Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00230

Target Information
NameGastrin-releasing peptide receptor    
Type of targetClinical trial target    
SynonymsBombesin/gastrin-releasing peptide receptor    
GRP-R    
GRP-preferring bombesin receptor    
DiseaseSmall cell lung cancer
[ICD9: 162.9   ICD10: C34.90]
[1]
Drug(s)GSK1292263Phase IIType 2 diabetes[2]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Neuroactive ligand-receptor interaction
UniProt IDP30550
FunctionReceptor for gastrin releasing peptide (grp). This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.    
SequenceMALNDCFLLNLEVDHFMHCNISSHSADLPVNDDWSHPGILYVIPAVYGVIILIGLIGNIT LIKIFCTVKSMRNVPNLFISSLALGDLLLLITCAPVDASRYLADRWLFGRIGCKLIPFIQ LTSVGVSVFTLTALSADRYKAIVRPMDIQASHALMKICLKAAFIWIISMLLAIPEAVFSD LHPFHEESTNQTFISCAPYPHSNELHPKIHSMASFLVFYVIPLSIISVYYYFIAKNLIQS AYNLPVEGNIHVKKQIESRKRLAKTVLVFVGLFAFCWLPNHVIYLYRSYHYSEVDTSMLH FVTSICARLLAFTNSCVNPFALYLLSKSFRKQFNTQLLCCQPGLIIRSHSTGRSTTCMTS LKSTNPSVATFSLINGNICHERYV
Target ValidationClick to Find Target Validation Information.    
Inhibitor (CH3)CCO-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2[3]
(D)Phe-Gln-Trp-Ala-Val-Gly-His-Leu-Leu-NH2[4]
Ac-His-Trp-Ala-Val-Ala-His-Leu-Met-NH2[3]
Ac-His-Trp-Ala-Val-D-Ala-His-Leu-Met-NH2[3]
Ac-His-Trp-Ala-Val-Gly-His-Leu-Met-NH2[3]
JMV 1535[4]
JMV 1693[4]
JMV 1719[4]
JMV 1799[4]
JMV 1801[4]
JMV 1802[4]
JMV 1803[4]
JMV 1813[4]
Universal ligand[5]
[ (N4-Bzdig)0,Nle14]BB[5]
[ (N4-Bzdig)0]BB[5]
[N40,Pro1,Tyr4,Nle 14]BB[5]
[N40,Pro1,Tyr4]BB[5]
[Tyr4]Bombesin[5]
AgonistGSK1292263[2]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Bombesin/gastrin-releasing peptide receptor: a potential target for antibody-mediated therapy of small cell lung cancer. Clin Cancer Res. 2003 Oct 15;9(13):4953-60. To Reference
Ref 2GSK. Product Development Pipeline. February 2009. To Reference
Ref 3J Med Chem. 1991 Jul;34(7):2102-7.Gastrin releasing peptide antagonists with improved potency and stability. To Reference
Ref 4J Med Chem. 2000 Jun 15;43(12):2356-61.Synthesis and biological evaluation of bombesin constrained analogues. To Reference
Ref 5J Med Chem. 2005 Jan 13;48(1):100-10.Potent bombesin-like peptides for GRP-receptor targeting of tumors with 99mTc: a preclinical study. To Reference



 

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