2fsz

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[[Image:2fsz.gif|left|200px]]
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{{Seed}}
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{{STRUCTURE_2fsz| PDB=2fsz | SCENE= }}
{{STRUCTURE_2fsz| PDB=2fsz | SCENE= }}
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'''A second binding site for hydroxytamoxifen within the coactivator-binding groove of estrogen receptor beta'''
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===A second binding site for hydroxytamoxifen within the coactivator-binding groove of estrogen receptor beta===
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==Overview==
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Evidence is presented that the estrogen antagonist 4-hydroxytamoxifen (HT) can occupy not only the core binding pocket within the ligand-binding domain of estrogen receptor (ER) beta but also a second site on its surface. The crystal structure of the ligand-binding domain (LBD) associated with HT was determined to 2.2 A and revealed two molecules of HT bound to the protein. One was located in the consensus ligand-binding pocket, whereas the other bound to a site that overlaps with the hydrophobic groove of the coactivator recognition surface. Relative to the ERalpha-tamoxifen structure, helix 12 has been displaced from the coactivator recognition surface and occupies a unique position. Although it has been demonstrated that association of the antagonist with the core ligand-binding pocket is sufficient to induce an antagonist ligand-binding domain conformation, this structure suggests that small molecules may directly antagonize receptor-coactivator interactions. These results provide a direct demonstration of two binding sites for HT in ERbeta, as has been previously suggested for ERalpha by using biochemical methods, and represent a crystal structure of a small nonpeptide molecule occupying the coactivator recognition site.
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The line below this paragraph, {{ABSTRACT_PUBMED_16782818}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16782818 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16782818}}
==About this Structure==
==About this Structure==
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[[Category: Wang, Yong]]
[[Category: Wang, Yong]]
[[Category: Nuclear hormone binding domain]]
[[Category: Nuclear hormone binding domain]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 04:16:46 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 13:44:08 2008''

Revision as of 10:44, 29 July 2008

Image:2fsz.png

Template:STRUCTURE 2fsz

A second binding site for hydroxytamoxifen within the coactivator-binding groove of estrogen receptor beta

Template:ABSTRACT PUBMED 16782818

About this Structure

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

Reference

A second binding site for hydroxytamoxifen within the coactivator-binding groove of estrogen receptor beta., Wang Y, Chirgadze NY, Briggs SL, Khan S, Jensen EV, Burris TP, Proc Natl Acad Sci U S A. 2006 Jun 27;103(26):9908-11. Epub 2006 Jun 16. PMID:16782818

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