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
Current Topics in Medicinal Chemistry
Title: HIV-1 Integrase Inhibitors: A Decade of Research and Two Drugs in Clinical Trial
Volume: 4 Issue: 10
Author(s): Allison A. Johnson, Christophe Marchand and Yves Pommier
Affiliation:
Keywords: hiv-1 integrase, diketo acids, hiv inhibitors, aids, integrase inhibitors
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.
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Cite this article as:
Johnson A. Allison, Marchand Christophe and Pommier Yves, HIV-1 Integrase Inhibitors: A Decade of Research and Two Drugs in Clinical Trial, Current Topics in Medicinal Chemistry 2004; 4 (10) . https://dx.doi.org/10.2174/1568026043388394
DOI https://dx.doi.org/10.2174/1568026043388394 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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