1kv6

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[[Image:1kv6.gif|left|200px]]
 
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{{Structure
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==X-ray structure of the orphan nuclear receptor ERR3 ligand-binding domain in the constitutively active conformation==
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|PDB= 1kv6 |SIZE=350|CAPTION= <scene name='initialview01'>1kv6</scene>, resolution 2.70&Aring;
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<StructureSection load='1kv6' size='340' side='right'caption='[[1kv6]], [[Resolution|resolution]] 2.70&Aring;' scene=''>
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|SITE=
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== Structural highlights ==
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|LIGAND=
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<table><tr><td colspan='2'>[[1kv6]] is a 4 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=1KV6 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1KV6 FirstGlance]. <br>
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|ACTIVITY=
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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]] 2.7&#8491;</td></tr>
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|GENE= NR3B3 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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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=1kv6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1kv6 OCA], [https://pdbe.org/1kv6 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1kv6 RCSB], [https://www.ebi.ac.uk/pdbsum/1kv6 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1kv6 ProSAT]</span></td></tr>
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}}
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/ERR3_HUMAN ERR3_HUMAN] Orphan receptor that acts as transcription activator in the absence of bound ligand. Binds specifically to an estrogen response element and activates reporter genes controlled by estrogen response elements (By similarity).<ref>PMID:19067653</ref> <ref>PMID:18063693</ref> <ref>PMID:11864604</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/kv/1kv6_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=1kv6 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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The crystal structure of the ligand binding domain (LBD) of the estrogen-related receptor 3 (ERR3) complexed with a steroid receptor coactivator-1 (SRC-1) peptide reveals a transcriptionally active conformation in absence of any ligand. The structure explains why estradiol does not bind ERRs with significant affinity. Docking of the previously reported ERR antagonists, diethylstilbestrol and 4-hydroxytamoxifen, requires structural rearrangements enlarging the ligand binding pocket that can only be accommodated with an antagonist LBD conformation. Mutant receptors in which the ligand binding cavity is filled up by bulkier side chains still interact with SRC-1 in vitro and are transcriptionally active in vivo, but are no longer efficiently inactivated by diethylstilbestrol or 4-hydroxytamoxifen. These results provide structural and functional evidence for ligand-independent transcriptional activation by ERR3.
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'''X-ray structure of the orphan nuclear receptor ERR3 ligand-binding domain in the constitutively active conformation'''
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Structural and functional evidence for ligand-independent transcriptional activation by the estrogen-related receptor 3.,Greschik H, Wurtz JM, Sanglier S, Bourguet W, van Dorsselaer A, Moras D, Renaud JP Mol Cell. 2002 Feb;9(2):303-13. PMID:11864604<ref>PMID:11864604</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 1kv6" style="background-color:#fffaf0;"></div>
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==Overview==
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==See Also==
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The crystal structure of the ligand binding domain (LBD) of the estrogen-related receptor 3 (ERR3) complexed with a steroid receptor coactivator-1 (SRC-1) peptide reveals a transcriptionally active conformation in absence of any ligand. The structure explains why estradiol does not bind ERRs with significant affinity. Docking of the previously reported ERR antagonists, diethylstilbestrol and 4-hydroxytamoxifen, requires structural rearrangements enlarging the ligand binding pocket that can only be accommodated with an antagonist LBD conformation. Mutant receptors in which the ligand binding cavity is filled up by bulkier side chains still interact with SRC-1 in vitro and are transcriptionally active in vivo, but are no longer efficiently inactivated by diethylstilbestrol or 4-hydroxytamoxifen. These results provide structural and functional evidence for ligand-independent transcriptional activation by ERR3.
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*[[Estrogen-related receptor 3D structures|Estrogen-related receptor 3D structures]]
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== References ==
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==About this Structure==
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<references/>
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1KV6 is a [[Protein complex]] structure of 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=1KV6 OCA].
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__TOC__
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</StructureSection>
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==Reference==
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Structural and functional evidence for ligand-independent transcriptional activation by the estrogen-related receptor 3., Greschik H, Wurtz JM, Sanglier S, Bourguet W, van Dorsselaer A, Moras D, Renaud JP, Mol Cell. 2002 Feb;9(2):303-13. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/11864604 11864604]
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Protein complex]]
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[[Category: Large Structures]]
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[[Category: Bourguet, W.]]
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[[Category: Bourguet W]]
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[[Category: Dorsselaer, A van.]]
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[[Category: Greschik H]]
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[[Category: Greschik, H.]]
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[[Category: Moras D]]
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[[Category: Moras, D.]]
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[[Category: Renaud J-P]]
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[[Category: Renaud, J P.]]
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[[Category: Sanglier S]]
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[[Category: SPINE, Structural Proteomics in Europe.]]
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[[Category: Wurtz J-M]]
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[[Category: Sanglier, S.]]
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[[Category: Van Dorsselaer A]]
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[[Category: Wurtz, J M.]]
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[[Category: spine]]
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[[Category: structural genomic]]
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[[Category: structural proteomics in europe]]
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[[Category: transcriptionally active conformation in absence of ligand]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 12:22:31 2008''
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Current revision

X-ray structure of the orphan nuclear receptor ERR3 ligand-binding domain in the constitutively active conformation

PDB ID 1kv6

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OCA

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