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FFAR2 encodes a member of the GP40 family of G protein-coupled receptors that are clustered together on chromosome 19. Additionally we are shipping FFAR2 Antibodies (83) and FFAR2 Kits (5) and many more products for this protein.
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the results of mutagenesis studies based on the crystal structure of hFFA1 bound to TAK (show CDK9 Proteins)-875 at 2.3 A resolution to identify important residues for orthosteric agonist 6e inducing FFA2 activation.
Although both agonist and antagonist ligands contain negatively charged carboxylates that interact with two key positively charged arginine residues in transmembrane domains V and VII (show TH Proteins) of FFA2, there are clear differences in how these interactions occur.
FFAR2 signaling occurs by divergent G protein pathways.
GPR3 agonism potentiates insulin secretion in isolated islets.
GPR43 expression is reduced in monocytes upon siRNA-knockdown of XBP1 (show XBP1 Proteins), while A549 cells overexpressing XBP1 (show XBP1 Proteins) displayed elevated GPR43 levels.
FFAR2 is a potential therapeutic target of T1 diabetes, representing a link between immune response and glucose homeostasis.
FFAR2 is expressed in pancreatic beta cells and mediates an inhibition of insulin (show INS Proteins) secretion by coupling to Gi-type G proteins.
[review] In vivo and in vitro studies suggest that short-chain fatty acid receptors (SCFAs) stimulate gut (show GUSB Proteins) hormone secretion; therefore, the SCFA-FFA signal is likely to be important for gut (show GUSB Proteins) physiological functions.
GPR43 modulates NF-kappaB (show NFKB1 Proteins) activity via beta-arrestin 2 (show ARRB2 Proteins).
Propionate-stimulated GPR41 (show FFAR3 Proteins) strongly coupled to ERK1/2 activation, while the coupling of linoleic acid-activated GPR40 and acetate-activated GPR43 was weaker.
A Western diet could aggravate the inflammatory colitis process; the activation of the GPR43 receptor pathway could be used as a new strategy to treat Crohn's Disease patients.
Data (including data from studies in knockout mice) suggest Ffar2 expression in pancreatic beta-cells plays role in gestational glucose homeostasis; this mechanism involves gut microbiome (which contributes to plasma short-chain fatty acid levels).
High fat diet fed GPR43 KO mice develop glucose intolerance due to a defect in insulin (show INS Proteins) secretion, reduced beta-cell mass and expression of differentiation genes. GPR3 (show GPR3 Proteins) agonism potentiates insulin (show INS Proteins) secretion.
GPR-43-deficient mice show a greatly decreased inflammatory reaction to knee injection of monosodium urate crystals in a mouse model of gout.
These findings establish GPR43 as a sensor for excessive dietary energy, thereby controlling body energy utilization while maintaining metabolic homoeostasis.
Data from transgenic mice suggest that Ffar2/Gpr43 and Ffar3/Gpr41 (show FFAR3 Proteins) both act as sensors for short-chain fatty acids in enteroendocrine cells; Ffar2/Gpr43 appears to play this role alone in enteric leukocytes and Ffar3/Gpr41 (show FFAR3 Proteins) alone in enteric neurons.
Short-chain fatty acids activate GPR43 and on intestinal epithelial cells, leading to mitogen-activated protein kinase (show MAPK1 Proteins) signaling and rapid production of chemokines and cytokines. These pathways mediate protective immunity and tissue inflammation in mice.
Data suggest that alpha-gustducin (show GNAT3 Proteins) in colonic mucosa is a key signaling molecule coupling free fatty acid receptors (Gpr43, Gpr119 (show GPR119 Proteins), Gpr120) and possibly bile acid receptor (show NR1H4 Proteins) (TGR5 (show GPBAR1 Proteins)) to secretion of GLP-1 (glucagon-like peptide 1 (show GCG Proteins)).
This gene encodes a member of the GP40 family of G protein-coupled receptors that are clustered together on chromosome 19. The encoded protein is a receptor for short chain free fatty acids and may be involved in the inflammatory response and in regulating lipid plasma levels.
G protein-coupled receptor 43
, G-protein coupled receptor 43
, free fatty acid activated receptor 2
, leukocyte-specific STAT-induced GPCR