FFAR1:FFAR1 ligands activate Gq

Stable Identifier
Reaction [transition]
Homo sapiens
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FFAR1 (GPR40) is a G-protein coupled receptor. Based on studies with inhibitors of G proteins such as pertussis toxin FFAR1 is believed to signal through Gq/11. Binding of free fatty acids by FFAR1 activates the heterotrimeric Gq complex, which then activates Phospholipase C. From experiments in knockout mice it is estimated that signaling through FFAR1 is responsible for about 50% of the augmentation of insulin secretion produced by free fatty acids. The rest of the augmentation is due to metabolism of the free fatty acids within the pancreatic beta cell.
Literature References
PubMed ID Title Journal Year
17395749 GPR40 is necessary but not sufficient for fatty acid stimulation of insulin secretion in vivo

Lin, DC, Tremblay, C, Alquier, T, Poitout, V, Oseid, E, Jetton, TL, Latour, MG, Luo, J

Diabetes 2007
17130640 Fatty acid signaling in the beta-cell and insulin secretion

Nolan, CJ, Peyot, ML, Delghingaro-Augusto, V, Prentki, M, Madiraju, MS

Diabetes 2006
15914509 Oleic acid interacts with GPR40 to induce Ca2+ signaling in rat islet beta-cells: mediation by PLC and L-type Ca2+ channel and link to insulin release

Maekawa, F, Fujiwara, K, Yada, T

Am J Physiol Endocrinol Metab 2005
16081037 Role of GPR40 in fatty acid action on the beta cell line INS-1E

Shachar, S, Hershfinkel, M, Shapiro, H, Sekler, I, Walker, MD

Biochem Biophys Res Commun 2005
18827341 Free fatty acid receptors and drug discovery

Hirasawa, A, Katsuma, S, Hara, T, Adachi, T, Tsujimoto, G

Biol Pharm Bull 2008
12496284 The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids

Minnick, DT, Ignar, DM, Muir, AI, Strum, JC, Goetz, AS, Elshourbagy, NA, Tadayyon, M, Briscoe, CP, Sauls HR, Jr, Spinage, LD, Eilert, MM, Szekeres, PG, Benson, WG, Shabon, U, Andrews, JL, Tan, KB, Wilson, S, Murdock, PR, Way, JM, Ellis, C, Chambers, JK

J Biol Chem 2003
18606873 Glycerolipid metabolism and signaling in health and disease

Prentki, M, Madiraju, SR

Endocr Rev 2008
19398560 The action and mode of binding of thiazolidinedione ligands at free fatty acid receptor 1

Devine, NM, Smith, NJ, Milligan, G, Stoddart, LA, Jenkins, L

J Biol Chem 2009
17101212 Free fatty acids increase cytosolic free calcium and stimulate insulin secretion from beta-cells through activation of GPR40

Schöfl, C, Schnell, S, Schaefer, M

Mol Cell Endocrinol 2007
Catalyst Activity

guanyl-nucleotide exchange factor activity of FFAR1:FFAR1 ligands [plasma membrane]

Orthologous Events
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