CDK2-targeted protein degrader

CDK2-targeted protein degrader (Blueprint Medicines) is an experimental targeted protein degrader (TPD) currently in preclinical development for the treatment of HR+/HER2- breast cancer and CCNE1-amplified solid tumors. Developed by Blueprint Medicines, the molecule is designed to selectively bind to Cyclin-dependent kinase 2 (CDK2) and recruit an E3 ubiquitin ligase, leading to the ubiquitination and subsequent degradation of the CDK2 protein via the proteasome. This approach aims to overcome the limitations of traditional kinase inhibitors, such as incomplete inhibition or the development of resistance, by completely removing the target protein. CDK2 is a critical driver of cell cycle progression, and its dysregulation is implicated in various cancers, particularly those with CCNE1 amplification or resistance to CDK4/6 inhibitors. The degradation of CDK2 is expected to provide therapeutic benefit in cancers where CDK2 activity is a primary driver of proliferation or a mechanism of resistance to existing therapies.

Other names

CDK2 degraderCDK-2 degraderCDK 2 degrader