Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells |
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Authors: | Hazuda D J Felock P Witmer M Wolfe A Stillmock K Grobler J A Espeseth A Gabryelski L Schleif W Blau C Miller M D |
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Institution: | Department of Antiviral Research, Merck Research Laboratories, West Point, PA 19486, USA. daria-hazuda@merck.com |
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Abstract: | 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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