Three optimized assays for the evaluation of compounds that can rescue p53 mutants

Published: 4 June 2021| Version 1 | DOI: 10.17632/y742f9j8v5.1
Contributors:
Jiale Wu,
Huaxin Song,
Zhengyuan Wang,
Min Lu

Description

Drugs targeting p53 remain a proverbial Holy Grail of precision oncology, with over twenty compounds that can rescue p53 mutants reported so far. Here, we suggest three easily accessible assays to determine the thermostability, protein folding, and transcriptional activity of p53 mutants – the three go-to criteria for evaluating a rescue compound that acts by increasing p53 thermostability. Because of the diversity of p53 mutants, a compound that meets the criteria of one assay does not necessarily meet the criteria of the two other assays. For complete details on the use and execution of these protocols, please refer to (Chen et al., 2021).

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