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Article

Structural basis of p53 inactivation by cavity-creating cancer mutations and its implications for the development of mutant p53 reactivators.

Cell death & disease - 11 Jun 2024

Balourdas Dimitrios-Ilias, Markl Anja M, Krämer Andreas, Settanni Giovanni, Joerger Andreas C

Abstract excerpt

The cavity-creating p53 cancer mutation Y220C is an ideal paradigm for developing small-molecule drugs based on protein stabilization. Here, we have systematically analyzed the structural and stability effects of all oncogenic Tyr-to-Cys mutations (Y126C, Y163C, Y205C, Y220C, Y234C, and Y236C) in the p53 DNA-binding domain (DBD). They were all highly destabilizing, drastically lowering the melting temperature of...

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Identifiers

PMID: 38862470
DOI: 10.1038/s41419-024-06739-x
PMCID: PMC11166945

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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