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Literature summary for 3.1.1.7 extracted from

  • Hoernberg, A.; Artursson, E.; Waerme, R.; Pang, Y.P.; Ekstroem, F.
    Crystal structures of oxime-bound fenamiphos-acetylcholinesterases: reactivation involving flipping of the His447 ring to form a reactive Glu334-His447-oxime triad (2010), Biochem. Pharmacol., 79, 507-515.
    View publication on PubMed

Crystallization (Commentary)

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

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

Organism UniProt Comment Textmining
Mus musculus P21836
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-

Synonyms

Synonyms Comment Organism
AChE
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Mus musculus