Journal
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Volume 144, Issue 7, Pages 3279-3284Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jacs.1c13492
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Funding
- Franco-Bavarian University Cooperation Center [FK03-2020]
- German Research Foundation (Deutsche Forschungsgemeinschaft) under DFG [DE 1546/10-1]
- Procope Mobility Program of the French Embassy in Germany
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Selective and pseudoirreversible photoswitchable BChE inhibitors were synthesized to investigate their biological functions and the mechanisms by which they affect Alzheimer's disease. One of the compounds showed significant differences in activity both in vitro and in vivo, and exhibited complete recovery in a murine cognition-deficit AD model.
To develop tools to investigate the biological functions of butyrylcholinesterase (BChE) and the mechanisms by which BChE affects Alzheimer's disease (AD), we synthesized several selective, nanomolar active, pseudoirreversible photoswitchable BChE inhibitors. The compounds were able to specifically influence different kinetic parameters of the inhibition process by light. For one compound, a 10-fold difference in the IC50-values (44.6 nM cis, 424 nM trans) in vitro was translated to an all or nothing response with complete recovery in a murine cognition-deficit AD model at dosages as low as 0.3 mg/kg.
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