5ek9: Difference between revisions

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'''Unreleased structure'''


The entry 5ek9 is ON HOLD  until Paper Publication
==Crystal structure of the second bromodomain of human BRD2 in complex with a tetrahydroquinoline inhibitor==
 
<StructureSection load='5ek9' size='340' side='right' caption='[[5ek9]], [[Resolution|resolution]] 2.08&Aring;' scene=''>
Authors: Tallant, C., Slavish, P.J., Siejka, P., Bharatham, N., Shadrick, W.R., Chai, S., Young, B.M., Boyd, V.A., Heroven, C., Picaud, S., Fedorov, O., Chen, T., Lee, R.E., Guy, R.K., Shelat, A.A., von Delft, F., Arrowsmith, C.H., Edwards, A.M., Bountra, C., Knapp, S., Structural Genomics Consortium (SGC)
== Structural highlights ==
 
<table><tr><td colspan='2'>[[5ek9]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5EK9 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5EK9 FirstGlance]. <br>
Description: Crystal structure of the second bromodomain of human BRD2 in complex with a tetrahydroquinoline inhibitor
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=5P4:PROPAN-2-YL+~{N}-[(2~{S},4~{R})-1-ETHANOYL-6-(FURAN-2-YL)-2-METHYL-3,4-DIHYDRO-2~{H}-QUINOLIN-4-YL]CARBAMATE'>5P4</scene></td></tr>
[[Category: Unreleased Structures]]
<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=5ek9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ek9 OCA], [http://pdbe.org/5ek9 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5ek9 RCSB], [http://www.ebi.ac.uk/pdbsum/5ek9 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5ek9 ProSAT]</span></td></tr>
[[Category: Boyd, V.A]]
</table>
[[Category: Slavish, P.J]]
== Function ==
[[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> 
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Arrowsmith, C H]]
[[Category: Bharatham, N]]
[[Category: Bountra, C]]
[[Category: Boyd, V A]]
[[Category: Chai, S]]
[[Category: Chen, T]]
[[Category: Delft, F von]]
[[Category: Edwards, A M]]
[[Category: Fedorov, O]]
[[Category: Fedorov, O]]
[[Category: Guy, R K]]
[[Category: Heroven, C]]
[[Category: Knapp, S]]
[[Category: Lee, R E]]
[[Category: Picaud, S]]
[[Category: Picaud, S]]
[[Category: Structural genomic]]
[[Category: Shadrick, W R]]
[[Category: Shelat, A A]]
[[Category: Siejka, P]]
[[Category: Siejka, P]]
[[Category: Knapp, S]]
[[Category: Slavish, P J]]
[[Category: Guy, R.K]]
[[Category: Lee, R.E]]
[[Category: Chen, T]]
[[Category: Bountra, C]]
[[Category: Chai, S]]
[[Category: Shelat, A.A]]
[[Category: Arrowsmith, C.H]]
[[Category: Von Delft, F]]
[[Category: Shadrick, W.R]]
[[Category: Edwards, A.M]]
[[Category: Heroven, C]]
[[Category: Structural Genomics Consortium (Sgc)]]
[[Category: Tallant, C]]
[[Category: Tallant, C]]
[[Category: Young, B.M]]
[[Category: Young, B M]]
[[Category: Bharatham, N]]
[[Category: Acetylation]]
[[Category: Chromatin and transcription regulator]]
[[Category: Sgc]]
[[Category: Transcription]]

Revision as of 06:21, 10 December 2016

Crystal structure of the second bromodomain of human BRD2 in complex with a tetrahydroquinoline inhibitorCrystal structure of the second bromodomain of human BRD2 in complex with a tetrahydroquinoline inhibitor

Structural highlights

5ek9 is a 2 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
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]

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

5ek9, resolution 2.08Å

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OCA
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