Glucagon and Related Receptors

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.

Targets
Literature
Receptor Data

The following table summarizes the properties of the glucagon and related peptide receptors and highlights the products available from Tocris in this subject area.

Literature for Glucagon and Related Receptors

GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
Peptide Hormone Receptors

Peptide Hormone Receptors Product Listing

A collection of over 200 products for peptide hormone receptors, the listing includes research tools for the study of:

  • Anterior Pituitary Regulation
  • Blood Pressure Regulation
  • Feeding and Appetite Regulation
  • Glucose Regulation
  • Peptide Hormone Processing
Peptides Involved in Appetite Modulation

Peptides Involved in Appetite Modulation Scientific Review

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.

Glucagon and Related Receptor Data

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)

References

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.