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[豚鼠输卵管雌激素受体系统的特征]

[Characteristics of the estrogen receptor system of the oviducts in guinea pigs].

作者信息

Fanchenko H D, Shchedrina R N, Minina L S, Novikov E A

出版信息

Biull Eksp Biol Med. 1978 Jan;85(1):75-9.

PMID:626787
Abstract

Kinetic and thermodynamic parameters of the estradiol receptor (E2-R) interact in the guinea pig oviduct cytozol were studied. Specificity of the receptor system was characterized by measurment of the affinity of 14 compounds to the system. It was shown that the guinea pig oviduct R-system had a high affinity to E2 and a limited capacity. Free energy change value (52 KJ/mol) indicated stability of the complex formed. Activity of the steroid-receptor (S-R) complex formation is determined by the presence of the intact hydroxils in positions 3 (phenolic) and 17-beta of the steroid molecule; dependence of the S-R interaction rate on the different steroid molecule modifications at a number of positions supports this point. Besides, the immediate enviroment of hydroxils in positions 3 and 17 beta also influences the S-R interaction rate. Some properties of the nonsteroid diethylstilbestrol estrogen attract attention.

摘要

对豚鼠输卵管胞质溶胶中雌二醇受体(E2-R)相互作用的动力学和热力学参数进行了研究。通过测量14种化合物对该系统的亲和力来表征受体系统的特异性。结果表明,豚鼠输卵管R-系统对E2具有高亲和力且容量有限。自由能变化值(52千焦/摩尔)表明形成的复合物具有稳定性。类固醇-受体(S-R)复合物形成的活性取决于类固醇分子3位(酚羟基)和17-β位完整羟基的存在;S-R相互作用速率对类固醇分子多个位置不同修饰的依赖性支持了这一点。此外,3位和17-β位羟基的直接环境也影响S-R相互作用速率。非甾体己烯雌酚雌激素的一些特性引起了关注。

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