Neurotensin receptor 1

Last updated
NTSR1
Available structures
PDB Ortholog search: PDBe RCSB
Identifiers
Aliases NTSR1 , NTR, Neurotensin receptor 1, neurotensin receptor 1 (high affinity), NTR1
External IDs OMIM: 162651 MGI: 97386 HomoloGene: 68261 GeneCards: NTSR1
Orthologs
SpeciesHumanMouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

NM_002531

NM_018766

RefSeq (protein)

NP_002522

NP_061236

Location (UCSC) Chr 20: 62.71 – 62.76 Mb Chr 2: 180.14 – 180.19 Mb
PubMed search [3] [4]
Wikidata
View/Edit Human View/Edit Mouse

Neurotensin receptor type 1 is a protein that in humans is encoded by the NTSR1 gene. [5] [6] For a crystal structure of NTS1, see pdb code 4GRV. In addition, high-resolution crystal structures have been determined in complex with the peptide full agonist NTS8-13, the non-peptide full agonist SRI-9829, the partial agonist RTI-3a, and the antagonists / inverse agonists SR48692 and SR142948A, as well as in the ligand-free apo state. [7] , see PDB codes 6YVR (NTSR1-H4X:NTS8–13), 6Z4V (NTSR1-H4bmX:NTS8–13), 6Z8N (NTSR1-H4X:SRI-9829), 6ZA8 (NTSR1-H4X:RTI-3a), 6Z4S (NTSR1-H4bmX:SR48692), 6ZIN (NTSR1-H4X:SR48692), 6Z4Q (NTSR1-H4X: SR142948A), and 6Z66 (apo NTSR1-H4X).

Contents

Function

Neurotensin receptor 1, also called NTR1, belongs to the large superfamily of G-protein coupled receptors and is considered a class-A GPCR. NTSR1 mediates multiple biological processes through modulation by neurotensin, such as low blood pressure, high blood sugar, low body temperature, antinociception, anti-neuronal damage [8] and regulation of intestinal motility and secretion. [6]

Ligands

See also

Related Research Articles

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References

  1. 1 2 3 GRCh38: Ensembl release 89: ENSG00000101188 - Ensembl, May 2017
  2. 1 2 3 GRCm38: Ensembl release 89: ENSMUSG00000027568 - Ensembl, May 2017
  3. "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. Laurent P, Clerc P, Mattei MG, Forgez P, Dumont X, Ferrara P, Caput D, Rostene W (May 1994). "Chromosomal localization of mouse and human neurotensin receptor genes". Mammalian Genome. 5 (5): 303–6. doi: 10.1007/BF00389545 . PMID   8075503. S2CID   30418560.
  6. 1 2 "Entrez Gene: NTSR1 neurotensin receptor 1 (high affinity)".
  7. Deluigi M, Klipp A, Klenk C, Merklinger L, Eberle SA, Morstein L, Heine P, Mittl PR, Ernst P, Kamenecka TM, He Y, Vacca S, Egloff P, Honegger A, Plückthun A (January 2021). "Complexes of the neurotensin receptor 1 with small-molecule ligands reveal structural determinants of full, partial, and inverse agonism". Science Advances. 7 (5): eabe5504. Bibcode:2021SciA....7.5504D. doi:10.1126/sciadv.abe5504. PMC   7840143 . PMID   33571132.
  8. Liu Q, Hazan A, Grinman E, et al. (2017). "Pharmacological activation of the neurotensin receptor 1 abrogates the methamphetamine-induced striatal apoptosis in the mouse brain". Brain Research. 1659: 148–155. doi:10.1016/j.brainres.2017.01.029. PMID   28130052. S2CID   6405660.
  9. Peddibhotla S, Hedrick MP, Hershberger P, et al. (2013). "Discovery of ML314, a Brain Penetrant Non-Peptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor". ACS Med Chem Lett. 4 (9): 846–851. doi:10.1021/ml400176n. PMC   3940307 . PMID   24611085.

Further reading

This article incorporates text from the United States National Library of Medicine, which is in the public domain.