Glucagon receptor family

Overview

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].

References

  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
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Species
Receptor
Family
Assays
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Endocrinology/Metabolism
Musculoskeletal
à la carte
Reference agonist:
GHRH
EC50:
2.0 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Endocrinology/Metabolism
à la carte
Reference agonist:
GIP
EC50:
3.4 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Oncology
Hematology
Endocrinology/Metabolism
Ophthalmology
Cardiology
Gastrointestinal
Musculoskeletal
Urology/Reproduction
à la carte
Reference agonist:
GLP1‐(7‐36)amide
EC50:
7.6 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
à la carte
Reference agonist:
GLP2
EC50:
7.4 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Endocrinology/Metabolism
à la carte
Reference agonist:
glucagon
EC50:
6.3 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
à la carte
Reference agonist:
secretin
EC50:
7.6 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
GHRH
EC50:
18 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
GIP
EC50:
30 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
GLP1‐(7‐36)amide
EC50:
3.4 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
GLP2
EC50:
3.2 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
glucagon
EC50:
1.3 nM