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Literature DB >> 11959615

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

Gabriel Birkus¹, Miroslav Hájek, Pavel Kramata, Ivan Votruba, Antonín Holý, Berta Otová.

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.

Entities: Chemical Gene Species

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Year: 2002 PMID： 11959615 PMCID： PMC127178 DOI： 10.1128/AAC.46.5.1610-1613.2002

Source DB: PubMed Journal: Antimicrob Agents Chemother ISSN： 0066-4804 Impact factor: 5.191

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Authors: G Birkus; I Votruba; A Holý; B Otová
Journal: Biochem Pharmacol Date: 1999-08-01 Impact factor: 5.858

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8. Assessment of mitochondrial toxicity in human cells treated with tenofovir: comparison with other nucleoside reverse transcriptase inhibitors.

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Authors: E De Clercq; T Sakuma; M Baba; R Pauwels; J Balzarini; I Rosenberg; A Holý
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Review 5. Clinical potential of the acyclic nucleoside phosphonates cidofovir, adefovir, and tenofovir in treatment of DNA virus and retrovirus infections.

Authors: Erik De Clercq
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9. Identifying the role of PrimPol in TDF-induced toxicity and implications of its loss of function mutation in an HIV+ patient.

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