Neurotensin receptor


Neurotensin receptors are transmembrane receptors that bind the neurotransmitter neurotensin. Two of the receptors encoded by the and genes contain seven transmembrane helices and are G protein coupled. Numerous crystal structures have been reported for the neurotensin receptor 1. The third receptor has a single transmembrane domain and is encoded by the gene.

Ligands

Agonists

;Peptide
;Non-peptide

Antagonists

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