4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 23, Pages 6097-6099

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.10.021

Keywords

Aminopyrazol; Benzamides; Crystal structure; Glucocorticoid receptor

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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.

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