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

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.

[edit] Ligands

[edit] 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]

[edit] Antagonists

Levocabastine (NTS₂ selective, also H₁ histamine antagonist)^[5]
SR-48692 (NTS₁ selective)^[6]
SR-142,948 (unselective, CAS# 184162-64-9)

[edit] 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].

[edit] 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. http://joi.jlc.jst.go.jp/JST.JSTAGE/bbb/67.940?lang=en&from=PubMed.
^ 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.

[edit] External links

"Neurotensin Receptors". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1342.
MeSH Neurotensin+Receptors

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[pmid10390649-0] 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.

[pmid16919370-1] 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.

[pmid12784648-2] 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. http://joi.jlc.jst.go.jp/JST.JSTAGE/bbb/67.940?lang=en&from=PubMed.

[pmid19195889-3] 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.

[pmid17074405-4] 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.

[pmid18096238-5] 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.

[pmid18976711-6] 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.

[pmid16708210-7] 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.

[pmid19186134-8] 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.

[pmid21218848-9] 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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Apr	MAY	Jun
	09
2011	2012	2013

Neurotensin receptor

Contents

[edit] Ligands

[edit] Agonists

[edit] Antagonists

[edit] Biophysical Investigation

[edit] References

[edit] External links

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