几丁质脱乙酰酶的生物学功能、三维结构及其抑制剂的研究进展  

Research progress on biological function,three-dimensional structure and inhibitors of chitin deacetylase:a review

作　　者：徐欢 何祺 崔佳琳 靳彬艳 路星星 张晓鸣 凌云[1] 张莉[1] XU Huan;HE Qi;CUI Jialin;JIN Binyan;LU Xingxing;ZHANG Xiaoming;LING Yun;ZHANG Li(Innovation Center of Pesticide Research,Department of Applied Chemistry,College of Science,China Agricultural University,Beijing 100193,China)

机构地区：[1]中国农业大学理学院应用化学系农药创新中心,北京100193

出　　处：《农药学学报》2024年第2期211-223,277,共14页Chinese Journal of Pesticide Science

基　　金：国家自然科学基金(22177132);国家重点研发计划(2022YFD1700204).

摘　　要：由于农用化学品存在靶标有限性和耐药性等问题,新靶标的开发成为农药研发的重中之重。几丁质是昆虫表皮和真菌细胞壁的主要组成成分,具有重要的生物学功能。几丁质脱乙酰酶(chitin deacetylase,CDA)可将几丁质脱乙酰化为壳聚糖,这一过程除了影响昆虫体壁和真菌细胞壁的形成外,还可调控昆虫的生长发育或决定病原菌的致病性。越来越多的研究表明,CDA有望成为新农药创制的候选靶标。本文介绍了CDA作为作物保护潜在靶标的研究进展,主要综述了当前不同来源CDA的生化功能、晶体结构、酶与底物的结合模式和以及近年来已报道的以CDA为靶标的抑制剂的研究进展,可为以几丁质脱乙酰酶为靶标的抑制剂的筛选以及新型农药的开发提供指导。The development of new targets has become a top priority in pesticide research and development due to the problems of limited targets and drug resistance in agrochemicals.Chitin is a major component of insect epidermis and fungal cell wall,and has important biological functions.Chitin deacetylase(CDA)can deacetylate chitin to chitosan,which not only affects the formation of insect body wall and fungal cell wall,but also regulates the growth and development of insects or determines the pathogenicity of fungi.More and more studies have shown that CDA is expected to be a candidate target for the development of new pesticides.Therefore,the research progress of CDA as a potential target for crop protection,especially the biochemical functions,crystal structures,enzymesubstrate binding modes,and reported inhibitors of CDA from different sources in recent years were summarized in this review.The aim is to provide guidance for the screening of inhibitors targeting CDA and the development of novel pesticides.

关 键 词：几丁质脱乙酰酶 生物功能 潜在应用价值 晶体结构 抑制剂 研究进展 

分 类 号：S482.38[农业科学—农药学]