirAtazanavir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。 |
||
| S4282 |
Nelfinavir MesylateNelfinavir Mesylate 是强效的HIV protease抑制剂，Ki为2 nM。 |
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| S7381 |
Pepstatin APepstatin A 是一种强效的aspartic protease抑制剂, 并可抑制HIV的复制。 |
||
| S5245 |
Raltegravir potassiumRaltegravir Potassium是一种具有口服活性的raltegravir钾盐。Raltegravir是HIV-1 integrase抑制剂。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1185 |
RitonavirRitonavir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。 |
(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 |
LopinavirLopinavir是一种有效的HIV protease抑制剂，无细胞试验中Ki为1.3 pM。 |
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 SulfateAtazanavir Sulfate是一种HIV protease抑制剂，无细胞试验中Ki值为2.66 nM。 |
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 EthanolateDarunavir Ethanolate是一种人类免疫缺陷病毒(HIV)蛋白酶抑制剂。 |
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 |
AmprenavirAmprenavir 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。 |
||
| S9567New |
Indinavir SulfateIndinavir 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。 |
||
| S5250 |
DarunavirDarunavir is a nonpeptidic HIV protease inhibitor, used to treat HIV infection. |
||
| S2319 |
LimoninLimonin又称Limonoate D-ring-lactone 和 Limonoic acid di-delta-lactone，化学上属于Furanolactone类化合物。 |
||
| S4662 |
AtazanavirAtazanavir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。 |
||
| S4282 |
Nelfinavir MesylateNelfinavir Mesylate 是强效的HIV protease抑制剂，Ki为2 nM。 |
||
| S7381 |
Pepstatin APepstatin A 是一种强效的aspartic protease抑制剂, 并可抑制HIV的复制。 |
||
| S5245 |
Raltegravir potassiumRaltegravir Potassium是一种具有口服活性的raltegravir钾盐。Raltegravir是HIV-1 integrase抑制剂。 |
