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Divergent synthesis and identification of the cellular targets of deoxyelephantopins

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Published in Nature Communications. 2016, vol. 7, p. 12470
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.
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Research groups Groupe Winssinger
Groupe Adibekian
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LAGOUTTE, Roman et al. Divergent synthesis and identification of the cellular targets of deoxyelephantopins. In: Nature Communications, 2016, vol. 7, p. 12470. https://archive-ouverte.unige.ch/unige:86480

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Deposited on : 2016-08-30

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