Crystallization (Comment) | Organism |
---|---|
purified recombinant enzyme bound to inhibitor fenamiphos and oxime-based reactivators [(E)-[1-[(4-carbamoylpyridin-1-ium-1-yl)methoxymethyl]pyridin-2-ylidene]methyl]-oxoazanium dichloride, and 1,7-heptylene-bis-N,N0-2-pyridiniumaldoxime dichloride, mixture of 0.001 ml 20 mg/ml AChE with 0.001 ml well solution containing 28% PEG750MME and 0.1mM HEPES, pH 7.0-7.2, saturated with fenamiphos, for 22-25 h, crystals are soakened in inhibitor solution, X-ray diffraction structure determination and analysis at 2.4-2.7 A resolution | Mus musculus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
fenamiphos | an organophosphorus compound and insecticide | Mus musculus | |
additional information | oxime-based reactivators, such as [(E)-[1-[(4-carbamoylpyridin-1-ium-1-yl)methoxymethyl]pyridin-2-ylidene]methyl]-oxoazanium dichloride, i.e. HI-6, and 1,7-heptylene-bis-N,N0-2-pyridiniumaldoxime dichloride, i.e. Ortho-7, restore the organophosphate-inhibited enzymatic activity by cleaving the phosphorous conjugate, overview. Flipping of the His447 imidazole ring allows the formation of a hydrogen bonding network among the Glu334-His447-Ortho-7 triad, which presumably deprotonates the Ortho-7 oxime hydroxyl group, increases the nucleophilicity of the oxime group, and leads to cleavage of the phosphorous conjugate. Binding structure determination and analysis, higher reactivation rate of HI-6 than Ortho-7, overview | Mus musculus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Mus musculus | P21836 | - |
- |
Synonyms | Comment | Organism |
---|---|---|
AChE | - |
Mus musculus |