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Abstract
Glucagon regulates glucolipid metabolism and body weight through binding to and activating glucagon receptor (GCGR), which is predominantly expressed in liver and pancreas. In the diabetic state, inappropriately increased glucagon secretion leads to elevated hepatic glucose output, while GCGR blockage restores blood glucose homeostasis. Various approaches including GCGR monoclonal antibodies (mAbs), antagonists, antisense oligonucleotides, and gene knockout can block GCGR signaling. It has shown that GCGR mAbs improve hyperglycemia in diabetic mice and humans without severe adverse effects, since they can specifically antagonize the action of glucagon. Therefore, GCGR signaling plays a critical role in the pathophysiology of diabetes and GCGR mAbs represent innovative approaches in the management of diabetes. (Chin J Endocrinol Metab, 2018, 34: 1052-1056) Key words: Glucagon receptor; Antibody, monoclonal; Diabetes mellitus
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