Neurotensin receptor

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

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

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

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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. PMC 4418176. 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. PMC 2716571. 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)

This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it.

[pmid10390649-1] 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.

[pmid16919370-2] 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.

[pmid12784648-3] 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.

[pmid19195889-4] 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.

[pmid17074405-5] 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.

[pmid18096238-6] 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.

[pmid18976711-7] 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.

[pmid16708210-8] 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.

[pmid19186134-9] 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.

[pmid21218848-10] 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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