Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells
Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells
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DOI：
10.1126/science.287.5453.646
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发表时间：
2000-01-28
期刊：
影响因子：
56.9
通讯作者：
Miller, MD
中科院分区：
文献类型：
--
作者：
Hazuda, DJ;Felock, P;Miller, MD
整合酶是人类免疫缺陷病毒1型（HIV-1）复制所必需的;然而，在生化测定中对分离酶的有效抑制并不容易以与整合抑制一致的方式转化为抗病毒活性。在这份报告中，我们描述了HIV-1整合酶的二酮酸抑制剂，表现出抗病毒活性，作为其整合效果的结果。这些化合物的抗病毒活性完全是由于抑制整合酶的两种催化功能之一，链转移。
Integrase is essential for human immunodeficiency virus-type 1 (HIV-1) replication; however, potent inhibition of the isolated enzyme in biochemical assays has not readily translated into antiviral activity in a manner consistent with inhibition of integration. In this report, we describe diketo acid inhibitors of HIV-1 integrase that manifest antiviral activity as a consequence of their effect on integration. The antiviral activity of these compounds is due exclusively to inhibition of one of the two catalytic functions of integrase, strand transfer.