Inhibitors of Strand Transfer That Prevent Integration and Inhibit HIV-1 Replication in Cells-Reference-Cited by-同舟云学术

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

Published:2000-01-28 Issue:5453 Volume:287 Page:646-650
ISSN:0036-8075
Container-title:Science
language:en
Short-container-title:Science

Author:

Hazuda Daria J.¹,Felock Peter¹,Witmer Marc¹,Wolfe Abigail¹,Stillmock Kara¹,Grobler Jay A.¹,Espeseth Amy¹,Gabryelski Lori¹,Schleif William¹,Blau Carol¹,Miller Michael D.¹

Affiliation:

1. Department of Antiviral Research, Merck Research Laboratories, West Point, PA 19486, USA.

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.

Publisher

American Association for the Advancement of Science (AAAS)

Subject

Multidisciplinary

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