Journal
CHINESE JOURNAL OF CHEMISTRY
Volume 40, Issue 11, Pages 1285-1292Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cjoc.202100910
Keywords
Butyrylcholinesterase; Alzheimer's disease; Fluorescent probes; Inhibitors; High-throughput screening
Categories
Funding
- National Natural Science Foundation of China [81872728, 82173652]
- Natural Science Foundation of Jiangsu Province [BK20191411]
- Qing Lan project of Jiangsu Province
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In this study, small-molecule fluorescence probes for BChE were designed and shown to have potential in detecting the affinity of non-fluorescent compounds to BChE. This provides a solid foundation for the development of small-molecule BChE inhibitors and better understanding the molecular biological mechanism of BChE.
Comprehensive Summary Butyrylcholinesterase (BChE) is regarded as a promising target for the treatment of Alzheimer's disease (AD), as its level significantly increases along with the progress of this disease. Therefore, the development of potent and high-affinity small-molecule BChE inhibitors may be a new strategy for the discovery of anti-AD drugs. However, the current Ellman's method is unable to evaluate the affinity of compounds with BChE, and has a few deficiencies in drug development. Herein, the first small-molecule fluorescence polarization (FP) probes for BChE were rationally designed based on a high affinity inhibitor. Studies indicated that probe F6 exhibited satisfactory fluorescence intensity and suitable fluorescent properties that were compatible with the filters in the FP system. Meanwhile, probe F6 exhibited potent binding affinity to BChE. It is feasible to be applied in detecting the affinity of non-fluorescent compounds to BChE, which lays a solid foundation for the development of small-molecule BChE inhibitors. At the same time, it also can be applied as a valuable chemical tool for better understanding the molecular biological mechanism of BChE.
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