- The fourth molybdenum containing enzyme mARC: Cloning and involvement in the activation of N-hydroxylated prodrugs
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The recently discovered mammalian molybdoprotein mARC1 is capable of reducing N-hydroxylated compounds. Upon reconstitution with cytochrome b 5 and b5 reductase, benzamidoxime, pentamidine, and diminazene amidoximes, N-hydroxymelagatran, guanoxabenz, and N-hydroxydebrisoquine are efficiently reduced. These substances are amidoxime/N-hydroxyguanidine prodrugs, leading to improved bioavailability compared to the active amidines/guanidines. Thus, the recombinant enzyme allows prediction about in vivo reduction of N-hydroxylated prodrugs. Furthermore, the prodrug principle is not dependent on cytochrome P450 enzymes.
- Gruenewald, Sanja,Wahl, Bettina,Bittner, Florian,Hungeling, Helen,Kanzow, Stephanie,Kotthaus, Joscha,Schwering, Ulrike,Mendel, Ralf R.,Clement, Bernd
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scheme or table
p. 8173 - 8177
(2009/12/07)
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- Therapeutic agents
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O-HALOBENZYLIDENEAMINOGUANIDINES ARE EMPLOYED AS CENTRAL NERVOUS SYSTEM DEPRESSANTS, AS CARDIOVASCULAR DEPRESSANTS, AND/OR AS ANTIDEPRESSANTS FOR OVERCOMING PSYCHIC DEPRESSION.
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- Substituted benzylidene hydrazines for treating hyperglycemia, obesity and inflammation
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Substituted benzylidene hydrazines e.g. N-(4-phenylbenzylidene)-N'-amidino hydrazine and their use as hypoglycemic-antihyperglycemic agents, anti-obesity agents and anti-inflammatory agents.
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