Enzyme | Relative Activity (%) and IC50 Value (μM)1-a | |||||||
---|---|---|---|---|---|---|---|---|
5 μM Probucol | 100 μM Pravastatin | 5 μM Fenofibrate | 100 μM Clofibrate | 100 μM Bezafibrate | 40 μM Clinofibrate | 400 μM Clofibric acid | 50 μM Fenofibric acid | |
AKR 1C1 | 76 ± 8 | 92 ± 2 | 93 ± 3 | 40 ± 9 | 93 ± 4 | 100 ± 1 | 85 ± 5 | 40 ± 7 |
(45 ± 5) | ||||||||
AKR 1C2 | 100 ± 2 | 100 ± 2 | 100 ± 1 | 20 ± 8 | 80 ± 4 | 60 ± 8 | 45 ± 8 | 65 ± 4 |
(102 ± 7) | (560 ± 20) | (99 ± 3) | ||||||
AKR 1C3 | 94 ± 5 | 87 ± 7 | 95 ± 2 | 40 ± 9 | 68 ± 5 | 95 ± 4 | 99 ± 1 | 8 ± 2 |
(244 ± 5) | (2.2 ± 0.4) | |||||||
AKR 1C4 | 95 ± 3 | 102 ± 4 | 95 ± 3 | 93 ± 6 | 202 ± 15 | 189 ± 18 | 242 ± 21 | 244 ± 1 |
↵1-a Relative activity was determined in the presence of the drug at the indicated concentration. For the drugs that activated AKR 1C4 but inhibited the other enzymes, their IC50 values for the respective enzymes were determined and are shown in parentheses under the values of the relative activities.