1xap

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{{Seed}}
 
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[[Image:1xap.png|left|200px]]
 
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==Structure of the ligand binding domain of the Retinoic Acid Receptor beta==
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The line below this paragraph, containing "STRUCTURE_1xap", creates the "Structure Box" on the page.
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<StructureSection load='1xap' size='340' side='right'caption='[[1xap]], [[Resolution|resolution]] 2.10&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'>[[1xap]] is a 1 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=1XAP OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1XAP 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]] 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=TTB:4-[(1E)-2-(5,5,8,8-TETRAMETHYL-5,6,7,8-TETRAHYDRONAPHTHALEN-2-YL)PROP-1-ENYL]BENZOIC+ACID'>TTB</scene></td></tr>
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{{STRUCTURE_1xap| PDB=1xap | 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=1xap FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1xap OCA], [https://pdbe.org/1xap PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1xap RCSB], [https://www.ebi.ac.uk/pdbsum/1xap PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1xap ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/RARB_HUMAN RARB_HUMAN] Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RXR/RAR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. In the absence or presence of hormone ligand, acts mainly as an activator of gene expression due to weak binding to corepressors. In concert with RARG, required for skeletal growth, matrix homeostasis and growth plate function.<ref>PMID:12554770</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/xa/1xap_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=1xap 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 of RARbeta, a suspect tumour suppressor, reveals important features that distinguish it from the two other RAR isotypes. The most striking difference is an extra cavity allowing RARbeta to bind more bulky agonists. Accordingly, we identified a ligand that shows RARbeta selectivity with a 100-fold higher affinity to RARbeta than to alpha or gamma isotypes. The structural differences between the three RAR ligand-binding pockets revealed a rationale explaining how a single retinoid can be at the same time an RARalpha, gamma antagonist and an RARbeta agonist. In addition, we demonstrate how to generate an RARbeta antagonist by gradually modifying the bulkiness of a single substitution. Together, our results provide structural guidelines for the synthesis of RARbeta-selective agonists and antagonists, allowing for the first time to address pharmacologically the tumour suppressor role of RARbeta in vitro and in animal models.
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===Structure of the ligand binding domain of the Retinoic Acid Receptor beta===
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Rational design of RAR-selective ligands revealed by RARbeta crystal stucture.,Germain P, Kammerer S, Perez E, Peluso-Iltis C, Tortolani D, Zusi FC, Starrett J, Lapointe P, Daris JP, Marinier A, de Lera AR, Rochel N, Gronemeyer H EMBO Rep. 2004 Sep;5(9):877-82. PMID:15319780<ref>PMID:15319780</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 1xap" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_15319780}}, adds the Publication Abstract to the page
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*[[Retinoic acid receptor 3D structures|Retinoic acid receptor 3D structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 15319780 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_15319780}}
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__TOC__
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</StructureSection>
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==About this Structure==
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1XAP is a [[Single protein]] structure of 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=1XAP OCA].
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==Reference==
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Rational design of RAR-selective ligands revealed by RARbeta crystal stucture., Germain P, Kammerer S, Perez E, Peluso-Iltis C, Tortolani D, Zusi FC, Starrett J, Lapointe P, Daris JP, Marinier A, de Lera AR, Rochel N, Gronemeyer H, EMBO Rep. 2004 Sep;5(9):877-82. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15319780 15319780]
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Single protein]]
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[[Category: Large Structures]]
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[[Category: Daris, J P.]]
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[[Category: Daris JP]]
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[[Category: Germain, P.]]
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[[Category: De Lera AR]]
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[[Category: Gronemeyer, H.]]
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[[Category: Germain P]]
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[[Category: Kammerer, S.]]
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[[Category: Gronemeyer H]]
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[[Category: Lapointe, P.]]
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[[Category: Kammerer S]]
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[[Category: Lera, A R.De.]]
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[[Category: Lapointe P]]
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[[Category: Marinier, A.]]
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[[Category: Marinier A]]
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[[Category: Peluso-Iltis, C.]]
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[[Category: Peluso-Iltis C]]
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[[Category: Rochel, N.]]
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[[Category: Rochel N]]
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[[Category: Starrett, J.]]
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[[Category: Starrett J]]
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[[Category: Tortolani, D.]]
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[[Category: Tortolani D]]
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[[Category: Zusi, F C.]]
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[[Category: Zusi FC]]
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[[Category: Ligand binding domain]]
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[[Category: Nuclear receptor]]
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[[Category: Retinoic acid receptor beta]]
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[[Category: Ttnpb]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 23:20:45 2008''
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Current revision

Structure of the ligand binding domain of the Retinoic Acid Receptor beta

PDB ID 1xap

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