The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist |
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| Authors: | Madauss Kevin P Bledsoe Randy K Mclay Iain Stewart Eugene L Uings Iain J Weingarten Gordon Williams Shawn P |
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| Institution: | Department of Computational and Structural Chemistry, Molecular Discovery Research, GlaxoSmithKline, 5 Moore Drive, Research Triangle Park, NC 27709, USA. kevin.p.madauss@gsk.com |
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| Abstract: | 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). |
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