Isoform-Selective ATAD2 chemical probe with novel chemical structure and unusual mode of action

Fernández-Montalván, A., Berger, M., Kuropka, B., et al.

American Chemical Society 2017, vol: 12(11) doi: 10.1021/acschembio.7b00708

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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Topics: Monolith – MicroScale Thermophoresis, MST,  Publications