Integrase
信号通路图
研究领域
抑制剂选择性比较
Integrase产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2005 |
Raltegravir (MK-0518)Raltegravir (MK-0518)是一种有效的integrase (IN)抑制剂，作用于WT和S217Q PFV IN，在无细胞试验中IC50分别为90 nM和40 nM。它对HIV-1 IN的选择性比对其他相关Mg2+依赖性酶要高1000倍以上，如HCV聚合酶、HIV反转录酶、HIV RNaseH、人类α-, β-, γ-聚合酶。 |
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| S2001 |
Elvitegravir (JTK-303)Elvitegravir (GS-9137, JTK-303)是一种HIV抑制剂，作用于HIV-1 IIIB，HIV-2 EHO和HIV-2 ROD，无细胞试验中IC50 分别为0.7，2.8和1.4 nM。 |
PhA efflux in MDCKII-BCRP cells. Concentration-dependent inhibition of BCRP/ABCG2 by elvitegravir and vicriviroc. Each curve depicts one representative experiment of a series of three or four; each concentration was tested in 30000 cells.
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| S2667 |
Dolutegravir (GSK1349572)Dolutegravir (GSK1349572, S/GSK1349572)是一种两个金属结合的HIV integrase抑制剂，无细胞试验中IC50为2.7 nM，对耐Raltegravir的显著突变体Y143R，Q148K，N155H，和G140S/Q148H具有适度的活性。 |
Strand transfer was carried out with RSV IN(1-269) (4 uM) and GU320R(2 uM)in the presence of 50mM NDSB201. Increasing concentrations of STIs were added as indicated at the top; DTG(Dolutegravir) in lanes 3-5, MK-2048 in lanes 6-8, and RAL in lanes 9-11. No STI was present in lane 2, and lane 1 contains the molecular weight markers. Strand transfer products and ODN substrate are identified on the right. CHS, circular half-site; OC target and SC target, open circular and supercoiled target DNA, respectively.
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| S1366 |
BMS-707035BMS-707035是一种特异性的HIV-I integrase (IN)（整合酶）抑制剂，IC50为15 nM。Phase 2。 |
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| S2765 |
MK-2048MK-2048是一种有效的integrase(IN)和INR263K抑制剂，IC50分别为2.6 nM和1.5 nM。 |
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| E0161New |
Bictegravir SodiumBictegravir (GS-9883) Sodium 是一种新型有效的 HIV-1 整合酶（HIV-1 integrase）抑制剂，专门针对 IN 链转移活性，IC50 为 7.5 nM。 |
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| S7766 |
Cabotegravir (GSK1265744)Cabotegravir (GSK744, GSK1265744, S/GSK1265744)是一种长效HIV integrase抑制剂，作用于广泛的HIV亚型，抑制了HIV-1 integrase 催化的链转移反应的IC50为3 nM。Phase 2。 |
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| S4642 |
Dolutegravir SodiumDolutegravir Sodium (GSK-1349572A)是HIV整合酶抑制剂，IC50为2.7 nM。 |
Comparison of the activity of dolutegravir (DTG), raltegravir (RAL), and elvitegravir (EVG) against wild-type HIV-2ROD9. Values for RAL and EVG include data from two previously-published studies of HIV-2 from our group [14,15] plus additional determinations; all data were obtained using the single-cycle assay. Bars indicate mean 50% effective concentrations (EC50); the number of independent determinations (n) for each strain is shown below the x-axis. P values were obtained via analysis of variance (ANOVA) of log10-transformed EC50 values with Tukey’s post test (Prism v6.0). No cytotoxic effects were observed in dolutegravir-treated MAGIC-5A cultures at concentrations as high as 10,000 nM.
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| S5911 |
BictegravirBictegravir (GS-9883)是一种新型的、有效的HIV-1 integrase抑制剂。 |
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| S4187 |
SalicylanilideSalicylanilides (WR10019)是一组具有广泛的生物活性的化合物，具有抗病毒效力，抗菌（包括抗分枝杆菌），和抗真菌活性。 |
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| S0235 |
Lavendustin BLavendustin B 抑制 HIV-1 integrase (IN) 与其同源的细胞辅助因子 lens epithelium-derived growth factor (LEDGF/p75) 的相互作用。Lavendustin B 是 Tyrosine Kinase 的抑制剂，也是 glucose transporter 1 (Glut1) 的竞争性抑制剂。 |
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| 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。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2005 |
Raltegravir (MK-0518)Raltegravir (MK-0518)是一种有效的integrase (IN)抑制剂，作用于WT和S217Q PFV IN，在无细胞试验中IC50分别为90 nM和40 nM。它对HIV-1 IN的选择性比对其他相关Mg2+依赖性酶要高1000倍以上，如HCV聚合酶、HIV反转录酶、HIV RNaseH、人类α-, β-, γ-聚合酶。 |
|
|
| S2001 |
Elvitegravir (JTK-303)Elvitegravir (GS-9137, JTK-303)是一种HIV抑制剂，作用于HIV-1 IIIB，HIV-2 EHO和HIV-2 ROD，无细胞试验中IC50 分别为0.7，2.8和1.4 nM。 |
PhA efflux in MDCKII-BCRP cells. Concentration-dependent inhibition of BCRP/ABCG2 by elvitegravir and vicriviroc. Each curve depicts one representative experiment of a series of three or four; each concentration was tested in 30000 cells.
|
|
| S2667 |
Dolutegravir (GSK1349572)Dolutegravir (GSK1349572, S/GSK1349572)是一种两个金属结合的HIV integrase抑制剂，无细胞试验中IC50为2.7 nM，对耐Raltegravir的显著突变体Y143R，Q148K，N155H，和G140S/Q148H具有适度的活性。 |
Strand transfer was carried out with RSV IN(1-269) (4 uM) and GU320R(2 uM)in the presence of 50mM NDSB201. Increasing concentrations of STIs were added as indicated at the top; DTG(Dolutegravir) in lanes 3-5, MK-2048 in lanes 6-8, and RAL in lanes 9-11. No STI was present in lane 2, and lane 1 contains the molecular weight markers. Strand transfer products and ODN substrate are identified on the right. CHS, circular half-site; OC target and SC target, open circular and supercoiled target DNA, respectively.
|
|
| S1366 |
BMS-707035BMS-707035是一种特异性的HIV-I integrase (IN)（整合酶）抑制剂，IC50为15 nM。Phase 2。 |
||
| S2765 |
MK-2048MK-2048是一种有效的integrase(IN)和INR263K抑制剂，IC50分别为2.6 nM和1.5 nM。 |
||
| E0161New |
Bictegravir SodiumBictegravir (GS-9883) Sodium 是一种新型有效的 HIV-1 整合酶（HIV-1 integrase）抑制剂，专门针对 IN 链转移活性，IC50 为 7.5 nM。 |
||
| S7766 |
Cabotegravir (GSK1265744)Cabotegravir (GSK744, GSK1265744, S/GSK1265744)是一种长效HIV integrase抑制剂，作用于广泛的HIV亚型，抑制了HIV-1 integrase 催化的链转移反应的IC50为3 nM。Phase 2。 |
||
| S4642 |
Dolutegravir SodiumDolutegravir Sodium (GSK-1349572A)是HIV整合酶抑制剂，IC50为2.7 nM。 |
Comparison of the activity of dolutegravir (DTG), raltegravir (RAL), and elvitegravir (EVG) against wild-type HIV-2ROD9. Values for RAL and EVG include data from two previously-published studies of HIV-2 from our group [14,15] plus additional determinations; all data were obtained using the single-cycle assay. Bars indicate mean 50% effective concentrations (EC50); the number of independent determinations (n) for each strain is shown below the x-axis. P values were obtained via analysis of variance (ANOVA) of log10-transformed EC50 values with Tukey’s post test (Prism v6.0). No cytotoxic effects were observed in dolutegravir-treated MAGIC-5A cultures at concentrations as high as 10,000 nM.
|
|
| S5911 |
BictegravirBictegravir (GS-9883)是一种新型的、有效的HIV-1 integrase抑制剂。 |
||
| S4187 |
SalicylanilideSalicylanilides (WR10019)是一组具有广泛的生物活性的化合物，具有抗病毒效力，抗菌（包括抗分枝杆菌），和抗真菌活性。 |
||
| S0235 |
Lavendustin BLavendustin B 抑制 HIV-1 integrase (IN) 与其同源的细胞辅助因子 lens epithelium-derived growth factor (LEDGF/p75) 的相互作用。Lavendustin B 是 Tyrosine Kinase 的抑制剂，也是 glucose transporter 1 (Glut1) 的竞争性抑制剂。 |
||
| 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。 |
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