Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00440

Target Information
NameGlucagon-like peptide 1 receptor    
Type of targetSuccessful target    
SynonymsGLP-1 receptor    
GLP-1-R    
GLP-1R    
DiseaseCentral nervous system diseases
[ICD9: 294.1, 307.23, 314.00, 314.01, 320-322, 323, 331.0, 332, 333.4, 340, 344.1, 344.81, 348.0   ICD10: A83-A86, B94.1, F02.2, F02.3, F90, F95.2, G00-G37, G83.5, G93.0]
[1]
Diabetic neuropathy
[ICD9: 250.6   ICD10: E10.4, E11.4, E13.4]
[1]
Noninsulin-dependent diabetes mellitus
[ICD9: 250   ICD10: E08-E13]
[2][3]
Obesity
[ICD9: 278   ICD10: E66]
[3]
Drug(s)ExenatideApprovedDiabetes mellitus[4]
LiraglutideApprovedType 2 diabetes[5]
PramlintidePhase IV completedType 1 and 2 diabetes, Obesity[6]
Bydureon Dual Chamber PenPhase IIIDiabetes
LiraglutidePhase II completedObesity[6]
GTP-010Phase IIIrritable bowel syndrome and Dyspepsia[7]
PB-1023Phase IIType 2 diabetes
TTP054Phase IIType 2 diabetes
CVX 096Phase IType 2 diabetes
NN9924Phase IType 2 diabetes
TT-401Phase IType 2 diabetes
ZYOG1Phase IDiabetes[8]
ZP2929PreclinicalObesity, Diabetes[9]
BioChemical ClassG-protein coupled receptor (Secretin family)    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP43220
PDB Structure3C59; 3C5T; 3IOL.    
FunctionThis is a receptor for glucagon-like peptide 1. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.    
SequenceMAGAPGPLRLALLLLGMVGRAGPRPQGATVSLWETVQKWREYRRQCQRSLTEDPPPATDL FCNRTFDEYACWPDGEPGSFVNVSCPWYLPWASSVPQGHVYRFCTAEGLWLQKDNSSLPW RDLSECEESKRGERSSPEEQLLFLYIIYTVGYALSFSALVIASAILLGFRHLHCTRNYIH LNLFASFILRALSVFIKDAALKWMYSTAAQQHQWDGLLSYQDSLSCRLVFLLMQYCVAAN YYWLLVEGVYLYTLLAFSVFSEQWIFRLYVSIGWGVPLLFVVPWGIVKYLYEDEGCWTRN SNMNYWLIIRLPILFAIGVNFLIFVRVICIVVSKLKANLMCKTDIKCRLAKSTLTLIPLL GTHEVIFAFVMDEHARGTLRFIKLFTELSFTSFQGLMVAILYCFVNNEVQLEFRKSWERW RLEHLHIQRDSSMKPLKCPTSSLSSGATAGSSMYTATCQASCS
Related US Patent6,469,021
Target ValidationClick to Find Target Validation Information.    
InhibitorGLP-17- (7-36) derivative[10]
GLP-17- (7-36) derivative[10]
GLP-17- (7-36) derivative[10]
GLP-17- (7-36) derivative[10]
GLP-17- (7-36) derivative[10]
GLP-17- (7-36) derivative[10]
GLP-17- (7-36) derivative[10]
Glu20-Lys24][Gly8][GLP-1 (7-37)-NH2[11]
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG-NH2[11]
HAEGTFTSDVSSYLEGQAAKEIFAWLVKGR[12]
NH2-HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR-CONH2[13]
[Gly8, aib22]GLP-1 (7-37)-NH2[11]
[Gly8,Glu22]GLP-1 (7,37)-NH2[11]
[Gly8]GLP-1 (7-37)-NH2[11]
c[Asp22-Lys26][Gly8]GLP-1 (7-37)-NH2[11]
c[Cpa19-Lys26][Gly8]GLP-1 (7-37)-NH2[11]
c[Glu18-Lys22][Gly8]GLP-1 (7-37)-NH2[11]
c[Glu19-Lys23][Gly8]GLP-1 (7-37)-NH2[11]
c[Glu21-Lys25][Gly8]GLP-1 (7-37)-NH2[11]
c[Glu21-Lys26][Gly8]GLP-1 (7-37)-NH2[11]
c[Glu22-Lys26][Gly8]GLP-1 (7-37)-NH2[11]
c[Glu22-Lys26][Gly8]GLP-1 (7-37)-NH2[11]
c[Glu22-Orn26][Gly8]GLP-1 (7-37)-NH2[11]
c[Glu23-Lys27][Gly8]GLP-1 (7-37)-NH2[11]
c[Glu24-Lys28][Gly8]GLP-1 (7-37)-NH2[11]
c[Glu26-Lys30][Gly8]GLP-1 (7-37)-NH2[11]
c[hGlu22-Lys26][Gly8]GLP-1 (7-37)-NH2[11]
AgonistExendin-4[1][3]
GTP-010[7]
Liraglutide[6]
Liraglutide[5]
Pramlintide[6]
ZP2929[9]
ZYOG1[8]
BinderExenatide[4]
MultitargetZP2929[9]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1A novel neurotrophic property of glucagon-like peptide 1: a promoter of nerve growth factor-mediated differentiation in PC12 cells. J Pharmacol Exp Ther. 2002 Mar;300(3):958-66. To Reference
Ref 2Cloning and functional expression of the human islet GLP-1 receptor. Demonstration that exendin-4 is an agonist and exendin-(9-39) an antagonist of the receptor. Diabetes. 1993 Nov;42(11):1678-82. To Reference
Ref 3Exendin-4 reduces fasting and postprandial glucose and decreases energy intake in healthy volunteers. Am J Physiol Endocrinol Metab. 2001 Jul;281(1):E155-61. To Reference
Ref 4Improved glycemic control and reduction of cardiometabolic risk factors in subjects with type 2 diabetes and metabolic syndrome treated with exenatide in a clinical practice setting. Diabetes Technol Ther. 2009 Jun;11(6):353-9. To Reference
Ref 5Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5. To Reference
Ref 6Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. To Reference
Ref 7Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313. To Reference
Ref 82011 Pipeline of Zydus Cadila Group. To Reference
Ref 92011 Pipeline of Zealand Pharma. To Reference
Ref 10Bioorg Med Chem Lett. 2004 Sep 6;14(17):4395-8.Identification of CJC-1131-albumin bioconjugate as a stable and bioactive GLP-1(7-36) analog. To Reference
Ref 11J Med Chem. 2008 May 8;51(9):2758-65. Epub 2008 Apr 15.Design and synthesis of conformationally constrained glucagon-like peptide-1 derivatives with increased plasma stability and prolonged in vivo activity. To Reference
Ref 12Bioorg Med Chem. 2008 Dec 1;16(23):10106-12. Epub 2008 Oct 5.Search for alpha-helical propensity in the receptor-bound conformation of glucagon-like peptide-1. To Reference
Ref 13J Med Chem. 2008 Nov 27;51(22):7303-7.Influence of selective fluorination on the biological activity and proteolytic stability of glucagon-like peptide-1. To Reference



 

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