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FLASH GENE
Symbol GCGR contributors: mct - updated : 11-09-2015
HGNC name glucagon receptor
HGNC id 4192
EXPRESSION
Type restricted
   expressed in (based on citations)
organ(s)
SystemOrgan level 1Organ level 2Organ level 3Organ level 4LevelPubmedSpeciesStageRna symbol
Digestiveintestinelarge intestinecolon highly Homo sapiens
Endocrinepancreas     Homo sapiens
Urinarykidney   lowly
cells
SystemCellPubmedSpeciesStageRna symbol
Endocrineislet cell (alpha,beta...) Homo sapiens
Lymphoid/Immunemacrophage Homo sapiens
cell lineage
cell lines
fluid/secretion
at STAGE
PROTEIN
PHYSICAL PROPERTIES
STRUCTURE
motifs/domains
  • seven transmembrane segments
  • conjugated GlycoP
    HOMOLOGY
    interspecies ortholog to murine Gcgr
    ortholog to rattus Gcgr
    Homologene
    FAMILY
  • secretin family, coupling with Gs alpha protein and activating adenylate cyclase
  • G-protein coupled receptor 2 family
  • superfamily of receptors characterize
  • class B G protein-coupled receptor family
  • CATEGORY receptor membrane G
    SUBCELLULAR LOCALIZATION     plasma membrane
        intracellular
    intracellular,cytoplasm,organelle,membrane
    intracellular,cytoplasm,organelle,endosome
    text
  • integral to plasma membrane
  • basic FUNCTION
  • playing a central role in regulating the level of blood glucose by controlling the rate of hepatic glucose production and insulin secretion
  • playing a role in the generation of precursor metabolites and energy
  • invovled in the regulation of blood pressure
  • is required for control of lipid metabolism during the adaptive metabolic response to fasting
  • activation of GCGR induced CTNNB1 stabilization and activated CTNNB1-mediated transcription
  • GCGR is expressed in the human colon and, once activated by exogenous GCG, mediates an inhibitory effect on large intestine motility through NO neural release
  • GLP1R, GIPR, and GCGR internalize with differential properties
  • CELLULAR PROCESS
    PHYSIOLOGICAL PROCESS
    PATHWAY
    metabolism energetic
    signaling hormonal
  • activity mediated by G proteins which activate adenylyl cyclase and also a phosphatidylinositol-calcium second messenger system
  • GCG, GCGR signaling correlates with STAT3 activation and macrophage polarization
  • a component
    INTERACTION
    DNA
    RNA
    small molecule
    protein
  • activation of GCGR by GCG leads to increased glucose production by the liver
  • LRP5 physically interacted with GCGR
  • GCG plays a pivotal role in glucose homeostasis through its receptor GCGR
  • interactors of GCGR, LDLR and TMED2, significantly enhanced glucagon-stimulated glucose production, while YWHAB inhibited glucose production
  • cell & other
    REGULATION
    ASSOCIATED DISORDERS
    corresponding disease(s) NIDDM11
    Other morbid association(s)
    TypeGene ModificationChromosome rearrangementProtein expressionProtein Function
    constitutional     --over  
    pancreatic beta-cell overexpression of GCGR results in enhanced beta-cell function and mass
    Susceptibility
    Variant & Polymorphism
    Candidate gene
    Marker
    Therapy target
    SystemTypeDisorderPubmed
    diabete  
    sweeteners and secretagogues that increase plasma concentrations of endogenous GCG may provide such an alternative means to promote GCG receptor activity as a treatment for type 2 diabetes and obesity
    ANIMAL & CELL MODELS
  • Glp-1 receptor (Glp-1r) null mice had reduced neural and behavioral responses specifically to sweet compounds compared to wild-type (WT) mice
  • mice genetically deficient in the glucagon receptor (Gcgr) are refractory to the pathophysiological symptoms of insulin deficiency
  • defective glucagon signaling causes pancreatic neuroendocrine tumors (PNETs) in the Gcgr(-/-) mice