3g8o

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[[Image:3g8o.png|left|200px]]
 
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{{STRUCTURE_3g8o| PDB=3g8o | SCENE= }}
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==Progesterone Receptor with bound Pyrrolidine 1==
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<StructureSection load='3g8o' size='340' side='right'caption='[[3g8o]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3g8o]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. This structure supersedes the now removed PDB entry [http://oca.weizmann.ac.il/oca-bin/send-pdb?obs=1&id=3g8n 3g8n]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3G8O OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3G8O 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]] 1.9&#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=30X:N~2~-[4-CYANO-3-(TRIFLUOROMETHYL)PHENYL]-N,N-DIMETHYL-N~2~-(2,2,2-TRIFLUOROETHYL)-L-ALANINAMIDE'>30X</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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=3g8o FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3g8o OCA], [https://pdbe.org/3g8o PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3g8o RCSB], [https://www.ebi.ac.uk/pdbsum/3g8o PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3g8o ProSAT]</span></td></tr>
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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>
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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/g8/3g8o_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=3g8o ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Using the X-ray crystal structure of an amide-based progesterone receptor (PR) partial agonist bound to the PR ligand binding domain, a novel PR partial agonist class containing a pyrrolidine ring was designed. Members of this class of N-alkylpyrrolidines demonstrate potent and highly selective partial agonism of the progesterone receptor, and one of these analogs was shown to be efficacious upon oral dosing in the OVX rat model of estrogen opposition.
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===Progesterone Receptor with bound Pyrrolidine 1===
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Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists.,Thompson SK, Washburn DG, Frazee JS, Madauss KP, Hoang TH, Lapinski L, Grygielko ET, Glace LE, Trizna W, Williams SP, Duraiswami C, Bray JD, Laping NJ Bioorg Med Chem Lett. 2009 Aug 15;19(16):4777-80. Epub 2009 Jun 17. PMID:19595590<ref>PMID:19595590</ref>
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{{ABSTRACT_PUBMED_19595590}}
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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==About this Structure==
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<div class="pdbe-citations 3g8o" style="background-color:#fffaf0;"></div>
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[[3g8o]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. This structure supersedes the now removed PDB entry [http://oca.weizmann.ac.il/oca-bin/send-pdb?obs=1&id=3g8n 3g8n]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3G8O OCA].
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==See Also==
==See Also==
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*[[Hormone|Hormone]]
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*[[Progesterone receptor|Progesterone receptor]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:019595590</ref><references group="xtra"/>
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__TOC__
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Madauss, K P.]]
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[[Category: Large Structures]]
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[[Category: Stewart, E L.]]
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[[Category: Madauss KP]]
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[[Category: Thompson, S K.]]
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[[Category: Stewart EL]]
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[[Category: Washburn, D G.]]
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[[Category: Thompson SK]]
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[[Category: Williams, S P.]]
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[[Category: Washburn DG]]
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[[Category: Alpha helical sandwich]]
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[[Category: Williams SP]]
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[[Category: Dna-binding]]
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[[Category: Lipid-binding]]
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[[Category: Metal-binding]]
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[[Category: Nuclear receptor]]
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[[Category: Nucleus]]
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[[Category: Phosphoprotein]]
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[[Category: Pr]]
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[[Category: Progesterone]]
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[[Category: Progesterone receptor]]
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[[Category: Receptor]]
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[[Category: Steroid hormone receptor]]
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[[Category: Steroid-binding]]
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[[Category: Transcription]]
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[[Category: Transcription regulation]]
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[[Category: Zinc-finger]]
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Current revision

Progesterone Receptor with bound Pyrrolidine 1

PDB ID 3g8o

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Proteopedia Page Contributors and Editors (what is this?)

OCA

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