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

• Tác giả: Argonne National Laboratory, United States, United States. Dept. of Energy. Office of Science
• Ngôn ngữ: eng
• Ký hiệu phân loại: 616.994 +Cancers
• Thông tin xuất bản: Washington, D.C. : Oak Ridge, Tenn. : United States. Dept. of Energy. Office of Science ; Distributed by the Office of Scientific and Technical Information, U.S. Dept. of Energy, 2017
• Mô tả vật lý: Size: p. 737-741 : , digital, PDF file.
• Bộ sưu tập: Metadata
• ID: 260547
• Chủ đề: 1. 60 applied life sciences; 2. Bromodomain; 3. Cecr2; 4. Epigenetics; 5. Probe

Tóm tắt

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.