Reactome | FFAR1:FFAR1 ligands activate Gq

FFAR1:FFAR1 ligands activate Gq

Stable Identifier

R-HSA-416530

Type

Reaction [transition]

Species

Homo sapiens

Compartment

plasma membrane, cytosol

ReviewStatus

5/5

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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