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

Overview

Journal Science

Specialty Science

Date 2000 Jan 29

PMID 10649997

Citations 361

Authors

D J Hazuda

P Felock

M Witmer

A Wolfe

K Stillmock

J A Grobler

A Espeseth

L Gabryelski

W Schleif

C Blau

M D Miller

Affiliations

Soon will be listed here.

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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