AFFINITY OF THE ANTIVIRAL ENANTIOMERS OF OXATHIOLANE CYTOSINE NUCLEOSIDES FOR HUMAN 2'-DEOXYCYTIDINE KINASE

被引：72

作者：

SHEWACH, DS

LIOTTA, DC

SCHINAZI, RF

机构：

[1] VET AFFAIRS MED CTR,1670 CLAIRMONT RD,DECATUR,GA 30033

[2] UNIV MICHIGAN,DEPT PHARMACOL,ANN ARBOR,MI 48109

[3] EMORY UNIV,DEPT CHEM,BIOCHEM PHARMACOL LAB,ATLANTA,GA 30322

[4] EMORY UNIV,DEPT PEDIAT,BIOCHEM PHARMACOL LAB,ATLANTA,GA 30322

来源：

BIOCHEMICAL PHARMACOLOGY | 1993年 / 45卷 / 07期

关键词：

D O I：

10.1016/0006-2952(93)90058-5

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The two enantiomers of 2',3'-dideoxy-3'-thiacytidine (BCH-189) and their 5-fluoro analogs (FTC) were found to be good substrates for human 2'-deoxycytidine kinase with K(m) values in the 5.7 to 42.1 muM range. The affinity of the (-)-enantiomers was greater than that of the (+)-compounds. These results may explain the greater in vitro antiviral potency against human immunodeficiency virus and hepatitis B virus of the (-)-enantiomers when compared to their (+)-counterparts. The (+)- and (-)-enantiomers of FTC and BCH-189 are the first nucleoside analogs for which we have observed lower apparent kinetic constants for this enzyme in the presence of ATP compared to UTP.

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页码：1540 / 1543

页数：4

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