Biology:Neurotensin receptor 1
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Short description: Protein-coding gene in the species Homo sapiens
 Generic protein structure example |
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. 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.[3], 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 [4] and regulation of intestinal motility and secretion.[2]
Ligands
- ML314 – β-arrestin biased agonist[5]
- Neurotensin (NT1)
See also
References
- ↑ "Chromosomal localization of mouse and human neurotensin receptor genes". Mammalian Genome 5 (5): 303–6. May 1994. doi:10.1007/BF00389545. PMID 8075503.
- ↑ 2.0 2.1 "Entrez Gene: NTSR1 neurotensin receptor 1 (high affinity)". https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=4923.
- ↑ "Complexes of the neurotensin receptor 1 with small-molecule ligands reveal structural determinants of full, partial, and inverse agonism". Science Advances 7 (5): eabe5504. January 2021. doi:10.1126/sciadv.abe5504. PMID 33571132. Bibcode: 2021SciA....7.5504D.
- ↑ "Pharmacological activation of the neurotensin receptor 1 abrogates the methamphetamine-induced striatal apoptosis in the mouse brain". Brain Research 1659: 148–155. 2017. doi:10.1016/j.brainres.2017.01.029. PMID 28130052.
- ↑ "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. 2013. doi:10.1021/ml400176n. PMID 24611085.
Further reading
- "Neurotensin receptors: binding properties, transduction pathways, and structure". Cellular and Molecular Neurobiology 15 (5): 501–12. Oct 1995. doi:10.1007/BF02071313. PMID 8719037.
- "Neurotensin and neurotensin receptors". Trends in Pharmacological Sciences 20 (7): 302–9. Jul 1999. doi:10.1016/S0165-6147(99)01357-7. PMID 10390649.
- "Cloning and expression of a complementary DNA encoding a high affinity human neurotensin receptor". FEBS Letters 317 (1–2): 139–42. Feb 1993. doi:10.1016/0014-5793(93)81509-X. PMID 8381365.
- "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. Jan 1997. doi:10.1074/jbc.272.2.1315. PMID 8995438.
- "Correlative ultrastructural distribution of neurotensin receptor proteins and binding sites in the rat substantia nigra". The Journal of Neuroscience 18 (20): 8473–84. Oct 1998. doi:10.1523/JNEUROSCI.18-20-08473.1998. PMID 9763490.
- "TRAF family proteins interact with the common neurotrophin receptor and modulate apoptosis induction". The Journal of Biological Chemistry 274 (42): 30202–8. Oct 1999. doi:10.1074/jbc.274.42.30202. PMID 10514511.
- "Neurotensin receptor-1 mRNA analysis in normal pancreas and pancreatic disease". Clinical Cancer Research 6 (2): 566–71. Feb 2000. PMID 10690540.
- "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. Sep 2000. doi:10.1016/S0006-2952(00)00409-3. PMID 10930533.
- "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. Jun 2001. doi:10.1074/jbc.M101450200. PMID 11279203.
- "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 268 (18): 4860–7. Sep 2001. doi:10.1046/j.0014-2956.2001.02407.x. PMID 11559354.
- "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. Feb 2002. doi:10.1046/j.1397-002x.2001.10946.x. PMID 11906607.
- "Neurotensin counteracts apoptosis in breast cancer cells". Biochemical and Biophysical Research Communications 295 (2): 482–8. Jul 2002. doi:10.1016/S0006-291X(02)00703-9. PMID 12150975.
- "Neurotensin receptor-1 and -3 complex modulates the cellular signaling of neurotensin in the HT29 cell line". Gastroenterology 123 (4): 1135–43. Oct 2002. doi:10.1053/gast.2002.36000. PMID 12360476.
- "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. Mar 2004. doi:10.1074/jbc.M303384200. PMID 14699144.
- "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. Jan 2004. doi:10.1046/j.0022-202X.2003.22131.x. PMID 14962098.
- "Neuropeptide neurotensin stimulates intestinal wound healing following chronic intestinal inflammation". American Journal of Physiology. Gastrointestinal and Liver Physiology 288 (4): G621–9. Apr 2005. 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. http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=3004.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
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