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Updated: May 21, 2026
10:51
Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
Published on: November 15, 2013
Farnesoid X Receptor (FXR) from normal to malignant state
Ioannis Koutsounas1, Constantinos Giaginis, Stamatios Theocharis
1Department of Forensic Medicine and Toxicology, Medical School, University of Athens, Athens, Greece.
Histology and Histopathology
|June 1, 2012
Summary
Farnesoid X Receptor (FXR) plays a role in metabolism and disease. Activating or inhibiting FXR shows promise for treating various human cancers, including colon and breast cancer.
Area of Science:
- Endocrinology
- Molecular Biology
- Oncology
Background:
- The Farnesoid X Receptor (FXR) is a nuclear receptor crucial for regulating bile acid, cholesterol, lipid, and glucose metabolism.
- FXR is implicated in metabolic disorders like non-alcoholic fatty liver disease and inflammatory conditions such as inflammatory bowel disease.
- Emerging evidence highlights FXR's involvement in apoptosis and cancer development.
Purpose of the Study:
- To explore the multifaceted roles of FXR in metabolic regulation and disease pathogenesis.
- To investigate the potential of FXR modulation as a therapeutic strategy in various cancers.
- To establish the antitumor effects of FXR in different cancer models.
Main Methods:
- Review of existing literature on FXR's function in metabolism and disease.
- Analysis of studies investigating FXR deficiency and activation in cancer models.
- Examination of FXR's impact on specific cancer types, including colon, breast, and Leydig cell tumors.
Main Results:
- FXR deficiency is linked to increased intestinal inflammation and tumorigenesis.
- FXR deficiency in mice promotes spontaneous hepatocarcinomas.
- FXR agonists down-regulate aromatase in breast cancer cells, and FXR inhibits Leydig tumor growth.
Conclusions:
- FXR plays a significant role in metabolic homeostasis and disease.
- Modulating FXR activity (activation or inhibition) presents potential therapeutic strategies for specific human cancers.
- Further research is warranted to fully elucidate FXR's antitumor effects and clinical applications.
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