[摘要]：The recently discovered mammalian molybdoprotein mARC1 is capable of reducing N-hydroxylated compds. Upon reconstitution with cytochrome b5 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 redn. of N-hydroxylated prodrugs. Furthermore, the prodrug principle is not dependent on cytochrome P 450 enzymes.
