Property Summary

NCBI Gene PubMed Count 40
PubMed Score 149.48
PubTator Score 236.28

Knowledge Summary

Patent (64,408)

Expression

Protein-protein Interaction (170)

Gene RIF (22)

PMID Text
27111510 2.5 A crystal structure of human GCGR in complex with the antagonist MK-0893, which is found to bind to an allosteric site outside the seven transmembrane helical bundle in a position between TM6 and TM7 extending into the lipid bilayer
26227798 Molecular dynamics and disulfide crosslinking studies suggest that apo-GCGR can adopt both an open and closed conformation associated with extensive contacts between the ECD and 7TM domain. Glucagon binds to GCGR by a conformational selection mechanism.
25695890 glucagon cell adenomatosis with GCGR germline mutations seems to follow an autosomal-recessive trait.
25451942 Using a real-time time-resolved FRET-based internalization assay, we show that GLP-1R, GIPR, and GCGR internalize with differential properties
23863937 crystal structure of the seven transmembrane helical domain of human GCGR at 3.4 A resolution, and a hybrid model of glucagon bound to GCGR to understand the molecular recognition of the receptor for its native ligand
23407487 Letter/Case Report: nonfunctional glucagon cell adenomatosis with no detectable glucagon receptor mutations.
23185367 GRA1 is a potent glucagon receptor antagonist with strong antihyperglycemic efficacy in preclinical models and prominent effects on hepatic gene-expression related to amino acid metabolism
22893257 F22, V23, M27, and D15 of GCGR are the most important residues for glucagon binding.
22438981 in addition to activation of the classic cAMP/protein kinase A (PKA) pathway, activation of GCGR also induced beta-catenin stabilization and activated beta-catenin-mediated transcription
22119466 analysis of glucagon receptor antagonists with reduced molecular weight and lipophilicity
21680267 The P86S mutant GCGR shows abnormal receptor internalization & calcium mobilization, & causes apoptosis. It cases Mahvash disease (hyperglucagonemia, hypoglycemia, pancreatic neuroendocrine tumors).
20647307 substituted cysteine accessibility method and 3D-molecular modeling to study the N-terminal domain; results showed that Asp(63), Arg(116), and Lys(98) are essential for the receptor structure and/or ligand binding
19903011 The [Ca2+] response is induced by glucagon mainly via the coupling of GCGR to the Galphaq/11 and Galphai/o proteins.
19578796 Observational study of gene-disease association and gene-environment interaction. (HuGE Navigator)
19051206 An analysis of some of these sequences shows that TCR from both human diabetics and NOD mice mimic insulin, glucagon, the insulin receptor, and the glucagon receptor.
17374560 Expression of peroxisome proliferator-activated receptor gamma coactivator 1alpha (PGC-1alpha), known to be upregulated in the liver by fasting, was found to abolish the cAMP-dependent downregulation of glucagon receptor mRNA expression in vitro.
12724331 Three distinct epitopes on the extracellular face of the glucagon receptor determine specificity for the glucagon amino terminus
12536714 Observational study of gene-disease association. (HuGE Navigator)
11961492 Gly40Ser mutation in the glucagon receptor gene is not associated with type 2 diabetes in a Brazilian population, but a reduction of insulin secretion was observed in Gly40Ser carriers.
11707539 Observational study of gene-disease association. (HuGE Navigator)
11692154 Observational study of gene-disease association. (HuGE Navigator)
11692154 The Gly40Ser polymorphism of the GCGR gene is associated with higher risk of hypertension and with enhanced proximal tubular sodium reabsorption.

AA Sequence

MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNRTFDKYSCWPD      1 - 70
TPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQCQMDGEEIEVQKEVAKMYSS     71 - 140
FQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANLFASFVLKASSVLVIDGLLRTRYSQKIGDDL    141 - 210
SVSTWLSDGAVAGCRVAAVFMQYGIVANYCWLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVV    211 - 280
PWAVVKCLFENVQCWTSNDNMGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKS    281 - 350
TLTLIPLLGVHEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRL    351 - 420
GKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF                 421 - 477
//

Text Mined References (44)

PMID Year Title
27111510 2016 Extra-helical binding site of a glucagon receptor antagonist.
26227798 2015 Conformational states of the full-length glucagon receptor.
25695890 2015 Glucagon cell hyperplasia and neoplasia with and without glucagon receptor mutations.
25451942 2015 Functional consequences of glucagon-like peptide-1 receptor cross-talk and trafficking.
24749050 2014 Action and therapeutic potential of oxyntomodulin.
24527772 2014 The discovery of N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): a potent and selective glucagon receptor antagonist.
24359917 2014 Insights into the structure of class B GPCRs.
24275569 2014 An enzyme assisted RP-RPLC approach for in-depth analysis of human liver phosphoproteome.
23863937 2013 Structure of the human glucagon class B G-protein-coupled receptor.
23407487 2013 Glucagon cell adenomatosis without glucagon receptor mutation.
23185367 2012 Anti-diabetic efficacy and impact on amino acid metabolism of GRA1, a novel small-molecule glucagon receptor antagonist.
22908259 2012 Molecular basis for negative regulation of the glucagon receptor.
22893257 2012 Identification of key residues for the binding of glucagon to the N-terminal domain of its receptor: an alanine scan and modeling study.
22438981 2012 Modulation of ?-catenin signaling by glucagon receptor activation.
22119466 2012 A novel series of glucagon receptor antagonists with reduced molecular weight and lipophilicity.
21680267 A natural inactivating mutant of human glucagon receptor exhibits multiple abnormalities in processing and signaling.
20647307 2010 Mutational and cysteine scanning analysis of the glucagon receptor N-terminal domain.
19903011 2009 Glucagon receptor mediates calcium signaling by coupling to G alpha q/11 and G alpha i/o in HEK293 cells.
19657311 2009 Homozygous P86S mutation of the human glucagon receptor is associated with hyperglucagonemia, alpha cell hyperplasia, and islet cell tumor.
19578796 2009 Association of genetic variants with chronic kidney disease in individuals with different lipid profiles.
19051206 Autoreactive T-cell receptor (Vbeta/D/Jbeta) sequences in diabetes are homologous to insulin, glucagon, the insulin receptor, and the glucagon receptor.
18240029 2008 Reviews in molecular biology and biotechnology: transmembrane signaling by G protein-coupled receptors.
17374560 2007 Identification of a novel human glucagon receptor promoter: regulation by cAMP and PGC-1alpha.
16221670 2006 Conformational dimorphism of self-peptides and molecular mimicry in a disease-associated HLA-B27 subtype.
15489334 2004 The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).
12724331 2003 Three distinct epitopes on the extracellular face of the glucagon receptor determine specificity for the glucagon amino terminus.
12626323 2003 Glucagon and regulation of glucose metabolism.
12536714 2001 [Gly40Ser mutation of glucagon receptor gene and NIDDM in Han nationality].
12477932 2002 Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.
12036966 2002 Selective inhibition of heterotrimeric Gs signaling. Targeting the receptor-G protein interface using a peptide minigene encoding the Galpha(s) carboxyl terminus.
11961492 2002 Role of the Gly40Ser mutation in the glucagon receptor gene in Brazilian patients with type 2 diabetes mellitus.
11707539 2001 Gly40Ser polymorphism of the glucagon receptor gene is associated with central adiposity in men.
9287038 1997 Role of the glucagon receptor COOH-terminal domain in glucagon-mediated signaling and receptor internalization.
9105899 1997 Tissue-specific and glucose-dependent expression of receptor genes for glucagon and glucagon-like peptide-1 (GLP-1).
8563746 1996 Glucagon receptor gene mutation in essential hypertension.
8382034 1993 The role of histidine-1 in glucagon action.
8144028 1994 The human glucagon receptor encoding gene: structure, cDNA sequence and chromosomal localization.
8020989 1994 Localization of the glucagon receptor gene to human chromosome band 17q25.
7773293 1995 A missense mutation in the glucagon receptor gene is associated with non-insulin-dependent diabetes mellitus.
7589886 1995 A mutation in the glucagon receptor gene (Gly40Ser): heterogeneity in the association with diabetes mellitus.
7507321 1994 Cloning and expression of a human glucagon receptor.
6303843 1983 Partial purification and characterization of the glucagon receptor.
1908089 1991 Glucagon induces disaggregation of polymer-like structures of the alpha subunit of the stimulatory G protein in liver membranes.
165216 1975 Characterization of the glucagon receptor in a pheochromocytoma.