ArticleCancer science2014
2-Methoxystypandrone inhibits signal transducer and activator of transcription 3 and nuclear factor-κB signaling by inhibiting Janus kinase 2 and IκB kinase.
Article in Cancer science, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed.
- Advances for pharmacological activities ofPharmaceutical biology · 2023Review
- In Silico and In Vitro Study of Janus Kinases Inhibitors from Naphthoquinones.Molecules (Basel, Switzerland) · 2023Article
- Inhibition of Jurkat T Cell Proliferation by Active Components ofJournal of microbiology and biotechnology · 2020Article
- High JAK2 Protein Expression Predicts a Poor Prognosis in Patients with Resectable Pancreatic Ductal Adenocarcinoma.Disease markers · 2020Article
- 3-Deoxy-2β,16-dihydroxynagilactone E, a natural compound from Podocarpus nagi, preferentially inhibits JAK2/STAT3 signaling by allosterically interacting with the regulatory domain of JAK2 and induces apoptosis of cancer cells.Acta pharmacologica Sinica · 2019Article
- 2-Ethoxystypandrone, a novel small-molecule STAT3 signaling inhibitor from Polygonum cuspidatum, inhibits cell growth and induces apoptosis of HCC cells and HCC Cancer stem cells.BMC complementary and alternative medicine · 2019Article
- Advances in the Regulatory Effects of Bioactive Peptides on Metabolic Signaling Pathways in Tumor Cells.Journal of Cancer · 2019Review
- Parthenolide Inhibits STAT3 Signaling by Covalently Targeting Janus Kinases.Molecules (Basel, Switzerland) · 2018Article
- Cancer Chemoprevention: Classic and Epigenetic Mechanisms Inhibiting Tumorigenesis. What Have We Learned So Far?Frontiers in oncology · 2018Review
- The STAT3 pathway as a therapeutic target in head and neck cancer: Barriers and innovations.Oral oncology · 2016Review
- Hitting the Bull's-Eye in Metastatic Cancers-NSAIDs Elevate ROS in Mitochondria, Inducing Malignant Cell Death.Pharmaceuticals (Basel, Switzerland) · 2015Review
- Cancer chemoprevention: current state of the art.Cancer growth and metastasis · 2014Review
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Authors and funding
9 authors.
Funding
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Abstract
Constitutive activation of the signal transducer and activator of transcription 3 (STAT3) or the nuclear factor-κB (NF-κB) pathway occurs frequently in cancer cells and contributes to oncogenesis. The activation of Janus kinase 2 (JAK2) and IκB kinase (IKK) are key events in STAT3 and NF-κB signaling, respectively. We have identified 2-methoxystypandrone (2-MS) from a traditional Chinese medicinal herb Polygonum cuspidatum as a novel dual inhibitor of JAK2 and IKK. 2-MS inhibits both interleukin-6-induced and constitutively-activated STAT3, as well as tumor necrosis factor-α-induced NF-κB activation. 2-MS specifically inhibits JAK and IKKβ kinase activities but has little effect on activities of other kinases tested. The inhibitory effects of 2-MS on STAT3 and NF-κB signaling can be eliminated by DTT or glutathione and can last for 4 h after a pulse treatment. Furthermore, 2-MS inhibits growth and induces death of tumor cells, particularly those with constitutively-activated STAT3 or NF-κB signaling. We propose that the natural compound 2-MS, as a potent dual inhibitor of STAT3 and NF-κB pathways, is a promising anticancer drug candidate.
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