Article
Pre-steady state kinetic analysis of cyclobutyl derivatives of 2'-deoxyadenosine 5'-triphosphate as inhibitors of HIV-1 reverse transcriptase.
Bioorganic & medicinal chemistry letters - 15 Jun 2012
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
Abstract excerpt
Pre-steady state kinetic analysis was utilized for biochemical evaluation of a series of cyclobutyl adenosine nucleotide analogs with HIV-1 RT(WT). 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 RT(WT). The kinetics of incorporation for 5 using the drug...
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