Neurotensin receptor
From Wikipedia, the free encyclopedia
| 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
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
- Levocabastine (NTS2 selective, also H1 histamine antagonist)[5]
- SR-48692 (NTS1 selective)[6]
- SR-142,948 (unselective, CAS# 184162-64-9)
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
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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. PMID 19186134.
- ↑ 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
- "Neurotensin Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
- Neurotensin Receptors at the US National Library of Medicine Medical Subject Headings (MeSH)
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