ArticleEBioMedicine2017
Deguelin, an Aurora B Kinase Inhibitor, Exhibits Potent Anti-Tumor Effect in Human Esophageal Squamous Cell Carcinoma.
Article in EBioMedicine, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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The trial behind it
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Who cites it
28 citing papers in PubMed, 48 citations in OpenAlex.
- Deguelin inhibits growth and prolactin synthesis in prolactinomas by targeting the PI3K/AKT/CREB3L1 pathway and ornithine decarboxylase.Acta pharmacologica Sinica · 2026Article
- Deguelin suppresses Nalm6 leukemia cell proliferation through lactate accumulation and ATP depletion.Molecular biology reports · 2025Article
- AURKB affects the proliferation of clear cell renal cell carcinoma by regulating fatty acid metabolism.Discover oncology · 2025Article
- Deguelin's Anticancer Bioactivity: Challenges and Opportunities in Medicinal Chemistry.Frontiers in pharmacology · 2025Review
- Bioinformatics Analysis and Verification of Metabolic Abnormalities in Esophageal Squamous Carcinoma.Combinatorial chemistry & high throughput screening · 2024Article
- Deguelin Restores Paclitaxel Sensitivity in Paclitaxel-Resistant Ovarian Cancer Cells via Inhibition of the EGFR Signaling Pathway.Cancer management and research · 2024Article
- The Aurora Kinase Inhibitor CYC116 Promotes the Maturation of Cardiomyocytes Derived from Human Pluripotent Stem Cells.Molecules and cells · 2022Article
- Discovery of a novel Aurora B inhibitor GSK650394 with potent anticancer and anti-Journal of enzyme inhibition and medicinal chemistry · 2022Article
- Cytokinesis regulators as potential diagnostic and therapeutic biomarkers for human hepatocellular carcinoma.Experimental biology and medicine (Maywood, N.J.) · 2021Review
- Downregulation of long non-coding RNA LOC101928477 correlates with tumor progression by regulating the epithelial-mesenchymal transition in esophageal squamous cell carcinoma.Thoracic cancer · 2021Article
- Review
- Targeting Aurora B kinase with Tanshinone IIA suppresses tumor growth and overcomes radioresistance.Cell death & disease · 2021Article
- An Electrophilic Deguelin Analogue Inhibits STAT3 Signaling in H-Biomedicines · 2020Article
- Xanthohumol targets the ERK1/2‑Fra1 signaling axis to reduce cyclin D1 expression and inhibit non‑small cell lung cancer.Oncology reports · 2020Article
- Tanshinone IIA inhibits oral squamous cell carcinoma via reducing Akt-c-Myc signaling-mediated aerobic glycolysis.Cell death & disease · 2020Article
- Epigenetic Alterations in Oesophageal Cancer: Expression and Role of the Involved Enzymes.International journal of molecular sciences · 2020Review
- Promotion of ubiquitination-dependent survivin destruction contributes to xanthohumol-mediated tumor suppression and overcomes radioresistance in human oral squamous cell carcinoma.Journal of experimental & clinical cancer research : CR · 2020Article
- Deguelin suppresses non-small cell lung cancer by inhibiting EGFR signaling and promoting GSK3β/FBW7-mediated Mcl-1 destabilization.Cell death & disease · 2020Article
- Article
- Inhibition of ERKs/Akt-Mediated c-Fos Expression Is Required for Piperlongumine-Induced Cyclin D1 Downregulation and Tumor Suppression in Colorectal Cancer Cells.OncoTargets and therapy · 2020Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Aurora B kinase has emerged as a key regulator of mitosis and deregulation of Aurora B activity is closely related to the development and progression of human cancers. In the present study, we found that Aurora B is overexpressed in human esophageal squamous cell carcinoma (ESCC), high levels of Aurora B protein were associated with a worse overall survival rate in ESCC patients. Depleting of Aurora B blunted the malignant phenotypes in ESCC cells. Importantly, we demonstrated that a natural compound, deguelin, has a profound anti-tumor effect on ESCC via inhibiting Aurora B activity. Deguelin potently inhibited in vitro Aurora B kinase activity. The in silico docking study further indicated that deguelin was docked into the ATP-binding pocket of Aurora B. Inhibition of Aurora B activity attenuated growth of ESCC cells, resulted in G2/M cell cycle arrest, polyploidy cells formation, and apoptosis induction. Knocking down of Aurora B decreased the sensitivity of ESCC cells to deguelin. The in vivo results showed that deguelin blocked the phosphorylation of histone H3 and inhibited the growth of ESCC tumor xenografts. Overall, we identified deguelin as an effective Aurora B inhibitor, which deserves further studies in other animal models and ESCC treatment.
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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.