Toxicology 2

Biotransformation: Bioactivation vs Detoxification

Cytochrome P450

  • Group of hemoproteins
  • Xenobiotic binds to cytochrome at a substrate binding site
  • Alters conformation to allow transfer of electrons to the heme from NADPH via a nearby flavoprotein (NADPH cytochrome P450 reductase)
  • Reduction of heme iron from its normal ferric state to the ferrous state allows a molecule of oxygen to bind
  • The xenobiotic-cytochrome-oxygen receives another electron resulting in splitting of the molecular oxygen
  • One atom oxidises the chemical, the other picks up protons to form water

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