Neurotensin receptors are transmembrane receptors that bind the neurotransmitterneurotensin.[1][2] Two of the receptors encoded by the NTSR1 and NTSR2 genes contain seven transmembrane helices and are G 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 the SORT1 gene.
Unusually for GPCRs, NTS1 can be expressed in an active form in the bacteria E. coli.[8] It can be purified and analysed in 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 have been determined for NTS1 in complex with the peptide full agonist NT8-13, non-peptide full agonist SRI-9829, partial agonist RTI-3a, antagonists / inverse agonists SR-48692 and SR-142948, as well as in the ligand-free state [3]
References[]
^Vincent JP, Mazella J, Kitabgi P (1999). "Neurotensin and neurotensin receptors". Trends Pharmacol. Sci. 20 (7): 302–309. doi:10.1016/S0165-6147(99)01357-7. PMID10390649.
^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.