Advanced

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

Kotarsky, Knut LU ; Nilsson, Niclas LU ; Flodgren, Erik LU ; Owman, Christer LU and Olde, Björn LU (2003) In Biochemical and Biophysical Research Communications 301(2). p.406-410
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... (More)
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. (Less)
Please use this url to cite or link to this publication:
author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
Reverse pharmacology, Arteriosclerosis, Obesity, Diabetes, Thiazolidinediones, Fatty acid, GPR40, Receptor, Cell surface, Preclinical, Drug evaluation
in
Biochemical and Biophysical Research Communications
volume
301
issue
2
pages
406 - 410
publisher
Elsevier
external identifiers
  • wos:000181099100023
  • pmid:12565875
  • scopus:0037423719
ISSN
1090-2104
DOI
10.1016/S0006-291X(02)03064-4
language
English
LU publication?
yes
id
9fc1526d-cd60-41e1-980a-a72aba55fa14 (old id 112366)
alternative location
http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12565875&dopt=Abstract
date added to LUP
2007-06-26 10:42:51
date last changed
2018-02-11 04:00:11
@article{9fc1526d-cd60-41e1-980a-a72aba55fa14,
  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.},
  author       = {Kotarsky, Knut and Nilsson, Niclas and Flodgren, Erik and Owman, Christer and Olde, Björn},
  issn         = {1090-2104},
  keyword      = {Reverse pharmacology,Arteriosclerosis,Obesity,Diabetes,Thiazolidinediones,Fatty acid,GPR40,Receptor,Cell surface,Preclinical,Drug evaluation},
  language     = {eng},
  number       = {2},
  pages        = {406--410},
  publisher    = {Elsevier},
  series       = {Biochemical and Biophysical Research Communications},
  title        = {A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs.},
  url          = {http://dx.doi.org/10.1016/S0006-291X(02)03064-4},
  volume       = {301},
  year         = {2003},
}