5WMD

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

Summary for 5WMD

• Entry DOI: 10.2210/pdb5wmd/pdb
• Descriptor: Bromodomain-containing protein 4, 2-[(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]-N-(4-hydroxyphenyl)acetamide (3 entities in total)
• Functional Keywords: bromodomain, brd4, transcription, otx-015, transcription-transcription inhibitor complex, transcription/transcription inhibitor
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 1
• Total formula weight: 15517.34

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 (1.27 Å)