Alfa-2C adrenergički receptor
| Adrenergički alfa-2C receptor | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
 PDB prikaz baziran na 1hll. | |||||||||||
| Dostupne strukture | |||||||||||
| 1hll, 1ho9, 1hod, 1hof | |||||||||||
| Identifikatori | |||||||||||
| Simboli | ADRA2C; ADRA2L2; ADRA2RL2; ADRARL2; ALPHA2CAR | ||||||||||
| Vanjski ID | OMIM: 104250 MGI: 87936 HomoloGene: 20170 IUPHAR: α2C-adrenoceptor GeneCards: ADRA2C Gene | ||||||||||
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| Ortolozi | |||||||||||
| Vrsta | Čovek | Miš | |||||||||
| Entrez | 152 | 11553 | |||||||||
| Ensembl | ENSG00000184160 | ENSMUSG00000045318 | |||||||||
| UniProt | P18825 | Q01337 | |||||||||
| RefSeq (mRNA) | XM_001128592 | XM_988195 | |||||||||
| RefSeq (protein) | XP_001128592 | XP_993289 | |||||||||
| Lokacija (UCSC) | n/a | Chr 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
Agonisti
- (R)-3-Nitrobifenilin (takođe slab antagonist α2A i α2B)[2]
Antagonisti
- 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
Reference
- ^ а б „Entrez Gene: ADRA2C adrenergic, alpha-2C-, receptor”.
- ^ 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 (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.
- ^ J, Sallinen; Höglund I; Engström M (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. - ^ Bavadekar SA, Ma G, Mustafa SM, Moore BM, Miller DD, Feller DR (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.
- ^ SD, Patel; Habeski WM; Min H (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
- 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.
- JW, Regan; Kobilka TS; Yang-Feng TL (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.
- O, Riess; Thies U; Siedlaczck I (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.
- S, Schaak; Devedjian JC; Cayla C (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.
- KM, Small; Forbes SL; Rahman FF (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.
- DE, Comings; Gade-Andavolu R; Gonzalez N (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.
- KM, Small; Wagoner LE; Levin AM (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.
- MA, Chotani; Mitra S; Su BY (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.
- KM, Small; Mialet-Perez J; Seman CA (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.
- MA, Chotani; Mitra S; Eid AH (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.
- I, Belfer; Buzas B; Hipp H (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.
- A, Neumeister; Charney DS; Belfer I (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.
- A, Neumeister; Drevets WC; Belfer I (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.
- JS, Park; Zhang SY; Jo SH (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
- „α2C-adrenoceptor”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
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PDB Galerija
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1hll: NMR struktura T3-I2, 32 ostatka dugog peptida sa alfa-2A adrenergičkog receptora -
1ho9: 20 najboljih NMR konformera D130I mutanta T3-I2, 32 ostatka dugog peptida sa alfa-2A adrenergičkog receptora -
1hod: NMR struktura D130I mutanta T3-I2,32 ostatka dugog peptida sa alfa-2A adrenergičkog receptora -
1hof: NMR struktura T3-I2, 32 ostatka dugog peptida sa alfa-2A adrenergičkog receptora
