The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist

被引：45

作者：

Madauss, Kevin P. ^{[1
]}

Bledsoe, Randy K. ^{[2
]}

Mclay, Iain ^{[1
]}

Stewart, Eugene L. ^{[1
]}

Uings, Iain J. ^{[3
]}

Weingarten, Gordon ^{[3
]}

Williams, Shawn P. ^{[1
]}

机构：

[1] GlaxoSmithKline Inc, Mol Discovery Res, Dept Computat & Struct Chem, Res Triangle Pk, NC 27709 USA

[2] GlaxoSmithKline Inc, Mol Discovery Res, Dept Biol Reagents & Assay Dev, Res Triangle Pk, NC 27709 USA

[3] GlaxoSmithKline Plc, Med Res Ctr, Immunoepigenet DPU, Immunoinflammat CEDD, Stevenage SG1 2NY, Herts, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 23期

关键词：

Aminopyrazol; Benzamides; Crystal structure; Glucocorticoid receptor;

D O I：

10.1016/j.bmcl.2008.10.021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The amino-pyrazole 2,6-dichloro-N-ethyl benzamide 1 is a selective GR agonist with dexamethasone-like in vitro potency. Its X-ray crystal structure in the GR LBD (Glucocorticoid ligand-binding domain) is described and compared to other reported structures of steroidal GR agonists in the GR LBD (3E7C). (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：6097 / 6099

页数：3

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