دورية أكاديمية
Parthenolide Covalently Targets and Inhibits Focal Adhesion Kinase in Breast Cancer Cells.
| العنوان: | Parthenolide Covalently Targets and Inhibits Focal Adhesion Kinase in Breast Cancer Cells. |
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| المؤلفون: | Berdan CA; Department of Nutritional Sciences and Toxicology, University of California, Berkeley, Berkeley, CA 94720, USA; Novartis-Berkeley Center for Proteomics and Chemistry Technologies, University of California, Berkeley, Berkeley, CA 94720, USA., Ho R; Department of Molecular and Cell Biology, University of California, Berkeley, Berkeley, CA 94720, USA., Lehtola HS; Department of Nutritional Sciences and Toxicology, University of California, Berkeley, Berkeley, CA 94720, USA., To M; Department of Nutritional Sciences and Toxicology, University of California, Berkeley, Berkeley, CA 94720, USA., Hu X; Department of Chemistry, University of California, Berkeley, Berkeley, CA 94720, USA., Huffman TR; Department of Chemistry, University of California, Berkeley, Berkeley, CA 94720, USA., Petri Y; Department of Chemistry, University of California, Berkeley, Berkeley, CA 94720, USA; Novartis-Berkeley Center for Proteomics and Chemistry Technologies, University of California, Berkeley, Berkeley, CA 94720, USA., Altobelli CR; Department of Chemistry, University of California, Berkeley, Berkeley, CA 94720, USA., Demeulenaere SG; Department of Chemistry, University of California, Berkeley, Berkeley, CA 94720, USA., Olzmann JA; Department of Nutritional Sciences and Toxicology, University of California, Berkeley, Berkeley, CA 94720, USA., Maimone TJ; Department of Chemistry, University of California, Berkeley, Berkeley, CA 94720, USA; Novartis-Berkeley Center for Proteomics and Chemistry Technologies, University of California, Berkeley, Berkeley, CA 94720, USA. Electronic address: maimone@berkeley.edu., Nomura DK; Department of Nutritional Sciences and Toxicology, University of California, Berkeley, Berkeley, CA 94720, USA; Department of Chemistry, University of California, Berkeley, Berkeley, CA 94720, USA; Department of Molecular and Cell Biology, University of California, Berkeley, Berkeley, CA 94720, USA; Novartis-Berkeley Center for Proteomics and Chemistry Technologies, University of California, Berkeley, Berkeley, CA 94720, USA. Electronic address: dnomura@berkeley.edu. |
| المصدر: | Cell chemical biology [Cell Chem Biol] 2019 Jul 18; Vol. 26 (7), pp. 1027-1035.e22. Date of Electronic Publication: 2019 May 09. |
| نوع المنشور: | Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't |
| اللغة: | English |
| بيانات الدورية: | Publisher: Cell Press Country of Publication: United States NLM ID: 101676030 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 2451-9448 (Electronic) Linking ISSN: 24519448 NLM ISO Abbreviation: Cell Chem Biol Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: Cambridge, MA : Cell Press, 2016- |
| مواضيع طبية MeSH: | Breast Neoplasms/*metabolism , Focal Adhesion Kinase 1/*metabolism , Sesquiterpenes/*metabolism, Biological Products ; Cell Line, Tumor ; Cell Movement/drug effects ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Female ; Focal Adhesion Kinase 1/antagonists & inhibitors ; Focal Adhesion Protein-Tyrosine Kinases ; Humans ; Lactones ; Sesquiterpenes/pharmacology ; Signal Transduction/drug effects ; Tanacetum parthenium |
| مستخلص: | 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. (Copyright © 2019 Elsevier Ltd. All rights reserved.) |
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| معلومات مُعتمدة: | R01 ES028096 United States ES NIEHS NIH HHS; P42 ES004705 United States ES NIEHS NIH HHS; R01 GM116952 United States GM NIGMS NIH HHS; R01 GM112948 United States GM NIGMS NIH HHS; R01 CA172667 United States CA NCI NIH HHS |
| فهرسة مساهمة: | Keywords: ABPP; FAK1; PTK2; activity-based protein profiling; chemoproteomics; covalent ligands; focal adhesion kinase 1; natural products; parthenolide |
| المشرفين على المادة: | 0 (Biological Products) 0 (Lactones) 0 (Sesquiterpenes) 0 (methylene-lactone) 2RDB26I5ZB (parthenolide) EC 2.7.10.2 (Focal Adhesion Kinase 1) EC 2.7.10.2 (Focal Adhesion Protein-Tyrosine Kinases) EC 2.7.10.2 (PTK2 protein, human) |
| تواريخ الأحداث: | Date Created: 20190514 Date Completed: 20200720 Latest Revision: 20200720 |
| رمز التحديث: | 20231215 |
| مُعرف محوري في PubMed: | PMC6756182 |
| DOI: | 10.1016/j.chembiol.2019.03.016 |
| PMID: | 31080076 |
| قاعدة البيانات: | MEDLINE |
| تدمد: | 2451-9448 |
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| DOI: | 10.1016/j.chembiol.2019.03.016 |