Alfa-2A adrenergički receptor
Alfa-2A adrenergički receptor (α2A adrenoceptor, ADRA2A) je alfa-2 adrenergički receptor. On je kodiran humanim ADRA2A 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 alfa2A tip receptora. On ne sadrži introne.[1]
Selektivni ligandi
[уреди | уреди извор]Agonisti
[уреди | уреди извор]Antagonisti
[уреди | уреди извор]Vidi još
[уреди | уреди извор]Reference
[уреди | уреди извор]Literatura
[уреди | уреди извор]- M, Perälä; Hirvonen H; Kalimo H (1993). „Differential expression of two alpha 2-adrenergic receptor subtype mRNAs in human tissues.”. Brain Res. Mol. Brain Res. 16 (1-2): 57—63. PMID 1334200. doi:10.1016/0169-328X(92)90193-F.
- Surprenant A, Horstman DA, Akbarali H, Limbird LE (1992). „A point mutation of the alpha 2-adrenoceptor that blocks coupling to potassium but not calcium currents.”. Science. 257 (5072): 977—80. PMID 1354394. doi:10.1126/science.1354394.
- Handy DE, Gavras H (1992). „Promoter region of the human alpha 2A adrenergic receptor gene.”. J. Biol. Chem. 267 (33): 24017—22. PMID 1385431.
- Suryanarayana S, Daunt DA, Von Zastrow M, Kobilka BK (1991). „A point mutation in the seventh hydrophobic domain of the alpha 2 adrenergic receptor increases its affinity for a family of beta receptor antagonists.”. J. Biol. Chem. 266 (23): 15488—92. PMID 1678390.
- Wang CD, Buck MA, Fraser CM (1991). „Site-directed mutagenesis of alpha 2A-adrenergic receptors: identification of amino acids involved in ligand binding and receptor activation by agonists.”. Mol. Pharmacol. 40 (2): 168—79. PMID 1678850.
- 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.
- CA, Guyer; Horstman DA; Wilson AL (1990). „Cloning, sequencing, and expression of the gene encoding the porcine alpha 2-adrenergic receptor. Allosteric modulation by Na+, H+, and amiloride analogs.”. J. Biol. Chem. 265 (28): 17307—17. PMID 2170371.
- Fraser CM, Arakawa S, McCombie WR, Venter JC (1989). „Cloning, sequence analysis, and permanent expression of a human alpha 2-adrenergic receptor in Chinese hamster ovary cells. Evidence for independent pathways of receptor coupling to adenylate cyclase attenuation and activation.”. J. Biol. Chem. 264 (20): 11754—61. PMID 2568356.
- BK, Kobilka; Matsui H; Kobilka TS (1987). „Cloning, sequencing, and expression of the gene coding for the human platelet al.pha 2-adrenergic receptor.”. Science. 238 (4827): 650—6. PMID 2823383. doi:10.1126/science.2823383.
- Lynch CJ, Steer ML (1981). „Evidence for high and low affinity alpha 2-receptors. Comparison of [3H]norepinephrine and [3H]phentolamine binding to human platelet membranes.”. J. Biol. Chem. 256 (7): 3298—303. PMID 6259160.
- Eason MG, Moreira SP, Liggett SB (1995). „Four consecutive serines in the third intracellular loop are the sites for beta-adrenergic receptor kinase-mediated phosphorylation and desensitization of the alpha 2A-adrenergic receptor.”. J. Biol. Chem. 270 (9): 4681—8. PMID 7876239. doi:10.1074/jbc.270.9.4681.
- Grassie MA, Milligan G (1995). „Analysis of the relative interactions between the alpha 2C10 adrenoceptor and the guanine-nucleotide-binding proteins G(o)1 alpha and Gi 2 alpha following co-expression of these polypeptides in rat 1 fibroblasts.”. Biochem. J. 306 ( Pt 2): 525—30. PMC 1136549
. PMID 7887906.
- L, Shilo; Sakaue M; Thomas JM (1994). „Enhanced transcription of the human alpha 2A-adrenergic receptor gene by cAMP: evidence for multiple cAMP responsive sequences in the promoter region of this gene.”. Cell. Signal. 6 (1): 73—82. PMID 8011430. doi:10.1016/0898-6568(94)90062-0.
- P, Valet; Senard JM; Devedjian JC (1993). „Characterization and distribution of alpha 2-adrenergic receptors in the human intestinal mucosa.”. J. Clin. Invest. 91 (5): 2049—57. PMC 288203
- J, Alblas; EJ, van Corven; Hordijk PL (1993). „Gi-mediated activation of the p21ras-mitogen-activated protein kinase pathway by alpha 2-adrenergic receptors expressed in fibroblasts.”. J. Biol. Chem. 268 (30): 22235—8. PMID 8226727.
- 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, Bétuing; Daviaud D; Pagès C (1998). „Gbeta gamma-independent coupling of alpha2-adrenergic receptor to p21(rhoA) in preadipocytes.”. J. Biol. Chem. 273 (25): 15804—10. PMID 9624180. doi:10.1074/jbc.273.25.15804.
- 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.
- S, Schaak; Cussac D; Cayla C (2000). „Alpha(2) adrenoceptors regulate proliferation of human intestinal epithelial cells.”. Gut. 47 (2): 242—50. PMC 1728001
Spoljašnje veze
[уреди | уреди извор]- „α2A-adrenoceptor”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Архивирано из оригинала 02. 04. 2015. г.
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