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Literature summary for 3.1.1.7 extracted from

  • Taylor, P.; Kovarik, Z.; Reiner, E.; Radic, Z.
    Acetylcholinesterase: converting a vulnerable target to a template for antidotes and detection of inhibitor exposure (2007), Toxicology, 233, 70-78.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
drug development AChE, when conjugated with organophosphorous compounds, is employed as a template for socalled click-chemistry, freeze-frame synthesis of nucleophilic reactivating agents that could potentially prove useful in AChE reactivation at the target site as well as in catalytic scavenging of organophosphates in plasma, overview Mus musculus

Cloned(Commentary)

Cloned (Comment) Organism
-
Mus musculus

Protein Variants

Protein Variants Comment Organism
F295L the mutant shows enhanced reactivation rate by the oximes HI-6 and 2-PAM compared to the wild-type enzyme Mus musculus
F295L/Y337A the mutant shows 120fold enhanced reactivation rate by the oximes HI-6 and 2-PAM compared to the wild-type enzyme Mus musculus
F297I the mutant shows enhanced reactivation rate by the oximes HI-6 and 2-PAM compared to the wild-type enzyme Mus musculus
Y337A the mutant shows enhanced reactivation rate by the oximes HI-6 and 2-PAM compared to the wild-type enzyme Mus musculus
Y337A/F338A the mutant shows enhanced reactivation rate by the oximes HI-6 and 2-PAM compared to the wild-type enzyme Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
methylorganophosphonates the Sp-enantiomer is more reactive Mus musculus
additional information organophosphate inhibitor binding and active site gorge structure, oveview, nucleophilic oximes, i.e. bis-quarternary oximes, aldoximes, and hydroxamates, act as reactivators of the inhibited enzyme and are of therapeutic use, overview Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus
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-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
alkyl methylphosphonfluoridate + H2O oxime-assisted catalysis of organophosphates by AChE, mechanism, reaction system, overview Mus musculus ?
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?

Subunits

Subunits Comment Organism
More primary and tertiary structure determination and anaylsis, the active site gorge forms asterically confined environment Mus musculus

Synonyms

Synonyms Comment Organism
AChE
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Mus musculus