RITA

RITA (Reactivation of p53 and Induction of Tumor cell Apoptosis) is a small molecule MDM2 inhibitor that functions by binding directly to the N-terminal domain of the p53 protein. This binding sterically hinders the interaction between p53 and its negative regulator, MDM2, thereby preventing p53 ubiquitination and subsequent proteasomal degradation. By stabilizing p53, RITA restores its transcriptional activity, leading to cell cycle arrest and the induction of apoptosis in various cancer types. Unlike other MDM2 inhibitors such as nutlin-3a, RITA's activity is often associated with the induction of DNA damage responses, which may contribute to its efficacy in both wild-type and mutated TP53 genetic backgrounds. It has been investigated preclinically for the treatment of malignant mesothelioma, often in combination with focal adhesion kinase (FAK) inhibitors like defactinib.

Other names

reactivation of p53 and induction of tumor cell apoptosis