Alfa-2C adrenergički receptor

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Adrenergički alfa-2C receptor

PDB prikaz baziran na 1hll.
Dostupne strukture
1hll, 1ho9, 1hod, 1hof
Identifikatori
SimboliADRA2C; ADRA2L2; ADRA2RL2; ADRARL2; ALPHA2CAR
Vanjski IDOMIM104250 MGI87936 HomoloGene20170 IUPHAR: α2C-adrenoceptor GeneCards: ADRA2C Gene
Ortolozi
VrstaČovekMiš
Entrez15211553
EnsemblENSG00000184160ENSMUSG00000045318
UniProtP18825Q01337
RefSeq (mRNA)XM_001128592XM_988195
RefSeq (protein)XP_001128592XP_993289
Lokacija (UCSC)n/aChr 5:
35.6 - 35.6 Mb
PubMed pretraga[1][2]

Alfa-2C adrenergički receptor (α2C adrenoceptor, ADRA2C) je alfa-2 adrenergički receptor. On je kodiran humanim ADRA2C genom.[1]

Receptor

Alfa-2-adrenergički receptori su 3 visoko homologna podtipa: alfa2A, alfa2B, i alfa2C. Ti receptori imaju kritičnu ulogu u regulaciji otpuštanja neurotransmitera iz simpatičkih nerva i iz adrenergičkih neurona centralnog nervnog sistema. Ispitivanja na miševima su pokazala da su oba, alfa2A i alfa2C, podtipa neophodna za normalnu presinaptičku kontrolu otpuštanja transmitera iz simpatičkih nerva u srcu i iz centralnih noradrenergičkih neurona. Alfa2A podtip inhibira otpuštanje transmitera na visokim stimulacionim frekvencijama, dok alfa2C podtip modulira neurotransmisiju na niskim nivoima nervne aktivnosti.

Gen

Ovaj gen kodira alfa2C tip receptora. On ne sadrži introne.[1]

Ligandi[uredi - уреди | uredi izvor]

Agonisti[uredi - уреди | uredi izvor]

Antagonisti[uredi - уреди | uredi izvor]

  • JP-1302: selektivan u odnosu na α2A, α2B, α2D[3]
  • spiroksatrin
  • johimbin derivati 9 i 10: >43 puta selektivniji nego za α2A, α2B i α1 tipove[4]
  • N2-[4-(2,3-dihidro-benzo[1,4]dioksin-2-ilmetil)-[1,4]diazepan-1-il]-etil2-fenoksi-nikotinamid[5]

Vidi još[uredi - уреди | uredi izvor]

Reference[uredi - уреди | uredi izvor]

  1. 1,0 1,1 "Entrez Gene: ADRA2C adrenergic, alpha-2C-, receptor". http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=152. 
  2. Crassous PA, Cardinaletti C, Carrieri A, Bruni B, Di Vaira M, Gentili F, Ghelfi F, Giannella M, Paris H, Piergentili A, Quaglia W, Schaak S, Vesprini C, Pigini M (August 2007). "Alpha2-adrenoreceptors profile modulation. 3.1 (R)-(+)-m-nitrobiphenyline, a new efficient and alpha2C-subtype selective agonist". Journal of Medicinal Chemistry 50 (16): 3964–8. PMID 17630725. doi:10.1021/jm061487a. 
  3. Sallinen J, Höglund I, Engström M et al. (February 2007). "Pharmacological characterization and CNS effects of a novel highly selective alpha2C-adrenoceptor antagonist JP-1302". Br. J. Pharmacol. 150 (4): 391–402. PMC 2189732. PMID 17220913. doi:10.1038/sj.bjp.0707005. 
  4. Bavadekar SA, Ma G, Mustafa SM, Moore BM, Miller DD, Feller DR (November 2006). "Tethered yohimbine analogs as selective human alpha2C-adrenergic receptor ligands". J. Pharmacol. Exp. Ther. 319 (2): 739–48. PMID 16873606. doi:10.1124/jpet.106.105981. 
  5. Patel SD, Habeski WM, Min H et al. (October 2008). "Identification and SAR around N2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl2-phenoxy-nicotinamide, a selective alpha2C adrenergic receptor antagonist". Bioorg. Med. Chem. Lett. 18 (20): 5689–93. PMID 18799310. doi:10.1016/j.bmcl.2008.08.055. 

Literatura[uredi - уреди | uredi izvor]

  • Coupry I, Duzic E, Lanier SM (1992). "Factors determining the specificity of signal transduction by guanine nucleotide-binding protein-coupled receptors. II. Preferential coupling of the alpha 2C-adrenergic receptor to the guanine nucleotide-binding protein, Go.". J. Biol. Chem. 267 (14): 9852–7. PMID 1349607. 
  • Chhajlani V, Rangel N, Uhlén S, Wikberg JE (1991). "Identification of an additional gene belonging to the alpha 2 adrenergic receptor family in the human genome by PCR.". FEBS Lett. 280 (2): 241–4. PMID 1849485. doi:10.1016/0014-5793(91)80301-I. 
  • Regan JW, Kobilka TS, Yang-Feng TL et al. (1988). "Cloning and expression of a human kidney cDNA for an alpha 2-adrenergic receptor subtype.". Proc. Natl. Acad. Sci. U.S.A. 85 (17): 6301–5. PMC 281957. PMID 2842764. doi:10.1073/pnas.85.17.6301. 
  • Eason MG, Liggett SB (1993). "Human alpha 2-adrenergic receptor subtype distribution: widespread and subtype-selective expression of alpha 2C10, alpha 2C4, and alpha 2C2 mRNA in multiple tissues.". Mol. Pharmacol. 44 (1): 70–5. PMID 7688069. 
  • Riess O, Thies U, Siedlaczck I et al. (1994). "Precise mapping of the brain alpha 2-adrenergic receptor gene within chromosome 4p16.". Genomics 19 (2): 298–302. PMID 8188260. doi:10.1006/geno.1994.1061. 
  • Klein U, Ramirez MT, Kobilka BK, von Zastrow M (1997). "A novel interaction between adrenergic receptors and the alpha-subunit of eukaryotic initiation factor 2B.". J. Biol. Chem. 272 (31): 19099–102. PMID 9235896. doi:10.1074/jbc.272.31.19099. 
  • Schaak S, Devedjian JC, Cayla C et al. (1998). "Molecular cloning, sequencing and functional study of the promoter region of the human alpha2C4-adrenergic receptor gene.". Biochem. J. 328 ( Pt 2): 431–8. PMC 1218938. PMID 9371698. 
  • DeGraff JL, Gagnon AW, Benovic JL, Orsini MJ (1999). "Role of arrestins in endocytosis and signaling of alpha2-adrenergic receptor subtypes.". J. Biol. Chem. 274 (16): 11253–9. PMID 10196213. doi:10.1074/jbc.274.16.11253. 
  • Prezeau L, Richman JG, Edwards SW, Limbird LE (1999). "The zeta isoform of 14-3-3 proteins interacts with the third intracellular loop of different alpha2-adrenergic receptor subtypes.". J. Biol. Chem. 274 (19): 13462–9. PMID 10224112. doi:10.1074/jbc.274.19.13462. 
  • Hein L, Altman JD, Kobilka BK (2000). "Two functionally distinct alpha2-adrenergic receptors regulate sympathetic neurotransmission.". Nature 402 (6758): 181–4. PMID 10647009. doi:10.1038/46040. 
  • Small KM, Forbes SL, Rahman FF et al. (2000). "A four amino acid deletion polymorphism in the third intracellular loop of the human alpha 2C-adrenergic receptor confers impaired coupling to multiple effectors.". J. Biol. Chem. 275 (30): 23059–64. PMID 10801795. doi:10.1074/jbc.M000796200. 
  • Comings DE, Gade-Andavolu R, Gonzalez N et al. (2001). "Multivariate analysis of associations of 42 genes in ADHD, ODD and conduct disorder.". Clin. Genet. 58 (1): 31–40. PMID 10945659. doi:10.1034/j.1399-0004.2000.580106.x. 
  • Small KM, Wagoner LE, Levin AM et al. (2002). "Synergistic polymorphisms of beta1- and alpha2C-adrenergic receptors and the risk of congestive heart failure.". N. Engl. J. Med. 347 (15): 1135–42. PMID 12374873. doi:10.1056/NEJMoa020803. 
  • Chotani MA, Mitra S, Su BY et al. (2004). "Regulation of alpha(2)-adrenoceptors in human vascular smooth muscle cells.". Am. J. Physiol. Heart Circ. Physiol. 286 (1): H59–67. PMID 12946937. doi:10.1152/ajpheart.00268.2003. 
  • Small KM, Mialet-Perez J, Seman CA et al. (2004). "Polymorphisms of cardiac presynaptic alpha2C adrenergic receptors: Diverse intragenic variability with haplotype-specific functional effects.". Proc. Natl. Acad. Sci. U.S.A. 101 (35): 13020–5. PMC 516511. PMID 15319474. doi:10.1073/pnas.0405074101. 
  • Chotani MA, Mitra S, Eid AH et al. (2005). "Distinct cAMP signaling pathways differentially regulate alpha2C-adrenoceptor expression: role in serum induction in human arteriolar smooth muscle cells.". Am. J. Physiol. Heart Circ. Physiol. 288 (1): H69–76. PMID 15345481. doi:10.1152/ajpheart.01223.2003. 
  • Belfer I, Buzas B, Hipp H et al. (2005). "Haplotype-based analysis of alpha 2A, 2B, and 2C adrenergic receptor genes captures information on common functional loci at each gene.". J. Hum. Genet. 50 (1): 12–20. PMID 15592690. doi:10.1007/s10038-004-0211-y. 
  • Neumeister A, Charney DS, Belfer I et al. (2005). "Sympathoneural and adrenomedullary functional effects of alpha2C-adrenoreceptor gene polymorphism in healthy humans.". Pharmacogenet. Genomics 15 (3): 143–9. PMID 15861038. doi:10.1097/01213011-200503000-00002. 
  • Neumeister A, Drevets WC, Belfer I et al. (2006). "Effects of an alpha 2C-adrenoreceptor gene polymorphism on neural responses to facial expressions in depression.". Neuropsychopharmacology 31 (8): 1750–6. PMID 16407897. doi:10.1038/sj.npp.1301010. 
  • Park JS, Zhang SY, Jo SH et al. (2006). "Common adrenergic receptor polymorphisms as novel risk factors for vasospastic angina.". Am. Heart J. 151 (4): 864–9. PMID 16569551. doi:10.1016/j.ahj.2005.06.009. 

Spoljašnje veze[uredi - уреди | uredi izvor]