Neurotensin receptors are transmembrane receptors that bind the neurotransmitter neurotensin. Two of the receptors encoded by the NTSR1 and NTSR2 genes are G protein-coupled receptors, while the third receptor, called NTS3 or Sortilin, is a single transmembrane domain receptor encoded by the gene SORT1. It is a multi-functional protein which also participates in protein sorting. NTSR1’s function is mediated by its binding to Gq alpha subunit family G-proteins, while NTSR2’s signaling pathway is not yet fully understood.
Ligands
Agonists
Peptide Beta-lactotensin (NTS2) 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 Partial agonists derived from SR-48692
Antagonists
Levocabastine (NTS2 selective, also H1 histamine antagonist) SR-48692 (NTS1 selective) 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. It can be purified and analysed in vitro and has been analysed by a number of biophysical techniques such as surface plasmon resonance, FRET and cryo-electron microscopy. 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
References
External links