Table 1

Rate constants for inactivation of P-450 2B4 and 2B5 enzymes1-a

P-45010 μM 2ENP-45010 μM 2EN
2B4 WT0.12  (46)1-b 2B5 WT0  (98)
2B4 S294T0.16  (58)2B5 T294S0  (98)
2B4 I363V0  (83)2B5 V363I0.06  (89)
2B4 V367A0.10  (85)2B5 A367V0.06  (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.