NTSR1
Available structures
PDBOrtholog search: PDBe RCSB
Identifiers
AliasesNTSR1, NTR, Neurotensin receptor 1, neurotensin receptor 1 (high affinity), NTR1
External IDsOMIM: 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 MbChr 2: 180.5 – 180.54 Mb
PubMed search[3][4]
Wikidata
View/Edit HumanView/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. High-resolution crystal structures have been determined in complex with the peptide full agonist NT8-13, non-peptide full agonist SRI-9829, partial agonist RTI-3a, antagonists / inverse agonists SR-48692 and SR-142948, as well as in the ligand-free state. [7]

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

References

  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000101188 - Ensembl, May 2017
  2. ^ a b c 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. ^ a b "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. 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.