Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action. Fernández-Montalván, A., E., Berger, M., Kuropka, B., Koo, S., J., Badock, V., Weiske, J., Puetter, V., Holton, S., J., Stöckigt, D., Ter Laak, A., Centrella, P., A., Clark, M., A., Dumelin, C., E., Sigel, E., A., Soutter, H., H., Troast, D., M., Zhang, Y., Cuozzo, J., W., Keefe, A., D., Roche, D., Rodeschini, V., Chaikuad, A., Díaz-Sáez, L., Bennett, J., M., Fedorov, O., Huber, K., V., Hübner, J., Weinmann, H., Hartung, I., V., & Gorjánácz, M. ACS Chemical Biology, 2017.
abstract   bibtex   
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.
@article{
 title = {Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action},
 type = {article},
 year = {2017},
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 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.},
 bibtype = {article},
 author = {Fernández-Montalván, Amaury E. and Berger, Markus and Kuropka, Benno and Koo, Seong Joo and Badock, Volker and Weiske, Joerg and Puetter, Vera and Holton, Simon J. and Stöckigt, Detlef and Ter Laak, Antonius and Centrella, Paolo A. and Clark, Matthew A. and Dumelin, Christoph E. and Sigel, Eric A. and Soutter, Holly H. and Troast, Dawn M. and Zhang, Ying and Cuozzo, John W. and Keefe, Anthony D. and Roche, Didier and Rodeschini, Vincent and Chaikuad, Apirat and Díaz-Sáez, Laura and Bennett, James M. and Fedorov, Oleg and Huber, Kilian V.M. and Hübner, Jan and Weinmann, Hilmar and Hartung, Ingo V. and Gorjánácz, Mátyás},
 journal = {ACS Chemical Biology}
}

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