Related Experiment Video

Updated: Jul 29, 2025

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

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Novel Medicinal Chemistry Strategies Targeting CDK5 for Drug Discovery

Wentao Tang1, Congcong Lin2, Quanwei Yu1

  • 1Department of Biotherapy, Cancer Center and State Key Laboratory of Biotherapy and Joint Research Institution of Altitude Health and National Clinical Research Center for Geriatrics, West China Hospital, Sichuan University, Chengdu 610041, China.

Journal of Medicinal Chemistry
|May 26, 2023
PubMed

Insights

Cyclin-dependent kinase 5 (CDK5) is crucial in the central nervous system and periphery, offering therapeutic potential for cancer and neurodegenerative diseases. New strategies like selective inhibitors and PROTACs aim to improve efficacy and reduce side effects.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Cyclin-dependent kinase 5 (CDK5) protein is implicated in central nervous system functions, immune responses, insulin secretion, and cancer.
  • Targeting CDK5 presents a therapeutic strategy for cancer and neurodegenerative diseases.
  • Existing pan-CDK inhibitors show limited efficacy and significant adverse effects.

Purpose of the Study:

  • To review the properties, functions, and signaling pathways of CDK5.
  • To analyze the role of CDK5 in cancer development and progression.
  • To discuss the clinical and preclinical status of CDK5 inhibitors and novel therapeutic approaches.

Main Methods:

  • Literature review and analysis of existing research on CDK5.
  • Examination of clinical trial data for pan-CDK inhibitors.
  • Assessment of preclinical data for CDK5-specific inhibitors and emerging therapeutic modalities.

Main Results:

  • CDK5 plays a multifaceted role in various physiological and pathological processes.
  • Pan-CDK inhibitors have shown limited success due to off-target effects.
  • Emerging CDK5-specific inhibitors, PROTACs, and dual-target agents show promise.

Conclusions:

  • CDK5 is a significant therapeutic target for multiple diseases.
  • Selective inhibition and novel drug delivery systems are crucial for improving treatment outcomes.
  • Further research into CDK5-specific therapeutics is warranted.

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