Therapeutic Targets Database
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TTD Target ID: TTDC00144

Target Information
NameNeurotensin receptor type 1    
Type of targetClinical trial target    
SynonymsHigh-affinity levocabastine-insensitive neurotensin receptor    
NT-R-1    
NT-R1    
NTR subtype 1    
NTR1    
NTRH    
DiseaseAnalgesics
[ICD9: 338   ICD10: R52]
[1][2]
Colorectal Cancer
[ICD9: 153, 154   ICD10: C18-C21]
[3][4][5]
Depression
[ICD9: 311   ICD10: F32]
[3][4][5]
Lung Cancer
[ICD9: 162   ICD10: C33-C34]
[3][4][5]
NTR-positive tumors
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[6]
Pain, Acute or Chronic
[ICD9: 338,780   ICD10: R52, G89]
[1][2]
Pancreatic cancer
[ICD9: 157   ICD10: C25]
[6]
Prostate cancer
[ICD9: 185   ICD10: C61]
[3][4][5]
Psychosis
[ICD9: 290-299   ICD10: F20-F29]
[3][4][5]
Schizophrenia and Schizoaffective Disorders
[ICD9: 295, 295.70   ICD10: F20, F25]
[3][4][5]
Drug(s)CGX-1160Phase I completedAcute or Chronic Pain[1][2]
MeclinertantDiscontinued in Phase IIIColorectal Cancer, Prostate Cancer, Schizophrenia, Schizoaffective Disorders, Psychosis, Depression, Lung Cancer[3][4][5]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayCalcium signaling pathway
Neuroactive ligand-receptor interaction
UniProt IDP30989
PDB Structure2LYW.    
FunctionReceptor for the tridecapeptide neurotensin. It is associated with G proteins that activate a phosphatidylinositol- calcium second messenger system.    
SequenceMRLNSSAPGTPGTPAADPFQRAQAGLEEALLAPGFGNASGNASERVLAAPSSELDVNTDI YSKVLVTAVYLALFVVGTVGNTVTAFTLARKKSLQSLQSTVHYHLGSLALSDLLTLLLAM PVELYNFIWVHHPWAFGDAGCRGYYFLRDACTYATALNVASLSVERYLAICHPFKAKTLM SRSRTKKFISAIWLASALLAVPMLFTMGEQNRSADGQHAGGLVCTPTIHTATVKVVIQVN TFMSFIFPMVVISVLNTIIANKLTVMVRQAAEQGQVCTVGGEHSTFSMAIEPGRVQALRH GVRVLRAVVIAFVVCWLPYHVRRLMFCYISDEQWTPFLYDFYHYFYMVTNALFYVSSTIN PILYNLVSANFRHIFLATLACLCPVWRRRRKRPAFSRKADSVSSNHTLSSNATRETLY
Target ValidationClick to Find Target Validation Information.    
Inhibitor4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one[7]
Arg-Arg-Pro-Tyr-Ile-Leu-OH[8]
Demotensin 1[9]
Demotensin 2[9]
Demotensin 3[9]
Demotensin 4[9]
H-Arg-Arg-Pro-Tyr-Ile-Aac-OH[10]
H-Arg-Arg-Pro-Tyr-Ile-N-Me-Leu-OH[10]
H-Arg-Arg-Pro-Tyr-N-Me-Ile-Leu-OH[10]
H-Arg-N-Me-Arg-Pro-Tyr-Ile-Leu-OH[10]
NEUROTENSIN[11]
Neurotensin (8-13)[12]
SR-48692[12]
AgonistCGX-1160[1][2]
AntagonistMeclinertant[3][4][5]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Clinical status of anti-cancer agents derived from marine sources. Anticancer Agents Med Chem. 2008 Aug;8(6):603-17. To Reference
Ref 2The pharmacokinetics of the conopeptide contulakin-G (CGX-1160) after intrathecal administration: an analysis of data from studies in beagles. Anesth Analg. 2007 Jun;104(6):1514-20, table of contents. To Reference
Ref 3Neurotensin inversely modulates maternal aggression. Neuroscience. 2009 Feb 18;158(4):1215-23. Epub 2008 Dec 7. To Reference
Ref 4Stimulation by neurotensin of dopamine and 5-hydroxytryptamine (5-HT) release from rat prefrontal cortex: possible role of NTR1 receptors in neuropsychiatric disorders. Neurochem Int. 2008 Dec;53(6-8):355-61. Epub 2008 Sep 12. To Reference
Ref 5High-affinity neurotensin receptor is involved in phosphoinositide turnover increase by inhibition of sodium pump in neonatal rat brain. Neurochem Res. 2008 Nov;33(11):2206-13. Epub 2008 Aug 29. To Reference
Ref 6Novel bioactive and stable neurotensin peptide analogues capable of delivering radiopharmaceuticals and molecular beacons to tumors. J Med Chem. 2003 Jul 17;46(15):3403-11. To Reference
Ref 7J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. To Reference
Ref 8Bioorg Med Chem Lett. 2008 Mar 15;18(6):2013-8. Epub 2008 Feb 2.Peptide backbone modifications on the C-terminal hexapeptide of neurotensin. To Reference
Ref 9J Med Chem. 2006 Jul 27;49(15):4767-76.Toward stable N4-modified neurotensins for NTS1-receptor-targeted tumor imaging with 99mTc. To Reference
Ref 10Bioorg Med Chem. 2008 Oct 15;16(20):9359-68. Epub 2008 Aug 27.Novel insights into GPCR-peptide interactions: mutations in extracellular loop 1, ligand backbone methylations and molecular modeling of neurotensin receptor 1. To Reference
Ref 11J Med Chem. 2008 Jul 24;51(14):4150-69. Epub 2008 Jun 28.Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity. To Reference
Ref 12J Med Chem. 2009 Apr 9;52(7):1803-13.Comparison of N-terminal modifications on neurotensin(8-13) analogues correlates peptide stability but not binding affinity with in vivo efficacy. To Reference



 

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Professor in Department of Pharmacy
National University of Singapore, Singapore


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