p53 Y220C reactivator JAB-30355

An orally bioavailable reactivator of the tumor suppressor protein p53 mutation TP53 Y220C, with potential antineoplastic activity. Upon oral administration, p53 Y220C reactivator JAB-30355 selectively targets, binds to and restores the conformation of TP53 Y220C. This restores the transcriptional activity of TP53 Y220C, reactivates p53-mediated signaling and restores p53 function. This induces cell cycle arrest and apoptosis in tumor cells expressing the TP53 Y220C mutation and inhibits proliferation of tumor cells expressing the TP53 Y220C mutant. p53, a tumor suppressor gene, plays a key role in the regulation of cell cycle arrest, apoptosis, senescence and DNA repair. P53 is often mutated in many tumor cells, resulting in the loss of apoptosis regulation and abnormal cell proliferation. TP53 Y220C is a hotspot loss-of-function mutation.