Comparison of CYP3A4 efficiency when sustained by ABS-CYPORs, using different in vitro systems and substrates
Bold indicates CYPOR variants of this present study with most deviating results compared with those of the Fluc̈k et al. (2010) and Agrawal et al. (2010) studies.
| BTC3A4_POR | kcat/Kma | ||||||
|---|---|---|---|---|---|---|---|
| Debenzylation DBFb | Debenzylation BOMCCc | 6β-Hydroxylation Testosteroned | 1-Hydroxylation Midazolamd | 4-Hydroxylation Midazolamd | 3-Hydroxylation Quinidined | N-Demethylation Erythromycind | |
| WT | 100 | 100 | 100 | 100 | 100 | 100 | 100 |
| Q153R | 60 | 119 | 129 | 94 | 92 | 150 | 76 |
| Y181D | N.D. | N.D. | —e | — | — | — | — |
| D211N | 107 | — | — | — | — | — | — |
| P228L | 95 | 101 | — | — | — | — | — |
| M263V | 119 | — | — | — | — | — | — |
| A287P | 93 | 26 | 17 | 17 | 14 | 3 | N.D. |
| G413S | 115 | 110 | — | — | — | — | — |
| R457H | 10 | N.D. | N.D. | N.D. | N.D. | — | N.D. |
| Y459H | N.D. | N.D. | — | — | — | — | — |
| V492E | N.D. | N.D. | — | — | — | — | — |
| G539R | 30 | — | — | — | — | — | — |
| L565P | N.D. | — | — | — | — | — | — |
| R616X | N.D. | N.D. | — | — | — | — | — |