Compounds showing strong inhibitory effects on PNPA hydrolysis by recombinant CES1, CES2, and AADAC
PNPA hydrolysis by recombinant CES1, CES2, and AADAC was determined at a substrate concentration of 100 μM. The control activity values of recombinant CES1, CES2, and AADAC were 167.0, 289.9, and 244.4 nmol/min/mg protein, respectively.
| Compound | % of Control | ||
|---|---|---|---|
| CES1 | CES2 | AADAC | |
| Acemetacin | 0 | 0 | 0 |
| 2,6-Dichloro-4-nitrophenol | 0 | 0 | 0 |
| Nordihydroguaiaretic acid | 0 | 0 | 0 |
| Simvastatin | 0 | 0 | 0 |
| Lithocholic acid | 0 | 4 | 2 |
| l-Thyroxine | 9 | 3 | 3 |
| Benzbromarone | 5 | 4 | 3 |
| 3,3′,5-Triiodo-l-thyroxine free acid | 4 | 8 | 5 |
| 4-Hydroxybenzoic acid n-hexyl ester | 10 | 11 | 12 |
| 4'-Hydroxydiclofenac | 8 | 7 | 13 |
| 4-Chloro-1-naphthol | 7 | 6 | 15 |
| 2-Chloro-3′,4'-dimethoxybenzil | 7 | 13 | 106 |
| Phenylmethylsulfonyl fluoride (PMSF) | 6 | 8 | 87 |
| JW480 | 8 | 9 | 81 |
| Digitonin | 14 | 87 | 96 |
| Flavoxate hydrochloride | 84 | 10 | 107 |
| Telmisartan (50 µM) | 86 | 10 | 110 |
| Vinblastine sulfate | 91 | 9 | 15 |