Literature DB >> 14561099

Inhibition of human immunodeficiency virus reverse transcriptase by synadenol triphosphate and its E-isomer.

Ruifang Wang1, Shigeyoshi Harada, Hiroaki Mitsuya, Jiri Zemlicka.   

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).

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Year:  2003        PMID: 14561099     DOI: 10.1021/jm030048y

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  2 in total

1.  Synthesis and enantioselectivity of cyclopropavir phosphates for cellular GMP kinase.

Authors:  Chengwei Li; Brian G Gentry; John C Drach; Jiri Zemlicka
Journal:  Nucleosides Nucleotides Nucleic Acids       Date:  2009-09       Impact factor: 1.381

2.  9-{[3-fluoro-2-(hydroxymethyl)cyclopropylidene]methyl}adenines and -guanines. Synthesis and antiviral activity of all stereoisomers1.

Authors:  Shaoman Zhou; Earl R Kern; Elizabeth Gullen; Yung-Chi Cheng; John C Drach; Sadahiro Tamiya; Hiroaki Mitsuya; Jiri Zemlicka
Journal:  J Med Chem       Date:  2006-10-05       Impact factor: 7.446

  2 in total

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