Exploiting drug-resistant enzymes as tools to identify thienopyrimidinone inhibitors of human immunodeficiency virus reverse transcriptase-associated ribonuclease H

…, JW Rausch, JA Wilson, H Taskent-Sezgin…

文献索引：Masaoka, Takashi; Chung, Suhman; Caboni, Pierluigi; Rausch, Jason W.; Wilson, Jennifer A.; Taskent-Sezgin, Humeyra; Beutler, John A.; Tocco, Graziella; Le Grice, Stuart F. J. Journal of Medicinal Chemistry, 2013 , vol. 56, # 13 p. 5436 - 5445

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被引用次数: 17

摘要

The thienopyrimidinone 5, 6-dimethyl-2-(4-nitrophenyl) thieno [2, 3-d] pyrimidin-4 (3 H)-one (DNTP) occupies the interface between the p66 ribonuclease H (RNase H) domain and p51 thumb of human immunodeficiency virus reverse transcriptase (HIV RT), thereby inducing a conformational change incompatible with catalysis. Here, we combined biochemical characterization of 39 DNTP derivatives with antiviral testing of selected compounds. In ...