7 alpha,11 beta-disubstituted estrogens: Probes for the shape of the ligand binding pocket in the estrogen receptor

被引：21

作者：

Tedesco, R

Katzenellenbogen, JA

Napolitano, E

机构：

[1] UNIV PISA,DIPARTIMENTO CHIM BIOORGAN,I-56126 PISA,ITALY

[2] UNIV ILLINOIS,DEPT CHEM,URBANA,IL 61801

[3] SCUOLA NORMALE SUPER PISA,I-56100 PISA,ITALY

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 22期

基金：

美国国家卫生研究院;

关键词：

D O I：

10.1016/S0960-894X(97)10099-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

To investigate whether the estrogen receptor accommodates 7 alpha and 11 beta substituents on estradiol in two subsites or in a single subsite, we have prepared three sets of ligands bearing single (7 alpha or 11 beta) or double (7 alpha and 11 beta) substituents and measured their binding affinity. The different behavior of each set precludes a definitive choice, but supports a two subsite model with some limitations. (C) 1997 Elsevier Science Ltd.

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页码：2919 / 2924

页数：6

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