Metabolism of RPR 106541 by CYP3A4 mutants expressed in E. coli
| Sample Purified Preparations | R-Sulfoxide Formation | S-Sulfoxide Formation | Ratio |
|---|---|---|---|
| nmol/min/nmol CYP | nmol/min/nmol CYP | (R:S-sulfoxide formation) | |
| WT3A4 | 9.93 | 11.10 | 0.89 |
| SRS 2 | |||
| L210A | 2.24 | 9.25 | 0.24 |
| L211A | 4.81 | 8.80 | 0.55 |
| L211F | 8.87 | 9.33 | 0.95 |
| D214E | 10.42 | 10.05 | 1.04 |
| SRS 4 | |||
| I301A | 4.56 | 10.74 | 0.42 |
| F304A | 3.62 | 14.53 | 0.25 |
| A305G | 7.26 | 16.74 | 0.43 |
| A305V | 1.64 | 8.13 | 0.20 |
| T309A | 11.20 | 13.55 | 0.83 |
| SRS 5 | |||
| I369V | 10.86 | 10.06 | 1.08 |
| A370V | 4.77 | 20.98 | 0.23 |
| L373A | 8.07 | 7.18 | 1.12 |
| SRS 6 | |||
| G480Q | 4.02 | 6.57 | 0.61 |
| L479F | 4.90 | 11.80 | 0.42 |
Assays were conducted as described in Materials and Methodssection for Mutant Enzyme Assays. Values are average of duplicate samples.