Dissecting the Biology of Mutant p53 with CETSA®

Unlocking the Complex Biology of Mutant p53 with CETSA: Revealing Target Engagement and Stability Profiles p53 target engagement is a critical factor in modern cancer drug discovery. The tumor suppressor p53 is frequently mutated in human cancers, leading to functional loss and therapy resistance. Our study applies CETSA (Cellular Thermal Shift Assay) to assess p53 target engagement and thermal stability in breast cancer cell lines—revealing how small molecules affect both wild-type and mutant forms of p53. At Pelago Bioscience, we used CETSA to study how these mutations impact p53 behavior in live cells. By quantifying protein thermal stability upon ligand binding, CETSA enables direct, physiologically relevant measurement of target engagement—a key metric in evaluating drug action. Compa...