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Publication Detail

Title: Parthenolide Covalently Targets and Inhibits Focal Adhesion Kinase in Breast Cancer Cells.

Authors: Berdan, Charles A; Ho, Raymond; Lehtola, Haley S; To, Milton; Hu, Xirui; Huffman, Tucker R; Petri, Yana; Altobelli, Chad R; Demeulenaere, Sasha G; Olzmann, James A; Maimone, Thomas J; Nomura, Daniel K

Published In Cell Chem Biol, (2019 07 18)

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.

PubMed ID: 31080076 Exiting the NIEHS site

MeSH Terms: No MeSH terms associated with this publication

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