5WMG

N-terminal bromodomain of BRD4 in complex with OTX-015

Summary for 5WMG

• Entry DOI: 10.2210/pdb5wmg/pdb
• Descriptor: Bromodomain-containing protein 4, 1,2-ETHANEDIOL, 4-{6-(3,5-dimethyl-1,2-oxazol-4-yl)-1-[(1S)-1-(pyridin-2-yl)ethyl]-1H-pyrrolo[3,2-b]pyridin-3-yl}benzoic acid, ... (4 entities in total)
• Functional Keywords: bromodomain, brd4, transcription, plx51107, transcription-transcription inhibitor complex, transcription/transcription inhibitor
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 1
• Total formula weight: 15650.02

Authors

Zhang, Y. (deposition date: 2017-07-28, release date: 2018-08-01, Last modification date: 2023-10-04)

• Primary citation: Ozer, H.G.,El-Gamal, D.,Powell, B.,Hing, Z.A.,Blachly, J.S.,Harrington, B.,Mitchell, S.,Grieselhuber, N.R.,Williams, K.,Lai, T.H.,Alinari, L.,Baiocchi, R.A.,Brinton, L.,Baskin, E.,Cannon, M.,Beaver, L.,Goettl, V.M.,Lucas, D.M.,Woyach, J.A.,Sampath, D.,Lehman, A.M.,Yu, L.,Zhang, J.,Ma, Y.,Zhang, Y.,Spevak, W.,Shi, S.,Severson, P.,Shellooe, R.,Carias, H.,Tsang, G.,Dong, K.,Ewing, T.,Marimuthu, A.,Tantoy, C.,Walters, J.,Sanftner, L.,Rezaei, H.,Nespi, M.,Matusow, B.,Habets, G.,Ibrahim, P.,Zhang, C.,Mathe, E.A.,Bollag, G.,Byrd, J.C.,Lapalombella, R.; BRD4 Profiling Identifies Critical Chronic Lymphocytic Leukemia Oncogenic Circuits and Reveals Sensitivity to PLX51107, a Novel Structurally Distinct BET Inhibitor.; Cancer Discov, 8:458-477, 2018; PubMed: 29386193; DOI: 10.1158/2159-8290.CD-17-0902

Experimental method

X-RAY DIFFRACTION (1.19 Å)