ArticleCancer management and research2021
Activation of FXR Suppresses Esophageal Squamous Cell Carcinoma Through Antagonizing ERK1/2 Signaling Pathway.
Article in Cancer management and research, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 15 citations in OpenAlex.
- Hepatic protein kinase Cβ antagonizing p38American journal of physiology. Gastrointestinal and liver physiology · 2025Article
- Lipids: Driving Forces in the Underlying Biology of Carcinogenesis.ACS pharmacology & translational science · 2025Review
- The role of the farnesoid X receptor in diabetes and its complications.Molecular and cellular biochemistry · 2025Review
- FXR activation suppresses NF-κB signaling, proliferation and migration in cervical cancer cells.Translational cancer research · 2025Article
- FXR promotes clear cell renal cell carcinoma carcinogenesis via MMP-7-regulated EMT pathway.Scientific reports · 2024Article
- Targeting Farnesoid X Receptor in Tumor and the Tumor Microenvironment: Implication for Therapy.International journal of molecular sciences · 2023Review
- Dietary Inflammatory Nutrients and Esophageal Squamous Cell Carcinoma Risk: A Case-Control Study.Nutrients · 2022Article
- Demystifying the Functional Role of Nuclear Receptors in Esophageal Cancer.International journal of molecular sciences · 2022Review
- Enhancement of Farnesoid X Receptor Inhibits Migration, Adhesion and Angiogenesis through Proteasome Degradation and VEGF Reduction in Bladder Cancers.International journal of molecular sciences · 2022Article
- How cancer cells remodel lipid metabolism: strategies targeting transcription factors.Lipids in health and disease · 2021Review
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
introductionFarnesoid X receptor (FXR), a member of nuclear receptors, functionally regulates bile acid, glucose and lipid homeostasis. It is also worth noting that FXR plays a suppressor role in cancer and inflammation. However, the contribution of FXR to esophageal squamous cell carcinoma (ESCC) remains unknown.
methodsThe role of FXR activation in ESCC progression was evaluated in ESCC cell lines KYSE150 and EC109 in vitro and BALB-C nude mice in vivo. In vitro, FXR synthetic ligand GW4064 was used to detect the effects on ESCC cell proliferation, migration, apoptosis and cell cycles. To assess the effects of GW4064 on ESCC development in vivo, a xenograft tumor model was constructed. And ERK1/2 activity was evaluated by immunoblot analysis.
resultsFXR synthetic ligand GW4064 impaired esophageal squamous cell carcinoma (ESCC) proliferation and migration, induced apoptosis and cell cycle arrest in vitro, accompanied by inhibition of some inflammatory genes and promotion of pro-apoptotic genes. We then found that FXR activation decreased the phosphorylation levels of ERK1/2 induced by tumor necrosis factor-α (TNF-α) in ESCC cells. Consistent with these results, GW4064 suppressed ESCC tumorigenesis in a xenograft model and suppressed the phosphorylation of ERK1/2 in tumors. DISCUSSION: These findings identify that activating FXR may serve as a promising therapy or adjuvant therapeutic tool for controlling ESCC development.
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