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GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2)

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journal contribution
posted on 01.06.2017, 00:00 by Terry D. Crawford, James E. Audia, Steve Bellon, Daniel J. Burdick, Archana Bommi-Reddy, Alexandre Côté, Richard T. Cummings, Martin Duplessis, E. Megan Flynn, Michael Hewitt, Hon-Ren Huang, Hariharan Jayaram, Ying Jiang, Shivangi Joshi, James R. Kiefer, Jeremy Murray, Christopher G. Nasveschuk, Arianne Neiss, Eneida Pardo, F. Anthony Romero, Peter Sandy, Robert J. Sims, Yong Tang, Alexander M. Taylor, Vickie Tsui, Jian Wang, Shumei Wang, Yongyun Wang, Zhaowu Xu, Laura Zawadzke, Xiaoqin Zhu, Brian K. Albrecht, Steven R. Magnuson, Andrea G. Cochran
The biological function of bromodomains, epigenetic readers of acetylated lysine residues, remains largely unknown. Herein we report our efforts to discover a potent and selective inhibitor of the bromodomain of cat eye syndrome chromosome region candidate 2 (CECR2). Screening of our internal medicinal chemistry collection led to the identification of a pyrrolopyridone chemical lead, and subsequent structure-based drug design led to a potent and selective CECR2 bromodomain inhibitor (GNE-886) suitable for use as an in vitro tool compound.