2p7z

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{{STRUCTURE_2p7z| PDB=2p7z | SCENE= }}
{{STRUCTURE_2p7z| PDB=2p7z | SCENE= }}
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'''Estrogen Related Receptor Gamma in complex with 4-hydroxy-tamoxifen'''
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===Estrogen Related Receptor Gamma in complex with 4-hydroxy-tamoxifen===
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==Overview==
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We screened the ligand-binding domain of estrogen-related receptor (ERR) gamma in ThermoFluor((R)), in an effort to develop chemical tools and decipher the biology of this orphan nuclear receptor. Several ligands were found to stabilize thermodynamically the protein. Amongst the ligands were bisphenol A (BPA) and 4-chloro-3-methyl phenol (ClCH(3)Ph). These ligands were further characterized and found to be competitive for 4-hydroxytamoxifen (4OHT) binding, a known reported antagonist ligand for ERRgamma, but functionally they did not enhance or disrupt affinity of the receptor for co-activator peptides. The preservation of the constitutive active conformation of the receptor in the presence of these two ligands was confirmed upon the determination of the co-crystal structures. The structures of BPA and ClCH(3)Ph were determined to a resolution of 2.1 and 2.3A, respectively, and the antagonist 4OHT was refined to 2.5A resolution. In the presence of BPA and ClCH(3)Ph the receptor maintained the transcriptional active conformation as reported previously for the apo-protein in the presence of a co-activator peptide fragment. In addition the ERRgamma-BPA structure identifies an interaction between the phenolic-OH and the side chain of N346. The preservation of the constitutive active conformation of the receptor in the presence of the small phenol compounds suggest that the biological activity of the receptor might be regulated by a natural occurring ligand.
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{{ABSTRACT_PUBMED_17964775}}
==About this Structure==
==About this Structure==
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[[Category: Hormone receptor]]
[[Category: Hormone receptor]]
[[Category: Three layered alpha helical sandwich]]
[[Category: Three layered alpha helical sandwich]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 12:34:36 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 21:29:29 2008''

Revision as of 18:29, 28 July 2008

Image:2p7z.png

Template:STRUCTURE 2p7z

Estrogen Related Receptor Gamma in complex with 4-hydroxy-tamoxifen

Template:ABSTRACT PUBMED 17964775

About this Structure

2P7Z is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structural determination of estrogen-related receptor gamma in the presence of phenol derivative compounds., Abad MC, Askari H, O'Neill J, Klinger AL, Milligan C, Lewandowski F, Springer B, Spurlino J, Rentzeperis D, J Steroid Biochem Mol Biol. 2008 Jan;108(1-2):44-54. Epub 2007 Sep 14. PMID:17964775

Page seeded by OCA on Mon Jul 28 21:29:29 2008

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