Glucagon is a peptide hormone, produced by alpha cells of the pancreas Glucagon generally elevates the concentration of glucose in the blood by promoting gluconeogenesis and glycogenolysis. Its effect is opposite that of insulin, which lowers the glucose.

Glucagon binds to the glucagon receptor, a G protein-coupled receptor, located in the plasma membrane. The conformation change in the receptor activates G proteins, a heterotrimeric protein with α, β, and γ subunits. When the G protein interacts with the receptor, it undergoes a conformational change that results in the replacement of the GDP molecule that was bound to the α subunit with a GTP molecule. This substitution results in the releasing of the α subunit from the β and γ subunits. The alpha subunit specifically activates the next enzyme in the cascade, adenylate cyclase.