Therapeutic Targets Database
BIDD Pharmainformatics Databases


TTD Target ID: TTDS00439

Target Information
NameGlucagon receptor    
Type of targetSuccessful target    
[ICD9: 790.29   ICD10: R73.9]
Insulin-dependent diabetes mellitus
[ICD9: 250   ICD10: E08-E13]
Lipid metabolic disorders
[ICD9: 270-279   ICD10: E70-E89]
Noninsulin-dependent diabetes mellitus
[ICD9: 250   ICD10: E08-E13]
[ICD9: 278   ICD10: E66]
Drug(s)Glucagon recombinantApprovedHypoglycemia[2][3]
LY2409021Phase IIType 2 diabetes
DwLIP-GCGRrxPhase IDiabetes[4]
ISIS-GCGRrxPhase IType 2 diabetes
ZP2929PreclinicalObesity, Diabetes[5]
BioChemical ClassG-protein coupled receptor (Secretin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP47871
PDB Structure3CZF; 4ERS.    
FunctionThis is a receptor for glucagon which plays a central role in regulating the level of blood glucose by controlling the rate of hepatic glucose production and insulin secretion. The activity of this receptor is mediated by G proteins.    
Related US Patent6,503,949
Target ValidationClick to Find Target Validation Information.    
Glucagon recombinant[2][3]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. To Reference
Ref 2Glucagon receptor expression and glucagon stimulation of ghrelin secretion in rat stomach. Biochem Biophys Res Commun. 2007 Jun 15;357(4):865-70. Epub 2007 Apr 9. To Reference
Ref 3Fully human monoclonal antibodies antagonizing the glucagon receptor improve glucose homeostasis in mice and monkeys. J Pharmacol Exp Ther. 2009 Apr;329(1):102-11. Epub 2009 Jan 7. To Reference
Ref 4ISIS. Product Development Pipeline. 2009. To Reference
Ref 52011 Pipeline of Zealand Pharma. To Reference
Ref 6J Nat Prod. 2004 Sep;67(9):1528-31.BI-32169, a bicyclic 19-peptide with strong glucagon receptor antagonist activity from Streptomyces sp. To Reference
Ref 7Bioorg Med Chem Lett. 2005 Mar 1;15(5):1401-5.Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor. To Reference
Ref 8J Med Chem. 1996 Jun 21;39(13):2449-55.Topographical amino acid substitution in position 10 of glucagon leads to antagonists/partial agonists with greater binding differences. To Reference


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