3g8o

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{{Seed}}
 
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[[Image:3g8o.jpg|left|200px]]
 
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==Progesterone Receptor with bound Pyrrolidine 1==
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The line below this paragraph, containing "STRUCTURE_3g8o", creates the "Structure Box" on the page.
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<StructureSection load='3g8o' size='340' side='right'caption='[[3g8o]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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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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or leave the SCENE parameter empty for the default display.
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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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{{STRUCTURE_3g8o| PDB=3g8o | SCENE= }}
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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 22===
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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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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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<div class="pdbe-citations 3g8o" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_19595590}}, adds the Publication Abstract to the page
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*[[Progesterone receptor|Progesterone receptor]]
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(as it appears on PubMed at http://www.pubmed.gov), where 19595590 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_19595590}}
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__TOC__
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</StructureSection>
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==About this Structure==
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3G8O is a 2 chains structure with 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=3G8O OCA].
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==Reference==
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<ref group="xtra">PMID:19595590</ref><references group="xtra"/>
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[[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: Alternative splicing]]
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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: Polymorphism]]
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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]]
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[[Category: Zinc-finger]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Feb 17 10:35:12 2010''
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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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