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

J Hepatol. 2011 Jun;54(6):1263-72. doi: 10.1016/j.jhep.2010.12.004. Epub 2010 Dec 9.


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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Bile Acids and Salts / metabolism*
  • Glucose / metabolism
  • Humans
  • Immunologic Factors / metabolism
  • Inflammation / metabolism
  • Insulin Resistance
  • Liver / metabolism
  • Metabolic Syndrome / drug therapy
  • Metabolic Syndrome / metabolism
  • Mice
  • Models, Biological
  • Receptors, G-Protein-Coupled / agonists
  • Receptors, G-Protein-Coupled / deficiency
  • Receptors, G-Protein-Coupled / genetics
  • Receptors, G-Protein-Coupled / metabolism*
  • Signal Transduction


  • Bile Acids and Salts
  • GPBAR1 protein, human
  • Gpbar1 protein, mouse
  • Gpbar1 protein, rat
  • Immunologic Factors
  • Receptors, G-Protein-Coupled
  • Glucose