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{{STRUCTURE_4lys|  PDB=4lys  |  SCENE=  }}
===Crystal Structure of BRD4(1) bound to inhibitor XD1===
{{ABSTRACT_PUBMED_24272870}}


==Disease==
==Crystal Structure of BRD4(1) bound to Colchiceine==
[[http://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>
<StructureSection load='4lys' size='340' side='right'caption='[[4lys]], [[Resolution|resolution]] 1.83&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[4lys]] 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=4LYS OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4LYS FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.83&#8491;</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=2SJ:N-[(7S)-10-HYDROXY-1,2,3-TRIMETHOXY-9-OXO-5,6,7,9-TETRAHYDROBENZO[A]HEPTALEN-7-YL]ACETAMIDE'>2SJ</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene></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=4lys FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4lys OCA], [https://pdbe.org/4lys PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4lys RCSB], [https://www.ebi.ac.uk/pdbsum/4lys PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4lys ProSAT]</span></td></tr>
</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 ==
Bromodomains are acetyllysine epigenetic mark reader proteins. Small molecules inhibiting them have potential as anti-inflammatory, antiviral, and anticancer agents. A 4-acyl pyrrole derivative (see yellow structure in recognition pocket) has been identified that potently inhibits specific bromodomains and exhibits antiproliferative activity against leukemia cell lines.


==Function==
4-acyl pyrroles: mimicking acetylated lysines in histone code reading.,Lucas X, Wohlwend D, Hugle M, Schmidtkunz K, Gerhardt S, Schule R, Jung M, Einsle O, Gunther S Angew Chem Int Ed Engl. 2013 Dec 23;52(52):14055-9. doi: 10.1002/anie.201307652. , Epub 2013 Nov 24. PMID:24272870<ref>PMID:24272870</ref>
[[http://www.uniprot.org/uniprot/BRD4_HUMAN BRD4_HUMAN]] Plays a role in a process governing chromosomal dynamics during mitosis (By similarity).  


==About this Structure==
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
[[4lys]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4LYS OCA].
</div>
<div class="pdbe-citations 4lys" style="background-color:#fffaf0;"></div>


==Reference==
==See Also==
<ref group="xtra">PMID:024272870</ref><references group="xtra"/><references/>
*[[Bromodomain-containing protein 3D structures|Bromodomain-containing protein 3D structures]]
[[Category: Einsle, O.]]
== References ==
[[Category: Gerhardt, S.]]
<references/>
[[Category: Wohlwend, D.]]
__TOC__
[[Category: Acetylated lysine]]
</StructureSection>
[[Category: Brd4 inhibitor]]
[[Category: Homo sapiens]]
[[Category: Bromodomain]]
[[Category: Large Structures]]
[[Category: Epigenetic reader protein]]
[[Category: Einsle O]]
[[Category: Histone tail]]
[[Category: Gerhardt S]]
[[Category: Nucleus]]
[[Category: Wohlwend D]]
[[Category: Protein binding-inhibitor complex]]

Latest revision as of 09:49, 25 December 2024

Crystal Structure of BRD4(1) bound to Colchiceine

4lys, resolution 1.83Å

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