3hq5

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[[Image:3hq5.png|left|200px]]
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==Progesterone Receptor bound to an Alkylpyrrolidine ligand.==
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<StructureSection load='3hq5' size='340' side='right' caption='[[3hq5]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3hq5]] 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=3HQ5 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3HQ5 FirstGlance]. <br>
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</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GKK:2-CHLORO-4-{[(3S)-1-METHYLPYRROLIDIN-3-YL][2-(TRIFLUOROMETHYL)BENZYL]AMINO}BENZONITRILE'>GKK</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene><br>
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<tr><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">PGR, NR3C3 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</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=3hq5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3hq5 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3hq5 RCSB], [http://www.ebi.ac.uk/pdbsum/3hq5 PDBsum]</span></td></tr>
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<table>
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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/hq/3hq5_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/chain_selection.php?pdb_ID=2ata 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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{{STRUCTURE_3hq5| PDB=3hq5 | SCENE= }}
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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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===Progesterone Receptor bound to an Alkylpyrrolidine ligand.===
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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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{{ABSTRACT_PUBMED_19595590}}
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==About this Structure==
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[[3hq5]] 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=3HQ5 OCA].
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==See Also==
==See Also==
*[[Hormone|Hormone]]
*[[Hormone|Hormone]]
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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]]
[[Category: Madauss, K P.]]
[[Category: Madauss, K P.]]

Revision as of 12:50, 29 September 2014

Progesterone Receptor bound to an Alkylpyrrolidine ligand.

3hq5, resolution 2.10Å

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