Phosphatases: An undervalued class of antitumor drug targets

Phosphatases are crucial for cell signaling, cell cycle regulation, and gene expression. Their abnormal expression or function is linked to tumor development. Despite their potential as antitumor targets, developing phosphatase-targeted drugs is challenging due to conserved active sites, complex substrate specificity, and diverse conformational changes. This article explores the importance of phosphatases in cancer, drug design challenges, and highlights two key studies: one on the PTPN2/PTPN1 inhibitor ABBV-CLS-484 and another on the cryo-EM structure of the CDK2–cyclin A–CDC25A complex. These insights offer new directions for antitumor drug development.