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TitleBET N-terminal bromodomain inhibition selectively blocks Th17 cell differentiation and ameliorates colitis in mice.
Journal, issue, pagesProc. Natl. Acad. Sci. U.S.A., Vol. 114, Page 2952-2957, Year 2017
Publish dateJan 24, 2017 (structure data deposition date)
AuthorsCheung, K. / Lu, G. / Sharma, R. / Vincek, A. / Zhang, R. / Plotnikov, A.N. / Zhang, F. / Zhang, Q. / Ju, Y. / Hu, Y. ...Cheung, K. / Lu, G. / Sharma, R. / Vincek, A. / Zhang, R. / Plotnikov, A.N. / Zhang, F. / Zhang, Q. / Ju, Y. / Hu, Y. / Zhao, L. / Han, X. / Meslamani, J. / Xu, F. / Jaganathan, A. / Shen, T. / Zhu, H. / Rusinova, E. / Zeng, L. / Zhou, J. / Yang, J. / Peng, L. / Ohlmeyer, M. / Walsh, M.J. / Zhang, D.Y. / Xiong, H. / Zhou, M.M.
External linksProc. Natl. Acad. Sci. U.S.A. / PubMed:28265070
MethodsX-ray diffraction
Resolution1.5 Å
Structure data

PDB-5ula:
Crystal Structure of the First Bromodomain of Human BRD4 in Complex With Cyclic Vinylogous Amide Inhibitor MS402
Method: X-RAY DIFFRACTION / Resolution: 1.5 Å

Chemicals

ChemComp-5MJ:
3-chloranyl-~{N}-(4-methoxyphenyl)-4-[(2-methyl-3-oxidanylidene-cyclopenten-1-yl)amino]benzamide

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
Keywordstranscription/inhibitor / bromodomain / inhibitor / transcription / transcription-inhibitor complex

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