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Divergent synthesis and identification of the cellular targets of deoxyelephantopins

Published inNature communications, vol. 7, 12470
Publication date2016
Abstract

Herbal extracts containing sesquiterpene lactones have been extensively used in traditional medicine and are known to be rich in α,β-unsaturated functionalities that can covalently engage target proteins. Here we report synthetic methodologies to access analogues of deoxyelephantopin, a sesquiterpene lactone with anticancer properties. Using alkyne-tagged cellular probes and quantitative proteomics analysis, we identified several cellular targets of deoxyelephantopin. We further demonstrate that deoxyelephantopin antagonizes PPARγ activity in situ via covalent engagement of a cysteine residue in the zinc-finger motif of this nuclear receptor.

Citation (ISO format)
LAGOUTTE, Roman et al. Divergent synthesis and identification of the cellular targets of deoxyelephantopins. In: Nature communications, 2016, vol. 7, p. 12470. doi: 10.1038/ncomms12470
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ISSN of the journal2041-1723
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