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Glucagon Receptor
- Molecular classification
- G protein-coupled receptor, Class B GPCR, Secretin receptor family
01
Overview
The glucagon receptor (GCGR) is a class B G-protein coupled receptor primarily activated by the peptide hormone glucagon. It plays a central role in maintaining blood glucose levels during fasting or hypoglycemia by stimulating hepatic glucose production and inhibiting insulin secretion. Dysregulation of GCGR contributes to hyperglucagonemia seen in diabetes mellitus. Recent structural studies have revealed detailed interactions between ECD/ECL/stalk/TMD regions critical for ligand recognition/activation.
02
Mechanism of action
Pharmacological antagonism of GCGR reduces blood glucose.
03
Biological functions
Signal transductionGlucose homeostasisRegulation of hepatic glucose productionRegulation of insulin secretion
04
Disease associations
Diabetes mellitus type 1Diabetes mellitus type 2Hyperglucagonemia
05
Safety considerations
Severe hypoglycemia if unchecked antagonism.
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