Human GIPR

Figure. Concentration-dependent activation of GIPR by GIP

Reporter cells were transfected with either the expression plasmid for human gastric inhibitory polypeptide receptor (GIPR) or the mock plasmid and treated with various concentrations of GIP. Data points shown are the mean ± SEM of an experiment (n = 3), and the curve is a fit to Hill equation with an EC50 of 3.4 nM.

gastric inhibitory polypeptide receptor
Available assay modes
Agonist, Inverse agonist, Antagonist, PAM, NAM
à la carte, Endocrinology/Metabolism, Human non-orphan GPCRs

Glucagon receptor family

The glucagon family of receptors are activated by the endogenous peptide (27-44 aa) hormones glucagon, glucagon-like peptide 1, glucagon-like peptide 2, glucose-dependent insulinotropic polypeptide (also known as gastric inhibitory polypeptide), GHRH and secretin. One common precursor (GCG) generates glucagon, glucagon-like peptide 1 and glucagon-like peptide 2 peptides [1]. For a recent review on the current understanding of the structures of GLP-1 and GLP-1R, the molecular basis of their interaction, and the associated signaling events see de Graaf et al., 2016 [2].


  1. Irwin DM. Molecular evolution of proglucagon. Regul Pept 2001;98:1-12.
  2. Graaf Cd, Donnelly D, Wootten D, et al. Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March to Therapeutic Successes. Pharmacol Rev 2016;68:954-1013.
Excerpt from IUPHAR/BPS Guide to Pharmacology

Related Receptors

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