ArticlePharmaceuticals (Basel, Switzerland)2024
EZH2 Inhibition to Counteract Oral Cancer Progression through Wnt/β-Catenin Pathway Modulation.
Article in Pharmaceuticals (Basel, Switzerland), 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed.
- Article
- SOX-2 and EZH-2 Expression in Primary Epithelial Malignant Salivary Gland Tumors.Medical sciences (Basel, Switzerland) · 2026Article
- Modulation of Wnt/β-Catenin Pathway by Aesculus hippocastanum Extract Enhances Temozolomide Sensitivity in Glioblastoma Cells.Journal of cellular and molecular medicine · 2026Article
- Aesculus hippocastanum Extract Exerts Neuroprotective Effects in an MPPJournal of cellular and molecular medicine · 2026Article
- Tempol Ameliorates Psoriatic Skin Inflammation: Evidence of TLR4/NF-κB/Nrf2 Axis Modulation.Mediators of inflammation · 2026Article
- Post-translational modifications in the oral microenvironment: Stem cell regulation from periodontal regeneration to oral cancer therapy.World journal of stem cells · 2025Review
- Molecular and Genetic Pathogenesis of Oral Cancer: A Basis for Customized Diagnosis and Treatment.Biology · 2025Review
- GSK343, an inhibitor of EZH2, prevents acquired cisplatin resistance in bladder cancer.Molecular genetics and genomics : MGG · 2025Article
- PI3K/mTOR Signaling Pathway Dual Inhibition for the Management of Neuroinflammation: Novel Insights from In Vitro Models.Biomolecules · 2025Article
- Anti-inflammatory effects of water-dispersible hesperetin on endotoxin-induced uveitis in rats involving the nuclear factor κB and Wnt/β-catenin signaling pathways.The Journal of veterinary medical science · 2025Article
- Understanding the tumor microenvironment for personalized immunotherapy in early-onset head and neck squamous cell carcinoma.Frontiers in immunology · 2024Review
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Authors and funding
13 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Oral squamous cell carcinoma (OSCC) is one of the most common human malignancies worldwide. The molecular mechanisms of OSCC pathogenesis are still unknown; however, in recent years, several reports have focused on the role of enhancer of zeste homolog 2 (EZH2) in OSCC. Therefore, in this study we aimed to investigate the effects of GSK343, a selective EZH2 inhibitor, and its impact on the signaling pathways in OSCC, using an in vitro and in vivo orthotopic model. In the in vitro model, GSK343 (1, 10, and 25 μM) significantly decreased OSCC cell viability and cell migration through EZH2 inhibition, modulating NF-κB/IκBα pathway activation and eNOS, VEGF, and TGFβ expression, important markers of angiogenesis. In the in vivo model, GSK343 (5 mg/kg and 10 mg/kg) restored tongue tissue architecture and reduced tumor progression through EZH2 inhibition and Wnt/β-catenin signaling pathway modulation. Moreover, GSK343 reduced the expression of inflammatory mediators; eNOS and TGFβ, markers of angiogenesis; and CD31 and CD34, markers of micro vessel density, respectively. In conclusion, our data demonstrate that GSK343 counteracts oral cancer progression through EZH2/Wnt/β-catenin pathway modulation, suggesting that it could be a promising therapeutic approach for OSCC management.
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Registered trials
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 Socratic graph.