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Updated: May 4, 2026

Using Multi-fluorinated Bile Acids and In Vivo Magnetic Resonance Imaging to Measure Bile Acid Transport
Published on: November 27, 2016
The bile acid TGR5 membrane receptor: from basic research to clinical application
Henri Duboc1, Yvette Taché2, Alan F Hofmann3
1Department of Medicine, CURE/Digestive Diseases Center and Center for Neurobiology of Stress, Digestive Diseases Division, University of California at Los Angeles, Los Angeles, CA, USA; Veterans Affairs Greater Los Angeles Healthcare System, David Geffen School of Medicine, University of California Los Angeles, Los Angeles, CA, USA; University Paris Diderot, Sorbonne Paris Cité, AP-HP, Louis Mourier Hospital, Department of Gastroenterology and Hepatology, Paris, France; University Pierre and Marie Curie, ERL INSERM U 1057/UMR 7203, AP-HP, Saint-Antoine Hospital, Paris, France.
The TGR5 receptor, activated by bile acids, plays a role in energy balance and intestinal function. Its widespread expression suggests involvement in metabolic diseases like obesity and diabetes.
Area of Science:
- Endocrinology
- Gastroenterology
- Metabolism
Background:
- TGR5 (GP-BAR1) is a G-protein coupled receptor specifically binding bile acids.
- It is expressed in diverse tissues including endocrine glands, adipose tissue, muscle, immune cells, and the nervous system.
- TGR5 signaling outcomes are tissue-dependent.
Purpose of the Study:
- To review TGR5-bile acid interactions in physiological conditions.
- To explore the role of TGR5 in human diseases, particularly metabolic disorders.
- To summarize current understanding of TGR5's function.
Main Methods:
- Literature review of studies on TGR5 and bile acids.
- Analysis of animal models investigating TGR5 activation.
- Synthesis of data on TGR5 expression and function across different tissues.
Main Results:
- TGR5 activation influences energy expenditure and glucose homeostasis in animal models.
- TGR5 impacts intestinal motility and function.
- Tissue-specific signaling pathways mediate TGR5 effects.
Conclusions:
- TGR5 is a key mediator of bile acid signaling with significant physiological roles.
- Dysregulation of TGR5 may contribute to obesity, diabetes, and other diseases.
- Further research is warranted to elucidate TGR5's therapeutic potential.
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