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2w8y

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==RU486 BOUND TO THE PROGESTERONE RECEPTOR IN A DESTABILIZED AGONISTIC CONFORMATION==
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<StructureSection load='2w8y' size='340' side='right' caption='[[2w8y]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
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==RU486 bound to the progesterone receptor in a destabilized agonistic conformation==
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<StructureSection load='2w8y' size='340' side='right'caption='[[2w8y]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[2w8y]] is a 2 chain structure with 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=2W8Y OCA]. <br>
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<table><tr><td colspan='2'>[[2w8y]] 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=2W8Y OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2W8Y FirstGlance]. <br>
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</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=486:11-(4-DIMETHYLAMINO-PHENYL)-17-HYDROXY-13-METHYL-17-PROP-1-YNYL-1,2,6,7,8,11,12,13,14,15,16,17-DODEC+AHYDRO-CYCLOPENTA[A]PHENANTHREN-3-ONE'>486</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=NDR:(14BETA,17ALPHA)-17-ETHYNYL-17-HYDROXYESTR-4-EN-3-ONE'>NDR</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene><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]] 1.8&#8491;</td></tr>
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<tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2c7a|2c7a]], [[1a28|1a28]], [[1zuc|1zuc]], [[1sqn|1sqn]], [[1sr7|1sr7]], [[1e3k|1e3k]]</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=486:11-(4-DIMETHYLAMINO-PHENYL)-17-HYDROXY-13-METHYL-17-PROP-1-YNYL-1,2,6,7,8,11,12,13,14,15,16,17-DODEC+AHYDRO-CYCLOPENTA[A]PHENANTHREN-3-ONE'>486</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=NDR:(14BETA,17ALPHA)-17-ETHYNYL-17-HYDROXYESTR-4-EN-3-ONE'>NDR</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Glucokinase Glucokinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.2 2.7.1.2] </span></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=2w8y FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2w8y OCA], [https://pdbe.org/2w8y PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2w8y RCSB], [https://www.ebi.ac.uk/pdbsum/2w8y PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2w8y ProSAT]</span></td></tr>
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<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2w8y FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2w8y OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2w8y RCSB], [http://www.ebi.ac.uk/pdbsum/2w8y PDBsum]</span></td></tr>
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</table>
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<table>
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== Function ==
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[https://www.uniprot.org/uniprot/PRGR_HUMAN PRGR_HUMAN] The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Progesterone receptor isoform B (PRB) is involved activation of c-SRC/MAPK signaling on hormone stimulation.<ref>PMID:15572662</ref> <ref>PMID:15798179</ref> <ref>PMID:17020914</ref> <ref>PMID:17347654</ref> <ref>PMID:17717077</ref> <ref>PMID:17173941</ref> <ref>PMID:18202149</ref> Isoform A is inactive in stimulating c-Src/MAPK signaling on hormone stimulation.<ref>PMID:15572662</ref> <ref>PMID:15798179</ref> <ref>PMID:17020914</ref> <ref>PMID:17347654</ref> <ref>PMID:17717077</ref> <ref>PMID:17173941</ref> <ref>PMID:18202149</ref>
== Evolutionary Conservation ==
== Evolutionary Conservation ==
[[Image:Consurf_key_small.gif|200px|right]]
[[Image:Consurf_key_small.gif|200px|right]]
Check<jmol>
Check<jmol>
<jmolCheckbox>
<jmolCheckbox>
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<scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/w8/2w8y_consurf.spt"</scriptWhenChecked>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/w8/2w8y_consurf.spt"</scriptWhenChecked>
<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
<text>to colour the structure by Evolutionary Conservation</text>
<text>to colour the structure by Evolutionary Conservation</text>
</jmolCheckbox>
</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/chain_selection.php?pdb_ID=2ata ConSurf].
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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=2w8y ConSurf].
<div style="clear:both"></div>
<div style="clear:both"></div>
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
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The X-ray structure of RU486 bound to the progesterone receptor in a destabilized agonistic conformation.,Raaijmakers HC, Versteegh JE, Uitdehaag JC J Biol Chem. 2009 Jul 17;284(29):19572-9. Epub 2009 Apr 16. PMID:19372222<ref>PMID:19372222</ref>
The X-ray structure of RU486 bound to the progesterone receptor in a destabilized agonistic conformation.,Raaijmakers HC, Versteegh JE, Uitdehaag JC J Biol Chem. 2009 Jul 17;284(29):19572-9. Epub 2009 Apr 16. PMID:19372222<ref>PMID:19372222</ref>
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
</div>
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<div class="pdbe-citations 2w8y" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[Progesterone receptor|Progesterone receptor]]
== References ==
== References ==
<references/>
<references/>
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</StructureSection>
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Raaijmakers, H C.A.]]
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[[Category: Large Structures]]
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[[Category: Uitdehaag, J C.M.]]
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[[Category: Raaijmakers HCA]]
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[[Category: Versteeg, J.]]
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[[Category: Uitdehaag JCM]]
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[[Category: Mifepristone]]
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[[Category: Versteeg J]]
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[[Category: Progesterone receptor]]
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[[Category: Receptor]]
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[[Category: Ru-486]]
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Current revision

RU486 bound to the progesterone receptor in a destabilized agonistic conformation

PDB ID 2w8y

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