3P5O

Crystal Structure of the First Bromodomain of Human Brd4 in complex with IBET inhibitor

Summary for 3P5O

Entry DOI	10.2210/pdb3p5o/pdb
Descriptor	Bromodomain-containing protein 4, 2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide, 1,2-ETHANEDIOL, ... (4 entities in total)
Functional Keywords	brd4, bromodomain containing protein 4, antagonist, ibet, inhibition of acetylated lysine histone binding, transcription regulator, signaling protein-inhibitor complex, signaling protein/inhibitor
Biological source	Homo sapiens (human)
Cellular location	Nucleus (By similarity): O60885
Total number of polymer chains	1
Total formula weight	15771.55
Authors	Chung, C. (deposition date: 2010-10-09, release date: 2010-11-17, Last modification date: 2023-11-01)
Primary citation	Nicodeme, E.,Jeffrey, K.L.,Schaefer, U.,Beinke, S.,Dewell, S.,Chung, C.,Chandwani, R.,Marazzi, I.,Wilson, P.,Coste, H.,White, J.,Kirilovsky, J.,Rice, C.M.,Lora, J.M.,Prinjha, R.K.,Lee, K.,Tarakhovsky, A. Suppression of inflammation by a synthetic histone mimic Nature, 468:1119-1123, 2010 Cited by PubMed: 21068722 DOI: 10.1038/nature09589 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (1.6 Å)

Structure validation