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

Dig Liver Dis. 2014 Apr;46(4):302-12. doi: 10.1016/j.dld.2013.10.021. Epub 2014 Jan 9.

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.

Keywords: Bile acids; Diabetes; Inflammation; Motility; TGR5 receptor.

Publication types

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

MeSH terms

  • Animals
  • Cardiovascular Diseases / genetics*
  • Cardiovascular Diseases / metabolism
  • Diabetes Mellitus / genetics*
  • Diabetes Mellitus / metabolism
  • Gastrointestinal Neoplasms / genetics
  • Gastrointestinal Neoplasms / metabolism
  • Hepatic Encephalopathy / genetics
  • Hepatic Encephalopathy / metabolism
  • Humans
  • Inflammatory Bowel Diseases / genetics
  • Inflammatory Bowel Diseases / metabolism
  • Irritable Bowel Syndrome / genetics
  • Irritable Bowel Syndrome / metabolism
  • Mice
  • Obesity / genetics*
  • Obesity / metabolism
  • Pancreatitis / genetics
  • Pancreatitis / metabolism
  • Receptors, G-Protein-Coupled / genetics
  • Receptors, G-Protein-Coupled / metabolism
  • Receptors, G-Protein-Coupled / physiology*

Substances

  • GPBAR1 protein, human
  • Gpbar1 protein, mouse
  • Receptors, G-Protein-Coupled