Inhibitors of Strand Transfer That Prevent Integration and Inhibit HIV-1 Replication in Cells

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Science  28 Jan 2000:
Vol. 287, Issue 5453, pp. 646-650
DOI: 10.1126/science.287.5453.646

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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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