5HLS

Crystal structure of the first bromodomain of human BRD4 bound to CPI-0610

Summary for 5HLS

Entry DOI	10.2210/pdb5hls/pdb
Descriptor	Bromodomain-containing protein 4, CPI-0610 (3 entities in total)
Functional Keywords	bromodomain, transcription
Biological source	Homo sapiens (Human)
Cellular location	Nucleus: O60885
Total number of polymer chains	1
Total formula weight	15492.15
Authors	Jayaram, H.,Poy, F.,Setser, J.W.,Bellon, S.F. (deposition date: 2016-01-15, release date: 2016-02-10, Last modification date: 2023-09-27)
Primary citation	Albrecht, B.K.,Gehling, V.S.,Hewitt, M.C.,Vaswani, R.G.,Cote, A.,Leblanc, Y.,Nasveschuk, C.G.,Bellon, S.,Bergeron, L.,Campbell, R.,Cantone, N.,Cooper, M.R.,Cummings, R.T.,Jayaram, H.,Joshi, S.,Mertz, J.A.,Neiss, A.,Normant, E.,O'Meara, M.,Pardo, E.,Poy, F.,Sandy, P.,Supko, J.,Sims, R.J.,Harmange, J.C.,Taylor, A.M.,Audia, J.E. Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials. J.Med.Chem., 59:1330-1339, 2016 Cited by PubMed: 26815195 DOI: 10.1021/acs.jmedchem.5b01882 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (2.182 Å)

Structure validation