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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.
The following table summarizes the properties of the glucagon and related peptide receptors and highlights the products available from Tocris in this subject area.
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.
|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|
Glucagon (1-29) amide (2216)
Glucagon-like peptide 1 (7-36) amide (2082)
Glucagon-like peptide 1 (1-37) (1851)
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)
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.