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5ULA

Crystal Structure of the First Bromodomain of Human BRD4 in Complex With Cyclic Vinylogous Amide Inhibitor MS402

Summary for 5ULA
Entry DOI10.2210/pdb5ula/pdb
DescriptorBromodomain-containing protein 4, 3-chloranyl-~{N}-(4-methoxyphenyl)-4-[(2-methyl-3-oxidanylidene-cyclopenten-1-yl)amino]benzamide (3 entities in total)
Functional Keywordsbromodomain, inhibitor, transcription, transcription-inhibitor complex, transcription/inhibitor
Biological sourceHomo sapiens (Human)
Cellular locationNucleus: O60885
Total number of polymer chains2
Total formula weight30940.42
Authors
Plotnikov, A.N.,Joshua, j.,Zhou, M.-M. (deposition date: 2017-01-24, release date: 2017-03-22, Last modification date: 2024-03-06)
Primary citationCheung, 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.
BET N-terminal bromodomain inhibition selectively blocks Th17 cell differentiation and ameliorates colitis in mice.
Proc. Natl. Acad. Sci. U.S.A., 114:2952-2957, 2017
Cited by
PubMed: 28265070
DOI: 10.1073/pnas.1615601114
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (1.5 Å)
Structure validation

217705

數據於2024-03-27公開中

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