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Open Access Articles- Top Results for Tachykinin receptor 2

Tachykinin receptor 2

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Identifiers
SymbolsTACR2 ; NK2R; NKNAR; SKR; TAC2R
External IDsOMIM162321 MGI98477 HomoloGene55548 IUPHAR: 361 ChEMBL: 2327 GeneCards: TACR2 Gene
RNA expression pattern
File:PBB GE TACR2 214348 at tn.png
More reference expression data
Orthologs
SpeciesHumanMouse
Entrez686521337
EnsemblENSG00000075073ENSMUSG00000020081
UniProtP21452P30549
RefSeq (mRNA)NM_001057NM_009314
RefSeq (protein)NP_001048NP_033340
Location (UCSC)Chr 10:
71.16 – 71.18 Mb
Chr 10:
62.25 – 62.27 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

External links

  • "Tachykinin Receptors: NK2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. 

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. PMID 1659296. doi:10.1111/j.1749-6632.1991.tb33132.x. 
  • 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. PMID 1659297. doi:10.1111/j.1749-6632.1991.tb33144.x. 
  • 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. doi:10.1007/bf00206072. 
  • 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. PMID 1710456. doi:10.1016/0006-291X(91)91940-E. 
  • 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. PMID 7721803. doi:10.1074/jbc.270.15.8944. 
  • 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. PMID 8307161. doi:10.1016/0014-5793(94)80119-3. 
  • Brunelleschi S, Bordin G, Colangelo D, Viano I (1999). "Tachykinin receptors on human monocytes: their involvement in rheumatoid arthritis". Neuropeptides 32 (3): 215–23. PMID 10189055. doi:10.1016/S0143-4179(98)90040-3. 
  • 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. PMID 10862829. doi:10.1016/S0014-2999(00)00346-0. 
  • 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. PMC 1573107. PMID 11786503. doi:10.1038/sj.bjp.0704443. 
  • 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. PMC 1573278. PMID 11906947. doi:10.1038/sj.bjp.0704650. 
  • 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. PMID 12427486. doi:10.1016/S0024-3205(02)02240-3. 
  • 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. PMC 139241. PMID 12477932. doi:10.1073/pnas.242603899. 
  • 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. PMID 12742655. doi:10.1016/S0165-5728(03)00096-1. 
  • 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. PMID 12801882. doi:10.1152/ajpgi.00064.2003. 
  • 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. PMID 14702039. doi:10.1038/ng1285. 
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