Peripheral and dual binding site inhibitors of acetylcholinesterase as neurodegenerative disease-modifying agents

被引：21

作者：

Dorronsoro, I ^{[1
]}

Castro, A ^{[1
]}

Martinez, A ^{[1
]}

机构：

[1] NeuroPharma SA, Madrid 28760, Spain

来源：

EXPERT OPINION ON THERAPEUTIC PATENTS | 2003年 / 13卷 / 11期

关键词：

beta-amyloid; acetylcholinesterase inhibitors; Alzheimer's disease; protein aggregation;

D O I：

10.1517/13543776.13.11.1725

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Current treatment approaches in Alzheimer's disease have been dominated by the use of acetylcholinesterase (ACNE) inhibitors, which increase the acetylcholine concentration in the brain, thus alleviating the decline in cognitive and mental function associated with this neurodegenerative disorder. However, ACNE itself has been implicated in the pathogenesis of Alzheimer's disease and it appears that ACNE may directly interact with (beta-amyloid, increasing the deposition of this peptide into insoluble plaques. This new role suggests that properly designed or biologically directed screened ACNE inhibitors might be able to act as disease-modifying agents rather than as a mere palliative treatment. This review discloses recent discoveries of small molecules targeting the non-cholinergic actions of this well-known cholinergic enzyme.

引用

页码：1725 / 1732

页数：8

共 80 条

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