Related Experiment Video

Updated: Jan 18, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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Therapeutic targeting of CDK12: a medicinal chemistry perspective

Feifei Wang1, Hongxue Dai2, Kuanxin Wan3

  • 1Zhongshan Institute for Drug Discovery, Chinese Academy of Sciences, Zhongshan 528400, Guangdong, China; School of Chinese Materia Medica, Nanjing University of Chinese Medicine, Nanjing 210023, China.

Bioorganic & Medicinal Chemistry
|January 16, 2026
PubMed

Insights

Cyclin-dependent kinase 12 (CDK12) is crucial for genomic stability and cancer progression. This review details CDK12 inhibitors and degraders, offering insights for developing targeted cancer therapies.

Area of Science:

  • Molecular Biology
  • Genetics
  • Oncology

Background:

  • Cyclin-dependent kinase 12 (CDK12) regulates gene transcription and maintains genomic stability.
  • CDK12 alterations are linked to tumorigenesis and cancer progression.
  • CDK12 is a potential therapeutic target and biomarker for cancer treatment.

Purpose of the Study:

  • To review various types of CDK12 small-molecule inhibitors and degraders.
  • To explore structure-activity relationships of CDK12 inhibitors.
  • To provide insights for developing novel CDK12-targeted cancer drugs.

Main Methods:

  • Literature review of CDK12 inhibitors and degraders.
  • Analysis of structural frameworks and structure-activity relationships.
  • Focus on small-molecule drug development.

Main Results:

  • Detailed review of existing CDK12 small-molecule inhibitors and degraders.
  • Exploration of structure-activity relationships for drug design.
  • Identification of CT7439 as a CDK12/13 inhibitor in clinical trials.

Conclusions:

  • CDK12 is a promising target for cancer therapy.
  • Understanding structure-activity relationships is key for developing selective inhibitors.
  • Further research into CDK12 inhibitors and degraders can lead to novel cancer treatments.
Keywords:
CDK12DegraderInhibitorMedical chemistry

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