Article
Crystal structures for HIV-1 reverse transcriptase in complexes with three pyridinone derivatives: a new class of non-nucleoside inhibitors effective against a broad range of drug-resistant strains.
Journal of medicinal chemistry - 1 Dec 2005
Himmel Daniel M, Das Kalyan, Clark Arthur D, Hughes Stephen H, Benjahad Abdellah, Oumouch Said, Guillemont Jérôme, Coupa Sophie, Poncelet Alain, Csoka Imre, Meyer Christophe, Andries Koen, Nguyen Chi Hung, Grierson David S, Arnold Eddy
Abstract excerpt
In the treatment of AIDS, the efficacy of all drugs, including non-nucleoside inhibitors (NNRTIs) of HIV-1 reverse transcriptase (RT), has been limited by the rapid appearance of drug-resistant viruses. Lys103Asn, Tyr181Cys, and Tyr188Leu are some of the most common RT mutations that cause resistance to NNRTIs in the clinic. We report X-ray crystal structures for RT complexed with three different pyridinone...
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