Related Experiment Video

Updated: Aug 28, 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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A patent and literature review of CDK12 inhibitors

Ruijun Tang1,2, Jing Liu1, Shuyao Li1

  • 1Hunan Key Laboratory of Molecular Precision Medicine, Department of Oncology, Central South University, Changsha, Hunan, China.

Expert Opinion on Therapeutic Patents
|September 19, 2022
PubMed
Abstract

Insights

Cyclin-dependent kinase 12 (CDK12) inhibitors are emerging as promising therapeutics for cancer and myotonic dystrophy type 1. This review details recent inhibitor discovery strategies and their preclinical efficacy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Medicinal Chemistry

Background:

  • Cyclin-dependent kinase 12 (CDK12) regulates gene transcription, mRNA processing, and translation.
  • CDK12 is implicated in human cancers and myotonic dystrophy type 1, presenting it as a therapeutic target.
  • Small molecule inhibitors are being developed to target CDK12.

Approach:

  • This review synthesizes information on patented and peer-reviewed CDK12 inhibitors from 2016 to the present.
  • It covers inhibitor discovery strategies, chemical structures, and molecular profiling.
  • The review examines various mechanisms of action for identified CDK12 inhibitors.

Key Points:

  • CDK12 inhibitors demonstrate therapeutic potential in preclinical models of myotonic dystrophy type 1 and cancer.
  • These inhibitors can be used as single agents or in combination therapies.
  • Diverse inhibitor scaffolds and mechanisms of action have been reported.

Conclusions:

  • CDK12 inhibitors represent valuable tools for evaluating CDK12's therapeutic utility.
  • Promising preclinical results warrant further investigation and clinical trials.
  • Continued research is essential to fully realize the therapeutic potential of CDK12 inhibition.
Keywords:
Anti-cancer agentsCDK12/cyclin KDNA damage responsePROTACmolecular-glue degradermyotonic dystrophy type 1transcription

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