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Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells.

Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells. 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. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Science (New York, N.Y.) Pubmed

Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells.

Science (New York, N.Y.) , Volume 287 (5453): 5 – Feb 18, 2000

Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells.


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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ISSN
0036-8075
DOI
10.1126/science.287.5453.646
pmid
10649997

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.

Journal

Science (New York, N.Y.)Pubmed

Published: Feb 18, 2000

There are no references for this article.