Target Information
Target General Infomation | |||||
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Target ID |
T02728
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Former ID |
TTDC00144
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Target Name |
Neurotensin receptor type 1
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Gene Name |
NTSR1
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Synonyms |
High-affinity levocabastine-insensitive neurotensin receptor; NT-R-1; NT-R1; NTR subtype 1; NTR1; NTRH; NTSR1
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Target Type |
Clinical Trial
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Disease | Alcohol use disorders [ICD9: 303; ICD10: F10.2] | ||||
Acute or chronic pain [ICD9: 338,780; ICD10: R52, G89] | |||||
Inflammatory bowel disease [ICD9: 555, 556; ICD10: K50, K51] | |||||
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89] | |||||
Pain [ICD9: 338, 356.0, 356.8,780; ICD10: G64, G90.0, R52, G89] | |||||
Function |
G-protein coupled receptor for the tridecapeptide neurotensin (NTS). Signaling is effected via G proteins that activate a phosphatidylinositol-calcium second messenger system. Signaling leads to the activation of downstream MAP kinases and protects cells against apoptosis.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T02728
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UniProt ID | |||||
Sequence |
MRLNSSAPGTPGTPAADPFQRAQAGLEEALLAPGFGNASGNASERVLAAPSSELDVNTDI
YSKVLVTAVYLALFVVGTVGNTVTAFTLARKKSLQSLQSTVHYHLGSLALSDLLTLLLAM PVELYNFIWVHHPWAFGDAGCRGYYFLRDACTYATALNVASLSVERYLAICHPFKAKTLM SRSRTKKFISAIWLASALLAVPMLFTMGEQNRSADGQHAGGLVCTPTIHTATVKVVIQVN TFMSFIFPMVVISVLNTIIANKLTVMVRQAAEQGQVCTVGGEHSTFSMAIEPGRVQALRH GVRVLRAVVIAFVVCWLPYHVRRLMFCYISDEQWTPFLYDFYHYFYMVTNALFYVSSTIN PILYNLVSANFRHIFLATLACLCPVWRRRRKRPAFSRKADSVSSNHTLSSNATRETLY |
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Drugs and Mode of Action | |||||
Inhibitor | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [531079] | ||
Arg-Arg-Pro-Tyr-Ile-Leu-OH | Drug Info | [529316] | |||
Demotensin 1 | Drug Info | [528326] | |||
Demotensin 2 | Drug Info | [528326] | |||
Demotensin 3 | Drug Info | [528326] | |||
Demotensin 4 | Drug Info | [528326] | |||
H-Arg-Arg-Pro-Tyr-Ile-Aac-OH | Drug Info | [529709] | |||
H-Arg-Arg-Pro-Tyr-Ile-N-Me-Leu-OH | Drug Info | [529709] | |||
H-Arg-Arg-Pro-Tyr-N-Me-Ile-Leu-OH | Drug Info | [529709] | |||
H-Arg-N-Me-Arg-Pro-Tyr-Ile-Leu-OH | Drug Info | [529709] | |||
NEUROTENSIN | Drug Info | [529569] | |||
Neurotensin(8-13) | Drug Info | [530025] | |||
Agonist | ABS-212 | Drug Info | [530926] | ||
CGX-1160 | Drug Info | [536424], [536806] | |||
EISAI-1 | Drug Info | [526673] | |||
JMV449 | Drug Info | [526673] | |||
JMV458 | Drug Info | [526207] | |||
Modulator | HBN-2 | Drug Info | [543760] | ||
NT-69-L | Drug Info | [543760] | |||
Antagonist | Meclinertant | Drug Info | [536827], [536871], [537002] | ||
SR142948A | Drug Info | [534320] | |||
SR48527 | Drug Info | [533717] | |||
[3H]meclinertant | Drug Info | [533717] | |||
Pathways | |||||
KEGG Pathway | Calcium signaling pathway | ||||
Neuroactive ligand-receptor interaction | |||||
Reactome | Peptide ligand-binding receptors | ||||
G alpha (q) signalling events | |||||
WikiPathways | GPCRs, Class A Rhodopsin-like | ||||
Gastrin-CREB signalling pathway via PKC and MAPK | |||||
Peptide GPCRs | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
GPCRs, Other | |||||
References | |||||
Ref 521800 | ClinicalTrials.gov (NCT00290953) Evaluation of the Overall Survival of Meclinertant Versus Placebo After a First Line Chemotherapy With Cisplatin + Etoposide. U.S. National Institutes of Health. | ||||
Ref 538956 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1575). | ||||
Ref 538961 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1582). | ||||
Ref 540761 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5307). | ||||
Ref 526207 | Agonism, inverse agonism, and neutral antagonism at the constitutively active human neurotensin receptor 2. Mol Pharmacol. 2001 Dec;60(6):1392-8. | ||||
Ref 526673 | Differential involvement of intracellular domains of the rat NTS1 neurotensin receptor in coupling to G proteins: a molecular basis for agonist-directed trafficking of receptor stimulus. Mol Pharmacol. 2003 Aug;64(2):421-9. | ||||
Ref 528326 | J Med Chem. 2006 Jul 27;49(15):4767-76.Toward stable N4-modified neurotensins for NTS1-receptor-targeted tumor imaging with 99mTc. | ||||
Ref 529316 | Bioorg Med Chem Lett. 2008 Mar 15;18(6):2013-8. Epub 2008 Feb 2.Peptide backbone modifications on the C-terminal hexapeptide of neurotensin. | ||||
Ref 529569 | J 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. | ||||
Ref 529709 | Bioorg 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 ofneurotensin receptor 1. | ||||
Ref 530025 | J 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. | ||||
Ref 530926 | Identification and functional characterization of a stable, centrally active derivative of the neurotensin (8-13) fragment as a potential first-in-class analgesic. J Med Chem. 2010 Jun 24;53(12):4623-32. | ||||
Ref 531079 | J 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. | ||||
Ref 533717 | [3H]SR 48692, the first nonpeptide neurotensin antagonist radioligand: characterization of binding properties and evidence for distinct agonist and antagonist binding domains on the rat neurotensin receptor. Mol Pharmacol. 1995 May;47(5):1050-6. | ||||
Ref 534320 | Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist. J Pharmacol Exp Ther. 1997 Feb;280(2):802-12. | ||||
Ref 536424 | The 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. | ||||
Ref 536806 | Clinical status of anti-cancer agents derived from marine sources. Anticancer Agents Med Chem. 2008 Aug;8(6):603-17. | ||||
Ref 536827 | High-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. | ||||
Ref 536871 | Stimulation 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. |
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