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Literature DB >> 18808097

Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir.

Andrey Y Kovalevsky¹, Arun K Ghosh, Irene T Weber.

Abstract

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 explain its antiviral potency.

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Year: 2008 PMID： 18808097 PMCID： PMC2771923 DOI： 10.1021/jm800283k

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

25 in total

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Review 3. Inhibitors of HIV-1 protease: a major success of structure-assisted drug design.

Authors: A Wlodawer; J Vondrasek
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