GCGR Membrane Protein Introduction

Introduction of GCGR

The glucagon receptor (GCGR) is a 62 kDa protein that is activated by glucagon and is a member of the class B G-protein coupled family of receptors, coupled to G alpha i, Gs and to a lesser extent G alpha q. GCGR is encoded by the GCGR gene in humans. It was reported that stimulation of the receptor leads to activation of adenylate cyclase and improved levels of intracellular cAMP.

Basic Information of GCGR
Protein Name	Glucagon receptor
Gene Name	GCGR
Aliases	GGR, GL-R, glucagon receptor
Organism	Homo sapiens (Human)
UniProt ID	P47871
Transmembrane Times	7
Length (aa)	477
Sequence	MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNRTFD KYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQCQMDGE EIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANLFASFVLKAS SVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYCWLLVEGLYLHNL LGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDNMGFWWILRFPVFLAI LINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGVHEVVFAFVTDEHAQGTLR SAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRLGKVLWEERNTSNHRASSSPGH GPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF

Function of GCGR Membrane Protein

Glucagon is a pancreatic peptide hormone that, as a counterregulatory hormone for insulin, stimulates glucose release through the liver and maintains glucose homeostasis. The GCGR is a Class B GPCR that first described as a glucagon binding entity functionally linked to adenylyl cyclase. It has a key role in maintenance of glucose homeostasis and, as such, is considered to be a valuable target for the treatment of diabetes. In the past years, considerable progress has been made in the identification of the molecular determinants of the GCGR that are important for ligand binding and signal transduction, in the development of glucagon analogs and of nonpeptide small molecules acting as receptor antagonists, and in the characterization of the mechanisms related to the regulation of expression of the glucagon receptor gene.

GCGR Membrane Protein Introduction Fig.1 Two classical GCGR-mediated intracellular signal pathways in glucagon-targeted cells.

Application of GCGR Membrane Protein in Literature

Adhikari B., et al. Impacts of pre- and postnatal nutrition on glucagon regulation and hepatic signalling in sheep. J Endocrinol. 2018, 238(1): 1-12. PubMed ID: 29674343

This article reports that Glucagon secretory responses to propionate were not related to the prenatal nutrition history, but negatively affected by the postnatal obesogenic diet. The pancreatic α-cell compared to β-cells may thus be less sensitive towards late gestation malnutrition, whereas hepatic glucagon signaling appears to be a target of prenatal programming.
Yagi T., et al. Glucagon promotes colon cancer cell growth via regulating AMPK and MAPK pathways. Oncotarget. 2018. PubMed ID: 29535833

This article reveals that hyperglucagonemia in type 2 diabetes promotes colon cancer progression via GCGR-mediated regulation of AMPK and MAPK pathways.
Shu S., et al. A novel series of 4-methyl substituted pyrazole derivatives as potent glucagon receptor antagonists: Design, synthesis and evaluation of biological activities. Bioorg Med Chem. 2018, 26(8): 1896-1908. PubMed ID: 29523469

The article reports that Compound 9r forms a broad hydrophobic interaction with the receptor binding pocket, making the possibility of a further investigation into GCGR antagonists reasonable.
Irwin D.M., et al. Diversification of the functions of proglucagon and glucagon receptor genes in fish. Gen Comp Endocrinol. 2018, 261: 148-165. PubMed ID: 29510149

This article shows that early in vertebrate evolution diverse regulatory mechanisms emerged for the control of glucose metabolism by proglucagon-derived peptides and their receptors and that in ray-finned fish they included subfunctionalization and neofunctionalization of these genes.
Li J., et al. Discovery of thiophene-containing biaryl amide derivatives as novel glucagon receptor antagonists. Chem Biol Drug Des. 2018. PubMed ID: 29469980

This article evaluates that they designed and synthesized a series of thiophene-containing biaryl glucagon receptor (GCGR) antagonists. The two compounds 14f and 14h of this series showed good GCGR binding and cAMP functional activity.

GCGR Preparation Options

To obtain the soluble and functional target protein, the versatile Magic™ membrane protein production platform in Creative Biolabs enables many flexible options, from which you can always find a better match for your particular project. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-GCGR antibody development services.

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Reference

Xiao C. Li and Jia L. Zhuo. (2007). Targeting glucagon receptor signalling in treating metabolic syndrome and renal injury in Type 2 diabetes: theory versus promise. ClinicalScience. 113 (4), 183-193.

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