Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells
DJ Hazuda, P Felock, M Witmer, A Wolfe, K Stillmock… - Science, 2000 - science.org
DJ Hazuda, P Felock, M Witmer, A Wolfe, K Stillmock, JA Grobler, A Espeseth, L Gabryelski…
Science, 2000•science.orgIntegrase 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.
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.
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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