ニューロテンシン受容体、ニューロテンシンレセプター

WordNet

a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response

PrepTutorEJDIC

=sense organ / 受信装置

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/05/18 17:08:30」(JST)

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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. 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.

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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1. グレリン ghrelin
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3. T細胞受容体の遺伝学 t cell receptor genetics
4. β-2アドレナリン受容体機能不全および喘息の多型性 beta 2 adrenergic receptor dysfunction and polymorphism in asthma
5. アンギオテンシン変換酵素阻害剤とアンギオテンシン受容体拮抗剤との相違 differences between angiotensin converting enzyme inhibitors and receptor blockers

English Journal

Kinetics of the early events of GPCR signalling.

Adamson RJ1, Watts A2.
FEBS letters.FEBS Lett.2014 Dec 20;588(24):4701-7. doi: 10.1016/j.febslet.2014.10.043. Epub 2014 Nov 11.
Neurotensin receptor type 1 (NTS1) is a G protein-coupled receptor (GPCR) that affects cellular responses by initiating a cascade of interactions through G proteins. The kinetic details for these interactions are not well-known. Here, NTS1-nanodisc-Gαs and Gαi1 interactions were studied. The bindi
PMID 25447525

The Neurotensin-HIF-1α-VEGFα Axis Orchestrates Hypoxia, Colonic Inflammation, and Intestinal Angiogenesis.

Bakirtzi K1, West G2, Fiocchi C2, Law IK1, Iliopoulos D3, Pothoulakis C4.
The American journal of pathology.Am J Pathol.2014 Dec;184(12):3405-14. doi: 10.1016/j.ajpath.2014.08.015. Epub 2014 Oct 7.
The expression of neurotensin (NT) and its receptor (NTR1) is up-regulated in experimental colitis and inflammatory bowel disease; NT/NTR1 interactions regulate gut inflammation. During active inflammation, metabolic shifts toward hypoxia lead to the activation of hypoxia-inducible factor (HIF)-1, w
PMID 25307345

Neurotensin signaling regulates stem-like traits of glioblastoma stem cells through activation of IL-8/CXCR1/STAT3 pathway.

Zhou J1, Yi L1, Ouyang Q1, Xu L1, Cui H2, Xu M3.
Cellular signalling.Cell Signal.2014 Dec;26(12):2896-902. doi: 10.1016/j.cellsig.2014.08.027. Epub 2014 Sep 6.
We recently found that neurotensin (NTS) and its primary receptor NTSR1 play a crucial role in glioblastoma cell proliferation and invasion. However, very little is known regarding the functional role of NTS/NTSR1 signaling in glioblastoma stem cells (GSCs). Here, we showed that NTSR1 is highly expr
PMID 25200966

Japanese Journal

グリア細胞におけるG蛋白質共役型受容体の機能 (特集情報伝達処理におけるグリアの機能と異常)

古田晶子,和田恵津子,和田圭司
Brain and nerve 59(7), 717-724, 2007-07
NAID 40015561876

The neuromedin u-growth hormone secretagogue receptor 1b/neurotensin receptor 1 oncogenic signaling pathway as a therapeutic target for lung cancer

TAKAHASHI K
Cancer Res 66, 9408-9419, 2006
NAID 30018590811

Related Pictures

★リンクテーブル★

リンク元	「ニューロテンシン受容体」「ニューロテンシンレセプター」

「ニューロテンシン受容体」

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

　　[★]

英: neurotensin receptor
関: ニューロテンシンレセプター

「ニューロテンシンレセプター」

　　[★]

英: neurotensin receptor
関: ニューロテンシン受容体

[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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neurotensin receptor