Kovarik_2020_Neuropharmacol__108111

Reference

Title : Efficient detoxification of nerve agents by oxime-assisted reactivation of acetylcholinesterase mutants - Kovarik_2020_Neuropharmacol__108111
Author(s) : Kovarik Z , Hrvat NM
Ref : Neuropharmacology , :108111 , 2020
Abstract : The recent advancements in crystallography and kinetics studies involving reactivation mechanism of acetylcholinesterase (AChE) inhibited by nerve agents have enabled a new paradigm in the search for potent medical countermeasures in case of nerve agents exposure. Poisonings by organophosphorus compounds (OP) that lead to life-threatening toxic manifestations require immediate treatment that combines administration of anticholinergic drugs and an aldoxime as a reactivator of AChE. An alternative approach to reduce the in vivo toxicity of OP centers on the use of bioscavengers against the parent organophosphate. Our recent research showed that site-directed mutagenesis of AChE can enable aldoximes to substantially accelerate the reactivation of OP-enzyme conjugates while dramatically slowing down rates of OP-conjugate dealkylation (aging). Therefore, this review focuses on oxime-assisted catalysis by AChE mutants that provides a potential means for degradation of organophosphates in the plasma before reaching the cellular target site.
ESTHER : Kovarik_2020_Neuropharmacol__108111
PubMedSearch : Kovarik_2020_Neuropharmacol__108111
PubMedID: 32333945

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Kovarik Z, Hrvat NM (2020)
Efficient detoxification of nerve agents by oxime-assisted reactivation of acetylcholinesterase mutants
Neuropharmacology :108111

Kovarik Z, Hrvat NM (2020)
Neuropharmacology :108111