期刊
NATURE COMMUNICATIONS
卷 7, 期 -, 页码 -出版社
NATURE PUBLISHING GROUP
DOI: 10.1038/ncomms12470
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资金
- SNSF
- NCCR Chemical Biology
Herbal extracts containing sesquiterpene lactones have been extensively used in traditional medicine and are known to be rich in a, b-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 PPARg activity in situ via covalent engagement of a cysteine residue in the zinc-finger motif of this nuclear receptor.
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