Targeted Degradation of CDK4/6: An Innovative Approach to Overcoming Cancer Drug Resistance.
Robert B KargboPublished in: ACS medicinal chemistry letters (2023)
Targeted protein degradation has emerged as a powerful approach for the selective elimination of disease-causing proteins. Cyclin-dependent kinases 4 and 6 (CDK4/6) are of significant interest in cancer research due to their crucial role in cell cycle regulation. However, resistance to CDK4/6 inhibitors is a considerable challenge. This Patent Highlight showcases the recent advances in strategies to degrade CDK4/6 to overcome drug resistance, explicitly focusing on proteolysis-targeting chimeras (PROTACs) and molecular glue degraders.