TABLE 1

 N-reduction of vorinostat, benzhydroxamic acid, bufexamac, CP544439, N-hydroxyphenacetin and benzamidoxime by the reconstituted recombinant mARC-system. Biotransformation assays were carried out as described in Materials and Methods

Activities are means ± S.D. of two biologic determinations.

SubstrateKm (mM)vmax (nmol·min−1·mg protein−1)
vorinostatmARC11.45 ± 0.3746.3 ± 5.5
mARC22.73 ± 0.1819.3 ± 0.8
benzhydroxamic acidmARC10.31 ± 0.1173.7 ± 7.0
mARC22.12 ± 0.28313.5 ± 22.5
bufexamacmARC11.09 ± 0.1513.4 ± 1.1
mARC21.07 ± 0.158.2 ± 0.7
CP544439mARC10.25 ± 0.0650.2 ± 4.4
mARC2−/−−/−a
N-hydroxyphenacetinmARC1−/−−/−b
mARC2−/−−/−b
benzamidoximemARC10.63 ± 0.06674.8 ± 25.1
mARC20.54 ± 0.03549.6 ± 12.1

  • ↵a LOQ = 0.9 nmol·min−1·mg protein−1.

  • ↵b LOQ = 3.5 nmol·min−1·mg protein−1.