Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00439

Target Information
NameGlucagon receptor    
Type of targetSuccessful target    
DiseaseHyperglycemia
[ICD9: 790.29   ICD10: R73.9]
[1]
Insulin-dependent diabetes mellitus
[ICD9: 250   ICD10: E08-E13]
[1]
Lipid metabolic disorders
[ICD9: 270-279   ICD10: E70-E89]
[1]
Noninsulin-dependent diabetes mellitus
[ICD9: 250   ICD10: E08-E13]
[1]
Obesity
[ICD9: 278   ICD10: E66]
[1]
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.    
SequenceMPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNR TFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQ CQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANL FASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYC WLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDN MGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGV HEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRL GKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF
Related US Patent6,503,949
6,562,807
6,649,641
Target ValidationClick to Find Target Validation Information.    
InhibitorBI-32169[6]
Des-His1[Glu9]glucagon-NH2[7]
[des-His1,Tyr5,Glu9,D-Ala10]glucagon-NH2[8]
[des-His1,Tyr5,Glu9,D-Phe10]glucagon-NH2[8]
[des-His1,Tyr5,Glu9,D-Tyr10]glucagon-NH2[8]
[des-His1,Tyr5,Glu9]glucagon-NH2[8]
AgonistZP2929[5]
BinderDwLIP-GCGRrx[4]
Glucagon recombinant[2][3]
MultitargetZP2929[5]
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



 

Welcome to sign our Guestbook.

If you find any error in data or bug in web service, please kindly report it to Dr. Zhu.


Dr. Chen Yuzong
Deputy Director of Center for Computational Science and Engineering
Professor in Department of Pharmacy
National University of Singapore, Singapore


All rights reserved.

   
 
 
Computer-aided Drug Design
about BIDD |  databases |  software |  teaching |  research |  links

 

Department of Computational Science | National University of Singapore | Blk S17, 3 Science Drive 2, Singapore 117543