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2z4b

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(New page: 200px<br /> <applet load="2z4b" size="450" color="white" frame="true" align="right" spinBox="true" caption="2z4b, resolution 2.34&Aring;" /> '''Estrogen receptor b...)
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[[Image:2z4b.gif|left|200px]]<br />
 
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<applet load="2z4b" size="450" color="white" frame="true" align="right" spinBox="true"
 
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caption="2z4b, resolution 2.34&Aring;" />
 
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'''Estrogen receptor beta ligand-binding domain complexed to a benzopyran ligand'''<br />
 
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==Overview==
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==Estrogen receptor beta ligand-binding domain complexed to a benzopyran ligand==
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Benzopyrans are selective estrogen receptor (ER) beta agonists (SERBAs), which bind the ER subtypes alpha and beta in opposite orientations. Here, we describe the syntheses of cyclopentanone and cyclohexanone, intermediates for SAR studies of the C-ring on the benzopyran scaffold., Modification of the C-ring disrupts binding to ERalpha, thus improving, ERbeta selectivity up to 100-fold. X-ray cocrystal structures confirm, previously observed binding modes.
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<StructureSection load='2z4b' size='340' side='right'caption='[[2z4b]], [[Resolution|resolution]] 2.34&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[2z4b]] 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=2Z4B OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2Z4B FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.34&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=DC8:(3AS,4R,9BR)-2,2-DIFLUORO-4-(4-HYDROXYPHENYL)-1,2,3,3A,4,9B-HEXAHYDROCYCLOPENTA[C]CHROMEN-8-OL'>DC8</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2z4b FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2z4b OCA], [https://pdbe.org/2z4b PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2z4b RCSB], [https://www.ebi.ac.uk/pdbsum/2z4b PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2z4b ProSAT]</span></td></tr>
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</table>
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== Function ==
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[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.
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/z4/2z4b_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</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=2z4b ConSurf].
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<div style="clear:both"></div>
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==About this Structure==
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==See Also==
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2Z4B is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with DC8 as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2Z4B OCA].
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*[[Estrogen receptor 3D structures|Estrogen receptor 3D structures]]
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__TOC__
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==Reference==
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</StructureSection>
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Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: Synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification., Richardson TI, Dodge JA, Durst GL, Pfeifer LA, Shah J, Wang Y, Durbin JD, Krishnan V, Norman BH, Bioorg Med Chem Lett. 2007 Sep 1;17(17):4824-8. Epub 2007 Jun 20. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17614275 17614275]
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Single protein]]
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[[Category: Large Structures]]
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[[Category: Wang, Y.]]
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[[Category: Wang Y]]
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[[Category: DC8]]
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[[Category: nuclear receptor ligand binding domain]]
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[[Category: transcription]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 23:46:45 2007''
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Current revision

Estrogen receptor beta ligand-binding domain complexed to a benzopyran ligand

PDB ID 2z4b

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