在HIV感染的细胞中,HIV蛋白酶特异性地裂解病毒前体蛋白,使感染性病毒颗粒能最终形成。这些病毒前体蛋白存在分解位点,只能被HIV和其密切相关病毒的蛋白酶识别。沙奎那韦是一种类肽,结构上模拟这型分解位点。因此,沙奎那韦与HIV-1和2蛋白酶的活性部位恰好可以紧密结合,体外显示可逆和选择性抑制蛋白酶的活性,而较人类蛋白酶的亲和力大约低50,000倍。与核苷类似物(齐多夫定等)不同,沙奎那韦直接作用于病毒靶酶,不需经代谢激活,对静止细胞也有潜在作用。在10-10摩尔/升浓度下,沙奎那韦对淋巴母细胞株和单核细胞株以及被实验室病毒株或临床分离的HIV-1感染的淋巴细胞和单核细胞的起始培养有作用。实验室细胞培养结果显示,沙奎那韦在与其他逆转录酶抑制剂(包括AZT(齐多夫定)、ddc(扎西他滨)、ddI(去羟肌苷)进行两联或三联治疗HIV-1感染时,有附加的协同抗病毒作用,但毒性并不增加。 Used in cell signaling and immunology studies.
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Saquinavir
CAS number:127779-20-8 molecular formula:C38H50N6O5
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| Chinese alias | 沙奎那韦 | ||
| English alias | SAQUINAVIR [JAN] | (2S)-N-[(2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)-decahydroisoquinolin-2-yl]-3-hydroxy-1-phenylbutan-2-yl]-2-[(quinolin-2-yl)formamido]butanediamide | (S)-N-((alphaS)-alpha-((1R)-2-((3S,4AS,8AS)-3-(TERT-BUTYLCARBAMOYL)OCTAHYDRO-2( | ||
| CAS number | 127779-20-8 | molecular formula | C38H50N6O5 |
| molecular weight | 670.84 g/mol | Exact mass | - |
| PSA | 167.000 Ų | logp | 4.2 |
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