Targeting mutant p53 for cancer therapy.

Moshe Oren,Perry Tal,Varda Rotter

doi:10.18632/aging.100992

Abstract

Targeting mutant p53 for cancer therapy.

Highlights

The p53 tumor suppressor protein serves as a major barrier against cancer; mutations in the TP53 gene, encoding p53, are the most frequent single genetic alteration in human cancer, occurring in about half of all individual cancer cases [1]
Since cancer cells bearing TP53 missense mutations often accumulate massive amounts of the mutant p53, its conversion into a wild type (WT)-like state will potentially flood the cancer cell with excessive amounts of tumor suppressive p53, far beyond what one finds in normal cells
The most advanced effort has been spearheaded by Wiman and coworkers, who identified a small molecule named PRIMA-1, which can reactivate mutant p53

Summary

Introduction

The p53 tumor suppressor protein serves as a major barrier against cancer; mutations in the TP53 gene, encoding p53, are the most frequent single genetic alteration in human cancer, occurring in about half of all individual cancer cases [1]. TP53 missense mutations, thereby restoring its ability to perform the tumor suppressive activities of WTp53 [1, 2]. It can simultaneously reinstate WTp53 tumor suppressive activity together with abrogating the gain-of-function oncogenic effects of the mutant p53 protein.

Results

Conclusion