2bj4

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{{STRUCTURE_2bj4| PDB=2bj4 | SCENE= }}
{{STRUCTURE_2bj4| PDB=2bj4 | SCENE= }}
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'''ESTROGEN RECEPTOR ALPHA LBD IN COMPLEX WITH A PHAGE-DISPLAY DERIVED PEPTIDE ANTAGONIST'''
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===ESTROGEN RECEPTOR ALPHA LBD IN COMPLEX WITH A PHAGE-DISPLAY DERIVED PEPTIDE ANTAGONIST===
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==Overview==
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Recent studies have identified a series of estrogen receptor (ER)-interacting peptides that recognize sites that are distinct from the classic coregulator recruitment (AF2) region. Here, we report the structural and functional characterization of an ERalpha-specific peptide that binds to the liganded receptor in an AF2-independent manner. The 2-A crystal structure of the ER/peptide complex reveals a binding site that is centered on a shallow depression on the beta-hairpin face of the ligand-binding domain. The peptide binds in an unusual extended conformation and makes multiple contacts with the ligand-binding domain. The location and architecture of the binding site provides an insight into the peptide's ER subtype specificity and ligand interaction preferences. In vivo, an engineered coactivator containing the peptide motif is able to strongly enhance the transcriptional activity of liganded ERalpha, particularly in the presence of 4-hydroxytamoxifen. Furthermore, disruption of this binding surface alters ER's response to the coregulator TIF2. Together, these results indicate that this previously unknown interaction site represents a bona fide control surface involved in regulating receptor activity.
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(as it appears on PubMed at http://www.pubmed.gov), where 15728727 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15728727}}
==About this Structure==
==About this Structure==
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[[Category: Steroid-binding]]
[[Category: Steroid-binding]]
[[Category: Transcription factor]]
[[Category: Transcription factor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:21:47 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 16:34:58 2008''

Revision as of 13:35, 27 July 2008

Image:2bj4.png

Template:STRUCTURE 2bj4

ESTROGEN RECEPTOR ALPHA LBD IN COMPLEX WITH A PHAGE-DISPLAY DERIVED PEPTIDE ANTAGONIST

Template:ABSTRACT PUBMED 15728727

About this Structure

2BJ4 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Delineation of a unique protein-protein interaction site on the surface of the estrogen receptor., Kong EH, Heldring N, Gustafsson JA, Treuter E, Hubbard RE, Pike AC, Proc Natl Acad Sci U S A. 2005 Mar 8;102(10):3593-8. Epub 2005 Feb 23. PMID:15728727

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