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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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Published on: October 26, 2015

Terapéutica dirigida de CDK12: una perspectiva de química medicinal

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

Abstract:

CDK12 (Cyclin-dependent kinase 12) is a cyclin-dependent kinase that regulates gene transcription by phosphorylating the C-terminal domain of RNA polymerase II, playing a crucial role in maintaining genomic stability. Mutations or alterations in the CDK12 genome can trigger tumorigenesis and progression. Inhibiting the overexpression of CDK12 suppresses tumor growth and proliferation, indicating that it serves both as a biomarker for tumorigenesis and a potential therapeutic target for cancer treatment. In recent years, the structure and biological functions of CDK12 have been progressively elucidated, attracting significant research attention. Currently, the CDK12/13 inhibitor CT7439 is undergoing Phase I/II clinical trials. This paper provides a detailed review of various types of CDK12 small-molecule inhibitors/degraders, primarily based on key structural frameworks. It focuses on exploring the existing structure-activity relationships, aiming to offer a comprehensive perspective for developing highly selective CDK12-targeted inhibitors/degraders and providing valuable insights for future novel drug development.

Palabras clave:

CDK12 Degradador Inhibidor Química medicinal

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