Nor-LAAM from LAAM | Dinor-LAAM from LAAM | Dinor-LAAM from Nor-LAAM | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Km1 | Vmax1 | Vmax1/Km1 | Km2 | Vmax2 | Km1 | Vmax1 | Vmax1/Km1 | Km2 | Vmax2 | Km1 | Vmax1 | Vmax1/Km1 | Km2 | Vmax2 | |
μM | nmol/min/mg | μM | nmol/min/mg | μM | nmol/min/mg | μM | nmol/min/mg | μM | nmol/min/mg | μM | nmol/min/mg | ||||
HLM135 | 23.0 | 1.8 | 0.08 | 569 | 3.3 | 4.9 | 0.12 | 0.02 | 1225 | 0.54 | 6.5 | 0.87 | 0.13 | 268 | 1.4 |
HLM158 | 16.2 | 1.3 | 0.08 | 219 | 1.6 | 2.6 | 0.03 | 0.01 | 1339 | 0.44 | 1.4 | 0.17 | 0.12 | 426 | 2.3 |
HLM167 | 19.1 | 0.7 | 0.04 | 1018 | 2.6 | 1.7 | 0.02 | 0.01 | 3783 | 0.70 | 3.9 | 0.37 | 0.09 | 667 | 2.6 |
μM | nmol/min/nmol | μM | nmol/min/nmol | μM | nmol/min/nmol | μM | nmol/min/nmol | μM | nmol/min/nmol | μM | nmol/min/nmol | ||||
CYP2B6 | 17.7 | 6.8 | 0.38 | 4.4 | 3.18 | 0.73 | 26.0 | 1.63 | 0.06 | ||||||
CYP3A4 | 5.9 | 2.7 | 0.46 | 1247 | 36.3 | 1.0 | 0.38 | 0.39 | 2773 | 2.31 | 0.2 | 0.35 | 1.42 | 528 | 11.0 |
Kinetic parameters were obtained using a single-enzyme Michaelis-Menten model for CYP2B6 and a dual-enzyme Michaelis-Menten model for HLM135, 158, 167, and CYP3A4.
Km1, Km2, Michaelis-Menten constants; Vmax1, Vmax2, maximum metabolic velocity.