类毒素Cycloxaprid的目标鉴定和作用机制
Xiaomu Qiao1, Yan-Chao Zhang2, Jianhui Qin3
1Collaborative Innovation Center of Green Pesticide, National Joint Local Engineering Laboratory of Biopesticide Preparation, School of Forestry and Biotechnology, Zhejiang A & F University, Hangzhou 311300, China.
Pesticide biochemistry and physiology
|October 29, 2025
概括
环氧沙普里德是一种新型的新型尼诺类杀虫剂,通过激活果中的尼古丁乙胆受体 (nAChRs) 来有效控制害虫. 它的独特作用为防虫剂耐药性管理提供了潜在的解决方案.
科学领域:
- 农业科学 农业科学
- 神经科学是一个神经科学.
- 分子生物学分子生物学
背景情况:
- 类杀虫剂对于害虫控制至关重要,但面临着耐药性和环境问题.
- 环氧沙,一种独特的新烟类类似物,由于其独特的药理性质,可以克服交叉耐药性.
研究的目的:
- 为了阐明cycloxaprid在Drosophila melanogaster中的作用模式.
- 研究cycloxaprid与尼古丁乙胆受体 (nAChRs) 的相互作用.
主要方法:
- 使用了综合遗传,电生理学和计算方法.
- 用nAChR亚单元突变和Xenopus卵细胞异质表达的生物测试.
- 以人工智能驱动的结构建模 (Chai-1) 来确定结合部位的相互作用.
主要成果:
- 环氧沙会诱导刺激性神经毒性和过活性,这表明nAChR过度活化.
- 草的nAChR子单元α1,α2,β1和β2对于它的杀虫作用至关重要.
- 环氧沙作为部分激动剂,增强乙胆引起的电流,并与α1-β1接口结合.
结论:
- 这项研究阐明了环氧沙的杀虫活性的分子机制.
- 赛克洛沙普里德与nAChRs的独特相互作用表明其在管理抗虫剂耐药性的潜力.
相关概念视频
Allosteric Proteins-ATCase
Binding sites linkages can regulate a protein's function. For example, enzyme activity is often regulated through a feedback mechanism where the end product of the biochemical process serves as an inhibitor.
Aspartate transcarbamoylase (ATCase) is a cytosolic enzyme that catalyzes the condensation of L-aspartate and carbamoyl phosphate to N-carbamoyl-L-aspartate. This reaction is the first step in pyrimidine biosynthesis. UTP and CTP, the end products of the pyrimidine synthesis pathway,...
Aspartate transcarbamoylase (ATCase) is a cytosolic enzyme that catalyzes the condensation of L-aspartate and carbamoyl phosphate to N-carbamoyl-L-aspartate. This reaction is the first step in pyrimidine biosynthesis. UTP and CTP, the end products of the pyrimidine synthesis pathway,...
Principles of Drug Action
Drugs are chemical substances that modify biological responses by interacting with macromolecular targets such as receptors, ion channels, transporters, and enzymes. Pharmacodynamics describes the course of action of drugs leading to the physiological effect at a specific site in the body.
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...
Targets for Drug Action: Overview
Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Pharmacogenomics: Identification of New Drug Targets
Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...
Inhibitors of Bacterial DNA Synthesis
Bacterial pathogens depend on precise and efficient DNA replication to sustain infection. Two type II topoisomerases—DNA gyrase and topoisomerase IV—are critical to this process, as they resolve DNA supercoiling and unlink chromosomes during replication. Fluoroquinolones, synthetic derivatives of quinolones, exploit this mechanism by stabilizing the transient DNA–enzyme cleavage complex, preventing strand religation, and causing lethal double-strand breaks. These antibiotics are selectively...
Antiviral Nucleoside Inhibitors
Antiviral Nucleoside InhibitorsAntiviral nucleoside inhibitors are structural analogs of natural nucleosides that interfere with viral DNA or RNA synthesis. These compounds selectively target viral polymerases due to their resemblance to host nucleosides, thereby disrupting viral genome replication.Mechanism of Acyclovir ActionAcyclovir is a guanosine analog with a three-carbon acyclic side chain. It selectively targets herpes simplex virus type 1 (HSV-1), herpes simplex virus type 2 (HSV-2),...


