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Updated: Jun 15, 2026

Sequence-specific Labeling of Nucleic Acids and Proteins with Methyltransferases and Cofactor Analogues
Published on: November 22, 2014
Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action
Amaury E Fernández-Montalván1, Markus Berger1, Benno Kuropka1
1Bayer AG , Pharmaceuticals, Drug Discovery, Berlin, Germany.
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.
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