Background: Acetylcholinesterase is a serine hydrolase that terminates the action of the neurotransmitter acetylcholine by hydrolyzing it into acetic acid and choline. Objective: The enzyme, containing an ellipsoidal structure, possesses three binding sites such as active site (with catalytic anionic and esteratic subsites), aromatic gorge and peripheral anionic site, where the inhibiting compounds interact. The acetylcholinesterase inhibitors bind to the enzyme and interfere with the breakdown of acetylcholine, leading to the deposition of acetylcholine in the nerve synapses and causing disrupted neurotransmission. Based on this principle of action, many therapeutic drugs for the treatment of different diseases, pesticides and chemical warfare agents have been synthesized targeting the actylcholinesterase. Conclusion: The present review summarizes the current knowledge about acetylcholinesterase, its structure, function and biosynthesis, its inhibitors, and mode of action of inhibitors on it. Besides, the review also presents an overview about the resistance mechanism that the organisms develop due to the over-application of acetylcholinesterase inhibitors. Keywords: Acetylcholine, acetylcholinesterase, neurotransmission, active sites, acetylcholinesterase inhibitors, insecticide resistance.

Sunita Thapa

Min Lv

Hui Xu

Mini-Reviews in Medicinal Chemistry

MINI-REVIEWS IN MEDICINAL CHEMISTRY 的目的是发表关于药物化学和相关学科近期重要进展的简短评论。MINI-REVIEWS IN MEDICINAL CHEMISTRY 涵盖药物化学的所有领域，包括药物合理设计、合成化学、生物有机化学的发展, 高通量筛选, 组合化学, 药物靶点, 天然产物研究和构效关系研究。MINI-REVIEWS IN MEDICINAL CHEMISTRY 是每一位希望随时了解最新情况的药物和药物化学家的重要期刊。日期与最新和最重要的发展。

The purpose of Mini-Reviews in Medicinal Chemistry is to publish concise reviews on recent significant advances in medicinal chemistry and related disciplines. This journal covers all areas of medicinal chemistry, including rational drug design, synthetic chemistry, developments in bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, natural product research, and structure-activity relationship studies. Mini-Reviews in Medicinal Chemistry is an essential journal for researchers who wish to stay updated on the latest and most important developments in the field.

《Mini-Reviews in Medicinal Chemistry》旨在发表关于药物化学及相关学科近期重要进展的简短评论。该期刊涵盖药物化学的各个领域，包括药物合理设计、合成化学、生物有机化学的发展、高通量筛选、组合化学、药物靶点、天然产物研究和构效关系研究。《Mini-Reviews in Medicinal Chemistry》是每位希望及时了解药物和药物化学最新进展的研究者的重要期刊。

Acetylcholinesterase: A Primary Target for Drugs and Insecticides

The present review summarizes the current knowledge about acetylcholinesterase, its structure, function and biosynthesis, its inhibitors, and mode of action of inhibitors on it and presents an overview about the resistance mechanism that the organisms develop due to the over-application of acetyl cholinestersterase inhibitors.

Category	Quartile
医学	3
医学, 药物化学	3

Acetylcholinesterase: A Primary Target for Drugs and Insecticides

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