Rate constants for inactivation of P-450 2B4 and 2B5 enzymes1-a
| P-450 | 10 μM 2EN | P-450 | 10 μM 2EN |
|---|---|---|---|
| 2B4 WT | 0.12 (46)1-b | 2B5 WT | 0 (98) |
| 2B4 S294T | 0.16 (58) | 2B5 T294S | 0 (98) |
| 2B4 I363V | 0 (83) | 2B5 V363I | 0.06 (89) |
| 2B4 V367A | 0.10 (85) | 2B5 A367V | 0.06 (98) |
| 2B4 QUAD1-c | 0 (91) | 2B5 QUAD1-d | 0.08 (66) |
↵1-a ki values (min−1) are the means of two independent experiments with the indicated enzyme, conducted as described in Experimental Procedures. Zero (0) is used to indicate ki values ≤ 0.01 min−1. Control values (no inhibitor) were all ≤0.02 min−1.
↵1-b Numbers in parentheses represent the percent activity remaining at the zero time point, as determined by linear regression analysis.
↵1-c 2B4 I114F-S294T-I363V-V367A.
↵1-d 2B5 F114I-T294S-V363I-A367V.