Neurotensin receptor
Family of proteins
From Wikipedia, the free encyclopedia
Neurotensin receptors are transmembrane receptors that bind the neurotransmitter neurotensin.[1][2] 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.[3] It is a multi-functional protein which also participates in protein sorting.[3] 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.[3]
| Neurotensin receptor 1 (high affinity) | |||||||
|---|---|---|---|---|---|---|---|
3D structure model of the neurotensin receptor NTS1 in complex with NTS(8-13) based on PDB 4GRV | |||||||
| Identifiers | |||||||
| Symbol | NTSR1 | ||||||
| Alt. symbols | NTR | ||||||
| NCBI gene | 4923 | ||||||
| HGNC | 8039 | ||||||
| OMIM | 162651 | ||||||
| RefSeq | NM_002531 | ||||||
| UniProt | P30989 | ||||||
| Other data | |||||||
| Locus | Chr. 20 q13-20q13 | ||||||
| |||||||
Ligands
Agonists
- Peptide
- Beta-lactotensin (NTS2)[4]
- JMV-449
- Neurotensin
- Neuromedin N (NTS1 selective)
- PD-149,163 (NTS1 selective, reduced amide bond 8-13 fragment of neurotensin)
- Non-peptide
Antagonists
- Levocabastine (NTS2 selective, also H1 histamine antagonist)[7]
- SR-48692 (NTS1 selective)[8]
- 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.[9] It can be purified and analysed in vitro and has been analysed by a number of biophysical techniques such as surface plasmon resonance,[10] FRET[11] and cryo-electron microscopy.[12] 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 [5]
