Identification of an agonist ligand for estrogen-related receptors ERRβ/γ

被引：63

作者：

Yu, DD ^{[1
]}

Forman, BM ^{[1
]}

机构：

[1] City Hope Natl Med Ctr, Gonda Diabetes & Genet Res Ctr, Dept Gene Regulat & Drug Discovery, Beckman Res Inst, Duarte, CA 91010 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 05期

关键词：

estrogen-related receptor; nuclear hormone receptor; agonist;

D O I：

10.1016/j.bmcl.2005.01.025

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In order to develop agonist ligands that are specific for the estrogen-related receptors ERR beta/gamma, a hydrazone with a 4-hydroxy group at one phenyl ring and a 4-diethylamino moiety at the other phenyl ring was synthesized. We demonstrate that compound 3 (DY131; N'-{(1E)-[4-(diethylamino)phenyl]methylene}-4-hydroxybenzohydrazide) effectively and selectively activates ERR beta/gamma. DY131 had no effect on the structurally related receptors ERR alpha or the estrogen receptors alpha and beta (ER alpha/beta). This work defines a convenient synthesis for a novel and selective pharmacologic tool that can be used to elucidate the biological activities of ERR beta/gamma. (c) 2005 Elsevier Ltd. All rights reserved.

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页码：1311 / 1313

页数：3

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