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Updated: Jan 24, 2026

Using Multi-fluorinated Bile Acids and In Vivo Magnetic Resonance Imaging to Measure Bile Acid Transport
Published on: November 27, 2016
Bile acid signaling in renal water regulation
Suchun Li1, Chunling Li1, Weidong Wang1,2
1Institute of Hypertension, Zhongshan School of Medicine, Sun Yat-Sen University , Guangzhou , China.
Abstract:
Emerging evidence has shown that bile acids play important roles in renal physiology and diseases by activating two major receptors, the nuclear farnesoid X receptor (FXR) and the membrane G protein-coupled bile acid receptor-1 (Gpbar1; also known as TGR5). Both FXR and TGR5 have been identified in human and rodent kidneys, where they are deeply involved in renal water handling. In mice, FXR- or TGR5-related gene deficiency has been associated with reduced aquaporin-2 expression accompanied with impaired urinary concentration ability. In this mini-review, we briefly discuss the current understanding of FXR/TGR5 signaling in the kidneys, with a special focus on the regulation of aquaporin-2 expression by bile acids in the collecting ducts and its potential significance in disease conditions.
Insights
Bile acids regulate kidney water handling by activating FXR and TGR5 receptors, influencing aquaporin-2 expression. This signaling pathway is crucial for urinary concentration and kidney health.
Area of Science:
- Nephrology
- Endocrinology
- Molecular Biology
Background:
- Bile acids are key signaling molecules impacting various physiological processes.
- Two major bile acid receptors, FXR and TGR5, are present in the kidneys.
- These receptors play a role in renal water handling.
Purpose of the Study:
- To review the current understanding of FXR and TGR5 signaling in the kidneys.
- To focus on the regulation of aquaporin-2 expression by bile acids.
- To discuss the potential significance in kidney diseases.
Main Methods:
- Review of existing scientific literature on bile acid signaling in renal physiology and disease.
- Analysis of studies investigating FXR and TGR5 roles in kidney water balance.
- Examination of evidence linking FXR/TGR5 to aquaporin-2 expression.
Main Results:
- FXR and TGR5 are identified in human and rodent kidneys.
- FXR/TGR5 signaling is involved in regulating renal water handling.
- Gene deficiency of FXR or TGR5 in mice impairs urinary concentration due to reduced aquaporin-2.
Conclusions:
- FXR and TGR5 signaling pathways are important in kidney physiology, particularly in regulating water balance.
- Bile acids, through FXR/TGR5, influence aquaporin-2 expression in the collecting ducts.
- Dysregulation of this pathway may contribute to kidney disease conditions.
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