Cited by 454Drug Transport and Resistance MechanismsCholesterol and Lipid MetabolismBerberine and alkaloids research

The bile acid membrane receptor TGR5 as an emerging target in metabolism and inflammation

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Pols, Thijs W.H., Noriega, Lilia G., Nomura, Mitsunori, Auwerx, Johan, Schoonjans, Kristina·2011·Journal of Hepatology

Abstract

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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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)
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
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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