Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells

被引：976

作者：

Hazuda, DJ ^{[1
]}

Felock, P ^{[1
]}

Witmer, M ^{[1
]}

Wolfe, A ^{[1
]}

Stillmock, K ^{[1
]}

Grobler, JA ^{[1
]}

Espeseth, A ^{[1
]}

Gabryelski, L ^{[1
]}

Schleif, W ^{[1
]}

Blau, C ^{[1
]}

Miller, MD ^{[1
]}

机构：

[1] Merck Sharp & Dohme Res Labs, Dept Antiviral Res, W Point, PA 19486 USA

来源：

SCIENCE | 2000年 / 287卷 / 5453期

关键词：

D O I：

10.1126/science.287.5453.646

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 [理学]; 0710 [生物学]; 09 [农学];

摘要：

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.

引用

页码：646 / 650

页数：5

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