4mr5

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'''Unreleased structure'''
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{{STRUCTURE_4mr5| PDB=4mr5 | SCENE= }}
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===Crystal Structure of the second bromodomain of human BRD2 in complex with a quinazolinone ligand (RVX-OH)===
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{{ABSTRACT_PUBMED_24248379}}
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The entry 4mr5 is ON HOLD until Paper Publication
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==Function==
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[[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>
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Authors: Filippakopoulos, P., Picaud, S., Felletar, I., Martin, S., Fedorov, O., von Delft, F., Arrowsmith, C.H., Edwards, A.M., Weigelt, J., Bountra, C., Knapp, S., Structural Genomics Consortium (SGC)
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==About this Structure==
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[[4mr5]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4MR5 OCA].
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Description: Crystal Structure of the second bromodomain of human BRD2 in complex with a quinazolinone ligand (RVX-OH)
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==Reference==
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<ref group="xtra">PMID:024248379</ref><references group="xtra"/><references/>
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[[Category: Arrowsmith, C H.]]
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[[Category: Bountra, C.]]
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[[Category: Delft, F von.]]
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[[Category: Edwards, A M.]]
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[[Category: Fedorov, O.]]
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[[Category: Felletar, I.]]
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[[Category: Filippakopoulos, P.]]
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[[Category: Knapp, S.]]
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[[Category: Martin, S.]]
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[[Category: Picaud, S.]]
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[[Category: Weigelt, J.]]
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[[Category: Brd2]]
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[[Category: Inhibitor complex]]
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[[Category: Ring3]]
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[[Category: Rvx-oh]]
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[[Category: Sgc]]
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[[Category: Small molecule inhibitor]]
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[[Category: Structural genomics consortium]]
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[[Category: Transcription-transcription inhibitor complex]]

Revision as of 10:24, 27 November 2013

Template:STRUCTURE 4mr5

Contents

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

Template:ABSTRACT PUBMED 24248379

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]

About this Structure

4mr5 is a 1 chain structure. Full crystallographic information is available from OCA.

Reference

  • Picaud S, Wells C, Felletar I, Brotherton D, Martin S, Savitsky P, Diez-Dacal B, Philpott M, Bountra C, Lingard H, Fedorov O, Muller S, Brennan PE, Knapp S, Filippakopoulos P. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc Natl Acad Sci U S A. 2013 Nov 18. PMID:24248379 doi:http://dx.doi.org/10.1073/pnas.1310658110
  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

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