Table 5.
Kinetic constants of the recombinant hCE-1 and hCE-2 for various substrates
Substrate | hCE-1 |
hCE-2 |
Preference indexa | ||||
---|---|---|---|---|---|---|---|
Km(μM) | kcat(min-1) | kcat/Km(μM-1 min1) | Km(μM) | kcat(min-1) | kcat/Km(μM-1 min-1) | ||
pNPA | 27 ± 1 | 1020 ± 30 | 38 ± 1.4 | 31 ± 2 | 4200 ± 240 | 140 ± 8 | |
(αR)(1R)-cis-A3 | 0.3 ± 0.1 | 0.19 ± 0.06 | 0.71 ± 0.29 | 0.9 ± 0.2 | 0.11 ± 0.03 | 0.14 ± 0.04 | 0.71 |
(αR)(1R)-trans-A3 | 1.7 ± 0.5 | 1.3 ± 0.3 | 0.74 ± 0.03 | 2.5 ± 0.1 | 0.32 ± 0.07 | 0.13 ± 0.03 | 0.76 |
(αR)(1S)-cis-A3 | 1.5 ± 0.5 | 0.09 ± 0.03 | 0.06 ± 0.03 | 1.7 ± 0.3 | 0.10 ± 0.02 | 0.06 ± 0.01 | -0.01 |
(αR)(1S)-trans-A3 | 1.9 ± 0.8 | 1.7 ± 0.4 | 0.87 ± 0.03 | 1.9 ± 0.7 | 2.2 ± 0.3 | 1.2 ± 0.4 | -0.14 |
(αS)(1R)-cis-A3 | 0.3 ± 0.1 | 0.19 ± 0.06 | 0.57 ± 0.03 | 2.5 ± 0.7 | 0.28 ± 0.04 | 0.11 ± 0.03 | 0.71 |
(αS)(1R)-trans-A3 | 0.7 ± 0.4 | 4.4 ± 0.6 | 6.6 ± 0.03 | 2.8 ± 0.1 | 0.48 ± 0.03 | 0.17 ± 0.01 | 1.59 |
(αS)(1S)-cis-A3 | 1.4 ± 0.4 | 0.07 ± 0.02 | 0.05 ± 0.03 | 4.0 ± 0.9 | 0.71 ± 0.21 | 0.18 ± 0.05 | -0.56 |
(αS)(1S)-trans-A3 | 2.4 ± 0.8 | 1.7 ± 0.4 | 0.71 ± 0.03 | 3.8 ± 0.4 | 4.6 ± 0.3 | 1.2 ± 0.1 | -0.23 |
(2R)(αR)-A4 | 0.7 ± 0.2 | 0.10 ± 0.02 | 0.15 ± 0.03 | 0.9 ± 0.3 | 0.51 ± 0.10 | 0.56 ± 0.16 | -0.57 |
(2R)(αS)-A4 | 0.8 ± 0.3 | 0.13 ± 0.02 | 0.16 ± 0.03 | 2.0 ± 0.3 | 3.5 ± 0.7 | 1.8 ± 0.4 | -1.05 |
(2S)(αR)-A4 | —b | — | — | — | — | — | |
(2S)(αS)-A4 | 0.8 ± 0.3 | 0.03 ± 0.01 | 0.04 ± 0.03 | — | — | — | |
A6 | 1.8 ± 0.3 | 0.25 ± 0.06 | 0.14 ± 0.03 | 2.1 ± 0.3 | 0.34 ± 0.05 | 0.16 ± 0.02 | |
A8 | 1.5 ± 0.2 | 0.30 ± 0.05 | 0.20 ± 0.03 | 5.4 ± 1.2 | 0.31 ± 0.05 | 0.06 ± 0.01 | |
Cypermethrin (B3) | 20 ± 2 | 1.3 ± 0.1 | 0.07 ± 0.01 | 9.1 ± 2.0 | 4.0 ± 0.9 | 0.44 ± 0.10 | |
4-Methylumbelliferyl acetatec | 800 | 2.0 | 150 | 60.0 | |||
Cocained | 120 | 390 | 0.0184 | ||||
Heroine | 6300 | 0.069 | 6800 | 0.314 | |||
6-Monoacetylmorphinee | 8300 | 0.000024 | 130 | 0.022 | |||
Meperidinef | 1900 | 0.00035 | |||||
CPT-11g | 42.7 | 0.031 | 0.00073 | 3.4 | 0.160 | 0.047 |