Neurotensin receptors are transmembrane receptors that bind the neurotransmitter neurotensin.[1][2] Two of the receptors encoded by the NTSR1 and NTSR2 genes contain seven transmembrane helices and are G protein coupled. Numerous crystal structures have been reported for the neurotensin receptor 1 (NTS1).[3] The third receptor has a single transmembrane domain and is encoded by the SORT1 gene.
neurotensin receptor 1 (high affinity) | |||||||
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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 | ||||||
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neurotensin receptor 2 | |||||||
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Identifiers | |||||||
Symbol | NTSR2 | ||||||
Alt. symbols | NTR2 | ||||||
NCBI gene | 23620 | ||||||
HGNC | 8040 | ||||||
OMIM | 605538 | ||||||
RefSeq | NM_012344 | ||||||
UniProt | O95665 | ||||||
Other data | |||||||
Locus | Chr. 2 p25.1 | ||||||
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sortilin 1 | |||||||
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Identifiers | |||||||
Symbol | SORT1 | ||||||
Alt. symbols | Gp95, NT3 | ||||||
NCBI gene | 6272 | ||||||
HGNC | 11186 | ||||||
OMIM | 602458 | ||||||
RefSeq | NM_002959 | ||||||
UniProt | Q99523 | ||||||
Other data | |||||||
Locus | Chr. 1 p21.3-1p13.1 | ||||||
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Unusually for GPCRs, NTS1 can be expressed in an active form in the bacteria E. coli.[8] It can be purified and analysed in vitro and has been analysed by a number of biophysical techniques such as surface plasmon resonance,[9] FRET[10] and cryo-electron microscopy.[11] 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 [3]