Structure-function of the glucagon receptor family of G protein-coupled receptors: the glucagon, GIP, GLP-1, and GLP-2 receptors

Recept Channels. 2002;8(3-4):179-88.


The glucagon-like peptides include glucagon, GLP-1, and GLP-2, and exert diverse actions on nutrient intake, gastrointestinal motility, islet hormone secretion, cell proliferation and apoptosis, nutrient absorption, and nutrient assimilation. GIP, a related member of the glucagon peptide superfamily, also regulates nutrient disposal via stimulation of insulin secretion. The actions of these peptides are mediated by distinct members of the glucagon receptor superfamily of G protein-coupled receptors. These receptors exhibit unique patterns of tissue-specific expression, exhibit considerable amino acid sequence identity, and share similar structural and functional properties with respect to ligand binding and signal transduction. This article provides an overview of the biology of these receptors with an emphasis on understanding the unique actions of glucagon-related peptides through studies of the biology of their cognate receptors.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Alternative Splicing
  • Animals
  • Cloning, Molecular
  • Gastric Inhibitory Polypeptide / metabolism
  • Genetic Diseases, Inborn
  • Glucagon / metabolism
  • Glucagon-Like Peptide 1
  • Glucagon-Like Peptide 2
  • Glucagon-Like Peptide-1 Receptor
  • Humans
  • Peptide Fragments / metabolism
  • Peptides / metabolism
  • Protein Precursors / metabolism
  • Receptors, Gastrointestinal Hormone / genetics*
  • Receptors, Gastrointestinal Hormone / metabolism
  • Receptors, Glucagon / genetics*
  • Receptors, Glucagon / metabolism
  • Structure-Activity Relationship


  • GLP1R protein, human
  • Glucagon-Like Peptide 2
  • Glucagon-Like Peptide-1 Receptor
  • Peptide Fragments
  • Peptides
  • Protein Precursors
  • Receptors, Gastrointestinal Hormone
  • Receptors, Glucagon
  • Gastric Inhibitory Polypeptide
  • Glucagon-Like Peptide 1
  • Glucagon
  • gastric inhibitory polypeptide receptor