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substance-P receptor; SPR; NK-1 receptor; NK-1R; Tachykinin receptor 1 (TACR1, NK1R, TAC1R)

Function: - receptor for the tachykinin neuropeptide substance P - probably associated with G proteins that activate phosphatidylinositol-Ca+2 second messenger system - rank order of affinity of this receptor to tachykinins is: substance P > substance K > neuromedin-K Structure: belongs to the G-protein coupled receptor 1 family Compartment: cell membrane

Interactions

molecular events

General

glycoprotein G-protein coupled receptor; serpentine receptor

Properties

SIZE: entity length = 407 aa MW = 46 kD COMPARTMENT: cellular membrane MOTIF: exoplasmic domain {1-31} MOTIF: N-glycosylation site {N14} N-glycosylation site {N18} transmembrane domain {32-54} cytoplasmic loop {55-64} transmembrane domain {65-86} exoplasmic loop {87-106} MOTIF: cysteine residue {C105} MODIFICATION: cysteine residue {C180} transmembrane domain {107-128} cytoplasmic loop {129-148} transmembrane domain {149-169} exoplasmic loop {170-194} MOTIF: cysteine residue {C180} MODIFICATION: cysteine residue {C105} transmembrane domain {195-219} MOTIF: binding site SITE: 197-197 FOR-BINDING-OF: CP 96345 cytoplasmic loop {220-248} transmembrane domain {249-270} exoplasmic loop {271-283} transmembrane domain {284-308} cytoplasmic domain {309-407} MOTIF: cysteine residue {C322} MODIFICATION: palmitate COMPARTMENT: membrane

Database Correlations

OMIM 162323 UniProt P25103 Pfam PF00001 Kegg hsa:6869

References

  1. UniProt :accession P25103
  2. Wikipedia; Note: Tachykinin entry http://en.wikipedia.org/wiki/Tachykinin
  3. Gerard NP, Eddy RL Jr, Shows TB, Gerard C. The human neurokinin A (substance K) receptor. Molecular cloning of the gene, chromosome localization, and isolation of cDNA from tracheal and gastric tissues. J Biol Chem. 1990 Nov 25;265(33):20455-62. Erratum in: J Biol Chem. 1991 Jan 15;266(2):1354. PMID: 2173708
  4. Fong TM, Cascieri MA, Yu H, Bansal A, Swain C, Strader CD. Amino-aromatic interaction between histidine 197 of the neurokinin-1 receptor and CP 96345. Nature. 1993 Mar 25;362(6418):350-3. PMID: 8384323
  5. Elling CE, Nielsen SM, Schwartz TW. Conversion of antagonist-binding site to metal-ion site in the tachykinin NK-1 receptor. Nature. 1995 Mar 2;374(6517):74-7. PMID: 7532789