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昆虫芳基烷基胺 - 乙酰转移酶作为新型杀虫剂设计的潜在靶点。

Insect Arylalkylamine -Acetyltransferases as Potential Targets for Novel Insecticide Design.

作者信息

O'Flynn Brian G, Hawley Aidan J, Merkler David J

机构信息

Department of Chemistry, University of South Florida, USA.

出版信息

Biochem Mol Biol J. 2018;4(1). doi: 10.21767/2471-8084.100053. Epub 2018 Feb 6.

Abstract

Crop protection against destructive pests has been at the forefront of recent agricultural advancements. Rapid adaptive evolution has led to insects becoming immune to the chemicals employed to quell their damage. Insecticide resistance is a serious problem that negatively impacts food production, food storage, human health, and the environment. To make matters more complicated are the strict regulations in place on insecticide development, driven by rising public concern relating to the harmful effects these chemicals have on the environment and on society. A key component to solving the problem of insecticide resistance, while keeping public welfare in mind, is the identification of novel insect-specific protein targets. One unexplored target for the development of new targeted insecticides are the insect arylalkylamine -acetyltransferases (iAANATs). This group of enzymes, shown to be intrinsic in the development of the insect cuticle, is an untapped well of potential for target-specific inhibition, while offering enough variety to ensure protection for non-target enzymes. In this review, we highlight kinetic, genetic and bioinformatic data showing that the iAANATs are intriguing insecticide targets that should be specific only for particular insect pests. Such a pest-specific insecticide would minimize environmental harm by eliminating such non-discriminate attacks which have made insecticides such a highly regulated industry, and would have negligible toxicity to humans and other mammals.

摘要

针对破坏性害虫的作物保护一直是近期农业发展的前沿问题。快速的适应性进化导致昆虫对用于抑制其危害的化学物质产生免疫。抗药性是一个严重问题,对粮食生产、粮食储存、人类健康和环境产生负面影响。更复杂的是,由于公众对这些化学物质对环境和社会的有害影响的关注度不断提高,杀虫剂开发受到严格监管。在考虑公共福利的同时,解决抗药性问题的一个关键因素是确定新的昆虫特异性蛋白质靶点。昆虫芳基烷基胺 - 乙酰转移酶(iAANATs)是开发新型靶向杀虫剂的一个未被探索的靶点。这组酶在昆虫表皮发育中显示出内在作用,是一个尚未开发的潜在靶点特异性抑制源,同时具有足够的多样性以确保对非靶标酶的保护。在本综述中,我们强调动力学、遗传学和生物信息学数据,表明iAANATs是有趣的杀虫剂靶点,应该只对特定的害虫具有特异性。这样一种针对特定害虫的杀虫剂将通过消除导致杀虫剂行业受到严格监管的这种无差别攻击来最大限度地减少环境危害,并且对人类和其他哺乳动物的毒性可以忽略不计。

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