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乙酰胆碱酯酶抑制剂作为阿尔茨海默病治疗药物:从神经毒素到神经保护。

Acetylcholinesterase inhibitors as Alzheimer therapy: from nerve toxins to neuroprotection.

机构信息

Pharmaceutical Chemistry Research Lab, Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, Punjab 147002, India.

出版信息

Eur J Med Chem. 2013;70:165-88. doi: 10.1016/j.ejmech.2013.09.050. Epub 2013 Oct 6.

Abstract

Acetylcholinesterase is a member of the α/β hydrolase protein super family, with a significant role in acetylcholine-mediated neurotransmission. Research in the modulators of AChEs has moved from a potent poison (Sarin, Soman) in war times to the potent medicine (physostigmine) in peaceful times. Natural anti-AChE includes carbamates, glycoalkaloids, anatoxins derived from green algae; synthetic anti-AChE includes highly poisonous organophosphates used as nerve gases and insecticides. Recently, the role of anti-AChE was reassessed from neurotoxins to neuron-protective in the diseases characterized by impaired acetylcholine-mediated neurotransmission like Alzheimer's disease (AD). So, the AChE has been proven to be the most viable therapeutic target for the symptomatic treatment of AD. This review article gives a spectrum of strategies to design AChE inhibitors used in the Alzheimer therapy.

摘要

乙酰胆碱酯酶是α/β水解酶蛋白超家族的一员,在乙酰胆碱介导的神经递质传递中起着重要作用。AChE 调节剂的研究已经从战争时期的强效毒药(沙林、梭曼)转变为和平时期的强效药物(毒扁豆碱)。天然抗乙酰胆碱酯酶包括氨基甲酸酯类、糖苷生物碱、来自绿藻的拟交感神经毒素;合成抗乙酰胆碱酯酶包括用作神经毒气和杀虫剂的剧毒有机磷酸酯。最近,抗乙酰胆碱酯酶的作用从神经毒素重新评估为在乙酰胆碱介导的神经递质传递受损的疾病(如阿尔茨海默病)中的神经元保护作用。因此,乙酰胆碱酯酶已被证明是治疗 AD 的症状性治疗的最可行的治疗靶点。本文综述了用于阿尔茨海默病治疗的乙酰胆碱酯酶抑制剂的设计策略。

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