ArticleJournal of cellular and molecular medicine2019
Xanthatin inhibits STAT3 and NF-κB signalling by covalently binding to JAK and IKK kinases.
Article in Journal of cellular and molecular medicine, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 25 citations in OpenAlex.
- Xanthatin induces apoptosis through ROS-mediated c-FLIP inhibition in human retinoblastoma cells.Frontiers in medicine · 2025Article
- Dietary curcumin alleviates intestinal damage induced by ochratoxin A in juvenile grass carp (Animal nutrition (Zhongguo xu mu shou yi xue hui) · 2024Article
- Recent advances in anti-inflammatory active components and action mechanisms of natural medicines.Inflammopharmacology · 2023Review
- Investigation of targets and anticancer mechanisms of covalently acting natural products by functional proteomics.Acta pharmacologica Sinica · 2023Article
- Xanthatin suppresses proliferation and tumorigenicity of glioma cells through autophagy inhibition via activation of the PI3K-Akt-mTOR pathway.Pharmacology research & perspectives · 2023Review
- RIPK1 and RIPK3 inhibitors: potential weapons against inflammation to treat diabetic complications.Frontiers in immunology · 2023Review
- Xanthanolides inMolecules (Basel, Switzerland) · 2022Review
- Covalent Modification of the JH2 Domain of Janus Kinase 2.ACS medicinal chemistry letters · 2022Article
- Xanthatin Alleviates LPS-Induced Inflammatory Response in RAW264.7 Macrophages by Inhibiting NF-κB, MAPK and STATs Activation.Molecules (Basel, Switzerland) · 2022Article
- Brevilin A Ameliorates Acute Lung Injury and Inflammation Through Inhibition of NF-κB SignalingFrontiers in pharmacology · 2022Article
- Xanthatin Selectively Targets Retinoblastoma by Inhibiting the PLK1-Mediated Cell Cycle.Investigative ophthalmology & visual science · 2021Article
- Xanthatin synergizes with cisplatin to suppress homologous recombination through JAK2/STAT4/BARD1 axis in human NSCLC cells.Journal of cellular and molecular medicine · 2021Article
- Xanthatin Induces Leishmanicidal Activity by Affecting Carbon Metabolism in Amastigotes.Iranian journal of pharmaceutical research : IJPR · 2021Article
- Xanthatin inhibits STAT3 and NF-κB signalling by covalently binding to JAK and IKK kinases.Journal of cellular and molecular medicine · 2019Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Aberrant activation of the signal transducer and activator of transcription 3 (STAT3) and the nuclear factor-κB (NF-κB) signalling pathways is associated with the development of cancer and inflammatory diseases. JAKs and IKKs are the key regulators in the STAT3 and NF-κB signalling respectively. Therefore, the two families of kinases have been the major targets for developing drugs to regulate the two signalling pathways. Here, we report a natural compound xanthatin from the traditional Chinese medicinal herb Xanthium L. as a potent inhibitor of both STAT3 and NF-κB signalling pathways. Our data demonstrated that xanthatin was a covalent inhibitor and its activities depended on its α-methylene-γ-butyrolactone group. It preferentially interacted with the Cys243 of JAK2 and the Cys412 and Cys464 of IKKβ to inactivate their activities. In doing so, xanthatin preferentially inhibited the growth of cancer cell lines that have constitutively activated STAT3 and p65. These data suggest that xanthatin may be a promising anticancer and anti-inflammation drug candidate.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.