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<p>The analysis of the literature indicates a dual role of acetylcholinesterase (AChE) as an enzyme that hydrolyzes the neurotransmitter acetylcholine and simultaneously acts as a “pathological chaperone” promoting β-amyloid oligomerization. The review examines the interaction with AChE of several groups of neuroactive pharmacophore conjugates synthesized in our research group. A set of data obtained using the methods of enzyme kinetics, molecular docking, and fluorescence determination of the competitive displacement of the selective propidium ligand from the peripheral anionic site of AChE is analyzed. The results show the contribution of AChE as a bifunctional target to the neuroprotective potential of new multitarget compounds of various structural classes, allow us to explain the mechanism of the antiaggregatory activity of the conjugates while the original pharmacophores have no this activity, and provide ways to develop new cholinesterase inhibitors with a neuroprotective potential.</p>

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New functions of cholinesterases in the development of Alzheimer’s disease as a target for neuroprotective drugs

  • 期刊论文

  • 发表日期：

    2025年8月1日

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  • G. F. Makhaeva,
  • V. P. Fisenko,
  • S. O. Bachurin

摘要

The analysis of the literature indicates a dual role of acetylcholinesterase (AChE) as an enzyme that hydrolyzes the neurotransmitter acetylcholine and simultaneously acts as a “pathological chaperone” promoting β-amyloid oligomerization. The review examines the interaction with AChE of several groups of neuroactive pharmacophore conjugates synthesized in our research group. A set of data obtained using the methods of enzyme kinetics, molecular docking, and fluorescence determination of the competitive displacement of the selective propidium ligand from the peripheral anionic site of AChE is analyzed. The results show the contribution of AChE as a bifunctional target to the neuroprotective potential of new multitarget compounds of various structural classes, allow us to explain the mechanism of the antiaggregatory activity of the conjugates while the original pharmacophores have no this activity, and provide ways to develop new cholinesterase inhibitors with a neuroprotective potential.