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[[Image:2nv7.jpg|left|200px]]


{{Structure
==Crystal Structure of Estrogen Receptor Beta Complexed with WAY-555==
|PDB= 2nv7 |SIZE=350|CAPTION= <scene name='initialview01'>2nv7</scene>, resolution 2.10&Aring;
<StructureSection load='2nv7' size='340' side='right'caption='[[2nv7]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
|SITE=  
== Structural highlights ==
|LIGAND= <scene name='pdbligand=555:4-(4-HYDROXYPHENYL)-1-NAPHTHALDEHYDE+OXIME'>555</scene>
<table><tr><td colspan='2'>[[2nv7]] 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=2NV7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2NV7 FirstGlance]. <br>
|ACTIVITY= <span class='plainlinks'>[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] </span>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.1&#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=555:4-(4-HYDROXYPHENYL)-1-NAPHTHALDEHYDE+OXIME'>555</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=2nv7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2nv7 OCA], [https://pdbe.org/2nv7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2nv7 RCSB], [https://www.ebi.ac.uk/pdbsum/2nv7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2nv7 ProSAT]</span></td></tr>
|RELATEDENTRY=
</table>
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2nv7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2nv7 OCA], [http://www.ebi.ac.uk/pdbsum/2nv7 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2nv7 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/nv/2nv7_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=2nv7 ConSurf].
<div style="clear:both"></div>


'''Crystal Structure of Estrogen Receptor Beta Complexed with WAY-555'''
==See Also==
 
*[[Estrogen receptor 3D structures|Estrogen receptor 3D structures]]
 
__TOC__
==Overview==
</StructureSection>
A series of 4'-hydroxyphenyl-aryl-carbaldehyde oximes (5b) was prepared and found to have high affinity (4nM) and modest selectivity (39-fold) for estrogen receptor-beta (ERbeta). Substitution of one of the core rings of the scaffold based around these novel ligands further expanded our knowledge in the quest toward achieving high affinity and selectivity for ERbeta. An X-ray co-crystal of structure 11 revealed that the oxime moiety was mimicking the C-ring of genistein, as previously predicted by SAR and docking studies.
 
==About this Structure==
2NV7 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=2NV7 OCA].
 
==Reference==
ERbeta ligands. Part 5: synthesis and structure-activity relationships of a series of 4'-hydroxyphenyl-aryl-carbaldehyde oxime derivatives., Mewshaw RE, Bowen SM, Harris HA, Xu ZB, Manas ES, Cohn ST, Bioorg Med Chem Lett. 2007 Feb 15;17(4):902-6. Epub 2006 Dec 1. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/17188490 17188490]
[[Category: Histone acetyltransferase]]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Protein complex]]
[[Category: Large Structures]]
[[Category: Bowen, M S.]]
[[Category: Bowen MS]]
[[Category: Cohn, S T.]]
[[Category: Cohn ST]]
[[Category: Harris, H A.]]
[[Category: Harris HA]]
[[Category: Manas, E S.]]
[[Category: Manas ES]]
[[Category: Mewshaw, R E.]]
[[Category: Mewshaw RE]]
[[Category: RSGI, RIKEN Structural Genomics/Proteomics Initiative.]]
[[Category: Xu ZB]]
[[Category: Xu, Z B.]]
[[Category: agonist]]
[[Category: er]]
[[Category: er-beta]]
[[Category: estrogen]]
[[Category: estrogen receptor]]
[[Category: estrogen receptor beta]]
[[Category: national project on protein structural and functional analyse]]
[[Category: nppsfa]]
[[Category: nuclear receptor]]
[[Category: riken structural genomics/proteomics initiative]]
[[Category: rsgi]]
[[Category: structural genomic]]
[[Category: transcription factor]]
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:08:51 2008''

Latest revision as of 09:28, 3 April 2024

Crystal Structure of Estrogen Receptor Beta Complexed with WAY-555Crystal Structure of Estrogen Receptor Beta Complexed with WAY-555

Structural highlights

2nv7 is a 4 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 2.1Å
Ligands:
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

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

Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.

See Also

2nv7, resolution 2.10Å

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