Tahikininski receptor 2

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Tahikininski receptor 2
Identifikatori
Simboli TACR2; NK2R; NKNAR; SKR; TAC2R
Vanjski ID OMIM162321 MGI98477 HomoloGene55548 IUPHAR: NK2 GeneCards: TACR2 Gene
Pregled RNK izražavanja
PBB GE TACR2 214348 at tn.png
podaci
Ortolozi
Vrsta Čovek Miš
Entrez 6865 21337
Ensembl ENSG00000075073 ENSMUSG00000020081
UniProt P21452 Q3KP19
RefSeq (mRNA) NM_001057 XM_974766
RefSeq (protein) NP_001048 XP_979860
Lokacija (UCSC) Chr 10:
70.83 - 70.85 Mb
Chr 10:
61.65 - 61.66 Mb
PubMed pretraga [1] [2]

Tahikininski receptor 2, receptor supstance-K, je protein koji je kod čoveka kodiran TACR2 genom.[1]

Ova gen pripada familiji gena koji dejstvuju kao receptori za tahikinine. Receptorski afiniteti određeni varijacijama 5'-kraja sekvence. Ovi receptori pripadaju familiji proteina koja interaguje sa G proteinima i sadrži sedam hidrofobnih transmembranskih regiona. Ovaj gen kodira receptor za tahikinin neuropeptida supstance K, koji je takođe poznat kao neurokinin A.[1]

Selektivni ligandi[uredi - уреди]

Nekoliko selektivnih liganda je dostupno za NK2, i mada su većina jedinjenja razvijenih do sad peptidi, jedan mali-molekul, antagonist Saredutant je u kliničkim ispitivanjima kao anksiolitik i antidepresant.

Agonisti[uredi - уреди]

  • GR-64349 je potentan i selektivan agonist, EC50 3.7nM. On sadrži 7-aminokiselinski polipeptidni lanac.

Antagonisti[uredi - уреди]

Vidi još[uredi - уреди]

Literatura[uredi - уреди]

Dodatna literatura[uredi - уреди]

  • 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. 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. 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. 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. 

Spoljašnje veze[uredi - уреди]