Endocrine functions of bile acids

EMBO J. 2006 Apr 5;25(7):1419-25. doi: 10.1038/sj.emboj.7601049. Epub 2006 Mar 16.


Bile acids (BAs), a group of structurally diverse molecules that are primarily synthesized in the liver from cholesterol, are the chief components of bile. Besides their well-established roles in dietary lipid absorption and cholesterol homeostasis, it has recently emerged that BAs are also signaling molecules, with systemic endocrine functions. BAs activate mitogen-activated protein kinase pathways, are ligands for the G-protein-coupled receptor TGR5, and activate nuclear hormone receptors such as farnesoid X receptor alpha. Through activation of these diverse signaling pathways, BAs can regulate their own enterohepatic circulation, but also triglyceride, cholesterol, energy, and glucose homeostasis. Thus, BA-controlled signaling pathways are promising novel drug targets to treat common metabolic diseases, such as obesity, type II diabetes, hyperlipidemia, and atherosclerosis.

Publication types

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

MeSH terms

  • Animals
  • Bile Acids and Salts / physiology*
  • Cholesterol / metabolism
  • DNA-Binding Proteins / metabolism
  • Endocrine System / physiology*
  • Energy Metabolism
  • Enzyme Activation
  • Glucose / metabolism
  • Homeostasis
  • Humans
  • Ligands
  • Lipid Metabolism
  • Liver / metabolism
  • MAP Kinase Signaling System / physiology
  • Receptors, Cytoplasmic and Nuclear
  • Receptors, G-Protein-Coupled / metabolism
  • Signal Transduction*
  • Transcription Factors / metabolism


  • Bile Acids and Salts
  • DNA-Binding Proteins
  • GPBAR1 protein, human
  • Ligands
  • Receptors, Cytoplasmic and Nuclear
  • Receptors, G-Protein-Coupled
  • Transcription Factors
  • farnesoid X-activated receptor
  • Cholesterol
  • Glucose