期刊
CURRENT OPINION IN CHEMICAL BIOLOGY
卷 63, 期 -, 页码 132-144出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.cbpa.2021.03.002
关键词
Histone post-translational modifications; Epigenetic reader proteins; Chemical probes; Acylated and methylated lysine; Peptidomimetic li-gands; Allosteric modulators; Protein degraders; Chromatin regulatory; factors; Bromodomains
资金
- National Cancer Institute NIH [R01CA218392]
- National Institute of General Medical Sciences, U.S. National Institutes of Health (NIH) [R01GM100919]
- National Cancer Institute, NIH [R01CA242305]
- University Cancer Research Fund, University of North Carolina at Chapel Hill
- National Institute on Drug Abuse NIH [R61DA047023]
Chemical probes targeting reader proteins are emerging as potential therapeutic targets for a wide range of diseases, including cancer and inflammation-related pathologies. Overcoming challenges associated with antagonizing reader domains involves targeting strategies such as using peptidomimetic ligands and protein degraders.
Responsible for interpreting histone post-translational modifications, epigenetic reader proteins have emerged as novel therapeutic targets for a wide range of diseases. Chemical probes have been critical in enabling target validation studies and have led to translational advances in cancer and inflammation-related pathologies. Here, we present the most recently reported probes of reader proteins that recognize acylated and methylated lysine. We will discuss challenges associated with achieving potent antagonism of reader domains and review ongoing efforts to overcome these hurdles, focusing on targeting strategies including the use of peptidomimetic ligands, allosteric modulators, and protein degraders.
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