关键词: PROTAC degraders cyclin-dependent kinase inhibitors glue degraders protein degradation ubiquitin-proteasome system

Mesh : Cyclin-Dependent Kinases / antagonists & inhibitors metabolism Humans Molecular Structure Protein Kinase Inhibitors / chemistry pharmacology Small Molecule Libraries / chemistry pharmacology

来  源:   DOI:10.4155/fmc-2021-0154

Abstract:
Proteolysis-targeting chimeras are a new modality of chemical tools and potential therapeutics involving the induction of protein degradation. Cyclin-dependent kinase (CDK) protein, which is involved in cycles and transcription cycles, participates in regulation of the cell cycle, transcription and splicing. Proteolysis-targeting chimeras targeting CDKs show several advantages over traditional CDK small-molecule inhibitors in potency, selectivity and drug resistance. In addition, the discovery of molecule glues promotes the development of CDK degraders. Herein, the authors describe the existing CDK degraders and focus on the discussion of the structural characteristics and design of these degraders.
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