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Neurotensin receptor

Introduction

The neurotensin receptors are transmembrane receptors that bind the neurotransmitter neurotensin.[1][2] Two of the receptors encoded by the NTSR1 and NTSR2 genes contain seven transmembrane helices and are G protein coupled. The third receptor has a single transmembrane domain and is encoded by the SORT1 gene.

Ligands

Ligands

Agonists

Peptide
  • Beta-lactotensin (NTS2)[3]
  • JMV-449
  • Neurotensin
  • Neuromedin N (NTS1 selective)
  • PD-149,163 (NTS1 selective, reduced amide bond 8-13 fragment of neurotensin)
Non-peptide
  • Partial agonists derived from SR-48692[4]

Antagonists

Biophysical Investigation

Biophysical Investigation

Unusually for GPCRs, NTS1 can be expressed in an active form in the bacteria E. coli.[7] It can be purified and analysed in vitro and has been analysed by a number of biophysical techniques such as surface plasmon resonance,[8] FRET[9] and cryo-electron microscopy.[10]

References

References

  1. ↑ 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. PMID 10390649.
  2. ↑ Pelaprat D (2006). “Interactions between neurotensin receptors and G proteins”. Peptides. 27 (10): 2476–2487. doi:10.1016/j.peptides.2006.04.027. PMID 16919370.
  3. ↑ Yamauchi R, Usui H, Yunden J, Takenaka Y, Tani F, Yoshikawa M (April 2003). “Characterization of beta-lactotensin, a bioactive peptide derived from bovine beta-lactoglobulin, as a neurotensin agonist”. Bioscience, Biotechnology, and Biochemistry. 67 (4): 940–3. doi:10.1271/bbb.67.940. PMID 12784648.
  4. ↑ Thomas JB, Navarro H, Warner KR, Gilmour B (March 2009). “The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay”. Bioorganic & Medicinal Chemistry Letters. 19 (5): 1438–1441. doi:10.1016/j.bmcl.2009.01.024. PMC 4418176. PMID 19195889.
  5. ↑ 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. PMID 17074405.
  6. ↑ 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. PMID 18096238.
  7. ↑ 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 Purification. 64 (1): 32–38. doi:10.1016/j.pep.2008.10.001. PMID 18976711.
  8. ↑ 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. PMID 16708210.
  9. ↑ Harding PJ, Attrill H, Boehringer J, Ross S, Wadhams GH, Smith E, Armitage JP, Watts A (2009). “Constitutive dimerization of the G-protein coupled receptor, neurotensin receptor 1, reconstituted into phospholipid bilayers”. Biophys. J. 96 (3): 964–973. doi:10.1016/j.bpj.2008.09.054. PMC 2716571. PMID 19186134.
  10. ↑ Selmi DN, Adamson RJ, Attrill H, Goddard AD, Gilbert RJ, Watts A, Turberfield AJ (2011). “DNA-templated protein arrays for single-molecule imaging”. Nano Lett. 11 (2): 657–660. doi:10.1021/nl1037769. PMID 21218848.
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