Definition

An orally bioavailable, small molecule reactivator of the p53 Y220C mutant, with potential antineoplastic activity. Upon oral administration, p53 Y220C mutant reactivator PC14586 selectively targets and binds to the crevice created by the p53 Y220C mutation, which normalizes and restores wild-type p53 protein structure and activity. This blocks tumor cell cycle progression and induces apoptosis in tumor cells expressing the p53 Y220C mutant. The p53 gene, a tumor suppressor gene, is mutated in many tumor types. The p53 protein plays a key role in the regulation of apoptosis and cellular proliferation.