The bile acid TGR5 membrane receptor: from basic research to clinical application

Duboc, Henri; Taché, Yvette; Hofmann, Alan F.

doi:10.1016/j.dld.2013.10.021

Cited by 473Drug Transport and Resistance MechanismsCholesterol and Lipid MetabolismReceptor Mechanisms and Signaling

The bile acid TGR5 membrane receptor: from basic research to clinical application

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Duboc, Henri, Taché, Yvette, Hofmann, Alan F.·2014·Digestive and Liver Disease

DOI 10.1016/j.dld.2013.10.021PMC PMC5953190

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Abstract

The TGR5 receptor (or GP-BAR1, or M-BAR) was characterized ten years ago as the first identified G-coupled protein receptor specific for bile acids. TGR5 gene expression is widely distributed, including endocrine glands, adipocytes, muscles, immune organs, spinal cord, and the enteric nervous system. The effect of TGR5 activation depends on the tissue where it is expressed and the signalling cascade that it induces. Animal studies suggest that TGR5 activation influences energy production and thereby may be involved in obesity and diabetes. TGR5 activation also influences intestinal motility. This review provides an overview of TGR5-bile acid interactions in health as well as the possible involvement of TGR5 in human disease.

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BAs can interact with TGR5 in the hypothalamic PVN, stimulating the HPA axis by increasing CRH.
“BAs can interact with TGR5, expressed in the hypothalamic PVN, stimulating the HPA axis by increasing CRH (310, 311).”
From Signalling cognition: The gut microbiota and hypothalamic-pituitary-adrenal axis (2023) · cites this paper as [310]

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Authors: Duboc, H., Taché, Y., & Hofmann, A. F.
Affiliations: Inserm (FR)
University of California, Los Angeles (US)
University of California San Diego (US)
ORCID: Duboc, Henri
Taché, Yvette
Venue: Digestive and Liver Disease
Publisher: Elsevier BV
Published: 2014-04
Volume: 46
Issue: 4
Pages: 302-312
ISSN: 1590-8658 (ISSN-L)
DOI: 10.1016/j.dld.2013.10.021
PMC: PMC5953190
OpenAlex: W2052638070
Cited by: 473
References: 95
Citations by year: 2026: 36 · 2025: 35 · 2024: 40 · 2023: 27 · 2022: 38 · 2021: 57 · 2020: 43 · 2019: 39 · 2018: 53 · 2017: 37 · 2016: 35 · 2015: 25 · 2014: 8
FWCI: 3.97
Type: journal article
Language: en
Open access: hybrid
doi.org
Licence: cc-by-nc-nd
www.elsevier.com/tdm/userlicense/1.0/ (tdm)
creativecommons.org/licenses/by-nc-nd/4.0/ (vor)
Locations: Digestive and Liver Disease (publishedVersion, cc-by-nc-nd)
PubMed (publishedVersion)
Europe PMC (PubMed Central) (acceptedVersion)
PubMed Central (acceptedVersion)
eScholarship (California Digital Library) (submittedVersion, cc-by-nc-nd)
Funders: U.S. Department of Veterans Affairs (I01 BX003951)
U.S. Public Health Service (NIHDDK R01 57238)
National Institute of Diabetes and Digestive and Kidney Diseases (DK 41301, R37DK033061, P30DK041301)
Topics: Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
Health Sciences › Medicine › Surgery › Cholesterol and Lipid Metabolism
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
Keywords: TGR5, G protein-coupled receptors, bile acids, receptor signaling, energy metabolism, obesity, diabetes mellitus, intestinal motility, tissue distribution
MeSH terms: Animals, Cardiovascular Diseases, Diabetes Mellitus, Gastrointestinal Neoplasms, Hepatic Encephalopathy, Humans, Obesity, Pancreatitis, Inflammatory Bowel Diseases, Irritable Bowel Syndrome, Receptors, G-Protein-Coupled, Mice

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The bile acid TGR5 membrane receptor: from basic research to clinical application

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