Neurotensin receptor 2 explained
Neurotensin receptor type 2 is a protein that in humans is encoded by the NTSR2 gene.[1] [2] [3]
Function
The protein encoded by this gene belongs to the G protein-coupled receptor family that activates a phosphatidylinositol-calcium second messenger system. Binding and pharmacological studies demonstrate that this receptor binds Neurotensin (NT) as well as several other ligands already described for Neurotensin receptor 1. NT function is known to be a neuromodulator of dopamine and has hypothermic and analgesic properties in the brain and some peripheral organ function as well.[4] NTS2 is found mostly in the brain through Northern-blot analysis.Unlike NTS1, NTS2 has a low affinity with NT and a high sensitivity to levocabastine, an antihistamine, which competes with NT for binding.
See also
Further reading
- Vincent JP, Mazella J, Kitabgi P . Neurotensin and neurotensin receptors . Trends in Pharmacological Sciences . 20 . 7 . 302–309 . July 1999 . 10390649 . 10.1016/S0165-6147(99)01357-7 .
- Mazella J, Botto JM, Guillemare E, Coppola T, Sarret P, Vincent JP . Structure, functional expression, and cerebral localization of the levocabastine-sensitive neurotensin/neuromedin N receptor from mouse brain . The Journal of Neuroscience . 16 . 18 . 5613–5620 . September 1996 . 8795617 . 6578974 . 10.1523/jneurosci.16-18-05613.1996 . free .
- Ramez M, Bagot M, Nikolova M, Boumsell L, Vita N, Chalon P, Caput D, Ferrara P, Bensussan A . Functional characterization of neurotensin receptors in human cutaneous T cell lymphoma malignant lymphocytes . The Journal of Investigative Dermatology . 117 . 3 . 687–693 . September 2001 . 11564178 . 10.1046/j.0022-202x.2001.01439.x . free .
- Martin S, Vincent JP, Mazella J . Recycling ability of the mouse and the human neurotensin type 2 receptors depends on a single tyrosine residue . Journal of Cell Science . 115 . Pt 1 . 165–173 . January 2002 . 11801734 . 10.1242/jcs.115.1.165 . free .
- Bourcier T, Rondeau N, Paquet S, Forgez P, Lombet A, Pouzaud F, Rostène W, Borderie V, Laroche L . Expression of neurotensin receptors in human corneal keratocytes . Investigative Ophthalmology & Visual Science . 43 . 6 . 1765–1771 . June 2002 . 12036977 .
- Leyton J, Garcia-Marin L, Jensen RT, Moody TW . Neurotensin causes tyrosine phosphorylation of focal adhesion kinase in lung cancer cells . European Journal of Pharmacology . 442 . 3 . 179–186 . May 2002 . 12065070 . 10.1016/S0014-2999(02)01539-X .
- Somaï S, Gompel A, Rostène W, Forgez P . Neurotensin counteracts apoptosis in breast cancer cells . Biochemical and Biophysical Research Communications . 295 . 2 . 482–488 . July 2002 . 12150975 . 10.1016/S0006-291X(02)00703-9 .
- Holst B, Holliday ND, Bach A, Elling CE, Cox HM, Schwartz TW . Common structural basis for constitutive activity of the ghrelin receptor family . The Journal of Biological Chemistry . 279 . 51 . 53806–53817 . December 2004 . 15383539 . 10.1074/jbc.M407676200 . free .
External links
- Web site: Neurotensin Receptors: NTS2 . IUPHAR Database of Receptors and Ion Channels . International Union of Basic and Clinical Pharmacology . 2008-12-05 . 2016-03-03 . https://web.archive.org/web/20160303202002/http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=3005 . dead .
Notes and References
- Chalon P, Vita N, Kaghad M, Guillemot M, Bonnin J, Delpech B, Le Fur G, Ferrara P, Caput D . Molecular cloning of a levocabastine-sensitive neurotensin binding site . FEBS Letters . 386 . 2–3 . 91–94 . May 1996 . 8647296 . 10.1016/0014-5793(96)00397-3 . 5802578 . free .
- Vita N, Oury-Donat F, Chalon P, Guillemot M, Kaghad M, Bachy A, Thurneyssen O, Garcia S, Poinot-Chazel C, Casellas P, Keane P, Le Fur G, Maffrand JP, Soubrie P, Caput D, Ferrara P . Neurotensin is an antagonist of the human neurotensin NT2 receptor expressed in Chinese hamster ovary cells . European Journal of Pharmacology . 360 . 2–3 . 265–272 . November 1998 . 9851594 . 10.1016/S0014-2999(98)00678-5 .
- Web site: Entrez Gene . U.S. National Library of Medicine . NTSR2 neurotensin receptor 2.
- Vincent JP, Mazella J, Kitabgi P . Neurotensin and neurotensin receptors . Trends in Pharmacological Sciences . 20 . 7 . 302–309 . July 1999 . 10390649 . 10.1016/s0165-6147(99)01357-7 .