Tenofovir diphosphate is a poor substrate and a weak inhibitor of rat DNA polymerases α,δ, and ε

Tenofovir diphosphate is a poor substrate and a weak inhibitor of rat DNA polymerases α,δ, and ε
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DOI:
10.1128/aac.46.5.1610-1613.2002
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发表时间:
2002-05-01
影响因子:
4.9
通讯作者:
Otová, B
Otová, B
中科院分区:
医学2区
文献类型:
--
作者:
Birkus, G;Hájek, M;Otová, B

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替诺福韦二磷酸(PMPApp)是DNA聚合酶的弱抑制剂,其K-I值(K-PMPAApp(I))相对于dATP(K-dATP(M))的K-m分别为10.2、10.2和15.2。它与DNA的结合效率约为dATP的1,000倍,其K-PMPApp(M)值分别是Pola、Delta和epsilon*的K-dATP(M)值的350倍、2,155倍和187倍。
Tenofovir diphosphate (PMPApp) is a weak inhibitor of DNA polymerases (pol) alpha, delta, and epsilon*, with values for the K-i for PMPApp (K-PMPAApp(i)) relative to the K-m for dATP (K-dATP(m)) 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 K-PMPApp(m) values 350-, 2,155-, and 187-fold higher than K-dATP(m) values for pol alpha, delta, and epsilon*, respectively.