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Science. 2000 Jan 28;287(5453):646-50.

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

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Department of Antiviral Research, Merck Research Laboratories, West Point, PA 19486, USA.


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.

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