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4mr6

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==Crystal Structure of the second bromodomain of human BRD2 in complex with a quinazolinone ligand (RVX-208)==
==Crystal Structure of the second bromodomain of human BRD2 in complex with a quinazolinone ligand (RVX-208)==
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<StructureSection load='4mr6' size='340' side='right' caption='[[4mr6]], [[Resolution|resolution]] 1.67&Aring;' scene=''>
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<StructureSection load='4mr6' size='340' side='right'caption='[[4mr6]], [[Resolution|resolution]] 1.67&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[4mr6]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4MR6 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4MR6 FirstGlance]. <br>
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<table><tr><td colspan='2'>[[4mr6]] 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=4MR6 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4MR6 FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=1K0:2-[4-(2-HYDROXYETHOXY)-3,5-DIMETHYLPHENYL]-5,7-DIMETHOXYQUINAZOLIN-4(3H)-ONE'>1K0</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene></td></tr>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1K0:2-[4-(2-HYDROXYETHOXY)-3,5-DIMETHYLPHENYL]-5,7-DIMETHOXYQUINAZOLIN-4(3H)-ONE'>1K0</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene></td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">BRD2, KIAA9001, RING3 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=4mr6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4mr6 OCA], [https://pdbe.org/4mr6 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4mr6 RCSB], [https://www.ebi.ac.uk/pdbsum/4mr6 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4mr6 ProSAT]</span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4mr6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4mr6 OCA], [http://pdbe.org/4mr6 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4mr6 RCSB], [http://www.ebi.ac.uk/pdbsum/4mr6 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4mr6 ProSAT]</span></td></tr>
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</table>
</table>
== Function ==
== Function ==
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[[http://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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[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>
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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==See Also==
==See Also==
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*[[Bromodomain-containing protein|Bromodomain-containing protein]]
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*[[Bromodomain-containing protein 3D structures|Bromodomain-containing protein 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Human]]
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[[Category: Homo sapiens]]
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[[Category: Arrowsmith, C H]]
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[[Category: Large Structures]]
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[[Category: Bountra, C]]
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[[Category: Arrowsmith CH]]
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[[Category: Delft, F von]]
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[[Category: Bountra C]]
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[[Category: Edwards, A M]]
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[[Category: Edwards AM]]
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[[Category: Fedorov, O]]
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[[Category: Fedorov O]]
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[[Category: Felletar, I]]
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[[Category: Felletar I]]
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[[Category: Filippakopoulos, P]]
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[[Category: Filippakopoulos P]]
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[[Category: Knapp, S]]
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[[Category: Knapp S]]
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[[Category: Martin, S]]
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[[Category: Martin S]]
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[[Category: Picaud, S]]
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[[Category: Picaud S]]
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[[Category: Structural genomic]]
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[[Category: Weigelt J]]
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[[Category: Weigelt, J]]
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[[Category: Von Delft F]]
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[[Category: Brd2]]
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[[Category: Inhibitor complex]]
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[[Category: Ring3]]
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[[Category: Rvx-208]]
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[[Category: Sgc]]
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[[Category: Small molecule inhibitor]]
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[[Category: Transcription-transcription inhibitor complex]]
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Revision as of 10:03, 28 December 2022

Crystal Structure of the second bromodomain of human BRD2 in complex with a quinazolinone ligand (RVX-208)

PDB ID 4mr6

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