烟碱乙酰胆碱受体:神经退行性疾病的多样性和生理重要性以及有机磷解毒剂的开发

Pub Date : 2020-12-30 DOI:10.18054/PB.V121-122I3-4.10547
A. Zandona, M. Katalinić
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引用次数: 0

摘要

生物体内的神经系统和其他系统之间的交流是通过神经冲动的传递来进行的。多种神经递质被释放到突触间隙,并与邻近细胞的特定受体结合,进一步传递信号。其中一种受体是烟碱型乙酰胆碱受体(nAChR),这是一种由神经递质乙酰胆碱结合激活的整合膜蛋白(配体门控离子通道)。nAChR的主要特征是其多样性,因为它们由五个相同或相互不同的亚基组成,这有助于特定受体的特性和生物活性。在五聚体蛋白质结构的组装过程中,各种亚基的组合被连接在一起。在发现nAChR参与各种疾病后,它们成为重要的治疗靶点,例如用于治疗神经退行性疾病(阿尔茨海默氏症和帕金森氏症)和治疗有机磷化合物中毒。本文概述了烟碱受体的最新知识,并对疾病、中毒、潜在药物和治疗方法进行了讨论。
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Nicotinic acetylcholine receptors: Diversity and physiological importance for neurodegenerative disorders and development of organophosphate antidotes
The communication between the nervous and other systems in the organism is carried out by the transmission of nerve impulses. Diverse neurotransmitters are released into the synaptic cleft and bind to the specific receptors at the neighbouring cell to transmit the signal further. One of such receptors are nicotinic acetylcholine receptors (nAChR), integrated membrane proteins (ligand-gated ion channels) activated by the binding of a neurotransmitter acetylcholine. nAChR’s main characteristic is their diversity, as they consist of five of the same or mutually different subunits, which contribute to the specific receptors properties and biological activity. During the assembly of a pentameric protein structure, various combinations of subunits are linked together. After the discovery of nAChR’s involvement in various diseases, they became an important therapeutic target, for example in the treatment of neurodegenerative diseases (Alzheimer’s and Parkinson’s) and in the treatment of organophosphorus compound poisoning. This paper presents an overview of current knowledge on nicotinic receptors and an accompanying discussion on diseases, poisonings, potential drugs and treatments is given.
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