Synthesized peptide derived from the C-terminal region of Human GPR43.
Immunogen Species
Homo sapiens (Human)
Conjugate
Non-conjugated
Isotype
IgG
Purification Method
The antibody was affinity-purified from rabbit antiserum by affinity-chromatography using epitope-specific immunogen.
Concentration
It differs from different batches. Please contact us to confirm it.
Buffer
Liquid in PBS containing 50% glycerol, 0.5% BSA and 0.02% sodium azide.
Tested Applications
IF, ELISA
Storage
Upon receipt, store at -20°C or -80°C. Avoid repeated freeze.
Lead Time
Basically, we can dispatch the products out in 1-3 working days after receiving your orders. Delivery time maybe differs from different purchasing way or location, please kindly consult your local distributors for specific delivery time.
Usage
For Research Use Only. Not for use in diagnostic or therapeutic procedures.
G protein-coupled receptor that is activated by a major product of dietary fiber digestion, the short chain fatty acids (SCFAs), and that plays a role in the regulation of whole-body energy homeostasis and in intestinal immunity. In omnivorous mammals, the short chain fatty acids acetate, propionate and butyrate are produced primarily by the gut microbiome that metabolizes dietary fibers. SCFAs serve as a source of energy but also act as signaling molecules. That G protein-coupled receptor is probably coupled to the pertussis toxin-sensitive, G(i/o)-alpha family of G proteins but also to the Gq family. Its activation results in the formation of inositol 1,4,5-trisphosphate, the mobilization of intracellular calcium, the phosphorylation of the MAPK3/ERK1 and MAPK1/ERK2 kinases and the inhibition of intracellular cAMP accumulation. May play a role in glucose homeostasis by regulating the secretion of GLP-1, in response to short-chain fatty acids accumulating in the intestine. May also regulate the production of LEP/Leptin, a hormone acting on the central nervous system to inhibit food intake. Finally, may also regulate whole-body energy homeostasis through adipogenesis regulating both differentiation and lipid storage of adipocytes. In parallel to its role in energy homeostasis, may also mediate the activation of the inflammatory and immune responses by SCFA in the intestine, regulating the rapid production of chemokines and cytokines. May also play a role in the resolution of the inflammatory response and control chemotaxis in neutrophils. In addition to SCFAs, may also be activated by the extracellular lectin FCN1 in a process leading to activation of monocytes and inducing the secretion of interleukin-8/IL-8 in response to the presence of microbes. Among SCFAs, the fatty acids containing less than 6 carbons, the most potent activators are probably acetate, propionate and butyrate. Exhibits a SCFA-independent constitutive G protein-coupled receptor activity.
Gene References into Functions
Data suggest that the free fatty acid receptor 2 (FFA2/GPR43 receptor) plays an integral role in survival during and after sepsis.PMID:29338778
we show functional similarities but also some important differences between GPR84 and FFA2R in human phagocytes, thus providing some mechanistic insights into GPR84 regulation in blood neutrophils and cells recruited to an aseptic inflammatory site in vivo.PMID:29477577
Compared with the control group, the densitometric quantification and mean density of GPR43 and ChAT proteins, and expression of GPR43 and CHAT genes, were significantly decreased in the patients with mixed refractory constipation.PMID:26921846
FFA2 processes mediated by Gi signaling, whereas, in concert with blockade by the Gq/G11 inhibitor FR900359, the inability of AZ1729 to mimic or regulate propionate-mediated release of GLP-1 from mouse colonic preparations defined this physiological response as an end point transduced via activation of Gq/G11.PMID:27385588
the results of mutagenesis studies based on the crystal structure of hFFA1 bound to TAK-875 at 2.3 A resolution to identify important residues for orthosteric agonist 6e inducing FFA2 activation.PMID:26808470
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 of FFA2, there are clear differences in how these interactions occur.PMID:26518871
FFAR2 signaling occurs by divergent G protein pathways.PMID:26075576
GPR3 agonism potentiates insulin secretion in isolated islets.PMID:26023106
GPR43 expression is reduced in monocytes upon siRNA-knockdown of XBP1, while A549 cells overexpressing XBP1 displayed elevated GPR43 levels.PMID:25633224
FFAR2 is a potential therapeutic target of T1 diabetes, representing a link between immune response and glucose homeostasis.PMID:25298143
FFAR2 is expressed in pancreatic beta cells and mediates an inhibition of insulin secretion by coupling to Gi-type G proteins.PMID:25581519
[review] In vivo and in vitro studies suggest that short-chain fatty acid receptors (SCFAs) stimulate gut hormone secretion; therefore, the SCFA-FFA signal is likely to be important for gut physiological functions.PMID:24458110
GPR43 modulates NF-kappaB activity via beta-arrestin 2.PMID:23985900
Data indicate that a single mutation in human FFA2 of C4.57G resulted in a human FFA2 receptor with ligand selectivity similar to the bovine receptor.PMID:22919070
They report the results of mutagenesis studies on the receptor, and the identification of previous unknown residues that may affect receptor activation as well as residues important for allosteric interactions on FFA2.PMID:21216233
Reduction of GPR43 expression is associated with colon cancers.PMID:20979106
Collaboration among C-reactive protein, M-ficolin, and GPR43 under acidosis curtails interleukin (IL)-8 production, thus preventing immune overactivation during bacterial infection.PMID:21037097
Mutational analysis revealed several important residues located in transmembrane domains 3, 4, 5, 6, and 7 for acetate binding.PMID:20837008
upregulation of FFAR2 expression may contribute to malignant transformation.PMID:19780758
might play pivotal role in differentiation and immune response of monocytes and granulocytesPMID:12393494
FFA2R is expressed on leukocytes and activated by short-chain fatty acids.PMID:12684041
the highly selective expression of GPR43 in leukocytes, particularly polymorphonuclear cells, suggests a role in the recruitment of these cell populations toward sites of bacterial infectionPMID:12711604
Results indicate that the short chain fatty acid receptor, GPR43 is expressed by enteroendocrine L cells containing peptide YY in the human large intestine.PMID:17899402
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Subcellular Location
Cell membrane; Multi-pass membrane protein.
Protein Families
G-protein coupled receptor 1 family
Tissue Specificity
Expressed at relatively high levels in peripheral blood leukocytes and, to lesser extent, in spleen.