4akn

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[[Image:4akn.png|left|200px]]
 
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{{STRUCTURE_4akn| PDB=4akn | SCENE= }}
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==N-Terminal Bromodomain of Human BRD2 With tbutyl-phenyl-amino- dimethyl-oxazolyl-quinoline-carboxylic acid==
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<StructureSection load='4akn' size='340' side='right'caption='[[4akn]], [[Resolution|resolution]] 1.82&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4akn]] is a 3 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=4AKN OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4AKN FirstGlance]. <br>
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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]] 1.82&#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=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=S5B:4-[(2-TERT-BUTYLPHENYL)AMINO]-7-(3,5-DIMETHYL-1,2-OXAZOL-4-YL)QUINOLINE-3-CARBOXYLIC+ACID'>S5B</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
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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=4akn FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4akn OCA], [https://pdbe.org/4akn PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4akn RCSB], [https://www.ebi.ac.uk/pdbsum/4akn PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4akn ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/BRD2_HUMAN BRD2_HUMAN] May play a role in spermatogenesis or folliculogenesis (By similarity). Binds hyperacetylated chromatin and plays a role in the regulation of transcription, probably by chromatin remodeling. Regulates transcription of the CCND1 gene. Plays a role in nucleosome assembly.<ref>PMID:18406326</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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A novel series of quinoline isoxazole BET family bromodomain inhibitors are discussed. Crystallography is used to illustrate binding modes and rationalize their SAR. One member, I-BET151 (GSK1210151A), shows good oral bioavailability in both the rat and minipig as well as demonstrating efficient suppression of bacterial induced inflammation and sepsis in a murine in vivo endotoxaemia model.
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===N-Terminal Bromodomain of Human BRD2 With tbutyl-phenyl-amino- dimethyl-oxazolyl-quinoline-carboxylic acid===
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Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).,Seal J, Lamotte Y, Donche F, Bouillot A, Mirguet O, Gellibert F, Nicodeme E, Krysa G, Kirilovsky J, Beinke S, McCleary S, Rioja I, Bamborough P, Chung CW, Gordon L, Lewis T, Walker AL, Cutler L, Lugo D, Wilson DM, Witherington J, Lee K, Prinjha RK Bioorg Med Chem Lett. 2012 Apr 15;22(8):2968-72. Epub 2012 Feb 24. PMID:22437115<ref>PMID:22437115</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 4akn" style="background-color:#fffaf0;"></div>
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==About this Structure==
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==See Also==
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[[4akn]] is a 3 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=4AKN OCA].
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*[[Bromodomain-containing protein 3D structures|Bromodomain-containing protein 3D structures]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:022437115</ref><references group="xtra"/>
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__TOC__
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Bouillot, A.]]
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[[Category: Large Structures]]
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[[Category: Chung, C.]]
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[[Category: Bouillot A]]
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[[Category: Donche, F.]]
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[[Category: Chung C]]
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[[Category: Lamotte, Y.]]
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[[Category: Donche F]]
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[[Category: Mirguet, O.]]
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[[Category: Lamotte Y]]
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[[Category: Epigenetic reader]]
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[[Category: Mirguet O]]
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[[Category: Histone]]
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[[Category: Inhibitor]]
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[[Category: Protein binding]]
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Current revision

N-Terminal Bromodomain of Human BRD2 With tbutyl-phenyl-amino- dimethyl-oxazolyl-quinoline-carboxylic acid

PDB ID 4akn

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