替诺福韦二磷酸是大鼠DNA聚合酶α、δ和ε*的不良底物及弱抑制剂。
Tenofovir diphosphate is a poor substrate and a weak inhibitor of rat DNA polymerases alpha, delta, and epsilon*.
作者信息
Birkus Gabriel, Hájek Miroslav, Kramata Pavel, Votruba Ivan, Holý Antonín, Otová Berta
机构信息
Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic.
出版信息
Antimicrob Agents Chemother. 2002 May;46(5):1610-3. 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.
摘要
替诺福韦二磷酸酯（PMPApp）是DNA聚合酶α、δ和ε的弱抑制剂，其PMPApp的Ki值相对于dATP的Km值分别为10.2、10.2和15.2。它掺入DNA的效率比dATP低约1000倍，PMPApp的Km值分别比聚合酶α、δ和ε的dATP的Km值高350倍、2155倍和187倍。
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本文引用的文献
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