Table 1.
Kinetics of CYP2D6 supported by POR variants, using EOMCC, dextromethorphan and bufuralol as substrates
| EOMCC | ||||
|---|---|---|---|---|
|
| ||||
| POR | Vmax ± SEM | Km ± SEM | Vmax / Km | % WT |
| WT | 3.8 ± 0.50 | 35.1 ± 2.11 | 0.111 | 100 |
| Q153R | 4.2 ± 0.04 | 29.6 ± 3.68 | 0.142 | 128* |
| A503V | 2.6 ± 0.51 | 27.4 ± 3.40 | 0.095 | 85* |
| A287P | NC | NC | NC | NC |
| R457H | NC | NC | NC | NC |
| Dextromethorphan | ||||
|---|---|---|---|---|
|
| ||||
| POR | Vmax ± SEM | Km ± SEM | Vmax / Km | % WT |
| WT | 9.3 ± 0.35 | 1.6 ± 0.67 | 5.813 | 100 |
| Q153R | 13.8 ± 2.27 | 1.2 ± 0.56 | 11.500 | 198* |
| A503V | 6.5 ± 0.86 | 1.8 ± 0.34 | 3.611 | 62* |
| A287P | 2.2 ± 0.41 | 1.4 ± 0.10 | 1.571 | 27* |
| R457H | NC | NC | NC | NC |
| Bufuralol | ||||
|---|---|---|---|---|
|
| ||||
| POR | Vmax ± SEM | Km ± SEM | Vmax / Km | % WT |
| WT | 24.4 ± 1.82 | 5.0 ± 0.26 | 4.880 | 100 |
| Q153R | 35.0 ± 6.18 | 4.7 ± 0.43 | 7.447 | 153* |
| A503V | 16.4 ± 2.29 | 6.4 ± 1.16 | 2.563 | 53* |
| A287P | 8.7 ± 0.46 | 7.5 ± 0.86 | 1.160 | 24* |
| R457H | NC | NC | NC | NC |
Note: The asterisk (*) indicates P < 0.05 for comparisons of WT and variant POR using ANOVA followed by post hoc test. NC = data could not be calculated.