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==Crystal Structure of the first bromodomain of human BRD4 in complex with a isoxazolylbenzimidazole ligand==
==Crystal Structure of the first bromodomain of human BRD4 in complex with a isoxazolylbenzimidazole ligand==
<StructureSection load='4gpj' size='340' side='right'caption='[[4gpj]], [[Resolution|resolution]] 1.60&Aring;' scene=''>
<StructureSection load='4gpj' size='340' side='right'caption='[[4gpj]]' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[4gpj]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4GPJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4GPJ FirstGlance]. <br>
<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4GPJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4GPJ FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=0Q1:(1R)-6-(3,5-DIMETHYL-1,2-OXAZOL-4-YL)-1-PHENYL-2,3-DIHYDRO-1H-INDEN-1-OL'>0Q1</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene></td></tr>
</td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4gpj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4gpj OCA], [https://pdbe.org/4gpj PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4gpj RCSB], [https://www.ebi.ac.uk/pdbsum/4gpj PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4gpj ProSAT]</span></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4gpj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4gpj OCA], [https://pdbe.org/4gpj PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4gpj RCSB], [https://www.ebi.ac.uk/pdbsum/4gpj PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4gpj ProSAT]</span></td></tr>
</table>
</table>
== Disease ==
[[https://www.uniprot.org/uniprot/BRD4_HUMAN BRD4_HUMAN]] Note=A chromosomal aberration involving BRD4 is found in a rare, aggressive, and lethal carcinoma arising in midline organs of young people. Translocation t(15;19)(q14;p13) with NUT which produces a BRD4-NUT fusion protein.<ref>PMID:12543779</ref> <ref>PMID:11733348</ref> 
== Function ==
[[https://www.uniprot.org/uniprot/BRD4_HUMAN BRD4_HUMAN]] Plays a role in a process governing chromosomal dynamics during mitosis (By similarity).
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Simple 1-substituted 5- and 6-isoxazolyl-benzimidazoles have been shown to be potent inhibitors of the BET bromodomains with selectivity over the related bromodomain of CBP. The reported inhibitors were prepared from simple starting materials in two steps followed by separation of the regioisomers or regioselectively in three steps.
The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains.,Hay D, Fedorov O, Filippakopoulos P, Martin S, Philpott M, Picaud S, Hewings DS, Uttakar S, Heightman TD, Conway SJ, Knapp S, Brennan PE Medchemcomm. 2013 Jan 1;4(1):140-144. doi: 10.1039/C2MD20189E. PMID:26682033<ref>PMID:26682033</ref>
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 4gpj" style="background-color:#fffaf0;"></div>


==See Also==
==See Also==
*[[Bromodomain-containing protein 3D structures|Bromodomain-containing protein 3D structures]]
*[[Bromodomain-containing protein 3D structures|Bromodomain-containing protein 3D structures]]
== References ==
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Large Structures]]
[[Category: Large Structures]]
[[Category: Arrowsmith, C H]]
[[Category: Arrowsmith CH]]
[[Category: Bountra, C]]
[[Category: Bountra C]]
[[Category: Brennan, P]]
[[Category: Brennan P]]
[[Category: Delft, F von]]
[[Category: Edwards A]]
[[Category: Edwards, A]]
[[Category: Felletar I]]
[[Category: Felletar, I]]
[[Category: Filippakopoulos P]]
[[Category: Filippakopoulos, P]]
[[Category: Heightman TD]]
[[Category: Heightman, T D]]
[[Category: Knapp S]]
[[Category: Knapp, S]]
[[Category: Picaud S]]
[[Category: Picaud, S]]
[[Category: Qi J]]
[[Category: Qi, J]]
[[Category: Von Delft F]]
[[Category: Structural genomic]]
[[Category: Bromodomain]]
[[Category: Cap]]
[[Category: Cell cycle]]
[[Category: Hunk1]]
[[Category: Mcap]]
[[Category: Mitotic chromosome associated protein]]
[[Category: Protein binding-inhibitor complex]]
[[Category: Sgc]]

Revision as of 10:43, 31 August 2022

Crystal Structure of the first bromodomain of human BRD4 in complex with a isoxazolylbenzimidazole ligand

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