Neurotensin receptor

Short description: InterPro Family

neurotensin receptor 1 (high affinity)

Identifiers
Symbol| NTSR1
Alt. symbols| NTR
NCBI gene| 4923
HGNC| 8039
OMIM| 162651
RefSeq| NM_002531
UniProt| P30989
Other data
Locus| Chr. 20 q13-20q13
neurotensin receptor 2

Identifiers
Symbol| NTSR2
Alt. symbols| NTR2
NCBI gene| 23620
HGNC| 8040
OMIM| 605538
RefSeq| NM_012344
UniProt| O95665
Other data
Locus| Chr. 2 p25.1
sortilin 1

Identifiers
Symbol| SORT1
Alt. symbols| Gp95, NT3
NCBI gene| 6272
HGNC| 11186
OMIM| 602458
RefSeq| NM_002959
UniProt| Q99523
Other data
Locus| Chr. 1 p21.3-1p13.1

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. Numerous crystal structures have been reported for the neurotensin receptor 1 (NTS1).[3] The third receptor has a single transmembrane domain and is encoded by the SORT1 gene.

## Contents

* 1 Ligands
* 1.1 Agonists
* 1.2 Antagonists
* 2 Biophysical Investigation
* 3 References
* 4 External links

## Ligands

### Agonists

Peptide

* Beta-lactotensin (NTS2)[4]
* JMV-449
* Neurotensin
* Neuromedin N (NTS1 selective)
* PD-149,163 (NTS1 selective, reduced amide bond 8-13 fragment of neurotensin)

Non-peptide

* NTS1 full agonist SRI-9829 [3]
* Partial agonists derived from SR-48692[5]

### Antagonists

* Levocabastine (NTS2 selective, also H1 histamine antagonist)[6]
* SR-48692 (NTS1 selective)[7]
* SR-142948 (unselective, CAS# 184162-64-9)

## Biophysical Investigation

Unusually for GPCRs, NTS1 can be expressed in an active form in the bacteria E. coli.[8] It can be purified and analysed in vitro and has been analysed by a number of biophysical techniques such as surface plasmon resonance,[9] FRET[10] and cryo-electron microscopy.[11] Furthermore, high-resolution crystal structures of NTS1 have been determined in complex with the peptide full agonist NT8-13, the non-peptide full agonist SRI-9829, the partial agonist RTI-3a, and the antagonists / inverse agonists SR-48692 and SR-142948, as well as in the ligand-free apo state [3]

## References

1. ↑ "Neurotensin and neurotensin receptors". Trends Pharmacol. Sci. 20 (7): 302–309. 1999. 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. http://www.hal.inserm.fr/inserm-00519739/document.
3. ↑ 3.0 3.1 3.2 "Complexes of the neurotensin receptor 1 with small-molecule ligands reveal structural determinants of full, partial, and inverse agonism". Science Advances 7 (5): eabe5504. January 2021. doi:10.1126/sciadv.abe5504. PMID 33571132. Bibcode: 2021SciA....7.5504D.
4. ↑ "Characterization of beta-lactotensin, a bioactive peptide derived from bovine beta-lactoglobulin, as a neurotensin agonist". Bioscience, Biotechnology, and Biochemistry 67 (4): 940–3. April 2003. doi:10.1271/bbb.67.940. PMID 12784648. http://joi.jlc.jst.go.jp/JST.JSTAGE/bbb/67.940?lang=en&from=PubMed.
5. ↑ "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. March 2009. doi:10.1016/j.bmcl.2009.01.024. PMID 19195889.
6. ↑ "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. December 2006. doi:10.1016/j.bbr.2006.09.016. PMID 17074405.
7. ↑ "Neurotensin receptors as modulators of glutamatergic transmission". Brain Research Reviews 58 (2): 365–373. August 2008. doi:10.1016/j.brainresrev.2007.11.001. PMID 18096238.
8. ↑ "Improved yield of a ligand-binding GPCR expressed in E. coli for structural studies.". Protein Expr Purif 64 (1): 32–38. 2009. doi:10.1016/j.pep.2008.10.001. PMID 18976711.
9. ↑ "Direct analysis of a GPCR-agonist interaction by surface plasmon resonance.". Eur Biophys J 35 (8): 709–712. 2006. doi:10.1007/s00249-006-0070-x. PMID 16708210.
10. ↑ "Constitutive dimerization of the G-protein coupled receptor, neurotensin receptor 1, reconstituted into phospholipid bilayers.". Biophys. J. 96 (3): 964–973. 2009. doi:10.1016/j.bpj.2008.09.054. PMID 19186134. Bibcode: 2009BpJ....96..964H.
11. ↑ "DNA-templated protein arrays for single-molecule imaging.". Nano Lett. 11 (2): 657–660. 2011. doi:10.1021/nl1037769. PMID 21218848. Bibcode: 2011NanoL..11..657S.

## 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.
* Neurotensin+Receptors at the US National Library of Medicine Medical Subject Headings (MeSH)

* v
* t
* e

Cell surface receptor: G protein-coupled receptors

Class A: Rhodopsin-like

| Neurotransmitter|

| Adrenergic|

* α1 (A
* B
* D)
* α2 (A
* B
* C)
* β1
* β2
* β3

|

Purinergic|

* Adenosine (A1
* A2A
* A2B
* A3)
* P2Y (1
* 2
* 4
* 5
* 6
* 8
* 9
* 10
* 11
* 12
* 13
* 14)

Serotonin|

* (all but 5-HT3) 5-HT1 (A
* B
* D
* E
* F)
* 5-HT2 (A
* B
* C)
* 5-HT (4
* 5A
* 6
* 7)

Other|

* Acetylcholine (M1
* M2
* M3
* M4
* M5)
* Dopamine
* D1
* D2
* D3
* D4
* D5
* GHB receptor
* Histamine
* H1
* H2
* H3
* H4
* Melatonin (1A
* 1B
* 1C)
* TAAR (1
* 2
* 5
* 6
* 8
* 9)

Metabolites and
signaling molecules|

| Eicosanoid|

* CysLT (1
* 2)
* LTB4
* 1
* 2
* FPRL1
* OXE
* Prostaglandin
* DP (1
* 2), EP (1
* 2
* 3
* 4), FP
* Prostacyclin
* Thromboxane

|

Other|

* Bile acid
* Cannabinoid (CB1
* CB2, GPR (18
* 55
* 119))
* EBI2
* Estrogen
* Free fatty acid (1
* 2
* 3
* 4)
* Hydroxycarboxylic acids
* 1
* 2
* 3
* Lysophosphatidic acid (1
* 2
* 3
* 4
* 5
* 6)
* Lysophospholipid (1
* 2
* 3
* 4
* 5
* 6
* 7
* 8)
* Oxoglutarate
* PAF
* Sphingosine-1-phosphate (1
* 2
* 3
* 4
* 5)
* Succinate

Peptide|

| Neuropeptide|

* B/W (1
* 2)
* FF (1
* 2)
* S
* Y (1
* 2
* 4
* 5)
* Neuromedin (B
* U (1
* 2))
* Neurotensin (1
* 2)

|

Other|

* Anaphylatoxin (C3a
* C5a)
* Angiotensin (1
* 2)
* Apelin
* Bombesin
* BRS3
* GRPR
* NMBR)
* Bradykinin (B1
* B2)
* Chemokine
* Cholecystokinin (A
* B)
* Endothelin
* A
* B
* Formyl peptide (1
* 2
* 3)
* FSH
* Galanin (1
* 2
* 3)
* Gonadotropin-releasing hormone (1
* 2)
* Ghrelin
* Kisspeptin
* Luteinizing hormone/choriogonadotropin
* MAS (1
* 1L
* D
* E
* F
* G
* X1
* X2
* X3
* X4)
* Melanocortin (1
* 2
* 3
* 4
* 5)
* MCHR (1
* 2)
* Motilin
* Opioid (Delta
* Kappa
* Mu
* Nociceptin & Zeta, but not Sigma)
* Orexin (1
* 2)
* Oxytocin
* Prokineticin (1
* 2)
* Prolactin-releasing peptide
* Relaxin (1
* 2
* 3
* 4)
* Somatostatin (1
* 2
* 3
* 4
* 5)
* Tachykinin (1
* 2
* 3)
* Thyrotropin
* Thyrotropin-releasing hormone
* Urotensin-II
* Vasopressin (1A
* 1B
* 2)

Miscellaneous|

| Taste, bitter|

* TAS2R
* 1
* 3
* 4
* 5
* 7
* 8
* 9
* 10
* 13
* 14
* 16
* 19
* 20
* 30
* 31
* 38
* 39
* 40
* 41
* 42
* 43
* 45
* 46
* 50
* 60
* Vomeronasal receptor type 1

|

Orphan|

* GPR (1
* 3
* 4
* 6
* 12
* 15
* 17
* 18
* 19
* 20
* 21
* 22
* 23
* 25
* 26
* 27
* 31
* 32
* 33
* 34
* 35
* 37
* 39
* 42
* 44
* 45
* 50
* 52
* 55
* 61
* 62
* 63
* 65
* 68
* 75
* 77
* 78
* 81
* 82
* 83
* 84
* 85
* 87
* 88
* 92
* 101
* 103
* 109A
* 109B
* 119
* 120
* 132
* 135
* 137B
* 139
* 141
* 142
* 146
* 148
* 149
* 150
* 151
* 152
* 153
* 160
* 161
* 162
* 171
* 173
* 174
* 176
* 177
* 182
* 183)

Other|

* Adrenomedullin
* Olfactory
* Opsin (3
* 4
* 5
* 1LW
* 1MW
* 1SW
* RGR
* RRH)
* Protease-activated (1
* 2
* 3
* 4)
* SREB (1
* 2
* 3)

Class B: Secretin-like

| Adhesion|

* ADGRG (1
* 2
* 3
* 4
* 5
* 6
* 7)

|

Orphan|

* GPR (56
* 64
* 97
* 98
* 110
* 111
* 112
* 113
* 114
* 115
* 116
* 123
* 124
* 125
* 126
* 128
* 133
* 143
* 144
* 155
* 157)

Other|

* Brain-specific angiogenesis inhibitor (1
* 2
* 3)
* Cadherin (1
* 2
* 3)
* Calcitonin
* CALCRL
* CD97
* Corticotropin-releasing hormone (1
* 2)
* EMR (1
* 2
* 3)
* Glucagon (GR
* GIPR
* GLP1R
* GLP2R)
* Growth-hormone-releasing hormone
* PACAPR1
* GPR
* Latrophilin (1
* 2
* 3
* ELTD1)
* Methuselah-like proteins
* Parathyroid hormone (1
* 2)
* Secretin
* Vasoactive intestinal peptide (1
* 2)

Class C: Metabotropic glutamate / pheromone

| Taste, sweet|

* TAS1R
* 1
* 2
* 3
* Vomeronasal receptor, type 2

|

Other|

* Calcium-sensing receptor
* GABAB (1
* 2)
* Glutamate receptor (Metabotropic glutamate (1
* 2
* 3
* 4
* 5
* 6
* 7
* 8))
* GPRC6A
* GPR (156
* 158
* 179)
* RAIG (1
* 2
* 3
* 4)

Class F: Frizzled & Smoothened

| Frizzled|

* Frizzled (1
* 2
* 3
* 4
* 5
* 6
* 7
* 8
* 9
* 10)

|

Smoothened|

* Smoothened

* v
* t
* e

Neuropeptide receptors

G protein-coupled receptor|

| Hormone receptors|

| Hypothalamic|

* CRH
* FSH
* LHRH
* TRH
* Somatostatin

|

Pituitary|

* Vasopressin
* 1A
* 1B
* 2
* Oxytocin
* LHCG
* TSH

Other|

* Atrial natriuretic factor
* NPR3
* Calcitonin
* Cholecystokinin
* A
* B
* VIP

Opioid receptors|

* Delta
* Kappa
* Mu
* Nociceptin

Other neuropeptide receptors|

* Angiotensin
* Bradykinin
* B1
* B2
* Tachykinin
* TACR1
* Calcitonin gene-related peptide
* Galanin
* GPCR neuropeptide
* B/W
* FF
* S
* Y
* Neurotensin

Type I cytokine receptor|

* GH
* Prolactin

Enzyme-linked receptor|

* Atrial natriuretic factor
* NPR1
* NPR2

Other|

* Sigma
* 1
* 2

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