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Article

Targeting Cavity-Creating p53 Cancer Mutations with Small-Molecule Stabilizers: the Y220X Paradigm.

ACS chemical biology - 20 Mar 2020

Bauer Matthias R, Krämer Andreas, Settanni Giovanni, Jones Rhiannon N, Ni Xiaomin, Khan Tareque Raysa, Fersht Alan R, Spencer John, Joerger Andreas C

Abstract excerpt

We have previously shown that the thermolabile, cavity-creating p53 cancer mutant Y220C can be reactivated by small-molecule stabilizers. In our ongoing efforts to unearth druggable variants of the p53 mutome, we have now analyzed the effects of other cancer-associated mutations at codon 220 on the structure, stability, and dynamics of the p53 DNA-binding domain (DBD). We found that the oncogenic Y220H, Y220N,...

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Identifiers

PMID: 31990523
DOI: 10.1021/acschembio.9b00748
PMCID: PMC7307883

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 6 Sept 2026. Manifest publication-graph-cohort-2026-09-06.1.

Source receipt: pubmed, retrieved 6 Sept 2026.

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