Neurotensin receptor 1
{{Short description|Protein-coding gene in the species Homo sapiens}}
{{Infobox_gene}}
Neurotensin receptor type 1 is a protein that in humans is encoded by the NTSR1 gene.{{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 | doi = 10.1007/BF00389545 | s2cid = 30418560 | doi-access = free }}{{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}} For a crystal structure of NTS1, see pdb code 4GRV. In addition, high-resolution crystal structures have been determined in complex with the peptide full agonist NTS8-13, the non-peptide full agonist SRI-9829, the partial agonist RTI-3a, and the antagonists / inverse agonists SR48692 and SR142948A, as well as in the ligand-free apo state.,{{cite journal |vauthors=Deluigi M, Klipp A, Klenk C, Merklinger L, Eberle SA, Morstein L, Heine P, Mittl PR, Ernst P, Kamenecka TM, He Y, Vacca S, Egloff P, Honegger A, Plückthun A |title=Complexes of the neurotensin receptor 1 with small-molecule ligands reveal structural determinants of full, partial, and inverse agonism |journal=Science Advances |volume=7 |issue=5 |pages=eabe5504 |date=January 2021 |pmc=7840143 |doi=10.1126/sciadv.abe5504 |pmid=33571132 |bibcode=2021SciA....7.5504D }} see PDB codes 6YVR (NTSR1-H4X:NTS8–13), 6Z4V (NTSR1-H4bmX:NTS8–13), 6Z8N (NTSR1-H4X:SRI-9829), 6ZA8 (NTSR1-H4X:RTI-3a), 6Z4S (NTSR1-H4bmX:SR48692), 6ZIN (NTSR1-H4X:SR48692), 6Z4Q (NTSR1-H4X: SR142948A), and 6Z66 (apo NTSR1-H4X).
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 processes through modulation by neurotensin, such as low blood pressure, high blood sugar, low body temperature, antinociception, anti-neuronal damage {{cite journal | vauthors = Liu Q, Hazan A, Grinman E, Angulo JA| display-authors = 3 | title = Pharmacological activation of the neurotensin receptor 1 abrogates the methamphetamine-induced striatal apoptosis in the mouse brain| journal =Brain Research| volume = 1659 | pages = 148–155| date = 2017 | doi = 10.1016/j.brainres.2017.01.029| pmid = 28130052 | s2cid = 6405660 }} and regulation of intestinal motility and secretion.
Ligands
- ML314 – β-arrestin biased agonist{{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 }}
- Neurotensin (NT1)
See also
References
{{reflist}}
Further reading
{{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 | s2cid = 13335185 | pmc = 11563118 }}
- {{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 | 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 | s2cid = 5929592 | doi-access = free }}
- {{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 | doi-access = free }}
- {{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 = 10.1523/JNEUROSCI.18-20-08473.1998| pmc = 6792847 | doi-access = free }}
- {{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 | doi-access = free }}
- {{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 }}
- {{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 | 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 | doi-access = free }}
- {{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 | volume = 268 | issue = 18 | pages = 4860–7 | date = Sep 2001 | pmid = 11559354 | doi = 10.1046/j.0014-2956.2001.02407.x | doi-access = free }}
- {{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 | 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 | 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 | doi-access = free }}
- {{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 | doi-access = free }}
- {{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 | doi-access = free }}
- {{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 }}
{{refend}}
External links
- {{cite web | url = http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=3004 | title = Neurotensin Receptors: NTS1 | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | access-date = 2008-12-05 | archive-date = 2012-04-02 | archive-url = https://web.archive.org/web/20120402212312/http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=3004 | url-status = dead }}
{{NLM content}}
{{G protein-coupled receptors|g1}}
Category:G protein-coupled receptors
{{transmembranereceptor-stub}}