4mr6
Crystal Structure of the second bromodomain of human BRD2 in complex with a quinazolinone ligand (RVX-208)Crystal Structure of the second bromodomain of human BRD2 in complex with a quinazolinone ligand (RVX-208)
Template:ABSTRACT PUBMED 24248379
FunctionFunction
[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 StructureAbout this Structure
4mr6 is a 1 chain structure. Full crystallographic information is available from OCA.
ReferenceReference
- ↑ 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
- ↑ 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
Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)
OCACategories:
- Arrowsmith, C H.
- Bountra, C.
- Delft, F von.
- Edwards, A M.
- Fedorov, O.
- Felletar, I.
- Filippakopoulos, P.
- Knapp, S.
- Martin, S.
- Picaud, S.
- SGC, Structural Genomics Consortium.
- Weigelt, J.
- Brd2
- Inhibitor complex
- Ring3
- Rvx-208
- Sgc
- Small molecule inhibitor
- Structural genomics consortium
- Transcription-transcription inhibitor complex