4c66: Difference between revisions
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{{STRUCTURE_4c66| PDB=4c66 | SCENE= }} | |||
===Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains=== | |||
{{ABSTRACT_PUBMED_24015967}} | |||
==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> | |||
==Function== | |||
[[http://www.uniprot.org/uniprot/BRD4_HUMAN BRD4_HUMAN]] Plays a role in a process governing chromosomal dynamics during mitosis (By similarity). | |||
==About this Structure== | |||
[[4c66]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4C66 OCA]. | |||
==Reference== | |||
<ref group="xtra">PMID:024015967</ref><references group="xtra"/><references/> | |||
[[Category: Homo sapiens]] | |||
[[Category: Chung, C.]] | |||
[[Category: Mirguet, O.]] | |||
[[Category: Antagonist]] | |||
[[Category: Cell cycle]] | |||
[[Category: Epigenetic reader]] | |||
[[Category: Inhibitor]] | |||
[[Category: Transcription regulation]] | |||
Revision as of 10:21, 2 October 2013
Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET BromodomainsDiscovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains
Template:ABSTRACT PUBMED 24015967
DiseaseDisease
[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]
FunctionFunction
[BRD4_HUMAN] Plays a role in a process governing chromosomal dynamics during mitosis (By similarity).
About this StructureAbout this Structure
4c66 is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.
ReferenceReference
- ↑ Mirguet O, Gosmini R, Toum J, Clement CA, Barnathan M, Brusq JM, Mordaunt JE, Grimes R, Crowe M, Pineau O, Ajakane M, Daugan A, Jeffrey P, Cutler L, Haynes A, Smithers N, Chung CW, Bamborough P, Uings IJ, Lewis T, Witherington J, Parr N, Prinjha R, Nicodeme E. Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains. J Med Chem. 2013 Sep 9. PMID:24015967 doi:10.1021/jm401088k
- ↑ 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
- ↑ 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