Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance
Language English Country United States Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
18598016
DOI
10.1021/jm8002334
Knihovny.cz E-resources
- MeSH
- HIV-1 drug effects enzymology MeSH
- HIV Protease chemistry genetics metabolism MeSH
- HIV Protease Inhibitors chemistry pharmacology MeSH
- Metals chemistry MeSH
- Crystallography, X-Ray MeSH
- Models, Molecular MeSH
- Molecular Structure MeSH
- Mutation genetics MeSH
- Boron Compounds chemistry pharmacology MeSH
- Drug Resistance, Viral drug effects MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- HIV Protease MeSH
- HIV Protease Inhibitors MeSH
- Metals MeSH
- Boron Compounds MeSH
HIV protease (PR) is a prime target for rational anti-HIV drug design. We have previously identified icosahedral metallacarboranes as a novel class of nonpeptidic protease inhibitors. Now we show that substituted metallacarboranes are potent and specific competitive inhibitors of drug-resistant HIV PRs prepared either by site-directed mutagenesis or cloned from HIV-positive patients. Molecular modeling explains the inhibition profile of metallacarboranes by their unconventional binding mode.
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