A Chemical Compound with Possible p53 Cancer Mutant Rescue Activity
Background: Mutants of the tumor suppressor protein are frequently found in human cancers. About three quarters of them have a single amino acid change in the core domain of p53 that is needed to bind to p53 DNA binding cites. There is great interest for identifying chemical compounds that can restore function to p53 cancer mutants because 1) the patient pool that would benefit from such drugs enormous and 2) cancers with p53 mutations have worse prognosis. One of the challenge is the remarkable diversity of several hundred different such p53 cancer mutants. Technology: UCI researchers established a yeast assay to perform screens for p53 mutant rescue drugs. The assay was designed to show whether a screened compound is capable of restoring function to one or more of p53 cancer mutants. Such compounds were identified and their activity was confirmed by additional screens. Application: If the activity of the compound is further confirmed, it may become the precursor to a new anti-cancer drug with specific effects on cancers with p53 mutants.
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