7LEK

Crystal structure of the second bromodomain (BD2) of human BRDT bound to ERK5-IN-1

Summary for 7LEK

• Entry DOI: 10.2210/pdb7lek/pdb
• Descriptor: Bromodomain testis-specific protein, 11-cyclopentyl-2-({2-ethoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]phenyl}amino)-5-methyl-5,11-dihydro-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one, CHLORIDE ION, ... (5 entities in total)
• Functional Keywords: brdt, bet, plk1, testis specific, bromodomain, gene regulation
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 4
• Total formula weight: 57471.89

Authors

Chan, A.,Karim, M.R.,Schonbrunn, E. (deposition date: 2021-01-14, release date: 2021-07-14, Last modification date: 2023-10-18)

• Primary citation: Karim, R.M.,Bikowitz, M.J.,Chan, A.,Zhu, J.Y.,Grassie, D.,Becker, A.,Berndt, N.,Gunawan, S.,Lawrence, N.J.,Schonbrunn, E.; Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors.; J.Med.Chem., 64:15772-15786, 2021; PubMed: 34710325; DOI: 10.1021/acs.jmedchem.1c01096

Experimental method

X-RAY DIFFRACTION (2.75 Å)