6ZB1

C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH GSK620

This is a non-PDB format compatible entry.

Summary for 6ZB1

• Entry DOI: 10.2210/pdb6zb1/pdb
• Descriptor: Bromodomain-containing protein 2, 1,2-ETHANEDIOL, ~{N}5-cyclopropyl-~{N}3-methyl-2-oxidanylidene-1-(phenylmethyl)pyridine-3,5-dicarboxamide, ... (4 entities in total)
• Functional Keywords: inhibitor, histone, epigenetic reader, bromodomain, brd2, bromodomain containing protein 2, antagonist, transcription
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 1
• Total formula weight: 13881.96

Authors

Chung, C. (deposition date: 2020-06-06, release date: 2020-08-05, Last modification date: 2020-09-23)

• Primary citation: Seal, J.T.,Atkinson, S.J.,Aylott, H.,Bamborough, P.,Chung, C.W.,Copley, R.C.B.,Gordon, L.,Grandi, P.,Gray, J.R.J.,Harrison, L.A.,Hayhow, T.G.,Lindon, M.,Messenger, C.,Michon, A.M.,Mitchell, D.,Preston, A.,Prinjha, R.K.,Rioja, I.,Taylor, S.,Wall, I.D.,Watson, R.J.,Woolven, J.M.,Demont, E.H.; The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor.; J.Med.Chem., 63:9093-9126, 2020; PubMed: 32702236; DOI: 10.1021/acs.jmedchem.0c00796

Experimental method

X-RAY DIFFRACTION (1.6 Å)