Table 2. Kinetic parameters for inhibition of various cholinesterases by the TZ2PA6 isomers.
|
syn1
|
anti1
|
|||||
|---|---|---|---|---|---|---|
| Enzyme | kon, 1010 M-1·min-1 | koff, 10-3 min-1 | Ki, fM | kon, 1010 M-1·min-1 | koff, 10-3 min-1 | Ki, fM |
| mAChE* | 1.7 | 7.1 | 410 | 2.5 | 220 | 8,900 |
| mAChE mutant Trp286Ala | 0.94 | 19 | 2,000 | 0.87 | 1,800 | 210,000 |
| AChE, Electrophorus electricus* | 1.5 | 1.5 | 99 | 1.8 | 250 | 14,000 |
| AChE, Torpedo californica* | 1.4 | 1.1 | 77 | 3.2 | 23 | 720 |
| AChE, Drosophila melanogaster | 2.0 | 72 | 3,600 | 3.4 | 58 | 1,700 |
| Butyrylcholinesterase, mouse | 0.36 | 2.6 | 720 | 0.69 | 3.2 | 460 |
Parameters are means of n ≥ 3 individual values with SD ≤ 20%.
*
Modified from ref. 7