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Updated: Jun 3, 2026
09:21
Real Time Monitoring of Intracellular Bile Acid Dynamics Using a Genetically Encoded FRET-based Bile Acid Sensor
Published on: January 4, 2016
Deciphering the nuclear bile acid receptor FXR paradigm
Salvatore Modica1, Raffaella M Gadaleta, Antonio Moschetta
1Laboratory of Lipid Metabolism and Cancer, Consorzio Mario Negri Sud, Santa Maria Imbaro, Chieti, Italy.
Nuclear Receptor Signaling
|March 9, 2011
Summary
Farnesoid X receptor (FXR) regulates bile acid and lipid metabolism, impacting liver and gut health. Targeting FXR with new drugs shows promise for treating metabolic diseases.
Area of Science:
- Endocrinology
- Molecular Biology
- Hepatology
Background:
- Farnesoid X receptor (FXR), initially named retinoid X receptor interacting protein 14 (RIP14), was identified by its rat form's binding to farnesol.
- FXR was de-orphanized in 1999 with the identification of primary bile acids as its natural ligands.
- FXR is highly expressed in the liver and intestine, playing a crucial role in entero-hepatic metabolic pathways.
Purpose of the Study:
- To investigate the role of FXR as a master transcriptional regulator in entero-hepatic metabolic pathways.
- To explore the significance of FXR in the gut-liver axis for lipid and glucose homeostasis.
- To evaluate the therapeutic potential of synthetic FXR ligands for metabolic diseases.
Main Methods:
- Review of cellular and animal models studying FXR function.
- Analysis of FXR's role in regulating metabolic pathways.
- Assessment of FXR's involvement in disease pathophysiology.
Main Results:
- FXR is implicated in the pathophysiology of cholestasis, fatty liver disease, cholesterol gallstone disease, intestinal inflammation, and tumors.
- FXR modulation is critical for lipid and glucose homeostasis via gut-liver axis feedbacks.
- FXR's involvement in metabolic syndrome and diabetes is significant.
Conclusions:
- FXR is a key regulator of metabolic pathways with implications for various diseases.
- Synthetic FXR ligands have been developed based on promising preclinical data.
- FXR-targeted therapies are progressing towards clinical application.
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