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

Summary, in English

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.

• Author: Knut Kotarsky; Niclas Nilsson; Erik Flodgren; Christer Owman; Björn Olde
• Department/s: Mucosal Immunology; Department of Experimental Medical Science; Drug Target Discovery; Immunology
• Publishing year: 2003
• Language: English
• Pages: 406-410
• Publication/Series: Biochemical and Biophysical Research Communications
• Volume: 301
• Issue: 2
• Links: http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12565875&dopt=Abstract; http://dx.doi.org/10.1016/S0006-291X(02)03064-4
• Document type: Journal article
• Publisher: Elsevier
• Topic: Biological Sciences
• Keywords: Reverse pharmacology; Arteriosclerosis; Obesity; Diabetes; Thiazolidinediones; Fatty acid; GPR40; Receptor; Cell surface; Preclinical; Drug evaluation
• Status: Published
• Research group: Mucosal Immunology; Drug Target Discovery; Immunology
• ISBN/ISSN/Other: ISSN: 1090-2104