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{{STRUCTURE_4nr8|  PDB=4nr8  |  SCENE=  }}
==Crystal structure of the first bromodomain of human BRD4 in complex with an isoxazolyl-benzimidazole ligand==
===Crystal structure of the first bromodomain of human BRD4 in complex with an isoxazolyl-benzimidazole ligand===
<StructureSection load='4nr8' size='340' side='right' caption='[[4nr8]], [[Resolution|resolution]] 1.64&Aring;' scene=''>
 
== Structural highlights ==
==Disease==
<table><tr><td colspan='2'>[[4nr8]] 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=4NR8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4NR8 FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=2LL:5-(3,5-DIMETHYL-1,2-OXAZOL-4-YL)-1-[2-(MORPHOLIN-4-YL)ETHYL]-2-(2-PHENYLETHYL)-1H-BENZIMIDAZOLE'>2LL</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=K:POTASSIUM+ION'>K</scene></td></tr>
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">BRD4, HUNK1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
<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=4nr8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4nr8 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4nr8 RCSB], [http://www.ebi.ac.uk/pdbsum/4nr8 PDBsum]</span></td></tr>
</table>
== Disease ==
[[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>   
[[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>   
 
== Function ==
==Function==
[[http://www.uniprot.org/uniprot/BRD4_HUMAN BRD4_HUMAN]] Plays a role in a process governing chromosomal dynamics during mitosis (By similarity).  
[[http://www.uniprot.org/uniprot/BRD4_HUMAN BRD4_HUMAN]] Plays a role in a process governing chromosomal dynamics during mitosis (By similarity).  
 
== References ==
==About this Structure==
<references/>
[[4nr8]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4NR8 OCA].
__TOC__
 
</StructureSection>
==Reference==
[[Category: Human]]
<references group="xtra"/><references/>
[[Category: Arrowsmith, C H]]
[[Category: Arrowsmith, C H.]]
[[Category: Bountra, C]]
[[Category: Bountra, C.]]
[[Category: Brennan, P]]
[[Category: Brennan, P.]]
[[Category: Delft, F Von]]
[[Category: Delft, F Von.]]
[[Category: Edwards, A M]]
[[Category: Edwards, A M.]]
[[Category: Fedorov, O]]
[[Category: Fedorov, O.]]
[[Category: Felletar, I]]
[[Category: Felletar, I.]]
[[Category: Filippakopoulos, P]]
[[Category: Filippakopoulos, P.]]
[[Category: Hay, D]]
[[Category: Hay, D.]]
[[Category: Knapp, S]]
[[Category: Knapp, S.]]
[[Category: Martin, S]]
[[Category: Martin, S.]]
[[Category: Picaud, S]]
[[Category: Picaud, S.]]
[[Category: Structural genomic]]
[[Category: SGC, Structural Genomics Consortium.]]
[[Category: Chemical tool]]
[[Category: Chemical tool]]
[[Category: Sgc]]
[[Category: Sgc]]
[[Category: Small molecule inhibitor]]
[[Category: Small molecule inhibitor]]
[[Category: Structural genomics consortium]]
[[Category: Transcription]]
[[Category: Transcription]]
[[Category: Transcription-inhibitor complex]]
[[Category: Transcription-inhibitor complex]]

Revision as of 20:08, 21 December 2014

Crystal structure of the first bromodomain of human BRD4 in complex with an isoxazolyl-benzimidazole ligandCrystal structure of the first bromodomain of human BRD4 in complex with an isoxazolyl-benzimidazole ligand

Structural highlights

4nr8 is a 1 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:, ,
Gene:BRD4, HUNK1 (HUMAN)
Resources:FirstGlance, OCA, RCSB, PDBsum

Disease

[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.[1] [2]

Function

[BRD4_HUMAN] Plays a role in a process governing chromosomal dynamics during mitosis (By similarity).

References

  1. ↑ French CA, Miyoshi I, Kubonishi I, Grier HE, Perez-Atayde AR, Fletcher JA. BRD4-NUT fusion oncogene: a novel mechanism in aggressive carcinoma. Cancer Res. 2003 Jan 15;63(2):304-7. PMID:12543779
  2. ↑ French CA, Miyoshi I, Aster JC, Kubonishi I, Kroll TG, Dal Cin P, Vargas SO, Perez-Atayde AR, Fletcher JA. BRD4 bromodomain gene rearrangement in aggressive carcinoma with translocation t(15;19). Am J Pathol. 2001 Dec;159(6):1987-92. PMID:11733348 doi:10.1016/S0002-9440(10)63049-0

4nr8, resolution 1.64Å

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