RITA (reactivation of p53 and induction of tumor cell apoptosis) binds to p53 (Kd = 1.5 nM), changing its conformation, preventing it from binding to HDM2 and preventing its proteasomal degradation. It also weakly (computed Kd = 22 µM) binds HDM2 in the cleft that contacts the p53...
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RITA (reactivation of p53 and induction of tumor cell apoptosis) binds to p53 (Kd = 1.5 nM), changing its conformation, preventing it from binding to HDM2 and preventing its proteasomal degradation. It also weakly (computed Kd = 22 µM) binds HDM2 in the cleft that contacts the p53 transactivation domain. Its restoration of mutant p53 function depends on eIF2α phosphorylation, and it induces apoptosis via p53-dependent and -independent (JNK/SAPK/p38; protein translation) pathways. Induces senescence in head and neck cancer cells
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