| Autor: |
John W. Cuozzo, Matthew A. Clark, Holly H. Soutter, Ying Zhang, Anthony D. Keefe, Vera Puetter, Hilmar Weinmann, Ingo Hartung, Detlef Stöckigt, Seong Joo Koo, Eric A. Sigel, Paolo A. Centrella, Oleg Fedorov, Simon Holton, Christoph E. Dumelin, Kilian Huber, Dawn M. Troast, Antonius Ter Laak, L. Diaz-Saez, Jan Hübner, Mátyás Gorjánácz, Volker Badock, Apirat Chaikuad, Markus Berger, Benno Kuropka, Vincent Rodeschini, James M. Bennett, Amaury Ernesto Fernandez-Montalvan, Didier M. Roche, Joerg Weiske |
| Jazyk: |
angličtina |
| Rok vydání: |
2017 |
| Předmět: |
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| Popis: |
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. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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