Table 1. Inhibition constants (Ki,app), Hill coefficients (h) and apparent dissociation constants derived from DSF experiments (KD,app) for wild-type NQO1 and the variants p.R139W and p.P187S.
Inhibitor | Wild-type NQO1 | p.R139W | p.P187S |
---|---|---|---|
Ki,app | |||
Dicoumarol | 1.15 ± 0.51 nM | 2.98 ± 1.04 nM | 10.95 ± 1.11 nM2 |
Nicotinamide | 14.01 ± 4.34 mM | 13.55 ± 3.22 mM | nd |
Resveratrol | 375 ±129 μM | nd | nd |
Hill coefficient (h) | |||
Dicoumarol | 0.56 ± 0.09 | 0.51 ± 0.09 | Inactive |
Dicoumarol + excess FAD | 0.47 ± 0.091,2 | 0.60 ± 0.042 | 0.48 ± 0.022 |
Resveratrol | 0.89 ± 0.08 | 0.85 ± 0.12 | nd |
Nicotinamide | 0.91 ± 0.06 | 0.92 ± 0.05 | nd |
KD,app | |||
Dicoumarol | 54 ± 4 nM | 66 ± 11 nM | 1100 ± 280 nM |
Nicotinamide | 6.0 ± 0.9 mM | 18.2 ± 5.2 mM | nd |
h is the mean value from three separate linear Hill plots ± the standard deviation of this mean.
Previously reported and included here for comparison [39].
In excess FAD (10×[active site]).
nd, not determined.