6Z8P

C-TERMINAL BROMODOMAIN OF HUMAN BRD2 WITH GSK973

This is a non-PDB format compatible entry.

Summary for 6Z8P

• Entry DOI: 10.2210/pdb6z8p/pdb
• Descriptor: Bromodomain-containing protein 2, 1,2-ETHANEDIOL, 2-(2-{2-[2-(2-METHOXY-ETHOXY)-ETHOXY]-ETHOXY}-ETHOXY)-ETHANOL, ... (5 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: 14281.41

Authors

Chung, C. (deposition date: 2020-06-02, release date: 2020-10-21, Last modification date: 2024-05-01)

Primary citation

Preston, A.,Atkinson, S.J.,Bamborough, P.,Chung, C.W.,Gordon, L.J.,Grandi, P.,Gray, J.R.J.,Harrison, L.A.,Lewis, A.J.,Lugo, D.,Messenger, C.,Michon, A.M.,Mitchell, D.J.,Prinjha, R.K.,Rioja, I.,Seal, J.,Taylor, S.,Thesmar, P.,Wall, I.D.,Watson, R.J.,Woolven, J.M.,Demont, E.H.
GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family.
Acs Med.Chem.Lett., 11:1581-1587, 2020

PubMed Abstract: Pan-BET inhibitors have shown profound efficacy in a number of in vivo preclinical models and have entered the clinic in oncology trials where adverse events have been reported. These inhibitors interact equipotently with the eight bromodomains of the BET family of proteins. To better understand the contribution of each domain to their efficacy and to improve from their safety profile, selective inhibitors are required. This Letter discloses the profile of GSK973, a highly selective inhibitor of the second bromodomains of the BET proteins that has undergone extensive preclinical in vitro and in vivo characterization.

PubMed: 32832027
DOI: 10.1021/acsmedchemlett.0c00247

Experimental method

X-RAY DIFFRACTION (1.55 Å)