2. Academic Validation
  3. Tenofovir diphosphate is a poor substrate and a weak inhibitor of rat DNA polymerases alpha, delta, and epsilon*

Tenofovir diphosphate is a poor substrate and a weak inhibitor of rat DNA polymerases alpha, delta, and epsilon*

  • Antimicrob Agents Chemother. 2002 May;46(5):1610-3. doi: 10.1128/AAC.46.5.1610-1613.2002.
Gabriel Birkus 1,  Miroslav Hájek,  Pavel Kramata,  Ivan Votruba,  Antonín Holý,  Berta Otová
Affiliations

Affiliation

  • 1 Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic. Gabriel_Birkus@gilead.com
PMID: 11959615 DOI: 10.1128/AAC.46.5.1610-1613.2002
Abstract

Tenofovir diphosphate (PMPApp) is a weak inhibitor of DNA polymerases (pol) alpha, delta, and epsilon*, with values for the Ki for PMPApp ((PMPApp)Ki) relative to the Km for dATP ((dATP)Km) of 10.2, 10.2, and 15.2, respectively. Its incorporation into DNA was about 1,000-fold less efficient than that of dATP, with (PMPApp)Km values 350-, 2,155-, and 187-fold higher than (dATP)Km values for pol alpha, delta, and epsilon*, respectively.

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