The bile acid membrane receptor TGR5 as an emerging target in metabolism and inflammation
Open accessAbstract
Bile acids (BAs) are amphipathic molecules that facilitate the uptake of lipids, and their levels fluctuate in the intestine as well as in the blood circulation depending on food intake. Besides their role in dietary lipid absorption, bile acids function as signaling molecules capable to activate specific receptors. These BA receptors are not only important in the regulation of bile acid synthesis and their metabolism, but also regulate glucose homeostasis, lipid metabolism, and energy expenditure. These processes are important in diabetes and other facets of the metabolic syndrome, which represents a considerable increasing health burden. In addition to the function of the nuclear receptor FXRα in regulating local effects in the organs of the enterohepatic axis, increasing evidence points to a crucial role of the G-protein coupled receptor (GPCR) TGR5 in mediating systemic actions of BAs. Here we discuss the current knowledge on BA receptors, with a strong focus on the cell membrane receptor TGR5, which emerges as a valuable target for intervention in metabolic diseases.
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TGR5 mediates immunosuppressive effects of bile acids on macrophages.
“Initial studies uncovered a key role of TGR5 in mediating immunosuppressive effects of BAs on macrophages.46”
From Novel therapeutic targets for cholestatic and fatty liver disease (2022) · cites this paper as [46]
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- Authors
- Pols, T. W. H., Noriega, L. G., Nomura, M., Auwerx, J., & Schoonjans, K.
- Affiliations
- École Polytechnique Fédérale de Lausanne (CH)
- Corresponding author
- Schoonjans, Kristina
- Venue
- Journal of Hepatology
- Publisher
- Elsevier BV
- Published
- 2011-06
- Volume
- 54
- Issue
- 6
- Pages
- 1263-1272
- ISSN
- 0168-8278 (ISSN-L)
- PMC
- PMC3650458
- OpenAlex
- W2025873966
- Cited by
- 454
- References
- 109
- Citations by year
- 2026: 52 · 2025: 30 · 2024: 28 · 2023: 22 · 2022: 37 · 2021: 25 · 2020: 31 · 2019: 18 · 2018: 35 · 2017: 25 · 2016: 27 · 2015: 25 · 2014: 33 · 2013: 40 · 2012: 14
- FWCI
- 2.36
- Type
- journal article
- Language
- en
- Open access
- hybrid
- doi.org
- Licence
- Locations
- Journal of Hepatology (publishedVersion, cc-by-nc-nd)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- Infoscience (Ecole Polytechnique Fédérale de Lausanne) (submittedVersion)
- Infoscience (Ecole Polytechnique Fédérale de Lausanne) (submittedVersion, cc-by-nc-nd)
- Funders
- Swiss National Science Foundation
- ERC
- NIH
- Nestlé and the Ecole Polytechnique Fédérale de Lausanne
- Topics
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Health Sciences › Medicine › Surgery › Cholesterol and Lipid Metabolism
- Health Sciences › Medicine › Pharmacology › Berberine and alkaloids research
- Keywords
- TGR5, bile acid receptors, G protein-coupled receptors, bile acids, enterohepatic circulation, glucose homeostasis, lipid metabolism, energy expenditure, metabolic syndrome, diabetes mellitus, inflammation, therapeutic target
- MeSH terms
- Animals, Bile Acids and Salts, Glucose, Humans, Immunologic Factors, Inflammation, Insulin Resistance, Liver, Models, Biological, Signal Transduction, Metabolic Syndrome, Receptors, G-Protein-Coupled, Mice
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