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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.

Original publication

DOI

10.1021/acschembio.7b00708

Type

Journal article

Journal

ACS Chem Biol

Publication Date

17/11/2017

Volume

12

Pages

2730 - 2736

Keywords

ATPases Associated with Diverse Cellular Activities, Cell Line, Tumor, Chromatin, DNA-Binding Proteins, Drug Discovery, Histones, Humans, Ligands, Models, Molecular, Molecular Probes, Protein Interaction Maps, Protein Isoforms, Protein Multimerization