Crystal structures for HIV-1 reverse transcriptase in complexes with three pyridinone derivatives: a new class of non-nucleoside inhibitors effective against a broad …

…, A Poncelet, I Csoka, C Meyer, K Andries…

Index: Benjahad, Abdellah; Croisy, Martine; Monneret, Claude; Bisagni, Emile; Mabire, Dominique; Coupa, Sophie; Poncelet, Alain; Csoka, Imre; Guillemont, Jerome; Meyer, Christophe; Andries, Koen; Pauwels, Rudi; De Bethune, Marie-Pierre; Himmel, Daniel M.; Das, Kalyan; Arnold, Eddy; Chi, Hung Nguyen; Grierson, David S. Journal of Medicinal Chemistry, 2005 , vol. 48, # 6 p. 1948 - 1964

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Citation Number: 118

Abstract

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 derivatives, R157208, ...