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GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family
- Source :
- ACS Med Chem Lett
- Publication Year :
- 2020
- Publisher :
- American Chemical Society (ACS), 2020.
-
Abstract
- [Image: see text] 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.
- Subjects :
- 010405 organic chemistry
business.industry
Organic Chemistry
chemical and pharmacologic phenomena
hemic and immune systems
Pharmacology
Highly selective
01 natural sciences
Biochemistry
In vitro
0104 chemical sciences
Bromodomain
010404 medicinal & biomolecular chemistry
Safety profile
In vivo
Drug Discovery
Medicine
business
Subjects
Details
- ISSN :
- 19485875
- Volume :
- 11
- Database :
- OpenAIRE
- Journal :
- ACS Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....a25fcee7700cf48b3d9393a0adacecd2