Related Experiment Video
Updated: Aug 19, 2025

Cell Type-specific Gene Expression Profiling in the Mouse Liver
Published on: September 17, 2019
The Farnesoid X Receptor as a Master Regulator of Hepatotoxicity
Magdalena Rausch1, Sophia L Samodelov1, Michele Visentin1
1Department of Clinical Pharmacology and Toxicology, University Hospital Zurich, University of Zurich, 8006 Zurich, Switzerland.
Abstract:
The nuclear receptor farnesoid X receptor (FXR, NR1H4) is a bile acid (BA) sensor that links the enterohepatic circuit that regulates BA metabolism and elimination to systemic lipid homeostasis. Furthermore, FXR represents a real guardian of the hepatic function, preserving, in a multifactorial fashion, the integrity and function of hepatocytes from chronic and acute insults. This review summarizes how FXR modulates the expression of pathway-specific as well as polyspecific transporters and enzymes, thereby acting at the interface of BA, lipid and drug metabolism, and influencing the onset and progression of hepatotoxicity of varying etiopathogeneses. Furthermore, this review article provides an overview of the advances and the clinical development of FXR agonists in the treatment of liver diseases.
Insights
The farnesoid X receptor (FXR) regulates bile acid and lipid metabolism, protecting liver cells from damage. FXR agonists are being developed for treating liver diseases.
Area of Science:
- Hepatology
- Endocrinology
- Pharmacology
Background:
- The nuclear receptor farnesoid X receptor (FXR) is a key regulator of bile acid metabolism and systemic lipid homeostasis.
- FXR plays a crucial role in maintaining hepatic function and protecting hepatocytes from injury.
- FXR acts at the intersection of bile acid, lipid, and drug metabolism.
Purpose of the Study:
- To review the mechanisms by which FXR modulates the expression of transporters and enzymes involved in metabolism.
- To summarize FXR's influence on the pathogenesis of hepatotoxicity.
- To provide an overview of the clinical development of FXR agonists for liver diseases.
Main Methods:
- Literature review of studies on FXR function and clinical trials.
- Analysis of FXR's role in regulating metabolic pathways.
- Synthesis of current knowledge on FXR agonists in liver disease treatment.
Main Results:
- FXR modulates specific and polyspecific transporters and enzymes.
- FXR influences the onset and progression of hepatotoxicity.
- FXR agonists show promise in treating various liver diseases.
Conclusions:
- FXR is a critical regulator of metabolic homeostasis and liver protection.
- Targeting FXR with agonists represents a promising therapeutic strategy for liver diseases.
- Further clinical development of FXR agonists is warranted.
More Related Videos
Related Concept Videos
Transducer Mechanism: Nuclear Receptors
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
Master Transcription Regulators
Liver Regeneration
Cells of Liver
The liver comprises four major types of cells— hepatocytes, stellate, Kupffer, and sinusoidal endothelial cells. The hepatocytes are...
Hepatic Drug Excretion: Influencing Factors
Regulation of the Unfolded Protein Response
Liver Physiology
Metabolic Regulation:
The liver is the central organ involved in regulating blood composition. It stabilizes blood glucose levels, maintaining them within the range of 70–110 mg/dL. When these levels drop, the liver breaks down glycogen reserves and releases glucose into the bloodstream. It can...

