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{{ | '''Neurotensin receptor type 1''' is a [[protein]] that in humans is encoded by the ''NTSR1'' [[gene]].<ref name="pmid8075503">{{cite journal | vauthors = Laurent P, Clerc P, Mattei MG, Forgez P, Dumont X, Ferrara P, Caput D, Rostene W | title = Chromosomal localization of mouse and human neurotensin receptor genes | journal = Mammalian Genome | volume = 5 | issue = 5 | pages = 303–6 | date = May 1994 | pmid = 8075503 | pmc = | doi = 10.1007/BF00389545 }}</ref><ref name="entrez">{{cite web | title = Entrez Gene: NTSR1 neurotensin receptor 1 (high affinity)| url = https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=4923| accessdate = }}</ref> For a crystal structure of NTS1, see pdb code 4GRV. | ||
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== Function == | |||
Neurotensin receptor 1, also called NTR1, belongs to the large superfamily of [[G-protein]] coupled receptors and is considered a class-A GPCR. NTSR1 mediates multiple biological through modulation by [[neurotensin]], such as [[hypotension|low blood pressure]], [[hyperglycemia|high blood sugar]], [[hypothermia|low body temperature]], antinociception, and regulation of intestinal motility and secretion.<ref name="entrez">{{cite web | title = Entrez Gene: NTSR1 neurotensin receptor 1 (high affinity)| url = https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=4923| accessdate = }}</ref> | |||
==See also== | == Ligands == | ||
* ML314 – β-arrestin biased agonist<ref name="pmid24611085">{{cite journal |vauthors=Peddibhotla S, Hedrick MP, Hershberger P, et al. |title=Discovery of ML314, a Brain Penetrant Non-Peptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor |journal=ACS Med Chem Lett |volume=4 |issue=9 |pages=846–851 |year=2013 |pmid=24611085 |pmc=3940307 |doi=10.1021/ml400176n |url=}}</ref> | |||
* Neurotensin (NT1) | |||
== See also == | |||
* [[Neurotensin receptor]] | * [[Neurotensin receptor]] | ||
==References== | == References == | ||
{{reflist | {{reflist}} | ||
==Further reading== | == Further reading == | ||
{{refbegin | 2}} | {{refbegin | 2}} | ||
* {{cite journal | vauthors = Vincent JP | title = Neurotensin receptors: binding properties, transduction pathways, and structure | journal = Cellular and Molecular Neurobiology | volume = 15 | issue = 5 | pages = 501–12 | date = Oct 1995 | pmid = 8719037 | doi = 10.1007/BF02071313 }} | |||
* {{cite journal | vauthors = Vincent JP, Mazella J, Kitabgi P | title = Neurotensin and neurotensin receptors | journal = Trends in Pharmacological Sciences | volume = 20 | issue = 7 | pages = 302–9 | date = Jul 1999 | pmid = 10390649 | doi = 10.1016/S0165-6147(99)01357-7 }} | |||
*{{cite journal | * {{cite journal | vauthors = Vita N, Laurent P, Lefort S, Chalon P, Dumont X, Kaghad M, Gully D, Le Fur G, Ferrara P, Caput D | title = Cloning and expression of a complementary DNA encoding a high affinity human neurotensin receptor | journal = FEBS Letters | volume = 317 | issue = 1-2 | pages = 139–42 | date = Feb 1993 | pmid = 8381365 | doi = 10.1016/0014-5793(93)81509-X }} | ||
*{{cite journal | * {{cite journal | vauthors = Le F, Groshan K, Zeng XP, Richelson E | title = Characterization of the genomic structure, promoter region, and a tetranucleotide repeat polymorphism of the human neurotensin receptor gene | journal = The Journal of Biological Chemistry | volume = 272 | issue = 2 | pages = 1315–22 | date = Jan 1997 | pmid = 8995438 | doi = 10.1074/jbc.272.2.1315 }} | ||
* {{cite journal | vauthors = Boudin H, Pélaprat D, Rostène W, Pickel VM, Beaudet A | title = Correlative ultrastructural distribution of neurotensin receptor proteins and binding sites in the rat substantia nigra | journal = The Journal of Neuroscience | volume = 18 | issue = 20 | pages = 8473–84 | date = Oct 1998 | pmid = 9763490 | doi = }} | |||
*{{cite journal | * {{cite journal | vauthors = Ye X, Mehlen P, Rabizadeh S, VanArsdale T, Zhang H, Shin H, Wang JJ, Leo E, Zapata J, Hauser CA, Reed JC, Bredesen DE | title = TRAF family proteins interact with the common neurotrophin receptor and modulate apoptosis induction | journal = The Journal of Biological Chemistry | volume = 274 | issue = 42 | pages = 30202–8 | date = Oct 1999 | pmid = 10514511 | doi = 10.1074/jbc.274.42.30202 }} | ||
*{{cite journal | * {{cite journal | vauthors = Wang L, Friess H, Zhu Z, Graber H, Zimmermann A, Korc M, Reubi JC, Büchler MW | title = Neurotensin receptor-1 mRNA analysis in normal pancreas and pancreatic disease | journal = Clinical Cancer Research | volume = 6 | issue = 2 | pages = 566–71 | date = Feb 2000 | pmid = 10690540 | doi = }} | ||
*{{cite journal | * {{cite journal | vauthors = Cusack B, Jansen K, McCormick DJ, Chou T, Pang Y, Richelson E | title = A single amino acid of the human and rat neurotensin receptors (subtype 1) determining the pharmacological profile of a species-selective neurotensin agonist | journal = Biochemical Pharmacology | volume = 60 | issue = 6 | pages = 793–801 | date = Sep 2000 | pmid = 10930533 | doi = 10.1016/S0006-2952(00)00409-3 }} | ||
*{{cite journal | * {{cite journal | vauthors = Oakley RH, Laporte SA, Holt JA, Barak LS, Caron MG | title = Molecular determinants underlying the formation of stable intracellular G protein-coupled receptor-beta-arrestin complexes after receptor endocytosis* | journal = The Journal of Biological Chemistry | volume = 276 | issue = 22 | pages = 19452–60 | date = Jun 2001 | pmid = 11279203 | doi = 10.1074/jbc.M101450200 }} | ||
*{{cite journal | * {{cite journal | vauthors = Leplatois P, Josse A, Guillemot M, Febvre M, Vita N, Ferrara P, Loison G | title = Neurotensin induces mating in Saccharomyces cerevisiae cells that express human neurotensin receptor type 1 in place of the endogenous pheromone receptor | journal = European Journal of Biochemistry / FEBS | volume = 268 | issue = 18 | pages = 4860–7 | date = Sep 2001 | pmid = 11559354 | doi = 10.1046/j.0014-2956.2001.02407.x }} | ||
*{{cite journal | * {{cite journal | vauthors = Lundquist JT, Büllesbach EE, Golden PL, Dix TA | title = Topography of the neurotensin (NT)(8-9) binding site of human NT receptor-1 probed with NT(8-13) analogs | journal = The Journal of Peptide Research | volume = 59 | issue = 2 | pages = 55–61 | date = Feb 2002 | pmid = 11906607 | doi = 10.1046/j.1397-002x.2001.10946.x }} | ||
*{{cite journal | * {{cite journal | vauthors = Somaï S, Gompel A, Rostène W, Forgez P | title = Neurotensin counteracts apoptosis in breast cancer cells | journal = Biochemical and Biophysical Research Communications | volume = 295 | issue = 2 | pages = 482–8 | date = Jul 2002 | pmid = 12150975 | doi = 10.1016/S0006-291X(02)00703-9 }} | ||
*{{cite journal | * {{cite journal | vauthors = Martin S, Navarro V, Vincent JP, Mazella J | title = Neurotensin receptor-1 and -3 complex modulates the cellular signaling of neurotensin in the HT29 cell line | journal = Gastroenterology | volume = 123 | issue = 4 | pages = 1135–43 | date = Oct 2002 | pmid = 12360476 | doi = 10.1053/gast.2002.36000 }} | ||
* {{cite journal | vauthors = Toy-Miou-Leong M, Cortes CL, Beaudet A, Rostène W, Forgez P | title = 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 | journal = The Journal of Biological Chemistry | volume = 279 | issue = 13 | pages = 12636–46 | date = Mar 2004 | pmid = 14699144 | doi = 10.1074/jbc.M303384200 }} | |||
*{{cite journal | * {{cite journal | vauthors = Magazin M, Poszepczynska-Guigné E, Bagot M, Boumsell L, Pruvost C, Chalon P, Culouscou JM, Ferrara P, Bensussan A | title = Sezary syndrome cells unlike normal circulating T lymphocytes fail to migrate following engagement of NT1 receptor | journal = The Journal of Investigative Dermatology | volume = 122 | issue = 1 | pages = 111–8 | date = Jan 2004 | pmid = 14962098 | doi = 10.1046/j.0022-202X.2003.22131.x }} | ||
*{{cite journal | * {{cite journal | vauthors = Brun P, Mastrotto C, Beggiao E, Stefani A, Barzon L, Sturniolo GC, Palù G, Castagliuolo I | title = Neuropeptide neurotensin stimulates intestinal wound healing following chronic intestinal inflammation | journal = American Journal of Physiology. Gastrointestinal and Liver Physiology | volume = 288 | issue = 4 | pages = G621-9 | date = Apr 2005 | pmid = 15764810 | doi = 10.1152/ajpgi.00140.2004 }} | ||
*{{cite journal | |||
*{{cite journal | |||
*{{cite journal | |||
*{{cite journal | |||
}} | |||
{{refend}} | {{refend}} | ||
{{ | == External links == | ||
* {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=3004 | title = Neurotensin Receptors: NTS<sub>1</sub> | accessdate = | authorlink = | date = | format = | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages = | archiveurl = | archivedate = | quote = }} | |||
{{transmembranereceptor-stub}} | |||
{{NLM content}} | {{NLM content}} | ||
{{G protein-coupled receptors}} | {{G protein-coupled receptors|g1}} | ||
[[Category:G protein coupled receptors]] | {{Neuropeptidergics}} | ||
[[Category:G protein-coupled receptors]] |
Latest revision as of 07:16, 10 January 2019
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External IDs | GeneCards: [1] | ||||||
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Species | Human | Mouse | |||||
Entrez |
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Ensembl |
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UniProt |
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RefSeq (mRNA) |
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Location (UCSC) | n/a | n/a | |||||
PubMed search | n/a | n/a | |||||
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Neurotensin receptor type 1 is a protein that in humans is encoded by the NTSR1 gene.[1][2] For a crystal structure of NTS1, see pdb code 4GRV.
Function
Neurotensin receptor 1, also called NTR1, belongs to the large superfamily of G-protein coupled receptors and is considered a class-A GPCR. NTSR1 mediates multiple biological through modulation by neurotensin, such as low blood pressure, high blood sugar, low body temperature, antinociception, and regulation of intestinal motility and secretion.[2]
Ligands
- ML314 – β-arrestin biased agonist[3]
- Neurotensin (NT1)
See also
References
- ↑ 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.
- ↑ 2.0 2.1 "Entrez Gene: NTSR1 neurotensin receptor 1 (high affinity)".
- ↑ 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 3940307. PMID 24611085.
Further reading
- 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
- "Neurotensin Receptors: NTS1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
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