Optimization of Cholinesterase-Based Catalytic Bioscavengers Against Organophosphorus Agents.

ABSTRACT: Organophosphorus agents (OPs) are irreversible inhibitors of acetylcholinesterase (AChE). OP poisoning causes major cholinergic syndrome. Current medical counter-measures mitigate the acute effects but have limited action against OP-induced brain damage. Bioscavengers are appealing alternative therapeutic approach because they neutralize OPs in bloodstream before they reach physiological targets. First generation bioscavengers are stoichiometric bioscavengers. However, stoichiometric neutralization requires administration of huge doses of enzyme. Second generation bioscavengers are catalytic bioscavengers capable of detoxifying OPs with a turnover. High bimolecular rate constants (k_cat/K_m > 10⁶ M^-1min^-1) are requir

SUBMITTER: Lushchekina SV 

PROVIDER: S-EPMC5859046 | biostudies-literature | 2018

REPOSITORIES: biostudies-literature