Article
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
Journal of medicinal chemistry - 14 Aug 2008
Kozísek Milan, Cígler Petr, Lepsík Martin, Fanfrlík Jindrich, Rezácová Pavlína, Brynda Jirí, Pokorná Jana, Plesek Jaromír, Grüner Bohumír, Grantz Sasková Klára, Václavíková Jana, Král Vladimír, Konvalinka Jan
Abstract excerpt
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...
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