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Article

Effectiveness of nonpeptide clinical inhibitor TMC-114 on HIV-1 protease with highly drug resistant mutations D30N, I50V, and L90M.

Journal of medicinal chemistry - 23 Feb 2006

Kovalevsky Andrey Yu, Tie Yunfeng, Liu Fengling, Boross Peter I, Wang Yuan-Fang, Leshchenko Sofiya, Ghosh Arun K, Harrison Robert W, Weber Irene T

Abstract excerpt

The potent new antiviral inhibitor TMC-114 (UIC-94017) of HIV-1 protease (PR) has been studied with three PR variants containing single mutations D30N, I50V, and L90M, which provide resistance to the major clinical inhibitors. The inhibition constants (K(i)) of TMC-114 for mutants PR(D30N), PR(I50V), and PR(L90M) were 30-, 9-, and 0.14-fold, respectively, relative to wild-type PR. The molecular basis for the...

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Identifiers

PMID: 16480273
DOI: 10.1021/jm050943c
PMCID: PMC3015180

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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