1zaf: Difference between revisions

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[[Image:1zaf.gif|left|200px]]


{{Structure
==Crystal structure of estrogen receptor beta complexed with 3-Bromo-6-hydroxy-2-(4-hydroxy-phenyl)-inden-1-one==
|PDB= 1zaf |SIZE=350|CAPTION= <scene name='initialview01'>1zaf</scene>, resolution 2.20&Aring;
<StructureSection load='1zaf' size='340' side='right'caption='[[1zaf]], [[Resolution|resolution]] 2.20&Aring;' scene=''>
|SITE=  
== Structural highlights ==
|LIGAND= <scene name='pdbligand=789:3-BROMO-6-HYDROXY-2-(4-HYDROXYPHENYL)-1H-INDEN-1-ONE'>789</scene>
<table><tr><td colspan='2'>[[1zaf]] is a 4 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=1ZAF OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1ZAF FirstGlance]. <br>
|ACTIVITY= [http://en.wikipedia.org/wiki/Histone_acetyltransferase Histone acetyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.48 2.3.1.48]  
</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=789:3-BROMO-6-HYDROXY-2-(4-HYDROXYPHENYL)-1H-INDEN-1-ONE'>789</scene></td></tr>
}}
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1zaf FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1zaf OCA], [https://pdbe.org/1zaf PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1zaf RCSB], [https://www.ebi.ac.uk/pdbsum/1zaf PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1zaf ProSAT]</span></td></tr>
</table>
== 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/za/1zaf_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=1zaf ConSurf].
<div style="clear:both"></div>


'''Crystal structure of estrogen receptor beta complexed with 3-Bromo-6-hydroxy-2-(4-hydroxy-phenyl)-inden-1-one'''
==See Also==
 
*[[Estrogen receptor 3D structures|Estrogen receptor 3D structures]]
 
__TOC__
==Overview==
</StructureSection>
The syntheses of a series of 2-arylindene-1-ones as potent ligands of ERbeta and ERalpha are described. Several compounds exhibited high potency and moderate selectivity for the ERbeta receptor. X-ray and modeling studies were used to understand ligand binding orientation and observed affinity.
 
==About this Structure==
1ZAF is a [[Protein complex]] structure of sequences 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=1ZAF OCA].
 
==Reference==
Estrogen receptor ligands: design and synthesis of new 2-arylindene-1-ones., McDevitt RE, Malamas MS, Manas ES, Unwalla RJ, Xu ZB, Miller CP, Harris HA, Bioorg Med Chem Lett. 2005 Jun 15;15(12):3137-42. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15876535 15876535]
[[Category: Histone acetyltransferase]]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Protein complex]]
[[Category: Large Structures]]
[[Category: Harris, H A.]]
[[Category: Harris HA]]
[[Category: Malamas, M S.]]
[[Category: Malamas MS]]
[[Category: Manas, E S.]]
[[Category: Manas ES]]
[[Category: McDevitt, R E.]]
[[Category: McDevitt RE]]
[[Category: Miller, C P.]]
[[Category: Miller CP]]
[[Category: Unwalla, R J.]]
[[Category: Unwalla RJ]]
[[Category: Xu, Z B.]]
[[Category: Xu ZB]]
[[Category: 789]]
[[Category: agonist]]
[[Category: er]]
[[Category: er-beta]]
[[Category: estrogen]]
[[Category: estrogen receptor]]
[[Category: estrogen receptor beta]]
[[Category: nuclear receptor]]
[[Category: transcription factor]]
 
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