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1gs4

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[[Category: prostate cancer]]
[[Category: prostate cancer]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 12:51:51 2007''
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 15:18:01 2007''

Revision as of 13:13, 30 October 2007

Image:1gs4.gif

1gs4, resolution 1.95Å

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STRUCTURAL BASIS FOR THE GLUCOCORTICOID RESPONSE IN A MUTANT HUMAN ANDROGEN RECEPTOR (ARCCR) DERIVED FROM AN ANDROGEN-INDEPENDENT PROSTATE CANCER

Overview

The crystal structure of a mutant androgen receptor (AR) ligand-binding, domain (LBD) in complex with the agonist 9alpha-fluorocortisol has been, determined at 1.95 A resolution. This mutant AR contains two mutations, (L701H and T877A) and was previously reported as a high-affinity, cortisol/cortisone responsive AR (AR(ccr)) isolated from the, androgen-independent human prostate cancer cell lines MDA PCa 2a and 2b, (Zhao et al. Nature Med. 2000, 6, 703-6). The three-dimensional structure, of the AR(ccr) LBD complexed with 9alpha-fluorocortisol shows the typical, conformation of an agonist-bound nuclear receptor in which helix 12 is, precisely positioned as a "lid" for the ligand-binding pocket. Binding of, 9alpha-fluorocortisol to the AR(ccr) involves favorable hydrogen bond, patterns on ... [(full description)]

About this Structure

1GS4 is a [Single protein] structure of sequence from [Homo sapiens] with PO4 and ZK5 as [ligands]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].

Reference

Structural basis for the glucocorticoid response in a mutant human androgen receptor (AR(ccr)) derived from an androgen-independent prostate cancer., Matias PM, Carrondo MA, Coelho R, Thomaz M, Zhao XY, Wegg A, Crusius K, Egner U, Donner P, J Med Chem. 2002 Mar 28;45(7):1439-46. PMID:11906285

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