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Free Fatty Acid GPCR Family Subtypes and Products

What Are Free Fatty Acid Receptors?

Free fatty acid receptors are a family of G protein-coupled receptors (GPCRs) comprised of four different receptor types: FFA1, FFA2, FFA3, and FFA4. While FFA1 and FFA4 receptors are activated by long-chain fatty acids, FFA2 and FFA3 receptors are activated by short-chain fatty acids. Fatty acids play a key role in metabolism and the immune response, and are currently a large research focus for therapeutic and medical applications.

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Free Fatty Acid Receptor Information

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GPR119

GPR120

GPR40

GPR41

GPR43

GPR84

GPR119 is a G protein-coupled receptor for the endogenous lipid signaling agent oleoylethanolamide (OEA). GPR119 is predominantly expressed in the pancreas (beta- cells) and gastrointestinal tract (enteroendocrine cells). In vitro studies have indicated a role for GPR119 in the modulation of insulin release by pancreatic beta-cells and of GLP-1 secretion by gut enteroendocrine cells.

GPR120 is a G protein-coupled receptor for the long-chain free fatty acids. GPR120 mediated calcium mobilization, Erk1/Erk2 activation and GLP1 secretion. Unsaturated long-chain FFAs had a dose-dependent stimulatory effect, and α-linolenic acid was the most potent. GPR120 and GLP1 colocalized in human colonic intraepithelial neuroendocrine cells, and GPR120 may mediate dietary FFA-stimulated GLP1 secretion.

G-protein coupled receptor 40 (GPR40 or FFA1) is specifically expressed in brain and pancreas. In pancreas, abundant GPR40 is localized to insulin-producing beta cells. Long-chain FFAs amplify glucose-stimulated insulin secretion from pancreatic beta cells by activating GPR40, indicating that GPR40 agonists and/or antagonists have potential for the development of new anti-diabetic drugs. GPR40 overexpression in breast cancer cells amplified oleate-induced proliferation, whereas silencing the GPR40 gene decreased it. These results suggest that GPR40 is implicated in the control of breast cancer cell growth by fatty acids and that GPR40 may provide a link between fat and cancer.

GPR41 or free fatty acid receptor 3 (FFAR3) shares 98% amino acid identity with GPR42 and closely related to GPR43. While GPR43 is expressed in immune cells, GPR41 appears to be expressed in blood vessel endothelial cells, particularly in adipose tissue, with significant expression also in immune cells and endothelial cells of other tissues. Although propionate and short chain fatty acids were identified recently as the cognate physiological ligands for GPR41, the functional roles of the receptor is still not clear and awaits the development of specific high affinity agonist and antagonists and the evaluation of knock-out animals.

GPR43, or free fatty acid receptor 2 (FFAR2), encodes a deduced 330-amino acid protein with 7 transmembrane domains. GPR43 is expressed by enteroendocrine L cells containing peptide YY in the human large intestine. The receptor binding of short-chain fatty acids potentially provides a molecular link between diet, gastrointestinal bacterial metabolism, and immune and inflammatory responses.

Human GPR84 is a G protein-coupled receptor with 396 amino acids. The hgpr84 transcript was found in brain, heart, muscle, colon, thymus, spleen, kidney, liver, intestine, placenta, lung and leukocytes. A study in GPR84-deficient mice revealed a novel role for GPR84 in regulating early IL-4 gene expression in activated T cells in response to CD3 crosslinking.

Receptor FamilyReceptorSpeciesParentalStable Cell Lines Division-Arrested Cells Membranes
Free Fatty AcidGPR119humanCHO-K1C1298-1aDC1298-1aMC1298-1a
GPR119humanHEK293TC1298DC1298MC1298
GPR119mouseCHO-K1Cm1298-1DCm1298-1MCm1298-1
GPR120humanHEK293TC1294DC1294MC1294
GPR120humanHEK293T Gαqi5CG1294DCG1294MCG1294
GPR120humanCHO-K1C1294-1DC1294-1MC1294-1
GPR120LhumanHEK293TC1522DC1522MC1522
GPR120LhumanHEK293T β-Arrestin2CA1522DCA1522MCA1522
GPR120mouseHEK293T Gαqi5CGm1294DCGm1294MCGm1294
GPR120ratHEK293TCr1294DCr1294MCr1294
GPR40cynomolgus monkeyCHO-K1Cpc1101-1DCpc1101-1MCpc1101-1
GPR40cynomolgus monkeyCHO-K1CApr1101-1DCApr1101-1MCApr1101-1
GPR40cynomolgus monkeyCHO-K1 β-Arrestin2CApc1101-1DCApc1101-1MCApc1101-1
GPR40dogCHO-K1Cd1101-1DCd1101-1MCd1101-1
GPR40humanHEK293TC1101DC1101MC1101
GPR40humanCHO-K1C1101-1DC1101-1MC1101-1
GPR40humanCHO-K1C1101-1ADC1101-1AMC1101-1A
GPR40humanCHO-K1 β-Arrestin2CA1101-1DCA1101-1MCA1101-1
GPR40mouseHEK293TCm1101DCm1101MCm1101
GPR40ratHEK293TCr1101DCr1101MCr1101
GPR40ratCHO-K1Cr1101-1DCr1101-1MCr1101-1
GPR40rhesus monkeyCHO-K1Cpr1101-1DCpr1101-1MCpr1101-1
GPR40ratCHO-K1 β-Arrestin2CAr1101-1DCAr1101-1MCAr1101-1
GPR41humanHEK293TC1102DC1102MC1102
GPR41humanCHO-K1 Gα16C1102-1DCG1102-1MC1102-1
GPR41humanHEK293T Gαqi5CG1102DCG1102MCG1102
GPR41mouseCHO-K1 Gα16CGm1102-1DCGm1102-1MCGm1102-1
GPR41ratHEK293TCr1102DCr1102MCr1102
GPR43humanHEK293TC1104DC1104MC1104
GPR43humanCHO-K1C1104-1DC1104-1MC1104-1
GPR43humanCHO-K1 Gα16HG1104-1DHG1104-1MHG1104-1
GPR43mouseHEK293TCm1104DCm1104MCm1104
GPR43ratHEK293TCr1104DCr1104MCr1104
GPR43dogCHO-K1Cd1104-1ADCd1104-1AMCd1104-1A
GPR43dogCHO-K1Cd1104-1BDCd1104-1BMCd1104-1B
GPR43cynomolgus monkeyCHO-K1Cpc1104-1ADCpc1104-1AMCpc1104-1A
GPR43cynomolgus monkeyCHO-K1Cpc1104-1BDCpc1104-1BMCpc1104-1B
GPR43rhesus monkeyCHO-K1Cpr1104-1ADCpr1104-1AMCpr1104-1A
GPR43rhesus monkeyCHO-K1Cpr1104-1BDCpr1104-1BMCpr1104-1B
GPR84humanCHO-K1C1137-1DC1137-1MC1137-1
GPR84humanCHO-K1 Gαqi5CG1137-1DCG1137-1MCG1137-1

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