Tachykinin receptor 2

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Tachykinin receptor 2
Identifiers
SymbolsTACR2; NK2R; NKNAR; SKR; TAC2R
External IDsOMIM: 162321 MGI: 98477 HomoloGene: 55548 IUPHAR: NK2 GeneCards: TACR2 Gene
RNA expression pattern
250px
More reference expression data
Orthologs
SpeciesHumanMouse
Entrez686521337
EnsemblENSG00000075073ENSMUSG00000020081
UniProtP21452Q3KP19
RefSeq (mRNA)NM_001057XM_974766
RefSeq (protein)NP_001048XP_979860
Location (UCSC)Chr 10:
70.83 - 70.85 Mb		Chr 10:
61.65 - 61.66 Mb
PubMed search[1][2]

Substance-K receptor is a protein that in humans is encoded by the TACR2 gene.[1]

This gene belongs to a family of genes that function as receptors for tachykinins. Receptor affinities are specified by variations in the 5'-end of the sequence. The receptors belonging to this family are characterized by interactions with G proteins and 7 hydrophobic transmembrane regions. This gene encodes the receptor for the tachykinin neuropeptide substance K, also referred to as neurokinin A.[1]

Selective Ligands

Several selective ligands for NK2 are now available, and although most of the compounds developed so far are peptides, one small-molecule antagonist Saredutant is currently in clinical trials as an anxiolytic and antidepressant.

Agonists

  • GR-64349 - potent and selective agonist, EC50 3.7nM, 7-amino acid polypeptide chain. CAS# 137593-52-3

Antagonists

See also

References

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External links

Further reading

  • Maggi CA, Giuliani S, Patacchini R; et al. (1992). "Tachykinin antagonists inhibit nerve-mediated contractions in the circular muscle of the human ileum. Involvement of neurokinin-2 receptors". Gastroenterology. 102 (1): 88–96. PMID 1370160. 
  • Gerard NP, Gerard C (1991). "Molecular cloning of the human neurokinin-2 receptor cDNA by polymerase chain reaction and isolation of the gene". Ann. N. Y. Acad. Sci. 632: 389–90. doi:10.1111/j.1749-6632.1991.tb33132.x. PMID 1659296. 
  • Cyr C, South V, Saltzman A; et al. (1991). "Cloning, expression of the human substance K receptor, and analysis of its role in mitogenesis". Ann. N. Y. Acad. Sci. 632: 426–7. doi:10.1111/j.1749-6632.1991.tb33144.x. PMID 1659297. 
  • Morten JE, Hopkins B, Powell SJ, Graham A (1992). "Human NK-2 receptor gene maps to chromosome region 10q11-21". Hum. Genet. 88 (2): 200–3. PMID 1661704. 
  • Graham A, Hopkins B, Powell SJ; et al. (1991). "Isolation and characterisation of the human lung NK-2 receptor gene using rapid amplification of cDNA ends". Biochem. Biophys. Res. Commun. 177 (1): 8–16. doi:10.1016/0006-291X(91)91940-E. PMID 1710456. 
  • Gerard NP, Eddy RL, Shows TB, Gerard C (1991). "The human neurokinin A (substance K) receptor. Molecular cloning of the gene, chromosome localization, and isolation of the cDNA from tracheal and gastric tissues". J. Biol. Chem. 266 (2): 1354. PMID 1845990. 
  • Kris RM, South V, Saltzman A; et al. (1991). "Cloning and expression of the human substance K receptor and analysis of its role in mitogenesis". Cell Growth Differ. 2 (1): 15–22. PMID 1848773. 
  • Gerard NP, Eddy RL, Shows TB, Gerard C (1990). "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. 265 (33): 20455–62. PMID 2173708. 
  • Alblas J, van Etten I, Khanum A, Moolenaar WH (1995). "C-terminal truncation of the neurokinin-2 receptor causes enhanced and sustained agonist-induced signaling. Role of receptor phosphorylation in signal attenuation". J. Biol. Chem. 270 (15): 8944–51. doi:10.1074/jbc.270.15.8944. PMID 7721803. 
  • Bhogal N, Donnelly D, Findlay JB (1994). "The ligand binding site of the neurokinin 2 receptor. Site-directed mutagenesis and identification of neurokinin A binding residues in the human neurokinin 2 receptor". J. Biol. Chem. 269 (44): 27269–74. PMID 7961636. 
  • Arkinstall S, Emergy I, Church D; et al. (1994). "Calcium influx and protein kinase C alpha activation mediate arachidonic acid mobilization by the human NK-2 receptor expressed in Chinese hamster ovary cells". FEBS Lett. 338 (1): 75–80. doi:10.1016/0014-5793(94)80119-3. PMID 8307161. 
  • Brunelleschi S, Bordin G, Colangelo D, Viano I (1999). "Tachykinin receptors on human monocytes: their involvement in rheumatoid arthritis". Neuropeptides. 32 (3): 215–23. doi:10.1016/S0143-4179(98)90040-3. PMID 10189055. 
  • Patacchini R, Giuliani S, Turini A; et al. (2000). "Effect of nepadutant at tachykinin NK(2) receptors in human intestine and urinary bladder". Eur. J. Pharmacol. 398 (3): 389–97. doi:10.1016/S0014-2999(00)00346-0. PMID 10862829. 
  • Bellucci F, Carini F, Catalani C; et al. (2002). "Pharmacological profile of the novel mammalian tachykinin, hemokinin 1". Br. J. Pharmacol. 135 (1): 266–74. doi:10.1038/sj.bjp.0704443. PMC 1573107 Freely accessible. PMID 11786503. 
  • Patacchini R, Barbagli G, Palminteri E; et al. (2002). "Tachykinin NK1 and NK2 receptors mediate inhibitory vs excitatory motor responses in human isolated corpus cavernosum and spongiosum". Br. J. Pharmacol. 135 (6): 1351–4. doi:10.1038/sj.bjp.0704650. PMC 1573278 Freely accessible. PMID 11906947. 
  • Candenas ML, Cintado CG, Pennefather JN; et al. (2002). "Identification of a tachykinin NK(2) receptor splice variant and its expression in human and rat tissues". Life Sci. 72 (3): 269–77. doi:10.1016/S0024-3205(02)02240-3. PMID 12427486. 
  • Strausberg RL, Feingold EA, Grouse LH; et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. doi:10.1073/pnas.242603899. PMC 139241 Freely accessible. PMID 12477932. 
  • Bandari PS, Qian J, Oh HS; et al. (2003). "Crosstalk between neurokinin receptors is relevant to hematopoietic regulation: cloning and characterization of neurokinin-2 promoter". J. Neuroimmunol. 138 (1-2): 65–75. doi:10.1016/S0165-5728(03)00096-1. PMID 12742655. 
  • Zhao A, Shea-Donohue T (2003). "PAR-2 agonists induce contraction of murine small intestine through neurokinin receptors". Am. J. Physiol. Gastrointest. Liver Physiol. 285 (4): G696–703. doi:10.1152/ajpgi.00064.2003. PMID 12801882. 
  • Ota T, Suzuki Y, Nishikawa T; et al. (2004). "Complete sequencing and characterization of 21,243 full-length human cDNAs". Nat. Genet. 36 (1): 40–5. doi:10.1038/ng1285. PMID 14702039. 
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This article incorporates text from the United States National Library of Medicine, which is in the public domain.

Class A: Rhodopsin like
α1 (A, B, D) · α2 (A, B, C) · β1 · β2 · β3
Adenosine (A1, A2A, A2B, A3) · P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(all but 5-HT3) 5-HT1 (A, B, D, E, F) · 5-HT2 (A, B, C) · 5-HT (4, 5A, 6, 7)
Other
Acetylcholine (M1, M2, M3, M4, M5) · Dopamine (D1, D2, D3, D4, D5) · Histamine (H1, H2, H3, H4) · Melatonin (1A, 1B, 1C) · TAAR (1, 2, 3, 5, 6, 8, 9)
Metabolites and
signaling molecules
CysLT (1, 2) · LTB4 (1, 2) · FPRL1 · OXE · Prostaglandin (DP (1, 2), EP (1, 2, 3, 4), FP) · Prostacyclin · Thromboxane
Other
Bile acid · Cannabinoid (CB1, CB2, GPR (18, 55, 119)) · EBI2 · Estrogen · Free fatty acid (1, 2, 3, 4) · Lactate  · Lysophosphatidic acid (1, 2, 3, 4, 5, 6)  · Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) · Niacin (1, 2) · Oxoglutarate · PAF · Sphingosine-1-phosphate (1, 2, 3, 4, 5) · Succinate
Peptide
B/W (1, 2) · FF (1, 2) · S · Y (1, 2, 4, 5) · Neuromedin (B, U (1, 2)) · Neurotensin (1, 2)
Other
Miscellaneous
GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 81, 82, 83, 84, 85, 87, 88, 92, 101, 103, 109A, 109B, 119, 120, 132, 135, 137B, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 173, 174, 176, 177, 182, 183)
Other
Class B: Secretin like
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157)
Other
Class C: Metabotropic
glutamate / pheromone
TAS1R (1, 2, 3) · TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 19, 20, 30, 31, 38, 39, 40, 41, 42, 43, 45, 46, 50)
Other
Class F:
Frizzled / Smoothened
Frizzled
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10)
Smoothened
  1. ↑ 1.0 1.1 "Entrez Gene: TACR2 tachykinin receptor 2". 
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