Neurotensin receptor 1

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NTSR1
Available structures
PDB Ortholog search: PDBe RCSB
Identifiers
Aliases NTSR1, NTR, Neurotensin receptor 1, neurotensin receptor 1 (high affinity)
External IDs MGI: 97386 HomoloGene: 68261 GeneCards: NTSR1
Targeted by Drug
meclinertant, SR142948A[1]
RNA expression pattern
PBB GE NTSR1 207360 s at tn.png
More reference expression data
Orthologs
Species Human Mouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

NM_002531

NM_018766

RefSeq (protein)

NP_002522.2

NP_061236.1

Location (UCSC) Chr 20: 62.71 – 62.76 Mb Chr 2: 180.5 – 180.54 Mb
PubMed search [2] [3]
Wikidata
View/Edit Human View/Edit Mouse

Neurotensin receptor type 1 is a protein that in humans is encoded by the NTSR1 gene.[4][5] For a crystal structure of NTS1, see pdb code 4GRV.

Function[edit]

Neurotensin receptor 1 belongs to the large superfamily of G-protein coupled receptors. NTSR1 mediates the multiple functions of testing as many as neurotensin, such as low blood pressure, high blood sugar, low body temperature, antinociception, and regulation of intestinal motility and secretion.[5]

Ligands[edit]

  • ML314 – β-arrestin biased agonist[6]

See also[edit]

References[edit]

  1. ^ "Drugs that physically interact with Neurotensin receptor type 1 view/edit references on wikidata". 
  2. ^ "Human PubMed Reference:". 
  3. ^ "Mouse PubMed Reference:". 
  4. ^ Laurent P, Clerc P, Mattei MG, Forgez P, Dumont X, Ferrara P, Caput D, Rostene W (May 1994). "Chromosomal localization of mouse and human neurotensin receptor genes". Mammalian Genome. 5 (5): 303–6. doi:10.1007/BF00389545. PMID 8075503. 
  5. ^ a b "Entrez Gene: NTSR1 neurotensin receptor 1 (high affinity)". 
  6. ^ Peddibhotla S, Hedrick MP, Hershberger P, et al. (2013). "Discovery of ML314, a Brain Penetrant Non-Peptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor". ACS Med Chem Lett. 4 (9): 846–851. doi:10.1021/ml400176n. PMC 3940307Freely accessible. PMID 24611085. 

Further reading[edit]

  • Vincent JP (Oct 1995). "Neurotensin receptors: binding properties, transduction pathways, and structure". Cellular and Molecular Neurobiology. 15 (5): 501–12. doi:10.1007/BF02071313. PMID 8719037. 
  • Vincent JP, Mazella J, Kitabgi P (Jul 1999). "Neurotensin and neurotensin receptors". Trends in Pharmacological Sciences. 20 (7): 302–9. doi:10.1016/S0165-6147(99)01357-7. PMID 10390649. 
  • Vita N, Laurent P, Lefort S, Chalon P, Dumont X, Kaghad M, Gully D, Le Fur G, Ferrara P, Caput D (Feb 1993). "Cloning and expression of a complementary DNA encoding a high affinity human neurotensin receptor". FEBS Letters. 317 (1-2): 139–42. doi:10.1016/0014-5793(93)81509-X. PMID 8381365. 
  • Le F, Groshan K, Zeng XP, Richelson E (Jan 1997). "Characterization of the genomic structure, promoter region, and a tetranucleotide repeat polymorphism of the human neurotensin receptor gene". The Journal of Biological Chemistry. 272 (2): 1315–22. doi:10.1074/jbc.272.2.1315. PMID 8995438. 
  • Boudin H, Pélaprat D, Rostène W, Pickel VM, Beaudet A (Oct 1998). "Correlative ultrastructural distribution of neurotensin receptor proteins and binding sites in the rat substantia nigra". The Journal of Neuroscience. 18 (20): 8473–84. PMID 9763490. 
  • Ye X, Mehlen P, Rabizadeh S, VanArsdale T, Zhang H, Shin H, Wang JJ, Leo E, Zapata J, Hauser CA, Reed JC, Bredesen DE (Oct 1999). "TRAF family proteins interact with the common neurotrophin receptor and modulate apoptosis induction". The Journal of Biological Chemistry. 274 (42): 30202–8. doi:10.1074/jbc.274.42.30202. PMID 10514511. 
  • Wang L, Friess H, Zhu Z, Graber H, Zimmermann A, Korc M, Reubi JC, Büchler MW (Feb 2000). "Neurotensin receptor-1 mRNA analysis in normal pancreas and pancreatic disease". Clinical Cancer Research. 6 (2): 566–71. PMID 10690540. 
  • Cusack B, Jansen K, McCormick DJ, Chou T, Pang Y, Richelson E (Sep 2000). "A single amino acid of the human and rat neurotensin receptors (subtype 1) determining the pharmacological profile of a species-selective neurotensin agonist". Biochemical Pharmacology. 60 (6): 793–801. doi:10.1016/S0006-2952(00)00409-3. PMID 10930533. 
  • Oakley RH, Laporte SA, Holt JA, Barak LS, Caron MG (Jun 2001). "Molecular determinants underlying the formation of stable intracellular G protein-coupled receptor-beta-arrestin complexes after receptor endocytosis*". The Journal of Biological Chemistry. 276 (22): 19452–60. doi:10.1074/jbc.M101450200. PMID 11279203. 
  • Leplatois P, Josse A, Guillemot M, Febvre M, Vita N, Ferrara P, Loison G (Sep 2001). "Neurotensin induces mating in Saccharomyces cerevisiae cells that express human neurotensin receptor type 1 in place of the endogenous pheromone receptor". European Journal of Biochemistry / FEBS. 268 (18): 4860–7. doi:10.1046/j.0014-2956.2001.02407.x. PMID 11559354. 
  • Lundquist JT, Büllesbach EE, Golden PL, Dix TA (Feb 2002). "Topography of the neurotensin (NT)(8-9) binding site of human NT receptor-1 probed with NT(8-13) analogs". The Journal of Peptide Research. 59 (2): 55–61. doi:10.1046/j.1397-002x.2001.10946.x. PMID 11906607. 
  • Somaï S, Gompel A, Rostène W, Forgez P (Jul 2002). "Neurotensin counteracts apoptosis in breast cancer cells". Biochemical and Biophysical Research Communications. 295 (2): 482–8. doi:10.1016/S0006-291X(02)00703-9. PMID 12150975. 
  • Martin S, Navarro V, Vincent JP, Mazella J (Oct 2002). "Neurotensin receptor-1 and -3 complex modulates the cellular signaling of neurotensin in the HT29 cell line". Gastroenterology. 123 (4): 1135–43. doi:10.1053/gast.2002.36000. PMID 12360476. 
  • Toy-Miou-Leong M, Cortes CL, Beaudet A, Rostène W, Forgez P (Mar 2004). "Receptor trafficking via the perinuclear recycling compartment accompanied by cell division is necessary for permanent neurotensin cell sensitization and leads to chronic mitogen-activated protein kinase activation". The Journal of Biological Chemistry. 279 (13): 12636–46. doi:10.1074/jbc.M303384200. PMID 14699144. 
  • Magazin M, Poszepczynska-Guigné E, Bagot M, Boumsell L, Pruvost C, Chalon P, Culouscou JM, Ferrara P, Bensussan A (Jan 2004). "Sezary syndrome cells unlike normal circulating T lymphocytes fail to migrate following engagement of NT1 receptor". The Journal of Investigative Dermatology. 122 (1): 111–8. doi:10.1046/j.0022-202X.2003.22131.x. PMID 14962098. 
  • Brun P, Mastrotto C, Beggiao E, Stefani A, Barzon L, Sturniolo GC, Palù G, Castagliuolo I (Apr 2005). "Neuropeptide neurotensin stimulates intestinal wound healing following chronic intestinal inflammation". American Journal of Physiology. Gastrointestinal and Liver Physiology. 288 (4): G621–9. doi:10.1152/ajpgi.00140.2004. PMID 15764810. 

External links[edit]

This article incorporates text from the United States National Library of Medicine, which is in the public domain.