1n4h

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(New page: 200px<br /> <applet load="1n4h" size="450" color="white" frame="true" align="right" spinBox="true" caption="1n4h, resolution 2.1&Aring;" /> '''Characterization of ...)
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[[Image:1n4h.gif|left|200px]]<br />
 
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<applet load="1n4h" size="450" color="white" frame="true" align="right" spinBox="true"
 
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caption="1n4h, resolution 2.1&Aring;" />
 
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'''Characterization of ligands for the orphan nuclear receptor RORbeta'''<br />
 
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==Overview==
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==Characterization of ligands for the orphan nuclear receptor RORbeta==
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Retinoids regulate gene expression through binding to the nuclear retinoic, acid receptors (RARs) and retinoid X receptors (RXRs). In contrast, no, ligands for the retinoic acid receptor-related orphan receptors beta and, gamma (ROR beta and gamma) have been identified, yet structural data and, structure-function analyses indicate that ROR beta is a ligand-regulated, nuclear receptor. Using nondenaturing mass spectrometry and scintillation, proximity assays we found that all-trans retinoic acid (ATRA) and several, retinoids bind to the ROR beta ligand-binding domain (LBD). The crystal, structures of the complex with ATRA and with the synthetic analog ALRT, 1550 reveal the binding modes of these ligands. ATRA and related retinoids, inhibit ROR beta but not ROR alpha transcriptional activity suggesting, that high-affinity, subtype-specific ligands could be designed for the, identification of ROR beta target genes. Our results identify ROR beta as, a retinoid-regulated nuclear receptor, providing a novel pathway for, retinoid action.
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<StructureSection load='1n4h' size='340' side='right'caption='[[1n4h]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
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== Structural highlights ==
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==About this Structure==
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<table><tr><td colspan='2'>[[1n4h]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1N4H OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1N4H FirstGlance]. <br>
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1N4H is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] with REA as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1N4H OCA].
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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]] 2.1&#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=REA:RETINOIC+ACID'>REA</scene></td></tr>
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==Reference==
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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=1n4h FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1n4h OCA], [https://pdbe.org/1n4h PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1n4h RCSB], [https://www.ebi.ac.uk/pdbsum/1n4h PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1n4h ProSAT]</span></td></tr>
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All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta., Stehlin-Gaon C, Willmann D, Zeyer D, Sanglier S, Van Dorsselaer A, Renaud JP, Moras D, Schule R, Nat Struct Biol. 2003 Oct;10(10):820-5. Epub 2003 Sep 7. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=12958591 12958591]
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</table>
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[[Category: Protein complex]]
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== Function ==
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[https://www.uniprot.org/uniprot/RORB_RAT RORB_RAT] Orphan nuclear receptor required for normal postnatal development of rod and cone photoreceptor cells. Regulates transcription of OPN1SW in cone photoreceptor cells by binding the sequence 5'-AGGTCA-3' in the OPN1SW promoter.
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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/n4/1n4h_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=1n4h ConSurf].
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<div style="clear:both"></div>
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__TOC__
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</StructureSection>
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[[Category: Homo sapiens]]
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[[Category: Large Structures]]
[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
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[[Category: Dorsselaer, A.Van.]]
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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: Sanglier, S.]]
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[[Category: Schuele R]]
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[[Category: Schuele, R.]]
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[[Category: Stehlin-Gaon C]]
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[[Category: Stehlin-Gaon, C.]]
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[[Category: Van Dorsselaer A]]
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[[Category: Willmann, D.]]
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[[Category: Willmann D]]
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[[Category: REA]]
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[[Category: alpha-helical sandwich]]
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[[Category: protein-peptide-ligand complex]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 18:17:38 2007''
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Current revision

Characterization of ligands for the orphan nuclear receptor RORbeta

PDB ID 1n4h

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