Alfa-1A adrenergički receptor

Из Википедије, слободне енциклопедије
Adrenergički alfa-1A receptor
Identifikatori
Simboli ADRA1A; ADRA1C; ADRA1L1; ALPHA1AAR
Vanjski ID OMIM104221 MGI104773 HomoloGene68078 IUPHAR: α1A-adrenoceptor GeneCards: ADRA1A Gene
Pregled RNK izražavanja
PBB GE ADRA1A 211492 s at tn.png
PBB GE ADRA1A 211490 at tn.png
PBB GE ADRA1A 211491 at tn.png
podaci
Ortolozi
Vrsta Čovek Miš
Entrez 148 11549
Ensembl ENSG00000120907 ENSMUSG00000045875
UniProt P35348 Q8BUE5
RefSeq (mRNA) NM_000680 NM_013461
RefSeq (protein) NP_000671 NP_038489
Lokacija (UCSC) Chr 8:
26.66 - 26.78 Mb
Chr 14:
65.59 - 65.69 Mb
PubMed pretraga [1] [2]

Alfa-1A adrenergički receptor (α1A adrenoreceptor, ADRA1A, alfa-1C adrenergički receptor) je alfa-1 adrenergički receptor. On je kodiran ADRA1A humanim genom.[1][2]

Receptor[уреди]

Postoje 3 tipa alfa-1 adrenergičkog receptora: alfa-1A, -1B i -1D, svi od kojih prenose signal kroz Gq/11 familiju G-proteina. Različiti podtipovi pokazuju različite oblike aktivacije.

Gen[уреди]

Alternativno splajsovanje ovog gena proizvodi različite transkriptne varijante, koje kodiraju četiri izoforme sa distinktinim C-terminusima. One imaju slična svojstva u pogledu vezivanja liganda.[1]

Ligandi[уреди]

Agonisti[уреди]

  • 6-(5-fluoro-2-pirimidin-5-il-fenil)-6,7-dihidro-5H-pirolo[1,2-a]imidazol EC50 = 1nM, Emax = 65%; dobra selektivnost u odnosu na α1B, α1D i α2A tipove[3]
  • više parcijalnih agonista sa imidazolnom osnovom[4][5]

Antagonisti[уреди]

Vidi još[уреди]

Literatura[уреди]

  1. 1,0 1,1 „Entrez Gene: ADRA1A adrenergic, alpha-1A-, receptor”. 
  2. Langer SZ (1998). „Nomenclature and state of the art on alpha1-adrenoceptors”. Eur. Urol. 33 Suppl 2: 2—6. doi:10.1159/000052227. PMID 9556189. 
  3. Roberts LR, Fish PV, Ian Storer R, Whitlock GA (2009). „6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective alpha(1A) adrenoceptor partial agonists”. Bioorg. Med. Chem. Lett. 19 (11): 3113. doi:10.1016/j.bmcl.2009.03.166. PMID 19414260. 
  4. Whitlock GA, Brennan PE, Roberts LR, Stobie A (2009). „Potent and selective alpha(1A) adrenoceptor partial agonists-Novel imidazole frameworks”. Bioorg. Med. Chem. Lett. 19 (11): 3118. doi:10.1016/j.bmcl.2009.03.162. PMID 19394220. 
  5. Roberts LR, Bryans J, Conlon K, McMurray G, Stobie A, Whitlock GA (2008). „Novel 2-imidazoles as potent, selective and CNS penetrant alpha1A adrenoceptor partial agonists”. Bioorg. Med. Chem. Lett. 18 (24): 6437—40. doi:10.1016/j.bmcl.2008.10.066. PMID 18980842. 

Further reading[уреди]

  • Mátyus P, Horváth K (1998). „Alpha-adrenergic approach in the medical management of benign prostatic hyperplasia.”. Med Res Rev. 17 (6): 523—35. doi:10.1002/(SICI)1098-1128(199711)17:6<523::AID-MED2>3.0.CO;2-3. PMID 9359081. 
  • Hoehe MR, Berrettini WH, Schwinn DA, Hsieh WT (1993). „A two-allele PstI RFLP for the alpha-1C adrenergic receptor gene (ADRA1C).”. Hum. Mol. Genet. 1 (5): 349. doi:10.1093/hmg/1.5.349-a. PMID 1363873. 
  • Schwinn DA, Lomasney JW, Lorenz W; et al. (1990). „Molecular cloning and expression of the cDNA for a novel alpha 1-adrenergic receptor subtype.”. J. Biol. Chem. 265 (14): 8183—9. PMID 1970822. 
  • Hirasawa A, Shibata K, Horie K; et al. (1995). „Cloning, functional expression and tissue distribution of human alpha 1c-adrenoceptor splice variants.”. FEBS Lett. 363 (3): 256—60. doi:10.1016/0014-5793(95)00330-C. PMID 7737411. 
  • Diehl NL, Shreeve SM (1995). „Identification of the alpha 1c-adrenoceptor in rabbit arteries and the human saphenous vein using the polymerase chain reaction.”. Eur. J. Pharmacol. 268 (3): 393—8. PMID 7805763. 
  • Schwinn DA, Johnston GI, Page SO; et al. (1995). „Cloning and pharmacological characterization of human alpha-1 adrenergic receptors: sequence corrections and direct comparison with other species homologues.”. J. Pharmacol. Exp. Ther. 272 (1): 134—42. PMID 7815325. 
  • Weinberg DH, Trivedi P, Tan CP; et al. (1994). „Cloning, expression and characterization of human alpha adrenergic receptors alpha 1a, alpha 1b and alpha 1c.”. Biochem. Biophys. Res. Commun. 201 (3): 1296—304. doi:10.1006/bbrc.1994.1845. PMID 8024574. 
  • Forray C, Bard JA, Wetzel JM; et al. (1994). „The alpha 1-adrenergic receptor that mediates smooth muscle contraction in human prostate has the pharmacological properties of the cloned human alpha 1c subtype.”. Mol. Pharmacol. 45 (4): 703—8. PMID 8183249. 
  • Hirasawa A, Horie K, Tanaka T; et al. (1993). „Cloning, functional expression and tissue distribution of human cDNA for the alpha 1C-adrenergic receptor.”. Biochem. Biophys. Res. Commun. 195 (2): 902—9. doi:10.1006/bbrc.1993.2130. PMID 8396931. 
  • Tseng-Crank J, Kost T, Goetz A; et al. (1996). „The alpha 1C-adrenoceptor in human prostate: cloning, functional expression, and localization to specific prostatic cell types.”. Br. J. Pharmacol. 115 (8): 1475—85. PMC 1908895слободно за читање. PMID 8564208. 
  • Shibata K, Hirasawa A, Moriyama N; et al. (1997). „Alpha 1a-adrenoceptor polymorphism: pharmacological characterization and association with benign prostatic hypertrophy.”. Br. J. Pharmacol. 118 (6): 1403—8. PMC 1909672слободно за читање. PMID 8832064. 
  • Chang DJ, Chang TK, Yamanishi SS; et al. (1998). „Molecular cloning, genomic characterization and expression of novel human alpha1A-adrenoceptor isoforms.”. FEBS Lett. 422 (2): 279—83. doi:10.1016/S0014-5793(98)00024-6. PMID 9490024. 
  • Daniels DV, Gever JR, Jasper JR; et al. (1999). „Human cloned alpha1A-adrenoceptor isoforms display alpha1L-adrenoceptor pharmacology in functional studies.”. Eur. J. Pharmacol. 370 (3): 337—43. doi:10.1016/S0014-2999(99)00154-5. PMID 10334511. 
  • Cogé F, Guenin SP, Renouard-Try A; et al. (1999). „Truncated isoforms inhibit [3H]prazosin binding and cellular trafficking of native human alpha1A-adrenoceptors.”. Biochem. J. 343 Pt 1: 231—9. doi:10.1042/0264-6021:3430231. PMC 1220546слободно за читање. PMID 10493934. 
  • Rudner XL, Berkowitz DE, Booth JV; et al. (1999). „Subtype specific regulation of human vascular alpha(1)-adrenergic receptors by vessel bed and age.”. Circulation. 100 (23): 2336—43. PMID 10587338. 
  • Ballou LM, Cross ME, Huang S; et al. (2000). „Differential regulation of the phosphatidylinositol 3-kinase/Akt and p70 S6 kinase pathways by the alpha(1A)-adrenergic receptor in rat-1 fibroblasts.”. J. Biol. Chem. 275 (7): 4803—9. doi:10.1074/jbc.275.7.4803. PMID 10671514. 
  • Keffel S, Alexandrov A, Goepel M, Michel MC (2000). „alpha(1)-adrenoceptor subtypes differentially couple to growth promotion and inhibition in Chinese hamster ovary cells.”. Biochem. Biophys. Res. Commun. 272 (3): 906—11. doi:10.1006/bbrc.2000.2850. PMID 10860850. 
  • Richman JG, Brady AE, Wang Q; et al. (2001). „Agonist-regulated Interaction between alpha2-adrenergic receptors and spinophilin.”. J. Biol. Chem. 276 (18): 15003—8. doi:10.1074/jbc.M011679200. PMID 11154706. 
  • Shibata K, Katsuma S, Koshimizu T; et al. (2003). „alpha 1-Adrenergic receptor subtypes differentially control the cell cycle of transfected CHO cells through a cAMP-dependent mechanism involving p27Kip1.”. J. Biol. Chem. 278 (1): 672—8. doi:10.1074/jbc.M201375200. PMID 12409310. 

Spoljašnje veze[уреди]

  • „α1A-adrenoceptor”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.