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Glucagon GPCR Family Subtypes and Products

What Are Glucagon Receptors?

Glucagon receptors are a family of G protein-coupled receptors (GPCRs) comprised of six receptor subtypes: glucagon, glucagon-like peptide 1 (GLP-1), glucagon-like peptide 2 (GLP-2), gastric inhibitory polypeptide (GIP), growth hormone-releasing hormone (GHRH), and secretin receptors. Glucagon receptors play a major role in the regulation of blood glucose, insulin release, appetite regulation, and other various CNS effects. Glucagon receptor mutations in humans is associated with type II diabetes, hypoglycemia, and islet cell tumors. There are therapeutic applications for glucose receptors in treating diabetes.

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Glucagon Receptor Information

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GHRH

GIP

GLP-1

GLP-2

Glucagon

Secretin

Growth hormone-releasing hormone (GHRH), acting through the GHRH receptor GHRHR, plays a pivotal role in the regulation of GH synthesis and secretion in the pituitary. The isolated cDNA of the GHRHR predicted a 423-amino acid protein that has 7 putative transmembrane domains, characteristic of G protein- coupled receptors. It is a member of the secretin family of G protein-coupled receptors and has 47%, 42%, 35%, and 28% identity with receptors for vasoactive intestinal peptide, secretin, calcitonin and parathyroid hormone, respectively.

GIP (gastric inhibitory polypeptide) is released from the gastrointestinal tract, stimulates insulin secretion from pancreatic beta-cells, and plays a crucial role in the regulation of insulin secretion. Its receptor GIPR is expressed in the pancreas, stomach, small intestine, adipose tissue, adrenal cortex, pituitary, heart, testis, endothelial cells, bone, trachea, spleen, thymus, lung, kidney, thyroid, and several regions in the CNS. GIPR may have therapeutic potential in the treatment of type 2 diabetes and obesity.

Glucagon-like peptide-1 receptor (GLP1R) is a G protein-coupled receptor for the endogenous insulinotropic peptide glucagon-like peptide-1 (GLP-1). GLP1R is expressed in pancreatic cells and the nervous system, and mediate the effects of GLP-1 in regulating glucose homeostasis through multiple mechanisms including direct actions on the endocrine pancreas and indirect activation of central nervous system controlling gastric emptying, satiety, and body weight. In the brain, receptor activation elicits neurotrophic actions through protection against metabolic and oxidative insults. GLP1R is also implicated in plasticity, memory, and learning. Thus, GLP1R is a potential therapeutic target for both cognitive-enhancing and neuroprotective agents and in the treatment of stroke and Parkinsonism.

Glucagon-like peptide 2 receptor belongs to the glucagon-secretin receptor superfamily of GPCRs. The human GLP-2 receptor gene is localized on chromosome 17p13.3. The GLP-2 receptor exhibits ~50% amino acid identity with GLP-1 receptor. GLP-2 receptor binds to Glucagon-like peptide-2 (GLP-2) is a nutrient-responsive hormone and activates adenylate cyclase pathway and to a lesser extent activates MAP kinases. GLP-2 receptors are found in the central nervous system and gastrointestinal tract, with the highest expression levels in jejunum. The principal role of GLP-2 receptors appears to be the maintenance of the growth, nutrient absorption, cell proliferation, apoptosis, mucosal blood flow and suppressing gastric motility and secretion. The regenerative and cytoprotective properties of GLP-2 contribute to its therapeutic potential for the treatment of patients with intestinal disease. Recent studies have suggested that GLP-2 not only modulates intestinal stem cell behavior but may also promote carcinogenesis in models of sporadic colon cancer. Further consideration of the molecular cross-talk and downstream signaling pathways mediating the intestinotropic effects of GLP-2 is important. A detailed delineation of the signaling pathways activated by gut peptide GPCRs, as exemplified by GLP-1and GLP-2, may provide new therapeutic targets for the treatment of human disorders such as diabetes and intestinal disease, respectively.

The human glucagon receptor GCGR mediates the action of the pancreatic peptide hormone glucagon. Glucagon regulates blood glucose via control of hepatic glycogenolysis and gluconeogenesis and via regulation of insulin release from the β cell. Type 2 diabetes is characterized by inappropriate regulation of hepatic glucose production, which is due to an imbalance in the bihormonal relationship between plasma levels of glucagon and insulin. The glucose-lowering effects of glucagon peptide antagonists and anti-glucagon antibodies have demonstrated the potential of glucagon receptor antagonism as a treatment for type 2 diabetes. Glucagon also elicits various effects in extrahepatic tissues, including adipose tissue, kidney, heart, pancreatic β cells, gastrointestinal tract, thyroid and central nervous system.

Human secretin receptor (gene name SCTR) is a G-protein-coupled receptor, a member of the class B GPCR subfamily. Secretin receptor binds to peptide secretin and the pituitary adenylate cyclase activating peptide. It was the first receptor that was cloned in the class B family of GPCRs. Secretin receptor is also regulated by peptide hormones from the glucagon hormone family. The receptor activates two distinct intracellular signaling pathways, i.e. the adenyl cyclase and the phosphatidyl-inositol calcium pathways. Northern blot analysis has shown that the secretin receptor is expressed in pancreas, kidney, small intestine, lung, liver, and in trace levels in the brain, heart and ovary. Secretin-receptor mRNA is abundant in all gastrinomas, enriched in one specific variant. Knockout of secretin receptor was shown to reduce large cholangiocyte hyperplasia. Studies have also demonstrated the potential use of secretin as a therapy for ductopenic liver diseases.

Glucagon Cell Lines

Receptor FamilyReceptorSpeciesParentalStable Cell Lines Division-Arrested Cells Membranes
GlucagonGHRHhumanHEK293TC1291DC1291MC1291
GIPhumanHEK293TC1290DC1290MC1290
GIPhumanHEK293T β-Arrestin2CA1290DCA1290MCA1290
GIPhumanHEK293T β-Arrestin2CA1290BA1DCA1290BA1MCA1290BA1
GIPmouseHEK293TCm1290DCm1290MCm1290
GIPratHEK293TCr1290DCr1290MCr1290
GIPdogHEK293TCd1290DCd1290MCd1290
GIPdogHEK293TCd1290aDCd1290aMCd1290a
GIPrabbitHEK293TCb1290DCb1290MCb1290
GIPpigHEK293TCp1290DCp1290MCp1290
GIPrhesus monkeyHEK293TCpr1290DCpr1290MCpr1290
GIPrhesus monkeyHEK293TCpr1290aDCpr1290aMCpr1290a
GIPferretHEK293TCf1290DCf1290MCf1290
GIPferretHEK293TCf1290aDCf1290aMCf1290a
GLP-1humanHEK293TC1267DC1267MC1267
GLP-1humanCHO-K1C1267-1DC1267-1MC1267-1
GLP-1humanCHO-K1C1267-1aDC1267-1aMC1267-1a
GLP-1humanCHO-K1 β-Arrestin2CA1267-1DCA1267-1MCA1267-1
GLP-1humanHEK293T β-Arrestin2CA1267BA2DCA1267BA2MCA1267BA2
GLP-1cynomolgus monkeyCHO-K1Cpc1267-1DCpc1267-1MCpc1267-1
GLP-1cynomolgus monkeyCHO-K1Cpc1267-1aDCpc1267-1aMCpc1267-1a
GLP-1ratCHO-K1Cr1267-1DCr1267-1MCr1267-1
GLP-1dogCHO-K1Cd1267-1DCd1267-1MCd1267-1
GLP-1dogHEK293TCd1267-1aDCd1267-1aMCd1267-1a
GLP-1mouse CHO-K1Cm1267-1DCm1267-1MCm1267-1
GLP-1mouse CHO-K1Cm1267-1aDCm1267-1aMCm1267-1a
GLP-1pigCHO-K1Cp1267-1DCp1267-1MCp1267-1
GLP-2humanHEK293TC1268DC1268MC1268
GLP-2ratHEK293TCr1268DCr1268MCr1268
GlucagonhumanHEK293TC1266DC1266MC1266
GlucagondogHEK293TCd1266DCd1266MCd1266
GlucagonpigHEK293TCp1266DCp1266MCp1266
GlucagonratHEK293TCr1266DCr1266MCr1266
GlucagonhumanHEK293TC1266ADC1266AMC1266A
GlucagonhumanCHO-K1C1266-1DC1266-1MC1266-1
GlucagonhumanCHO-K1C1266-1aDC1266-1aMC1266-1a
GlucagonhumanCHO-K1 β-Arrestin2CA1266-1DCA1266-1MCA1266-1
Glucagoncynomolgus monkeyCHO-K1Cpc1266-1DCpc1266-1MCpc1266-1
Glucagoncynomolgus monkeyCHO-K1Cpc1266-1aDCpc1266-1aMCpc1266-1a
Glucagoncynomolgus monkeyHEK293TCpc1266DCpc1266MCpc1266
Glucagoncynomolgus monkeyHEK293TCpc1266aDCpc1266aMCpc1266a
SecretinhumanCHO-K1C1228-1DC1228-1MC1228-1

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