Department of Bio-engineering, Integral University, Lucknow, 226026, India.
CNS Neurol Disord Drug Targets. 2014 Apr;13(3):391-401. doi: 10.2174/18715273113126660166.
This review presents a concise update on the inhibitors of the neuroenzyme, acetylcholinesterase (AChE; EC 3.1.1.7). AChE is a serine protease, which hydrolyses the neurotransmitter, acetylcholine into acetate and choline thereby terminating neurotransmission. Molecular interactions (mode of binding to the target enzyme), clinical applications and limitations have been summarized for each of the inhibitors discussed. Traditional inhibitors (e.g. physostigmine, tacrine, donepezil, rivastigmine etc.) as well as novel inhibitors like various physostigmine-derivatives have been covered. This is followed by a short glimpse on inhibitors derived from nature (e.g. Huperzine A and B, Galangin). Also, a discussion on 'hybrid of pre-existing drugs' has been incorporated. Furthermore, current status of therapeutic applications of AChEinhibitors has also been summarized.
本综述简要介绍了神经酶乙酰胆碱酯酶（AChE；EC 3.1.1.7）抑制剂的最新进展。AChE 是一种丝氨酸蛋白酶，可将神经递质乙酰胆碱水解为乙酸和胆碱，从而终止神经传递。讨论的每种抑制剂都总结了分子相互作用（与靶酶结合的模式）、临床应用和局限性。涵盖了传统抑制剂（如毒扁豆碱、他克林、多奈哌齐、加兰他敏等）以及新型抑制剂，如各种毒扁豆碱衍生物。接下来是对天然来源抑制剂（如石杉碱甲和乙、高良姜素）的简要介绍。此外，还讨论了“现有药物的混合物”。此外，还总结了 AChE 抑制剂的治疗应用现状。
