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ACS Chem Biol. 2017 Nov 17;12(11):2730-2736. doi: 10.1021/acschembio.7b00708. Epub 2017 Oct 24.

Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action.

Author information

1
Bayer AG , Pharmaceuticals, Drug Discovery, Berlin, Germany.
2
X-Chem Pharmaceuticals , Waltham, Massachusetts United States.
3
Edelris , Lyon, France.
4
Structural Genomics Consortium, Nuffield Department of Medicine, University of Oxford , Oxford, United Kingdom.
5
Target Discovery Institute, Nuffield Department of Medicine, University of Oxford , Oxford, United Kingdom.

Abstract

ATAD2 (ANCCA) is an epigenetic regulator and transcriptional cofactor, whose overexpression has been linked to the progress of various cancer types. Here, we report a DNA-encoded library screen leading to the discovery of BAY-850, a potent and isoform selective inhibitor that specifically induces ATAD2 bromodomain dimerization and prevents interactions with acetylated histones in vitro, as well as with chromatin in cells. These features qualify BAY-850 as a chemical probe to explore ATAD2 biology.

PMID:
29043777
PMCID:
PMC6218015
DOI:
10.1021/acschembio.7b00708
[Indexed for MEDLINE]
Free PMC Article

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