6DL2

BRD4 bromodomain 1 in complex with HYB157

Summary for 6DL2

• Entry DOI: 10.2210/pdb6dl2/pdb
• Descriptor: Bromodomain-containing protein 4, 3-benzyl-2,9-dimethyl-4H,6H-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,4]oxazepine, 1,2-ETHANEDIOL, ... (4 entities in total)
• Functional Keywords: bromodomain, transcription
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 1
• Total formula weight: 15526.83

Authors

Meagher, J.L.,Stuckey, J.A. (deposition date: 2018-05-31, release date: 2019-04-17, Last modification date: 2023-10-11)

• Primary citation: Qin, C.,Hu, Y.,Zhou, B.,Fernandez-Salas, E.,Yang, C.Y.,Liu, L.,McEachern, D.,Przybranowski, S.,Wang, M.,Stuckey, J.,Meagher, J.,Bai, L.,Chen, Z.,Lin, M.,Yang, J.,Ziazadeh, D.N.,Xu, F.,Hu, J.,Xiang, W.,Huang, L.,Li, S.,Wen, B.,Sun, D.,Wang, S.; Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression.; J. Med. Chem., 61:6685-6704, 2018; PubMed: 30019901; DOI: 10.1021/acs.jmedchem.8b00506

Experimental method

X-RAY DIFFRACTION (1.47 Å)