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[[Image:2fsz.gif|left|200px]]


{{Structure
==A second binding site for hydroxytamoxifen within the coactivator-binding groove of estrogen receptor beta==
|PDB= 2fsz |SIZE=350|CAPTION= <scene name='initialview01'>2fsz</scene>, resolution 2.200&Aring;
<StructureSection load='2fsz' size='340' side='right'caption='[[2fsz]], [[Resolution|resolution]] 2.20&Aring;' scene=''>
|SITE=  
== Structural highlights ==
|LIGAND= <scene name='pdbligand=OHT:4-HYDROXYTAMOXIFEN'>OHT</scene>
<table><tr><td colspan='2'>[[2fsz]] is a 2 chain structure with sequence from [https://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]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2FSZ FirstGlance]. <br>
|ACTIVITY=  
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.2&#8491;</td></tr>
|GENE= ESR2, ESTRB, NR3A2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=OHT:4-HYDROXYTAMOXIFEN'>OHT</scene></td></tr>
|DOMAIN=
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2fsz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2fsz OCA], [https://pdbe.org/2fsz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2fsz RCSB], [https://www.ebi.ac.uk/pdbsum/2fsz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2fsz ProSAT]</span></td></tr>
|RELATEDENTRY=
</table>
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2fsz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2fsz OCA], [http://www.ebi.ac.uk/pdbsum/2fsz PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2fsz RCSB]</span>
== Function ==
}}
[https://www.uniprot.org/uniprot/ESR2_HUMAN ESR2_HUMAN] Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform beta-cx lacks ligand binding ability and has no or only very low ere binding activity resulting in the loss of ligand-dependent transactivation ability. DNA-binding by ESR1 and ESR2 is rapidly lost at 37 degrees Celsius in the absence of ligand while in the presence of 17 beta-estradiol and 4-hydroxy-tamoxifen loss in DNA-binding at elevated temperature is more gradual.
== Evolutionary Conservation ==
[[Image:Consurf_key_small.gif|200px|right]]
Check<jmol>
  <jmolCheckbox>
    <scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/fs/2fsz_consurf.spt"</scriptWhenChecked>
    <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
    <text>to colour the structure by Evolutionary Conservation</text>
  </jmolCheckbox>
</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=2fsz ConSurf].
<div style="clear:both"></div>


'''A second binding site for hydroxytamoxifen within the coactivator-binding groove of estrogen receptor beta'''
==See Also==
 
*[[Estrogen receptor 3D structures|Estrogen receptor 3D structures]]
 
__TOC__
==Overview==
</StructureSection>
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 [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==
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: Large Structures]]
[[Category: Wang, Yong]]
[[Category: Wang Y]]
[[Category: nuclear hormone binding domain]]
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 03:07:21 2008''

Latest revision as of 09:25, 14 February 2024

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

2fsz, resolution 2.20Å

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