Abstract The condensation of tacrine aminopolymethylene derivatives with diethyl (ethoxymethylidene)malonate led to the new hybrid compounds—conjugates, which were effective inhibitors acetylcholinesterase (AChE) (IC 50 up 0.538 μM) and butyrylcholinesterase 0.0314 μM). They can displace propidium iodide from peripherical anionic site AChE at level reference drug donepezil demonstrate a weak an...

A butyrylcholinesterase, purified from porcine parotid glands, behaved as a single component in sedimentation velocity and sedimentation equilibrium centrifugation and migrated as a single esterase in starch gel electrophoresis. The molecular weight of the enzyme was estimated to be 368,000. Amino acid analysis showed a high proline content (7.6%) and the presence of two unidentified components...

To address the problem of acute cocaine overdose, we undertook molecular engineering of butyrylcholinesterase (BChE) as a cocaine hydrolase so that modest doses could be used to accelerate metabolic clearance of this drug. Molecular modeling of BChE complexed with cocaine suggested that the inefficient hydrolysis (k(cat) = 4 min(-1)) involves a rotation toward the catalytic triad, hindered by T...

Human butyrylcholinesterase (hBChE) is currently being developed as a detoxication enzyme for stoichiometric binding and/or catalytic hydrolysis of organophosphates. Herein, we describe the use of a molecular evolution method to develop novel hBChE variants with increased resistance to stereochemically defined nerve agent model compounds of soman, sarin, and cyclosarin. Novel hBChE variants (Y3...

This study compared obese (N = 134) and unobese (N = 92) male blood donors, regarding the relative intensity (RI) and activity of different molecular forms (G1, G2, G4 and G1-ALB) of butyrylcholinesterase (BChE, EC 3.1.1.8) found in plasma, thereby searching for an association between these variables with obesity and SNPs of exons 1 and 4 of the BCHE gene. It was shown that obese and unobese in...

Acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) catalyze the hydrolysis of the neurotransmitter acetylcholine and, thereby, function as coregulators of cholinergic neurotransmission. For both enzymes, hydrolysis takes place near the bottom of a 20 Å deep active site gorge. A number of amino acid residues within the gorge have been identified as important in facilitating efficient ...

Corresponding author: Eun Sung Kim, M.D., Ph.D., Department of Anesthesiology and Pain Medicine, Seoul St. Mary’s Hospital, College of Medicine, The Catholic University of Korea, 505, Banpo-dong, Seocho-gu, 137-040, Korea. Tel: 82-2-2258-2236, Fax: 82-2-591-1592, E-mail: [email protected] This is an open-access article distributed under the terms of the Creative Commons Attribution Non-Co...