Article
Relationship of potency and resilience to drug resistant mutations for GW420867X revealed by crystal structures of inhibitor complexes for wild-type, Leu100Ile, Lys101Glu, and Tyr188Cys mutant HIV-1 reverse transcriptases.
Journal of medicinal chemistry - 17 May 2007
Ren Jingshan, Nichols Charles E, Chamberlain Philip P, Weaver Kurt L, Short Steven A, Chan Joseph H, Kleim Jörg-Peter, Stammers David K
Abstract excerpt
The selection of drug resistant viruses is a major problem in efforts to combat HIV and AIDS, hence, new compounds are required. We report crystal structures of wild-type and mutant HIV-1 RT with bound non-nucleoside (NNRTI) GW420867X, aimed at investigating the basis for its high potency and improved drug resistance profile compared to the first-generation drug nevirapine. GW420867X occupies a smaller volume...
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