| Autor: |
Arianne Neiss, Martin Duplessis, Hariharan Jayaram, Shumei Wang, F. Anthony Romero, Christopher G. Nasveschuk, Daniel J. Burdick, James E. Audia, Terry Crawford, Steve Bellon, Hon-Ren Huang, Zhaowu Xu, Yongyun Wang, Ying Jiang, Michael C. Hewitt, Jeremy Murray, Andrea G. Cochran, Peter Sandy, Yong Tang, Brian K. Albrecht, E. Megan Flynn, James R. Kiefer, Archana Bommi-Reddy, Jian Wang, Laura Zawadzke, Shivangi Joshi, Vickie Tsui, Xiaoqin Zhu, Alexander M. Taylor, Robert J. Sims, Eneida Pardo, Alexandre Côté, Steven Magnuson, Richard T. Cummings |
| Rok vydání: |
2017 |
| Předmět: |
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| Zdroj: |
ACS Medicinal Chemistry Letters. 8:737-741 |
| ISSN: |
1948-5875 |
| Popis: |
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. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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