More than half of all human tumors express mutant forms of p53, with the ovary,
lung, pancreas, and colorectal cancers among the tumor types that display the highest prevalence
of p53 mutations. In addition, the expression of mutant forms of p53 in tumors is associated
with poor prognosis due to increased chemoresistance and invasiveness. Therefore, the
pharmacological restoration of wild-type-like activity to mutant p53 arises as a promising therapeutic
strategy against cancer. This review is focused on the most relevant mutant p53 small
molecule reactivators described to date. Despite some of them have entered into clinical trials,
none has reached the clinic, which emphasizes that new pharmacological alternatives, particularly
with higher selectivity and lower adverse toxic side effects, are still required.
Keywords: cancer, chemotherapy, p53 tumor suppressor, reactivators, mutant p53, small molecules.
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