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{{STRUCTURE_4mr5|  PDB=4mr5  |  SCENE=  }}
===Crystal Structure of the second bromodomain of human BRD2 in complex with a quinazolinone ligand (RVX-OH)===
{{ABSTRACT_PUBMED_24248379}}


==Function==
==Crystal Structure of the second bromodomain of human BRD2 in complex with a quinazolinone ligand (RVX-OH)==
[[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>
<StructureSection load='4mr5' size='340' side='right'caption='[[4mr5]], [[Resolution|resolution]] 1.63&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[4mr5]] 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=4MR5 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4MR5 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]] 1.63&#8491;</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>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4mr5 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4mr5 OCA], [https://pdbe.org/4mr5 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4mr5 RCSB], [https://www.ebi.ac.uk/pdbsum/4mr5 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4mr5 ProSAT]</span></td></tr>
</table>
== Function ==
[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>  


==About this Structure==
==See Also==
[[4mr5]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4MR5 OCA].
*[[Bromodomain-containing protein 3D structures|Bromodomain-containing protein 3D structures]]
 
== References ==
==Reference==
<references/>
<ref group="xtra">PMID:024248379</ref><references group="xtra"/><references/>
__TOC__
[[Category: Arrowsmith, C H.]]
</StructureSection>
[[Category: Bountra, C.]]
[[Category: Homo sapiens]]
[[Category: Delft, F von.]]
[[Category: Large Structures]]
[[Category: Edwards, A M.]]
[[Category: Arrowsmith CH]]
[[Category: Fedorov, O.]]
[[Category: Bountra C]]
[[Category: Felletar, I.]]
[[Category: Edwards AM]]
[[Category: Filippakopoulos, P.]]
[[Category: Fedorov O]]
[[Category: Knapp, S.]]
[[Category: Felletar I]]
[[Category: Martin, S.]]
[[Category: Filippakopoulos P]]
[[Category: Picaud, S.]]
[[Category: Knapp S]]
[[Category: Weigelt, J.]]
[[Category: Martin S]]
[[Category: Brd2]]
[[Category: Picaud S]]
[[Category: Inhibitor complex]]
[[Category: Weigelt J]]
[[Category: Ring3]]
[[Category: Von Delft F]]
[[Category: Rvx-oh]]
[[Category: Sgc]]
[[Category: Small molecule inhibitor]]
[[Category: Structural genomics consortium]]
[[Category: Transcription-transcription inhibitor complex]]

Latest revision as of 15:28, 1 March 2024

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

Structural highlights

4mr5 is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 1.63Å
Ligands:, ,
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

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.[1]

See Also

References

  1. ↑ LeRoy G, Rickards B, Flint SJ. The double bromodomain proteins Brd2 and Brd3 couple histone acetylation to transcription. Mol Cell. 2008 Apr 11;30(1):51-60. doi: 10.1016/j.molcel.2008.01.018. PMID:18406326 doi:10.1016/j.molcel.2008.01.018

4mr5, resolution 1.63Å

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