Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 2, Pages 552-555Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.12.019
Keywords
Fluorescein-based sensor; AChE activity; Acetylthiocholine; Inhibitor
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Funding
- NSF of China [21002049, 21376117]
- Natural Science Foundation of the Jiangsu Higher Education Institutions of China [10KJB150005]
- Project of Priority Academic Program Development of Jiangsu Higher Education Institutions (PAPD)
- Scientific Research Foundation for the Returned Overseas Chinese Scholars of State Education Ministry
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A fluorescein-based sensor was developed for the AChE activity assay and the inhibitor screening. The sensor provided the dual assay methods for the screening of AChE activity in the presence or absence of inhibitor. The colorimetric and fluorometric assays were based on the following processes: (1) owing to the hydrolysis of acetylthiocholine in the presence of AChE, the fluorescein-based probe can rapidly induce 1,4-addition of the hydrolysis product thiocholine to alpha,beta-unsaturated ketone in the compound 1, resulting in strong fluorescence and absorption changes; (2) in the presence of the corresponding inhibitor, the fluorescence enhancement or the absorption change would be inhibited in that the formation of thiocholine was hindered. Crown Copyright (C) 2013 Published by Elsevier Ltd. All rights reserved.
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