Inhibitors of Strand Transfer That Prevent Integration and Inhibit HIV-1 Replication in Cells
Daria J. Hazuda(United States Military Academy), Peter J. Felock(United States Military Academy), Marc Witmer(United States Military Academy), Abigail Wolfe(United States Military Academy), Kara A. Stillmock(United States Military Academy), Jay A. Grobler(United States Military Academy), Amy S. Espeseth(United States Military Academy), Lori J. Gabryelski(United States Military Academy), William A. Schleif(United States Military Academy), Carol Blau(United States Military Academy), Michael D. Miller(United States Military Academy)
Cited by 1,128
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.
Related Papers
No related papers found
Powered by citation graph analysis