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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
15
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pubmed:dateCreated |
2008-8-8
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pubmed:abstractText |
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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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
1520-4804
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pubmed:author |
pubmed-author:BryndaJiríJ,
pubmed-author:CíglerPetrP,
pubmed-author:FanfrlíkJindrichJ,
pubmed-author:GrünerBohumírB,
pubmed-author:Grantz SaskováKláraK,
pubmed-author:KonvalinkaJanJ,
pubmed-author:KozísekMilanM,
pubmed-author:KrálVladimírV,
pubmed-author:LepsíkMartinM,
pubmed-author:PlesekJaromírJ,
pubmed-author:PokornáJanaJ,
pubmed-author:RezácováPavlínaP,
pubmed-author:VáclavíkováJanaJ
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pubmed:issnType |
Electronic
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pubmed:day |
14
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pubmed:volume |
51
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4839-43
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pubmed:meshHeading |
pubmed-meshheading:18598016-Boron Compounds,
pubmed-meshheading:18598016-Crystallography, X-Ray,
pubmed-meshheading:18598016-Drug Resistance, Viral,
pubmed-meshheading:18598016-HIV Protease,
pubmed-meshheading:18598016-HIV Protease Inhibitors,
pubmed-meshheading:18598016-HIV-1,
pubmed-meshheading:18598016-Metals,
pubmed-meshheading:18598016-Models, Molecular,
pubmed-meshheading:18598016-Molecular Structure,
pubmed-meshheading:18598016-Mutation
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pubmed:year |
2008
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pubmed:articleTitle |
Inorganic polyhedral metallacarborane inhibitors of HIV protease: a new approach to overcoming antiviral resistance.
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pubmed:affiliation |
Gilead Sciences and IOCB Research Center Prague, Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Praha, Czech Republic.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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