Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 11, Issue 8, Pages 1581-1587Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.0c00247
Keywords
Bromodomain; BET; constrain; selectivity; dihydrobenzofuran; fluorine
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Funding
- GSK
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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.
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