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Molecules inducing specific cyclin-dependent kinase degradation and their possible use in cancer therapy.

Mingming ZhengXiao-Yu ZhangWeijiao ChenFei XiaHuanaoyu YangKai YuanPeng Yang
Published in: Future medicinal chemistry (2024)
Cyclin-dependent kinases (CDKs) play an important role in the regulation of cell proliferation, and many CDK inhibitors were developed. However, pan-CDK inhibitors failed to be approved due to intolerant toxicity or low efficacy and the use of selective CDK4/6 inhibitors is limited by resistance. Protein degraders have the potential to increase selectivity, efficacy and overcome resistance, which provides a novel strategy for regulating CDKs. In this review, we summarized the function of CDKs in regulating the cell cycle and transcription, and introduced the representative CDK inhibitors. Then we made a detailed introduction about four types of CDKs degraders, including their action mechanisms, research status and application prospects, which could help the development of novel CDKs degraders.
Keyphrases
  • cell cycle
  • cell proliferation
  • cancer therapy
  • oxidative stress
  • transcription factor
  • cell death
  • cross sectional
  • signaling pathway
  • protein kinase