5D24

First bromodomain of BRD4 bound to inhibitor XD26

Summary for 5D24

• Entry DOI: 10.2210/pdb5d24/pdb
• Descriptor: Bromodomain-containing protein 4, 4-acetyl-N-[3-(2-amino-2-oxoethoxy)phenyl]-3-ethyl-5-methyl-1H-pyrrole-2-carboxamide, 1,2-ETHANEDIOL, ... (4 entities in total)
• Functional Keywords: gene regulation, inhibitor, bromodomain, transcription
• Biological source: Homo sapiens (Human)
• Cellular location: Nucleus: O60885
• Total number of polymer chains: 1
• Total formula weight: 15603.95

Authors

Wohlwend, D.,Huegle, M.,Gerhardt, S. (deposition date: 2015-08-05, release date: 2016-01-20, Last modification date: 2024-05-01)

• Primary citation: Hugle, M.,Lucas, X.,Weitzel, G.,Ostrovskyi, D.,Breit, B.,Gerhardt, S.,Einsle, O.,Gunther, S.,Wohlwend, D.; 4-Acyl Pyrrole Derivatives Yield Novel Vectors for Designing Inhibitors of the Acetyl-Lysine Recognition Site of BRD4(1).; J.Med.Chem., 59:1518-1530, 2016; PubMed: 26731611; DOI: 10.1021/acs.jmedchem.5b01267

Experimental method

X-RAY DIFFRACTION (1.65 Å)