Partition ratios for the inactivation of P450 2B6 by the substituted phenyldiaziridines
Assay conditions are described under Materials and Methods. The partition ratio is determined by incubating various concentrations of the inactivator molecules with P450 2B6 in the reconstituted system and allowing the reaction to go to completion. The partition ratio was then calculated from the graph of the percentage of activity remaining as a function of the ratio of the inactivator to enzyme concentration (Kent et al., 2001). The numbers represent the average of the results from three experiments with each substituted phenyl diaziridine.
Substituted Phenyl Diaziridines | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| 4-Methoxy (1a) | 4-Ethoxy (1b) | 3,4-Dimethoxy (1c) | 3-Methyl,4-methoxy (1e) | 3,4,5-Trimethoxy (1f) | |||||
| Partition ratio | 41 | 62 | 9.6 | 29 | 45 | ||||