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Hazuda, Daria J.; Felock, Peter; Witmer, Marc; Wolfe, Abigail; Stillmock, Kara; Grobler, Jay A.; Espeseth, Amy; Gabryelski, Lori; Schleif, William; Blau, Carol; Miller, Michael D.
Science (American Association for the Advancement of Science), 01/2000, Letnik: 287, Številka: 5453Journal Article
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.
