Glucagon and related peptide receptors are a group of G-protein-coupled receptors that are currently classified into six subtypes; Glucagon, Glucagon-Like Peptide 1 (GLP-1), GLP-2, Secretin, Growth Hormone Releasing Hormone (GHRH) and Gastric Inhibitory Peptide (GIP) based on their pharmacology. This family of class II G-protein-coupled receptors serve multiple biological functions including the regulation of nutrient homeostasis through effects on islet hormone secretion, gastrointestinal motility and cell proliferation.
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Tocris offers the following scientific literature for Glucagon and Related Receptors to showcase our products. We invite you to request* your copy today!
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Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.
Receptor Subtype | Glucagon | GLP-1 | GLP-2 | Secretin | GHRH | GIP |
---|---|---|---|---|---|---|
G protein | Gs | Gs | Gs | Gs / Gq | Gs | Gs |
Receptor Localisation | Pancreas, liver, kidneys | Pancreas, CNS, stomach, heart | CNS, GI tract | Pancreas, GI tract, CNS | Anterior pituitary, placenta, kidney | Pancreas, CNS |
Tissue Functions | Glucoregulation; controls glycogenolysis and gluconeogenesis via regulation of insulin secretion | Glucoregulation; stimulates insulin secretion and suppresses glucagon secretion | Maintains growth and absorptive function of the intestinal mucosal villus epithelium | Regulates pancreatic exocrine and gastric secretions | Regulates pituitary growth hormone synthesis and secretion | Glucoregulation; potentiates insulin secretion |
Selective Products |
L-168,049 (2311) des-His1-[Glu9]- Glucagon (1-29) amide (2216) |
Glucagon-like peptide 1 (7-36) amide (2082) Glucagon-like peptide 1 (1-37) (1851) Exendin-4 (1933) Exendin-3 (9-39) amide (2081) GLP-1 (9-36) amide (3266) |
GLP-2 (human) (2258) GLP-2 (rat) (2259) |
Secretin (human) (1918) Secretin (rat) (1919) |
GRF (ovine) |
GIP (1-39) (2257) GIP (human) (2084) |
Brubaker and Drucker (2002) Structure-function of the glucagon receptor family of G protein-coupled recptors; the glucagon, GIP, GLP-1, and GLP-2 receptors. Receptors Channels 8 179. Mayo et al (2003) International union of pharmacology. XXXV. The glucagon receptor family. Pharmacol.Rev. 55 167. Alexander et al (2008) Guide to receptors and channels (GRAC). Br.J.Pharmacol. 153 S1-209.