Cyclin-Dependent Kinase Degradation via E3 Ligase Binding for Potential Disease Modulation in Cancer Treatment.

Cyclin-dependent kinases (CDKs) are crucial regulators of cell cycle progression and transcription. Their dysregulation has been implicated in various diseases, including cancer. This Patent Highlight focuses on recent advances in the development of CDK inhibitor-E3 ligase binding moiety conjugates for targeted CDK degradation and their potential applications in treating diseases modulated by CDKs. The exemplary PROTAC compounds exhibit a broad range of pharmacological activities associated with degradation of the CDK protein target for the treatment of cancer.