Alkynol natural products target ALDH2 in cancer cells by irreversible binding to the active site

Wolfgang Heydenreuter, Elena Kunold, Stephan A. Sieber

Research output: Contribution to journalArticlepeer-review

44 Scopus citations

Abstract

Falcarinol and stipudiol are natural products with potent anti-cancer activity found in several vegetables. Here, we use a chemical proteomic strategy to identify ALDH2 as a molecular target of falcarinol in cancer cells and confirm enzyme inhibition via covalent alkylation of the active site. Furthermore, the synthesis of stipudiol led to the observation that ALDH2 exhibits preference for alkynol-based binders. Inhibition of ALDH2 impairs detoxification of reactive aldehydes and limits oxidative stress response, two crucial pathways for cellular viability.

Original languageEnglish
Pages (from-to)15784-15787
Number of pages4
JournalChemical Communications
Volume51
Issue number87
DOIs
StatePublished - 2015

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