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| [[Image:2fsz.gif|left|200px]] | | {{Seed}} |
| | [[Image:2fsz.png|left|200px]] |
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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'''
| | ===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.
| | The line below this paragraph, {{ABSTRACT_PUBMED_16782818}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 16782818 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_16782818}} |
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| ==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]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 04:16:46 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 13:44:08 2008'' |
