Recent advances in the development of peptide-based inhibitors targeting epigenetic readers of histone lysine acetylation and methylation marks |
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| Affiliation: | 1. Departments of Chemistry, The University of Hong Kong, Pokfulam Road, Hong Kong, China;2. Greater Bay Biomedical InnoCenter, Shenzhen Bay Laboratory, Shenzhen, 518107, China;1. Shanghai Key Laboratory of Green Chemistry and Chemical Process, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, China;2. State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai, China;3. State Key Laboratory of Elemento-Organic Chemistry, Nankai University, China;1. Department of Biology, Technion-Israel Institute of Technology, Haifa 3200003, Israel;2. Centre for Structural Systems Biology (CSSB) and Deutsches Elektronen-Synchrotron DESY, Hamburg, Germany;3. Universitätsklinikum Hamburg-Eppendorf (UKE), Hamburg, Germany;4. European Molecular Biology Laboratory (EMBL), Hamburg, Germany;1. Department of Molecular Genetics and Microbiology, Duke University, Durham, NC, USA;2. Department of Chemistry, Duke University, Durham, NC, USA;1. Department of Molecular, Cellular, and Developmental Biology, Yale University, New Haven, CT, 06520, USA;2. Department of Chemistry, Yale University, New Haven, CT, 06520, USA;3. Microbial Sciences Institute, Yale University, West Haven, CT, 06516, USA |
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| Abstract: | Inhibitors for epigenetic readers of histone modifications are useful chemical probes to interrogate the functional roles played by their cognate targets in epigenetic regulation and can even serve as drugs for the treatment of diseases associated with the dysregulated targets. However, many epigenetic readers are intractable to small molecules, as the recognition of modified histone peptides commonly involves flat and extended protein surfaces. In contrast, the relatively large sizes and structural complexity of peptides help them achieve tight and specific binding to the target proteins. Increasing efforts have been made to target epigenetic readers using peptide-based inhibitors that can complement small molecules. In this review, we discuss the recent advances in the development of peptide-based inhibitors of lysine acetylation and methylation readers. |
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| Keywords: | Epigenetic reader Peptide-based inhibitor Chemical probe Lysine acetylation Lysine methylation |
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