A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs

Biochem Biophys Res Commun. 2003 Feb 7;301(2):406-10. doi: 10.1016/s0006-291x(02)03064-4.


Fatty acids, which are essential nutritional components, are also involved in cardiovascular and metabolic diseases. Here we report a human cell surface receptor that we name free fatty acid receptor (FFAR), because it is specifically activated by medium to long-chain free fatty acids. The receptor belongs to the class of seven-transmembrane, G-protein coupled receptors (GPCRs) and also mediates responses to antidiabetic drugs of the thiazolidinedione type. It is expressed in skeletal muscle, heart, liver, and pancreatic beta-cells. Stimulation of FFAR increases the intracellular calcium concentration in cells expressing the receptor in a native (pancreatic beta-cell line) or in a recombinant form. In view of the nature of the activating substances, their physiological role in the body, and the tissue distribution of FFAR we suggest the term "nutrient sensing receptor" for receptors acting at the interface between dietary components and signalling molecules.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aequorin / genetics
  • Aequorin / metabolism
  • Animals
  • Calcium / metabolism
  • Cell Line
  • Dose-Response Relationship, Drug
  • Fatty Acids, Nonesterified / metabolism*
  • Genes, Reporter
  • Humans
  • Hypoglycemic Agents / metabolism*
  • Islets of Langerhans / cytology
  • Islets of Langerhans / metabolism
  • Mice
  • Palmitic Acids / metabolism
  • Receptors, Cell Surface / metabolism*
  • Rosiglitazone
  • Thiazoles / metabolism*
  • Thiazolidinediones*
  • Time Factors
  • Tissue Distribution


  • Fatty Acids, Nonesterified
  • Hypoglycemic Agents
  • Palmitic Acids
  • Receptors, Cell Surface
  • Thiazoles
  • Thiazolidinediones
  • free fatty acid receptor R10, human
  • Rosiglitazone
  • Aequorin
  • MEDICA 16
  • 2,4-thiazolidinedione
  • Calcium