Tahikininski receptor 2
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| Tahikininski receptor 2 | |||||||||||
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| Identifikatori | |||||||||||
| Simboli | TACR2; NK2R; NKNAR; SKR; TAC2R | ||||||||||
| Vanjski ID | OMIM: 162321 MGI: 98477 HomoloGene: 55548 IUPHAR: NK2 GeneCards: TACR2 Gene | ||||||||||
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| Pregled RNK izražavanja | |||||||||||
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| 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
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
- GR-64349 je potentan i selektivan agonist, EC50 3.7nM. On sadrži 7-aminokiselinski polipeptidni lanac.
Antagonisti
- Ibodutant
- Saredutant
- GR-159,897
- MEN-10376 je potentan i selektivan antagonist. On sadrži 7-aminokiselinski polipeptidni lanac.
Vidi još
Literatura
Dodatna literatura
- 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
- „Tachykinin Receptors: NK2”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Arhivirano iz originala na datum 2012-05-31.
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Drugi | Moždano specifični angiogenezni inhibitor (1, 2, 3) • Cadherin (1, 2, 3) • Kalcitonin • CALCRL • CD97 • Kortikotropin-oslobađajući hormon (1, 2) • EMR (1, 2, 3) • Glukagon (GR, GIPR, GLP1R, GLP2R) • Hormon rasta oslobađajući hormon • PACAPR1 • GPR • Latrofilin (1, 2, 3, ELTD1) • Metuselah-slični proteini • Paratiroidni hormon (1, 2) • Sekretin • Vazoaktivni intestinalni peptid (1, 2) |
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glutamat / feromon
Drugi |
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Frizzled / Zaglađeni
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Zaglađeni |
B trdu: peptidi (nrpl/grfl/cytl/horl), receptori (lgic, enzr, gprc, igsr, intg, nrpr/grfr/cytr), itra (adap, gbpr, mapk), calc, lipd, signalni putevi (hedp, wntp, tgfp+mapp, notp, jakp, fsap, hipp, tlrp)
