期刊
TRENDS IN PHARMACOLOGICAL SCIENCES
卷 43, 期 3, 页码 249-262出版社
CELL PRESS
DOI: 10.1016/j.tips.2021.12.002
关键词
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资金
- National Institutes of Health [DA043571]
- Melanoma Research Alliance
- University of Virginia Cancer Center (NCI Cancer Center) [5P30CA044579-27]
- Mark Foundation for Cancer Research (Emerging Leader Award)
This review discusses bioactive small molecules that form covalent bonds with target proteins and their applications in drug research. The emphasis is on the chemistry of modifying catalytic residues and the exploration of reactive groups in understudied residues on proteins.
Bioactive small molecules that form covalent bonds with a target protein are important tools for basic research and can be highly effective drugs. This review highlights reactive groups found in a collection of thiophilic and oxophilic drugs that mediate pharmacological activity through a covalent mechanism of action (MOA). We describe the application of advanced proteomic and bioanalytical methodologies for assessing selectivity of these covalent agents to guide and inspire the search for additional electrophiles suitable for covalent probe and therapeutic development. While the emphasis is on chemistry for modifying catalytic serine, threonine or cysteine residues, we devote a substantial fraction of the review to a collection of exploratory reactive groups of understudied residues on proteins.
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