4.5 Review

Small-molecule degraders of cyclin-dependent kinase protein: a review

Journal

FUTURE MEDICINAL CHEMISTRY
Volume 14, Issue 3, Pages 167-185

Publisher

Newlands Press Ltd
DOI: 10.4155/fmc-2021-0154

Keywords

cyclin-dependent kinase inhibitors; glue degraders; PROTAC degraders; protein degradation; ubiquitin-proteasome system

Funding

  1. National Natural Science Foundation of China [81872746, 81703347]
  2. National Natural Science Foundation of Jiangsu Province of China [BK20170743, BK20171393]
  3. State Key Laboratory of Drug Research [SIMM1903KF-03]
  4. Postgraduate Research & Practice Innovation Program of Jiangsu Province [KYCX18 0770]

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Proteolysis-targeting chimeras are a new modality of chemical tools and potential therapeutics that induce protein degradation, with CDK-targeting degraders showing advantages in potency, selectivity, and drug resistance compared to traditional CDK inhibitors. The discovery of molecule glues has further promoted the development of CDK degraders, with a focus on discussing the structural characteristics and design of these degraders.
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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