Neurotensin receptors are transmembrane receptors that bind theneurotransmitterneurotensin.[1][2] Two of the receptors encoded by theNTSR1 andNTSR2 genes contain seven transmembrane helices and areG protein coupled. Numerous crystal structures have been reported for the neurotensin receptor 1 (NTS1).[3] The third receptor has a single transmembrane domain and is encoded by theSORT1 gene.
Unusually for GPCRs, NTS1 can be expressed in an active form in the bacteriaE. coli.[8] It can be purified and analysedin vitro and has been analysed by a number of biophysical techniques such as surface plasmon resonance,[9] FRET[10] and cryo-electron microscopy.[11]Furthermore, high-resolution crystal structures of NTS1 have been determined in complex with the peptide full agonist NT8-13, the non-peptide full agonist SRI-9829, the partial agonist RTI-3a, and the antagonists / inverse agonists SR-48692 and SR-142948, as well as in the ligand-free apo state[3]
^Bredeloux P, Costentin J, Dubuc I (December 2006). "Interactions between NTS2 neurotensin and opioid receptors on two nociceptive responses assessed on the hot plate test in mice".Behavioural Brain Research.175 (2):399–407.doi:10.1016/j.bbr.2006.09.016.PMID17074405.S2CID24790151.
^Ferraro L, Tomasini MC, Mazza R, Fuxe K, Fournier J, Tanganelli S, Antonelli T (August 2008). "Neurotensin receptors as modulators of glutamatergic transmission".Brain Research Reviews.58 (2):365–373.doi:10.1016/j.brainresrev.2007.11.001.PMID18096238.S2CID25434443.
^Attrill H, Harding PJ, Smith E, Ross S, Watts A (2009). "Improved yield of a ligand-binding GPCR expressed in E. coli for structural studies".Protein Expr Purif.64 (1):32–38.doi:10.1016/j.pep.2008.10.001.PMID18976711.
^Harding PJ, Hadingham TC, McDonnell JM, Watts A (2006). "Direct analysis of a GPCR-agonist interaction by surface plasmon resonance".Eur Biophys J.35 (8):709–712.doi:10.1007/s00249-006-0070-x.PMID16708210.S2CID7844675.
"Neurotensin Receptors".IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived fromthe original on 2016-03-03. Retrieved2007-04-24.
