AI Article Synopsis
- Parthenolide, derived from the feverfew plant, shows anti-inflammatory and anti-cancer properties, and this study aims to understand its mechanism in breast cancer cells.
- Using advanced chemoproteomic techniques, researchers discovered that parthenolide covalently modifies a specific cysteine in focal adhesion kinase 1 (FAK1), disrupting its signaling pathways.
- This impairment results in reduced breast cancer cell growth, survival, and movement, highlighting an important target for other natural anti-cancer compounds.
Article Abstract
Parthenolide, a natural product from the feverfew plant and member of the large family of sesquiterpene lactones, exerts multiple biological and therapeutic activities including anti-inflammatory and anti-cancer effects. Here, we further study the parthenolide mechanism of action using activity-based protein profiling-based chemoproteomic platforms to map additional covalent targets engaged by parthenolide in human breast cancer cells. We find that parthenolide, as well as other related exocyclic methylene lactone-containing sesquiterpenes, covalently modify cysteine 427 of focal adhesion kinase 1 (FAK1), leading to impairment of FAK1-dependent signaling pathways and breast cancer cell proliferation, survival, and motility. These studies reveal a functional target exploited by members of a large family of anti-cancer natural products.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6756182 | PMC |
| http://dx.doi.org/10.1016/j.chembiol.2019.03.016 | DOI Listing |
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