In vitro screening of compounds for targeting gastric cancer with Y220C p53 mutation: a molecule combining zinc chelation and a Michael acceptor drives CDKN1 and BBC3 expression to restore a p53-dependent cytotoxicity.

doi:10.1080/14756366.2026.2638836

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Article

In vitro screening of compounds for targeting gastric cancer with Y220C p53 mutation: a molecule combining zinc chelation and a Michael acceptor drives CDKN1 and BBC3 expression to restore a p53-dependent cytotoxicity.

Journal of enzyme inhibition and medicinal chemistry - 1 Dec 2026

Nannini Simon, Sieffert Céline, McGown Andrew, Gao Xin-Yue, Jarvis Amanda, Kostakis Georges E, Galvacsi Antal, Kallay Csilla, Moraru Ruxandra, Baud Matthias G, Mandel Sebastian, Balourdas Dimitros-Ilias, Joerger Andreas C, Orvain Christophe, Peschard Simon, Nion Audrey, Mellitzer Georg, Lottiaux Sophie, Spencer John, Gross Isabelle, Gaiddon Christian

Abstract excerpt

Point mutations in p53 favour tumour aggressivity, particularly in gastric cancer (GC), and offer a target for small molecule-based anticancer treatments. This study focused on the p53-Y220C mutation, which causes p53 misfolding due to thermal instability associated with the creation of a pocket that may accommodate small molecules. This mutation also creates an additional free cysteine thiol group that may react...

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Identifiers

PMID: 42163716
DOI: 10.1080/14756366.2026.2638836
PMCID: PMC13195717

Genes

GC
BBC3

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026.

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