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  • Title: [Factors regulating mono-oxygenase induction by phenobarbital xenobiotics].
    Author: Tsyrlov IB, Gerasimov KE.
    Journal: Ukr Biokhim Zh (1978); 1987; 59(1):39-44. PubMed ID: 3810888.
    Abstract:
    The main nongenetic factors are revealed which regulate the catalytic activity and substrate specificity of microsomal monooxygenases preinduced by phenobarbital-type xenobiotics (barbituric acid and pyrazolone derivatives). It is shown that a blockage of the primary microsomal metabolism of an inducer is the obligate condition for its inductive effect on the content and activity of cytochrome P-450. On this basis it is practicable to convert the typical monooxygenase substrates into inducers of the enzyme biosynthesis by the blockage of the molecule site subjected to monooxygenation. A model is suggested which shows the phenobarbital participation in the formation of the specific configuration of the active site of cytochrome P-450 synthesized; the latter catalyzes the oxidation of a number of substrates by the way typical of inducer itself.
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