Glucagon receptor

Definition:

G-protein coupled receptor for glucagon that plays a central role in the regulation of blood glucose levels and glucose homeostasis. Regulates the rate of hepatic glucose production by promoting glycogen hydrolysis and gluconeogenesis. Plays an important role in mediating the responses to fasting. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Promotes activation of adenylate cyclase. Besides, plays a role in signaling via a phosphatidylinositol-calcium second messenger system.

References:

[1]. Ali Jazayeri, et al. Extra-helical binding site of a glucagon receptor antagonist. Nature. 2016 May 12;533(7602):274-7. [Content Brief]

[2]. Fai Yiu Siu, et al. Structure of the human glucagon class B G-protein-coupled receptor. Nature. 2013 Jul 25;499(7459):444-9. [Content Brief]

[3]. D J MacNeil, et al. Cloning and expression of a human glucagon receptor. Biochem Biophys Res Commun. 1994 Jan 14;198(1):328-34. [Content Brief]

[4]. Haonan Zhang, et al. Structure of the full-length glucagon class B G-protein-coupled receptor. Nature. 2017 Jun 8;546(7657):259-264. [Content Brief]

[5]. Christopher M Koth, et al. Molecular basis for negative regulation of the glucagon receptor. Proc Natl Acad Sci U S A. 2012 Sep 4;109(36):14393-8. [Content Brief]

[6]. J J Buggy, et al. Role of the glucagon receptor COOH-terminal domain in glucagon-mediated signaling and receptor internalization. Diabetes. 1997 Sep;46(9):1400-5. [Content Brief]

[7]. Cuiqi Zhou, et al. Homozygous P86S mutation of the human glucagon receptor is associated with hyperglucagonemia, alpha cell hyperplasia, and islet cell tumor. Pancreas. 2009 Nov;38(8):941-6. [Content Brief]

[8]. Guangyao Lin, et al. Characterization of a naturally occurring mutation V368M in the human glucagon receptor and its association with metabolic disorders. Biochem J. 2020 Jul 17;477(13):2581-2594. [Content Brief]

[9]. Hong Li, et al. The first pediatric case of glucagon receptor defect due to biallelic mutations in GCGR is identified by newborn screening of elevated arginine. Mol Genet Metab Rep. 2018 Oct 2;17:46-52. [Content Brief]

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