2fsz: Difference between revisions
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[[Image:2fsz.gif|left|200px]] | [[Image:2fsz.gif|left|200px]] | ||
'''A second binding site for hydroxytamoxifen within the coactivator-binding groove of estrogen receptor beta''' | {{Structure | ||
|PDB= 2fsz |SIZE=350|CAPTION= <scene name='initialview01'>2fsz</scene>, resolution 2.200Å | |||
|SITE= | |||
|LIGAND= <scene name='pdbligand=OHT:4-HYDROXYTAMOXIFEN'>OHT</scene> | |||
|ACTIVITY= | |||
|GENE= ESR2, ESTRB, NR3A2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |||
}} | |||
'''A second binding site for hydroxytamoxifen within the coactivator-binding groove of estrogen receptor beta''' | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
2FSZ is a [ | 2FSZ is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2FSZ OCA]. | ||
==Reference== | ==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:[http:// | 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:[http://www.ncbi.nlm.nih.gov/pubmed/16782818 16782818] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
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[[Category: nuclear hormone binding domain]] | [[Category: nuclear hormone binding domain]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 16:56:26 2008'' | ||
Revision as of 14:56, 20 March 2008
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| 2fsz, resolution 2.200Å | |||||||||||||
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| Ligands: | OHT | ||||||||||||
| Gene: | ESR2, ESTRB, NR3A2 (Homo sapiens) | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
A second binding site for hydroxytamoxifen within the coactivator-binding groove of estrogen receptor beta
Overview
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.
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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