APR-246 reactivates mutant p53 by targeting cysteines 124 and 277

Abstract excerpt

Abstract The TP 53 tumor suppressor gene is frequently inactivated in human tumors by missense mutations in the DNA binding domain. TP 53 mutations lead to protein unfolding, decreased thermostability and loss of DNA binding and transcription factor function. Pharmacological targeting of mutant p53 to restore its tumor suppressor function is a promising strategy for cancer therapy. The mutant p53 reactivating...

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