Neurotensin receptor

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neurotensin receptor 1 (high affinity)
Identifiers
Symbol NTSR1
Alt. symbols NTR
Entrez 4923
HUGO 8039
OMIM 162651
RefSeq NM_002531
UniProt P30989
Other data
Locus Chr. 20 q13-20q13
neurotensin receptor 2
Identifiers
Symbol NTSR2
Alt. symbols NTR2
Entrez 23620
HUGO 8040
OMIM 605538
RefSeq NM_012344
UniProt O95665
Other data
Locus Chr. 2 p25.1
sortilin 1
Identifiers
Symbol SORT1
Alt. symbols Gp95, NT3
Entrez 6272
HUGO 11186
OMIM 602458
RefSeq NM_002959
UniProt Q99523
Other data
Locus Chr. 1 p21.3-1p13.1

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[edit]

Agonists[edit]

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[edit]

Biophysical Investigation[edit]

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[edit]

  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. 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. 

External links[edit]