Substrate selectivity of high-activity mutants of human butyrylcholinesterase.

Design, preparation, and characterization of high-activity mutants of human butyrylcholinesterase specific for detoxification of cocaine.

Cocaine is a widely abused drug without a U.S. Food and Drug Administration-approved medication. There is a recognized, promising anticocaine medication to accelerate cocaine metabolism, producing biologically inactive metabolites via a route similar to the primary cocaine-metabolizing pathway [i.e., cocaine hydrolysis catalyzed by butyrylcholinesterase (BChE) in plasma]. An ideal, therapeutica...

Homodimeric bis-quaternary heterocyclic ammonium salts as potent acetyl- and butyrylcholinesterase inhibitors: a systematic investigation of the influence of linker and cationic heads over affinity and selectivity.

A molecular library of quaternary ammonium salts (QASs), mainly composed of symmetrical bis-quaternary heterocyclic bromides exhibiting choline kinase (ChoK) inhibitory activity, were evaluated for their ability to inhibit acetyl- and butyrylcholinesterase (AChE and BChE, respectively). The molecular framework of QASs consisted of two positively charged heteroaromatic (pyridinium or quinolinium...

Activity of cholinesterases in human whole blood measured with acetylthiocholine as substrate and ethopropazine as selective inhibitor of plasma butyrylcholinesterase.

A procedure is suggested for measuring acetylcholinesterase and butyrylcholinesterase activities in human whole blood using acetylthiocholine as a substrate and ethopropazine as a selective inhibitor of butyrylcholinesterase. The procedure is suitable for screening cholinesterase activities in routine and/or field tests.

High-Activity Mutants of Butyrylcholinesterase for Cocaine Hydrolysis and Method of Generating the Same

Effect of Gallic Acid on Reactivation of Acetylcholinesterase and Butyrylcholinesterase Inhibited by Diazinon in Vitro and in Vivo

Background and purpose: Diazinon is an organophosphate insecticide that binds to the acetylcholinesterase enzyme after metabolization causing its inactivation. Galic acid is a polyphenolic compound with nucleophilic properties. The aim of this study was to investigate the effects of gallic acid on reactivation of acetylcholine and butyrylcholinesterase inhibited by diazinon in mice and human se...