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

Knut Kotarsky, Niclas Nilsson, Erik Flodgren, Christer Owman, Björn Olde

Research output: Contribution to journalArticlepeer-review

298 Citations (SciVal)

Abstract

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 β-cells. Stimulation of FFAR increases the intracellular calcium concentration in cells expressing the receptor in a native (pancreatic β-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.
Original languageEnglish
Pages (from-to)406-410
JournalBiochemical and Biophysical Research Communications
Volume301
Issue number2
DOIs
Publication statusPublished - 2003

Bibliographical note

The information about affiliations in this record was updated in December 2015.
The record was previously connected to the following departments: Molecular Neurobiology (0131000140), Department of Experimental Medical Science (013210000), Mucosal Immunology (013212072), Immunology (013212020), Drug Target Discovery (013212045)

Subject classification (UKÄ)

  • Biological Sciences

Keywords

  • Reverse pharmacology
  • Arteriosclerosis
  • Obesity
  • Diabetes
  • Thiazolidinediones
  • Fatty acid
  • GPR40
  • Receptor
  • Cell surface
  • Preclinical
  • Drug evaluation

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