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GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2).
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2017 Jun 01; Vol. 8 (7), pp. 737-741. Date of Electronic Publication: 2017 Jun 01 (Print Publication: 2017). - Publication Year :
- 2017
-
Abstract
- The biological function of bromodomains, epigenetic readers of acetylated lysine residues, remains largely unknown. Herein we report our efforts to discover a potent and selective inhibitor of the bromodomain of cat eye syndrome chromosome region candidate 2 (CECR2). Screening of our internal medicinal chemistry collection led to the identification of a pyrrolopyridone chemical lead, and subsequent structure-based drug design led to a potent and selective CECR2 bromodomain inhibitor (GNE-886) suitable for use as an in vitro tool compound.
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 8
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 28740608
- Full Text :
- https://doi.org/10.1021/acsmedchemlett.7b00132