Inhibition of Human Immunodeficiency Virus Reverse Transcriptase by Synadenol Triphosphate and Its E-Isomer
- 24 September 2003
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 46 (22) , 4799-4802
- https://doi.org/10.1021/jm030048y
Abstract
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).Keywords
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