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- W1036194730 abstract "Tumor protein p53 (TP53) is the most commonly mutated gene in human cancer. The majority of mutations are missense, and generate a defective protein that is druggable. Yet, for decades, the small-molecule restoration of wild-type (WT) p53 function in mutant p53 tumors (so-called p53 mutant 'reactivation') has been elusive to researchers. The p53 protein requires the binding of a single zinc ion for proper folding, and impairing zinc binding is a major mechanism for loss of function in missense mutant p53. Here, we describe recent work defining a new class of drugs termed zinc metallochaperones that restore WT p53 structure and function by restoring Zn(2+) to Zn(2+)-deficient mutant p53." @default.
- W1036194730 created "2016-06-24" @default.
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- W1036194730 date "2015-11-01" @default.
- W1036194730 modified "2023-09-30" @default.
- W1036194730 title "Reactivating mutant p53 using small molecules as zinc metallochaperones: awakening a sleeping giant in cancer" @default.
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- W1036194730 doi "https://doi.org/10.1016/j.drudis.2015.07.006" @default.
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