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Cytochroma P450 CYP2C8 (-atis, n.) (Numerus EC: 1.14.14.1) est haemoproteinum oxidoreductasisque et pars gregis cytochromatum P450.

Cytochroma P450 CYP2C8.

Natura structuraque biochemicaRecensere

Cytochroma P450 CYP2C8 abunde in iecore reperiuntur[1]. CYP2C8 est et polypeptidum et haemoproteinum, quod ex 476 acidis aminicis constitutum est. Plus quam 100 medicamenta substrata nota sunt. Nonnullae substantiae etiam, ut Gemfibrozilum vel Clopidogrelum, gravissime CYP2C8 inhibere possunt.

GeneticaRecensere

Nomen geni cytochromatis est CYP2C8 locus cuius geneticus in chromosomate 10 humano locatus est (cytogeneticus: 10q23.33 / coordinatae genomicae: chr10:96,796,884-96,829,159)[2]. Varia allela descripta sunt (CYP2C8*2, CYP2C8*3, CYP2C8*4, CYP2C8*5)[3][4]. Plus quam 20 singularis nucleotidi polymorphismorum (SNP) notae sunt[5]:

Polymorphismi CYP2C8
Polyphormismus Locus
nucleotidi
Nota
CYP2C8*2 I269F
CYP2C8*3 R139K
K399R
G416A
A1196G
CYP2C8*4 I264M
CYP2C8*5 T130N
E154D
N193K
K249R
L390S
P404A
H411L

Pharmaca ad CYP2C8 relataRecensere

Adhuc solum Rifampicinum inductor notum est.

Pharmaca relata ad CYP2C8[6][7].
Substrati Inhibitores[8] Inductores[9]
  • Chemotherapeutica contra malariam
    • Amodiaquinum
    • Chloroquinum
  • Antidiabetica
    • Repaglinidum
    • Rosiglitazonum
  • Analgetica
  • Buprenorphinum
  • Inhibitor CSE
    • Cerivastatinum
  • Dasabuvirum
  • Enzalutamidum
  • Loperamidum
  • Montelukastum
  • Paclitaxelum[10]
  • Sorafenibum
  • Torasemidum
  • Antibiotica
    • Cotrimoxazolum
    • Trimethoprimum
  • Clopidogrelum (forte)
  • Deferasiroxum
  • Gemfibrozilum (forte)
  • Leflunomidum
  • Montelukastum
  • Teriflunomidum
  • Lapatinibum
  • Quercetinum

NotaeRecensere

  1. Backman J. T., Filppula A. M., Niemi M., Neuvonen P. J. (2016). "Role of Cytochrome P450 2C8 in Drug Metabolism and Interactions". Pharmacol Rev 68 (1): 168-241 
  2. [https://www.rcsb.org/pdb/gene/CYP2C8 PDB proteinorum collegium datis (Protein Data Bank)
  3. Wu X., Zuo J., Guo T., Yuan L. (2013). "CYP2C8 polymorphism frequencies among Han, Uighur, Hui, and Mongolian Chinese populations". Genet Test Mol Biomarkers 17 (2): 104-8 
  4. Nakajima M., Fujiki Y., Noda K., Ohtsuka H., Ohkuni H., Kyo S., Inoue M., Kuroiwa Y., Yokoi T. (2003). "Genetic polymorphisms of CYP2C8 in Japanese population". Drug Metab Dispos 31 (6): 687-90 
  5. Pechandova K., Buzkova H., Matouskova O., Perlik F., Slanar O. (2012). "Genetic polymorphisms of CYP2C8 in the Czech Republic". Genet Test Mol Biomarkers 16 (7): 812-6 
  6. Cozza KL, Armstrong SC (2001). The Cytochrome P450 System. Drug Interaction Principles for Medical Practice. Washington, DC: American Psychiatric Publishing
  7. Preskorn SH (1996). Clinical Pharmacology of Selective Serotonin Reuptake Inhibitors. 1st ed.: Professional Communications, Inc.
  8. Inhibitor cum subtratorum effectibus fortioribus
  9. Inductor cum subtratorum effectibus minoribus
  10. Rodríguez-Antona C. (2010). "Pharmacogenomics of paclitaxel". Pharmacogenomics 11 (5): 621-3 

Nexus externiRecensere