Abstract
There is a great need for alternative modes of inhibition for the design of anti-HIV therapies, due to the increased resistance of HIV to currently approved drugs. A novel strategy for generating potent dimerization inhibitors of HIV-1 protease is described based on sidechain-linked interfacial peptides. In a number of cases the activity of these agents against HIV-1 protease was found to be among the most potent reported, with inhibitory constants in the low nM range.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Cross-Linking Reagents / chemical synthesis
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Cross-Linking Reagents / chemistry
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Cross-Linking Reagents / pharmacology
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Dimerization
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HIV Protease / chemistry
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HIV Protease / metabolism*
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HIV Protease Inhibitors / chemistry*
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HIV Protease Inhibitors / pharmacology
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HIV-1 / drug effects
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Kinetics
Substances
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Cross-Linking Reagents
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HIV Protease Inhibitors
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HIV Protease
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p16 protease, Human immunodeficiency virus 1