Related Experiment Video

Updated: Dec 10, 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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Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update

Tizhi Wu1, Zhen Qin1, Yucheng Tian1

  • 1Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, People's Republic of China.

Journal of Medicinal Chemistry
|September 1, 2020
PubMed

Insights

Cyclin-dependent kinase 9 (CDK9) modulators are promising cancer therapeutics. This review highlights recent advances in CDK9 inhibitors and degraders, including PROTACs, for treating cancers driven by transcriptional dysregulation.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Cyclin-dependent kinase 9 (CDK9) is crucial for transcriptional elongation and frequently dysregulated in cancers.
  • CDK9's role in RNA polymerase II pause/release makes it a key target for cancer therapy.
  • Selective CDK9 inhibition or degradation shows therapeutic potential in preclinical and clinical studies.

Purpose of the Study:

  • To provide a comprehensive overview of recent advancements in CDK9 modulators.
  • To focus on CDK9 inhibitors and degraders currently under clinical evaluation.
  • To explore emerging therapeutic strategies targeting CDK9, such as PROTACs.

Main Methods:

  • Review of current scientific literature on CDK9 modulators.
  • Analysis of clinical trial data for CDK9-targeting agents.
  • Examination of novel drug development strategies, including proteolysis targeting chimeras (PROTACs).

Main Results:

  • Several CDK9 inhibitors and degraders are in clinical development for various cancers.
  • Emerging strategies like PROTACs offer new avenues for selective CDK9 targeting.
  • CDK9 modulation demonstrates promise in cancers characterized by transcriptional dysregulation.

Conclusions:

  • CDK9 modulators represent a significant therapeutic advancement in oncology.
  • Ongoing clinical development of CDK9 inhibitors and degraders warrants close attention.
  • Novel approaches like PROTACs are expanding the therapeutic landscape for CDK9-targeted cancer treatment.

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