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標題: Cage amines as the stopper inhibitors of cholinesterases
作者: Lin, G.
Tsai, H.J.
Tsai, Y.H.
關鍵字: active-site gorge;human butyrylcholinesterase;acetylcholinesterase;binding;analogs;residues
Project: Bioorganic & Medicinal Chemistry Letters
期刊/報告no:: Bioorganic & Medicinal Chemistry Letters, Volume 13, Issue 17, Page(s) 2887-2890.
Cage amines 1-4 are potent peripheral anionic site-bound reversible inhibitors of both acetylcholinesterase and butyrylcholinesterase. Cage amines 1-3 are selective butyrylcholinesterase inhibitor versus acetylcholinesterase. For both enzymes, the -log K-i values linearly correlate with the difference of substituted phenyl radius of cage amines (-log K-i = 5.4 + 3.4Deltagamma for acetylcholinesterase, -log K-i = 5.9 + 3.2Deltagamma for butyrylcholinesterase). Moreover, the relationship between the enzymes and cage amines mimics that between bottles and stoppers. (C) 2003 Elsevier Ltd. All rights reserved.
ISSN: 0960-894X
DOI: 10.1016/s0960-894(03)00599-7
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