Pre-steady state kinetic analysis of cyclobutyl derivatives of 2′-deoxyadenosine 5′-triphosphate as inhibitors of HIV-1 reverse transcriptase

…, SJ Garforth, VR Prasad, RF Schinazi, DC Liotta…

文献索引：Kim, Jiae; Wang, Ligong; Li, Yongfeng; Becnel, Kimberlynne D.; Frey, Kathleen M.; Garforth, Scott J.; Prasad, Vinayaka R.; Schinazi, Raymond F.; Liotta, Dennis C.; Anderson, Karen S. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 12 p. 4064 - 4067

全文：HTML全文

被引用次数: 4

摘要

Pre-steady state kinetic analysis was utilized for biochemical evaluation of a series of cyclobutyl adenosine nucleotide analogs with HIV-1 RTWT. The phosphonyl-diphosphate form of the cyclobutyl nucleotide, 5, was the most efficiently incorporated of the series. Nucleotide 5 was fourfold more efficiently incorporated than the FDA approved TFV-DP by RTWT. The kinetics of incorporation for 5 using the drug resistant mutant enzyme K65R ...