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Updated: May 31, 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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Advances in Structural Types and Pharmacochemistry of CDK12 Inhibitors

Dan Wang1, Ming-Tao Xia1, Jia-Xin Yan1

  • 1Key Laboratory of Traditional Chinese Medicine Research and Development of Hebei Province, Institute of Traditional Chinese Medicine, Chengde Medical University, Chengde 067000, P.R. China.

Medicinal Chemistry (Shariqah (United Arab Emirates))
|January 24, 2025
PubMed

Insights

Cyclin-Dependent Kinase (CDK) 12 is crucial for DNA repair and gene transcription. This review details novel CDK12 inhibitors since 2020, analyzing their structures, clinical potential, and future development for cancer treatment.

Area of Science:

  • Molecular Biology
  • Medicinal Chemistry
  • Oncology

Background:

  • Cyclin-Dependent Kinase (CDK) 12 regulates gene transcription, DNA damage response (DDR), and other vital cellular processes.
  • CDK12 is an emerging therapeutic target for various cancers, including prostate, breast, and ovarian cancers.
  • Developing selective CDK12 inhibitors is challenging due to high homology with other CDKs, like CDK13.

Purpose of the Study:

  • To review novel CDK12 inhibitors reported since 2020.
  • To analyze the structural characteristics and biological activities of these inhibitors.
  • To summarize the clinical application potential, challenges, and future trends of CDK12 inhibitors.

Main Methods:

  • Literature review of scientific publications and patents.
  • Structural analysis of reported CDK12 inhibitors.
  • Assessment of biological activities and clinical data.

Main Results:

  • Identification and summarization of various novel CDK12 inhibitors.
  • Analysis of structure-activity relationships for selected inhibitors.
  • Overview of the current landscape of CDK12 inhibitor development.

Conclusions:

  • Significant progress has been made in developing novel CDK12 inhibitors.
  • Challenges remain in achieving selectivity and advancing clinical applications.
  • Future research should focus on overcoming these challenges for effective cancer therapies.
Keywords:
CDK12 inhibitorsbiological activityfuture prospectstructural characteristicsstructure-activity relationship

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