Institute of Insect Science, Zhejiang University, Hangzhou, China.
Curr Drug Targets. 2012 Apr;13(4):495-501. doi: 10.2174/138945012799499712.
Acetylcholinesterase (AChE; EC 3.1.1.7) is a primary target of many insecticides including organophosphates (OP) and carbamates (CB). Because AChE is expressed in all invertebrate and vertebrate animals as a key enzyme of the cholinergic system, the toxicity of anticholinesterase insecticides to mammals and non-target species such as beneficial insects has been a great concern. In addition, the intensive use of OP and CB insecticides has resulted in the development of resistance in many insect pests, which has limited the use of anticholinesterase insecticides. Many aces encoding AChEs have been sequenced from a variety of vertebrates, insects and other invertebrates, and crystal structures of four AChEs have been determined in the past 20 years. Although the primary motifs and the three dimensional (3D) structures of different AChEs are similar, differences among AChEs are obvious. The catalytic properties and inhibition kinetics of AChEs from different groups of insects and mammals may be quite different, and two AChEs from a single insect may also show distinct differences. These differences may provide new opportunities for designing more selective insecticides for pest management.
乙酰胆碱酯酶（AChE；EC 3.1.1.7）是许多杀虫剂的主要靶标，包括有机磷（OP）和氨基甲酸酯（CB）。由于 AChE 作为胆碱能系统的关键酶在所有无脊椎动物和脊椎动物中表达，因此抗胆碱酯酶杀虫剂对哺乳动物和有益昆虫等非靶标物种的毒性一直是人们关注的焦点。此外，OP 和 CB 杀虫剂的大量使用导致许多害虫产生了抗药性，这限制了抗胆碱酯酶杀虫剂的使用。过去 20 年来，已经从各种脊椎动物、昆虫和其他无脊椎动物中测序了许多编码 AChE 的基因，并确定了四种 AChE 的晶体结构。尽管不同 AChE 的主要基序和三维（3D）结构相似，但 AChE 之间的差异是明显的。不同组别的昆虫和哺乳动物的 AChE 的催化特性和抑制动力学可能有很大的不同，而且来自单个昆虫的两种 AChE 也可能表现出明显的差异。这些差异可能为设计更具选择性的害虫管理杀虫剂提供新的机会。
