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

被引:31
作者
Birkus, G
Hájek, M
Kramata, P
Votruba, I
Holy, A
Otová, B
机构
[1] Acad Sci Czech Republ, Inst Organ Chem & Biochem, Prague, Czech Republic
[2] Charles Univ Prague, Fac Med 1, Inst Biol & Med Genet, Prague, Czech Republic
[3] Charles Univ Prague, Gen Teaching Hosp, Prague, Czech Republic
关键词
D O I
10.1128/AAC.46.5.1610-1613.2002
中图分类号
Q93 [微生物学];
学科分类号
071005 ; 100705 ;
摘要
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.
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页码:1610 / 1613
页数:4
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