6P05

Bromodomain-containing protein 4 (BRD4) bromodomain 1 (BD1) complexed with compound 27

Summary for 6P05

• Entry DOI: 10.2210/pdb6p05/pdb
• Descriptor: Bromodomain-containing protein 4, GLYCEROL, N-{1-[1,1-di(pyridin-2-yl)ethyl]-6-(1-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-3-yl)-1H-indol-4-yl}ethanesulfonamide, ... (4 entities in total)
• Functional Keywords: inhibitor, brd4, bromodomain, transcription
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 1
• Total formula weight: 15860.21

Authors

Ratia, K.M.,Xiong, R.,Li, Y.,Zhao, J.,Gutgesell, L.M.,Shen, Z.,Dye, K.,Dubrovyskyii, O.,Zhao, H.,Huang, F.,Tonetti, D.A.,Thatcher, G.R. (deposition date: 2019-05-16, release date: 2020-05-20, Last modification date: 2023-10-11)

• Primary citation: Li, Y.,Zhao, J.,Gutgesell, L.M.,Shen, Z.,Ratia, K.,Dye, K.,Dubrovskyi, O.,Zhao, H.,Huang, F.,Tonetti, D.A.,Thatcher, G.R.J.,Xiong, R.; Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib.; J.Med.Chem., 63:7186-7210, 2020; PubMed: 32453591; DOI: 10.1021/acs.jmedchem.0c00456

Experimental method

X-RAY DIFFRACTION (1.54 Å)