GCGR

Glucagon receptor (GCGR) belong to the family of class B G-protein-coupled receptors (GPCRs) that play a key role in the maintenance of glucose homeostasis in humans. It binds to the natural ligand-glucagon to regulate blood glucose balance in the body and is an important drug target for type 2 diabetes. GCGR is mainly distributed in the liver, followed by the kidney, muscle, fat, brain, intestine, adrenal gland, spleen, ovary, thyroid, islet a and b cells in the pancreas and other tissue cells.

The physiological functions of GPCRs are largely determined by the intracellular effector proteins (G proteins, etc.) activated by GPCRs. G proteins can be divided into Gs, Gi, Go, and Gq. Among them, after Gs and Gi are activated by GPCRs, they activate and inhibit adenylate cyclase, respectively, resulting in opposite biological effects. It was found that GCGR exerts its typical physiological role through Gs signaling and can also bind to other G proteins such as Gi and Gq. Although the G protein-binding pocket formed by GCGR is similar in size when bound to Gs and Gi, its interaction pattern with the two G proteins differs greatly. The area of the interaction interface between GCGR and Gs is twice that of its interaction interface with Gi, which makes the affinity of the receptor to Gs higher than that of Gi, which provides a structural basis for GCGR to conduct signal transduction mainly through Gs.

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Popular Product

Recombinant Human Glucagon receptor(GCGR),partial (Active) (CSB-MP009316HU1)

Validated Data

Purity determined
by SDS-PAGE

Greater than 95% as determined by SDS-PAGE.

The binding activity of antigen-antibody validated by functional ELISA

Immobilized human GCGR at 2 μg/ml can bind Anti-GCGR recombinant antibody (CSB-RA009316A1HU), the EC₅₀ is 3.747-6.666 ng/mL.