This is a mutant p53-dependent activator of p73, an activator of p53-regulated genes, and a suppressor of mutant p53-bearing tumor cells. Greater than 50% of tumors express mutant p53 which is defective for the tumor-suppressor function and contributes to malignancy by blocking a p53 family member p73. Activation of p73 in human cancer produces a cytotoxic effect. RETRA increases the expression level of p73 and releases p73 from the inhibitory complex with mutant 53. This then produces a tumor-supressor effect, in vitro and in vivo.
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PMID: 35327630 | NAMPT Inhibitor and P73 Activator Represses P53 R175H Mutated HNSCC Cell Proliferation in a Synergistic Manner. | Cai, BH. et al. 2022. Biomolecules. 12: