Glucagon receptor (GCGR) (GCGR)

The Glucagon receptor (GCGR) is a member of the Class B G protein-coupled receptor family, primarily located on the surface of hepatocytes in the liver (UniProt: P47871). It serves as the primary mediator for the hormone glucagon, which signals the body to increase blood glucose levels through the processes of glycogenolysis and gluconeogenesis. In patients with Type 2 diabetes, glucagon levels are often inappropriately high, leading to excessive hepatic glucose production and fasting hyperglycemia. Therapeutic strategies targeting GCGR, such as the antagonist LY2409021 (iravadadstat), aim to reduce blood sugar by blocking these pathways (PubChem: CID 56951715). However, pharmacological inhibition of GCGR is associated with specific safety concerns, including elevations in liver transaminases and potential increases in LDL cholesterol and blood pressure. The specific mention of LY2409021 in the presence of clarithromycin refers to clinical investigations into drug-drug interactions, as LY2409021 is a substrate for the CYP3A4 enzyme, which clarithromycin inhibits (PMID: 25183540).

Other names

GCGRGL-RGlucagon receptor precursor

Glucagon receptor antagonism