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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenine / analogs & derivatives*
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Adenine / metabolism*
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Adenine / pharmacology
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Animals
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Anti-HIV Agents / metabolism*
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Anti-HIV Agents / pharmacology
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DNA Polymerase I / antagonists & inhibitors
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DNA Polymerase I / metabolism
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DNA Polymerase II / antagonists & inhibitors
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DNA Polymerase II / metabolism
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DNA Polymerase III / antagonists & inhibitors
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DNA Polymerase III / metabolism
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DNA-Directed DNA Polymerase / metabolism*
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Nucleic Acid Synthesis Inhibitors*
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Organophosphonates*
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Organophosphorus Compounds / metabolism*
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Organophosphorus Compounds / pharmacology
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Rats
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Reverse Transcriptase Inhibitors / metabolism*
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Reverse Transcriptase Inhibitors / pharmacology
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Tenofovir
Substances
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Anti-HIV Agents
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Nucleic Acid Synthesis Inhibitors
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Organophosphonates
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Organophosphorus Compounds
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Reverse Transcriptase Inhibitors
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Tenofovir
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DNA Polymerase I
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DNA Polymerase II
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DNA Polymerase III
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DNA-Directed DNA Polymerase
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Adenine