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己烯雌酚衍生物对脱氧核糖核酸核苷酸转移酶的抑制作用。

The inhibition of deoxyribonucleic acid nucleotidyltransferase by stilboestrol derivatives.

作者信息

Fahmy A R, Griffiths K

出版信息

Biochem J. 1968 Aug;108(5):749-53. doi: 10.1042/bj1080749.

Abstract

The inhibition by diethylstilboestrol of DNA nucleotidyltransferase isolated from calf thymus was studied. The inhibition exercised by diethylstilboestrol appears to obey competitive kinetics with respect to DNA primer. The activities of both replicative and terminal enzymes were affected to the same extent. There was no evidence of binding between DNA and diethylstilboestrol. A comparative study of the inhibitory effects of some stilboestrol derivatives is presented. The alkyl substitution in the alphaalpha'-positions seem to alter the inhibitory effect of these compounds: dimethylstilboestrol was more inhibitory than stilbene, and diethylstilboestrol was more inhibitory than dimethylstilboestrol. Hexoestrol, in which the alphaalpha'-ethylenic linkage is saturated, was the most effective inhibitor.

摘要

研究了己烯雌酚对从小牛胸腺分离的DNA核苷酸转移酶的抑制作用。己烯雌酚所产生的抑制作用似乎遵循关于DNA引物的竞争性动力学。复制酶和末端酶的活性受到同等程度的影响。没有证据表明DNA与己烯雌酚之间存在结合。本文对一些己烯雌酚衍生物的抑制作用进行了比较研究。αα′位的烷基取代似乎改变了这些化合物的抑制作用:二甲基己烯雌酚比芪的抑制作用更强,而己烯雌酚比二甲基己烯雌酚的抑制作用更强。αα′位烯键饱和的己烷雌酚是最有效的抑制剂。

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