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.

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Targets | Receptor Data

Targets

Glucagon and Related Receptor Target Files

GIP Receptor (GIPR) GIP Receptor Agonists GIP Receptor Antagonists	Glucagon-Like Peptide 2 Receptors (GLP-2R) GLP-2 Receptor Antagonists GLP-2 Receptor Peptides
Glucagon Receptors (GCGR) Glucagon Receptor Agonists Glucagon Receptor Antagonists Glucagon Receptor Modulators	Secretin Receptors (Secretin R) Secretin Receptor Agonists
Glucagon-Like Peptide 1 Receptors (GLP-1R) GLP-1 Receptor Agonists GLP-1 Receptor Antagonists GLP-1 Receptor Modulators

Related Targets

Dipeptidyl Peptidase IV (DPPIV/CD26)
- Dipeptidyl Peptidase IV Inhibitors

Receptor Data

Glucagon and Related Receptor Data

Receptor Subtype	Glucagon	GLP-1	GLP-2	Secretin	GHRH	GIP
G protein	G_s	G_s	G_s	G_s / G_q	G_s	G_s
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)	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.