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A Structure-Guided Molecular Chaperone Approach for Restoring the Transcriptional Activity of the p53 Cancer Mutant Y220C

1 Oct 2019

Abstract excerpt

The p53 cancer mutation Y220C creates a conformationally unstable protein with a unique elongated surface crevice that can be targeted by molecular chaperones. We report the structure-guided optimization of the carbazole-based stabilizer PK083. Materials & methods: Biophysical, cellular and x-ray crystallographic techniques have been employed to elucidate the mode of action of the carbazole scaffolds. Results:...

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PMID: 31633398
DOI: 10.4155/fmc-2019-0181

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