2e2r

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{{STRUCTURE_2e2r| PDB=2e2r | SCENE= }}
{{STRUCTURE_2e2r| PDB=2e2r | SCENE= }}
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'''Crystal structure of human estrogen-related receptor gamma ligand binding domain complex with bisphenol A'''
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===Crystal structure of human estrogen-related receptor gamma ligand binding domain complex with bisphenol A===
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==Overview==
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Many lines of evidence reveal that bisphenol A (BPA) functions at very low doses as an endocrine disruptor. The human estrogen-related receptor gamma (ERR gamma) behaves as a constitutive activator of transcription, although the endogenous ligand is unknown. We have recently demonstrated that BPA binds strongly to ERR gamma (K(D) = 5.5 nM), but not to the estrogen receptor (ER). BPA preserves the ERR gamma's basal constitutive activity, and protects the selective ER modulator 4-hydroxytamoxifen from its deactivation of ERR gamma. In order to shed light on a molecular mechanism, we carried out the X-ray analysis of crystal structure of the ERR gamma ligand-binding domain (LBD) complexed with BPA. BPA binds to the receptor cavity without changing any internal structures of the pocket of the ERR gamma-LBD apo form. The hydrogen bonds of two phenol-hydroxyl groups, one with both Glu275 and Arg316, the other with Asn346, anchor BPA in the pocket, and surrounding hydrophobic bonds, especially with Tyr326, complete BPA's strong binding. Maintaining the 'activation helix' (helix 12) in an active conformation would as a result preserve receptor constitutive activity. Our results present the first evidence that the nuclear receptor forms complexes with the endocrine disruptor, providing detailed molecular insight into the interaction features.
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(as it appears on PubMed at http://www.pubmed.gov), where 17761695 is the PubMed ID number.
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{{ABSTRACT_PUBMED_17761695}}
==About this Structure==
==About this Structure==
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[[Category: Nuclear receptor]]
[[Category: Nuclear receptor]]
[[Category: Transcription]]
[[Category: Transcription]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 01:49:00 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 19:22:40 2008''

Revision as of 16:22, 28 July 2008

Image:2e2r.png

Template:STRUCTURE 2e2r

Crystal structure of human estrogen-related receptor gamma ligand binding domain complex with bisphenol A

Template:ABSTRACT PUBMED 17761695

About this Structure

2E2R is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structural evidence for endocrine disruptor bisphenol A binding to human nuclear receptor ERR gamma., Matsushima A, Kakuta Y, Teramoto T, Koshiba T, Liu X, Okada H, Tokunaga T, Kawabata S, Kimura M, Shimohigashi Y, J Biochem. 2007 Oct;142(4):517-24. Epub 2007 Aug 30. PMID:17761695

Page seeded by OCA on Mon Jul 28 19:22:40 2008

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