Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir.
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ABSTRACT:
SUBMITTER: Kovalevsky AY
PROVIDER: S-EPMC2771923 | biostudies-literature | 2008 Oct
REPOSITORIES: biostudies-literature
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Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir.
Kovalevsky Andrey Y AY Ghosh Arun K AK Weber Irene T IT
Journal of medicinal chemistry 20080920 20
Darunavir, a potent antiviral drug, showed an unusual second binding site on the HIV-1 protease dimer surface of the V32I drug resistant mutant and normal binding in the active site cavity. Kinetic analysis for wild type and mutant protease showed mixed-type competitive-uncompetitive inhibition for darunavir and the chemically related amprenavir, while saquinavir showed competitive inhibition. The inhibition model is consistent with the observed second binding site for darunavir and helps to exp ...[more]
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