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Details for receptor: GLP-1R

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EndoNet ID: ENR00579

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Synonyms

  • GLP-1R
  • glucagon-like peptide-1 receptor
  • GLP-1 receptor
  • GLP-1-R
  • GLP1R
  • glucagon-like peptide 1 receptor

General information

  • The receptor binds specifically GLP-1 and does not bind peptides of related structure and similar function, such as glucagon, gastric inhibitory peptide, vasoactive intestinal peptide, or secretin. [1]
  • GLP-1 is a gut peptide that, together with its receptor, GLP-1R, is expressed in the brain. [2]
  • Glucagon-like peptide-1 receptor is involved in learning and neuroprotection. [2]
  • Multi-pass membrane receptor for glucagon-like peptide 1 which activity is mediated by G proteins activating adenylyl cyclase. [3]
  • Gene expression of the human glucagon-like peptide-1 receptor is regulated by Sp1 and Sp3. [4]

Links to other resources

UniProt P43220
Ensembl ENST00000373256

Subunit information

Glucagon-like peptide 1 receptor

Sequence 
RPQGATVSL WETVQKWRE YRRQCQRSL 
TEDPPPATD LFCNRTFDE YACWPDGEP 
GSFVNVSCP WYLPWASSV PQGHVYRFC 
TAEGLWLQK DNSSLPWRD LSECEESKR 
GERSSPEEQ LLFLYIIYT VGYALSFSA 
LVIASAILL GFRHLHCTR NYIHLNLFA 
SFILRALSV FIKDAALKW MYSTAAQQH 
QWDGLLSYQ DSLSCRLVF LLMQYCVAA 
NYYWLLVEG VYLYTLLAF SVFSEQWIF 
RLYVSIGWG VPLLFVVPW GIVKYLYED 
EGCWTRNSN MNYWLIIRL PILFAIGVN 
FLIFVRVIC IVVSKLKAN LMCKTDIKC 
RLAKSTLTL IPLLGTHEV IFAFVMDEH 
ARGTLRFIK LFTELSFTS FQGLMVAIL 
YCFVNNEVQ LEFRKSWER WRLEHLHIQ 
RDSSMKPLK CPTSSLSSG ATAGSSMYT 
ATCQASCS
UniProt P43220

Binding hormones

  • GLP-1
  • oxyntomodulin
    • Oxyntomodulin is a glucagon-like peptide 1 (GLP-1) receptor agonist. [5]

Anatomical structures with this receptor

  • beta_cell_of_islet_of_Langerhans

    Influences

    • positive insulin
      • GLP-1 as attractive therapeutic approach for treatment of type 2 diabetes. [6]
      • GLP-1 induces glucose-dependent insulin secretion from pancreas and thereby acts to lower plasma glucose concentration without risk of hypoglycemia. [6]

    Induced phenotypes

    • regulation of glucose homeostasis
      • Upon secretion, GLP-1 acts on a small selection of tissues to regulate glucose homeostasis. [7]
      • When administered to type 2 diabetic subjects, GLP-1 normalizes blood glucose levels, increases circulating insulin, and diminishes glucagon secretion. [8]
    • positive regulation of anti-apoptosis
      • The action of GLP-1 on cell proliferation is complemented by its effect on cell survival. Indeed, GLP-1 and its analogs exhibited anti-apoptotic properties in several rodent models. [7]
      • Mice with disruption of the Glp1r gene exhibit enhanced β-cell death and more severe hyperglycaemia following administration of the β-cell toxin, steptozotocin . [9]
    • pancreatc B cell differentiation
      • The biologic actions of GLP-1 in the β-cell include restoration of glucose competence in glucose-resistant β-cells. [10]
      • The biologic actions of GLP-1 in the β-cell include stimulation of β-cell mass expansion. [7]
      • GLP-1 acts as a growth factor for the β-cell both in experimental animal models and cultured β-cells by stimulating proliferation, survival and differentiation. [7]
      • GLP-1 has been initially shown to promote β-cell replication in vitro as well as in vivo in a partial pancreatectomy rat model of type 2 diabetes. [11]
    • inhibition of gastric emptying
    • The GLP-1 receptor is expressed in beta cells of the islet of Langerhans [12]
    • The GLP-1 receptor is strongly expressed on the surface of the β cells facing the endothelium. [13]

  • pancreas

  • pancreatic_islets

  • alpha_cell_of_islet_of_Langerhans

    Influences

    • negative glucagon
      • This is supported by the observation that GLP-1 also inhibits glucagon release from a glucagon-secreting cell line [14]
    • The effects of GLP-1 or exenatide on glucagon levels during stepped hyperglycaemic and hypoglycaemic clamps provided the first information about GLP-1 receptor activation and alpha cell glucose sensing in human subjects. [14]

  • proximal_tubule_of_nephron

    Induced phenotypes

    • reduction of sodium re-absorption
      • GLP-1R is functionally expressed in porcine proximal tubular kidney cells. Addition of GLP-1 to these cells resulted in a reduced sodium re-absorption. [15]

  • hypothalamus

    Induced phenotypes

    • reduction of food intake
      • Such data indicate that hypothalamic GLP-1 receptors is likely to participate in the ability of GLP-1 to reduce food intake. [16]
Reference