Neurotensin receptor 1 explained

Neurotensin receptor type 1 is a protein that in humans is encoded by the NTSR1 gene.[1] [2] 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.,[3] 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).

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 [4] and regulation of intestinal motility and secretion.[2]

Ligands

See also

Further reading

External links

Notes and References

  1. Laurent P, Clerc P, Mattei MG, Forgez P, Dumont X, Ferrara P, Caput D, Rostene W . Chromosomal localization of mouse and human neurotensin receptor genes . Mammalian Genome . 5 . 5 . 303–6 . May 1994 . 8075503 . 10.1007/BF00389545 . 30418560 . free .
  2. Web site: Entrez Gene: NTSR1 neurotensin receptor 1 (high affinity).
  3. 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 . 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 . 7840143 . 10.1126/sciadv.abe5504 . 33571132 . 2021SciA....7.5504D .
  4. Liu Q, Hazan A, Grinman E, Angulo JA. 3 . Pharmacological activation of the neurotensin receptor 1 abrogates the methamphetamine-induced striatal apoptosis in the mouse brain. Brain Research. 1659 . 148–155. 2017 . 10.1016/j.brainres.2017.01.029. 28130052 . 6405660 .
  5. Peddibhotla S, Hedrick MP, Hershberger P, et al. . 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 . 2013 . 24611085 . 3940307 . 10.1021/ml400176n .