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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

HIV-1 Integrase Inhibitors: A Decade of Research and Two Drugs in Clinical Trial

Author(s): Allison A. Johnson, Christophe Marchand and Yves Pommier

Volume 4, Issue 10, 2004

Page: [1059 - 1077] Pages: 19

DOI: 10.2174/1568026043388394

Price: $65

Abstract

AIDS is currently treated with a combination therapy of reverse transcriptase and protease inhibitors. Recently, the FDA approved a drug targeting HIV-1 entry into cells. There are currently no FDA approved drugs targeting HIV-1 integrase, though many scientists and drug companies are actively in pursuit of clinically useful integrase inhibitors. The objective of this review is to provide an update on integrase inhibitors reported in the last two years, including two novel inhibitors in early clinical trials, recently developed hydroxylated aromatics, natural products, peptide, antibody and oligonucleotide inhibitors. Additionally, the proposed mechanism of diketo acid inhibition is reviewed.

Keywords: hiv-1 integrase, diketo acids, hiv inhibitors, aids, integrase inhibitors


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