Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action
Year: 2017
Type: article
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.
Source: ACS Chemical Biology
Authors: Amaury E. Fernández-Montalván, Markus Berger, Benno Kuropka, Seong Joo Koo, Volker Badock, Joerg Weiske, Vera Puetter, Simon J. Holton, Detlef Stöckigt, Antonius ter Laak, Paolo A. Centrella, Matthew A. Clark, Christoph E. Dumelin, Eric A. Sigel, Holly H. Soutter, Dawn M. Troast, Ying Zhang, John W. Cuozzo, Anthony D. Keefe, Didier Roche, Vincent Rodeschini, Apirat Chaikuad, Laura Díaz-Sáez, James M. Bennett, Oleg Fedorov, Kilian V. M. Huber, Jan Hübner, Hilmar Weinmann, Ingo V. Hartung, Mátyás Gorjánácz
Institutions: Bayer (Germany), University of Oxford
Language: English
Subfield: Molecular Biology
Domain: Life Sciences
Open Access status: hybrid
Estimated APC paid: $4,500
OpenAlex ID: W2765540468