Inhibition of human immunodeficiency virus reverse transcriptase by synadenol triphosphate and its E-isomer.
Triphosphate 1c is a potent competitive inhibitor of wild-type HIV-1 reverse transcriptase with K(i) close to ddATP. The E-isomer 2c is about 30-times weaker. Triphosphates 1c and 2c interact with the same active site of reverse transcriptase as ddATP. The extent of inhibition of two mutant forms of reverse transcriptase (RT), RT(M184V) and RT(M184I), with triphosphate 1c was about 5 and 8 times lower than that of wild-type RT(wt).
Wang
Ruifang
R
Department of Chemistry, Developmental Therapeutics Program, Barbara Ann Karmanos Cancer Institute, Wayne State University School of Medicine, Detroit, Michigan 48201-1379, USA.
Harada
Shigeyoshi
S
Mitsuya
Hiroaki
H
Zemlicka
Jiri
J
D019380:Anti-HIV Agents / Q000737:chemistry*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000235:genetics; D009154:Mutation; D009705:Nucleosides / Q000737:chemistry*; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry*; D013237:Stereoisomerism
D019380:Anti-HIV Agents; D009705:Nucleosides; D018894:Reverse Transcriptase Inhibitors; C478627:synadenol triphosphate; D054303:HIV Reverse Transcriptase