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Tenofovir diphosphate is a poor substrate and a weak inhibitor of rat DNA polymerases alpha, delta, and epsilon*.
- Source :
-
Antimicrobial agents and chemotherapy [Antimicrob Agents Chemother] 2002 May; Vol. 46 (5), pp. 1610-3. - Publication Year :
- 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.
- Subjects :
- Adenine pharmacology
Animals
Anti-HIV Agents pharmacology
DNA Polymerase I antagonists & inhibitors
DNA Polymerase I metabolism
DNA Polymerase II antagonists & inhibitors
DNA Polymerase II metabolism
DNA Polymerase III antagonists & inhibitors
DNA Polymerase III metabolism
Organophosphorus Compounds pharmacology
Rats
Reverse Transcriptase Inhibitors pharmacology
Tenofovir
Adenine analogs & derivatives
Adenine metabolism
Anti-HIV Agents metabolism
DNA-Directed DNA Polymerase metabolism
Nucleic Acid Synthesis Inhibitors
Organophosphonates
Organophosphorus Compounds metabolism
Reverse Transcriptase Inhibitors metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 0066-4804
- Volume :
- 46
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Antimicrobial agents and chemotherapy
- Publication Type :
- Academic Journal
- Accession number :
- 11959615
- Full Text :
- https://doi.org/10.1128/AAC.46.5.1610-1613.2002