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標題: Substrate activation of butyrylcholinesterase and substrate inhibition of acetylcholinesterase by 3,3-dimethylbutyl-N-n-butylcarbamate and 2-trimethylsilyl-ethyl-N-n-butylcarbamate
作者: Chiou, S.Y.
Wu, Y.G.
Lin, Y.F.
Lin, L.Y.
Lin, G.L.
關鍵字: butyrylcholinesterase;acetylcholinesterase;carbamates;activator;inhibitor;structure-reactivity relationships;steady-state kinetics;cholesterol;esterase;molecular recognition;cholinesterases;site;mechanism;binding;hydrolysis;rivastigmine
Project: Journal of Biochemical and Molecular Toxicology
期刊/報告no:: Journal of Biochemical and Molecular Toxicology, Volume 21, Issue 1, Page(s) 24-31.
Carbamates are used to treat Alzheimer's disease. These compounds inhibit acetylcholinesterase and butyrylcholinesterase. The goal of this work is to use the substrate analogs of butyrylcholinesterase, 3,3-dimethylbutyl-N-n-butylcarbamate (1) and 2-trimethylsilyl-ethyl-N-n-butylcarbamate (2) to probe the substrate activation mechanism of butyrylcholinesterase. Compounds 1 and 2 are characterized as the pseudo substrate inhibitors of acetylcholinesterase; however, compounds 1 and 2 are characterized as the essential activators of butyrylcholinesterase. Therefore, compounds 1 and 2 mimic the substrate in the acetylcholinesterase-catalyzed reactions, but the behavior of compounds 1 and 2 mimics the substrate activation in the butyrylcholinesterase-catalyzed reactions. (c) 2007 Wiley Periodicals, Inc.
ISSN: 1095-6670
DOI: 10.1002/jbt.20158
Appears in Collections:化學系所

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