GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family.

Authors :: Preston A
Atkinson SJ
Bamborough P
Chung CW
Gordon LJ
Grandi P
Gray JRJ
Harrison LA
Lewis AJ
Lugo D
Messenger C
Michon AM
Mitchell DJ
Prinjha RK
Rioja I
Seal J
Taylor S
Thesmar P
Wall ID
Watson RJ
Woolven JM
Demont EH
Source :: ACS medicinal chemistry letters [ACS Med Chem Lett] 2020 Jul 06; Vol. 11 (8), pp. 1581-1587. Date of Electronic Publication: 2020 Jul 06 (Print Publication: 2020).
Publication Year :: 2020
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.<br />Competing Interests: The authors declare no competing financial interest.<br /> (Copyright © 2020 American Chemical Society.)

Full Text Access

Tools