Free Fatty Acid Receptors
Cambridge Bioscience, through our collaboration with ChanTest, offers access to GPCR screening and profiling services to the following free fatty acid receptor targets:
GPR119
Validated Assay/Platform: cAMP
Description: GPR119 is expressed in insulin-producing beta cells where it modulates insulin release, thus making it a very attractive therapeutic target for metabolic disorders. GPR119 is activated by oleoylethanolamide (OEA) and by a novel selective small-molecule (PSN632408) which, when administered to high-fat-fed rats, suppresses food intake and reduces body weight gain. Another small molecule full-agonist (AR231453) enhances glucose-dependent insulin release, and improves oral glucose tolerance in wild-type mice, but not in GPR119 knock-out mice.
GPR120
Synonym: GT01, PGR4, GPR129, MGC119984
Validated Assay/Platform: Calcium
Description: GPR120 is a member of the free fatty acid G protein-coupled receptor family that includes GPR40, GPR41 and GPR43, and is activated by unsaturated long chain free fatty acids (Hirasawa et al., 2005). Expression analysis shows that GPR120 is abundantly expressed in intestine. Stimulation of GPR120 by free fatty acids has been shown to promote the secretion of glucagon-like peptide-1 (GLP-1) and activate the ERK cascade (Hirasawa et al., 2005). More recently, Katsuma et al showed that activation of GPR120 by free fatty acids such as linolenic acid inhibits apoptosis of a murine enteroendocrine cell line.
GPR40
Synonym: FFAR1
Validated Assay/Platform: Calcium
Description: GPR40 is a member of the free fatty acid G protein coupled receptor family and is activated by saturated and unsaturated carboxylic acids with carbon chain lengths greater than six. Expression analysis shows that GPR40 is specifically expressed in brain and in insulin-producing beta cells in the pancreas. Activation of GPR40 by long-chain fatty acids has been shown to amplify glucose-stimulated insulin secretion, suggesting that GPR40 may represent an important target for drugs that regulate diabetes. GPR40 has also been shown to be overexpressed in breast cancer cells, where it may regulate cell growth.
GPR41
Synonym: FFAR3
Validated Assay/Platform: Calcium
Description: GPR41 is a member of the free fatty acid G protein coupled receptor family and is activated by saturated and unsaturated carboxylic acids with carbon chain lengths equal to or less than six. Expression analysis shows that GPR41 is expressed in adipose tissue and to a lesser amount, in immune cells and elsewhere. GPR41 has been shown to be activated by short-chain fatty acids such as propionate.
GPR43
Synonym: FFAR2
Validated Assay/Platform: Calcium
Description: GPR43 is a member of the free fatty acid G protein-coupled receptor family and is activated by short-chain fatty acids (SCFAs). Expression analysis shows that GPR43 is expressed selectively in leukocytes and to a lesser extent, in spleen. Upon activation by propionate or acetate, GPR43 has been shown to mobilize intracellular calcium in both recombinant systems as well as in human granulocytes.
Platforms Available
Cambridge Bioscience, through our collaboration with ChanTest, offers access to both FLIPRTETRA® and FlexStation® 3 allowing you to select the right balance of speed, throughput and data quality to suit your needs.
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