Table 1 Inhibition of rPpAChE1 and rPpAChE1-G119S by different classes of AChE inhibitors
Compound | Inhibitor class | Wild type rPpAChE1 | G119S rPpAChE1 | Resistance Ratio |
|---|---|---|---|---|
aIC50(95% CI) | aIC50(95% CI) | |||
Paraoxon | acylation site | 2.863 (1.862–4.401) | 3,819 (3,205–4,550) | 1336 |
Malaoxon | acylation site | 4.361 (3.184–5.972) | 1,972 (1,665–2,340) | 452 |
Eserine | acylation site | 3.2 (2.6–4.0) | 86 (73–102) | 27 |
Propoxur | acylation site | 220 (147–329) | 4,227,000 (−−)b | 19,213 |
Carbofuran | acylation site | 24 (17–33) | 124,000 (−−) | 5,200 |
1 | acylation site | 14 (10–19) | 236,800 (7,404–7,575,000) | 17,000 |
2 | acylation site | 36 (28–48) | 123,100 (−−) | 3,400 |
3 | acylation site | 13 (9.4–19) | 235 (164–336) | 18 |
4 | acylation site | 75 (36–152) | 4,775 (3,048–7,482) | 64 |
5 | acylation site | 76 (50–117) | 2,128 (1,267–3,573) | 28 |
Tacrine | choline binding site | 67 (56–81) | 388 (318–473) | 5.8 |
6 | bivalent | 0.42 (0.35–0.52) | 2.7 (2.3–3.2) | 6.4 |
7 | bivalent | 14 (13–15) | 35 (28–42) | 2.5 |
Donepezil | bivalent | 52 (39–70) | 262 (202–341) | 5.0 |
Tubocurarine | peripheral site | 143,200 (94,630–216,700) | 661,800 (290,000–1,511,000) | 4.6 |
Ethidium Bromide | peripheral site | 17,100 (13,890–21,060) | 6,433 (4,380–9,448) | 0.4 |