新型OSBP抑制剂Y18501在赋予抗性的PscORP1中的抗性风险评估及点突变（G705V、L798W和I812F）
Resistance Risk Assessment for the New OSBP Inhibitor Y18501 in and Point Mutations (G705V, L798W, and I812F) in PscORP1 that Confer Resistance.
作者信息
Xue Zhaolin, Wang Bin, Li Chengcheng, Yang Huixin, Gao Xuheng, Sun Mingyou, Huang Zhongqiao, Miao Jianqiang, Liu Xili
机构信息
China Agricultural University, Beijing 100193, China.
State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Sinochem Agrochemicals R&D Co. Ltd, Shenyang 110021, China.
出版信息
J Agric Food Chem. 2023 Mar 22;71(11):4510-4520. doi: 10.1021/acs.jafc.3c00188. Epub 2023 Mar 10.
Y18501 is a new oxysterol-binding protein inhibitor (OSBPI) that shows strong inhibitory activity against . In this study, the sensitivities of 159 isolates to Y18501 were determined, with EC values ranging from 0.001 to 11.785 μg/mL, indicating that a Y18501-resistant subpopulation has appeared in the field. Ten Y18501-resistant mutants were obtained by fungicide adaptation and displayed fitness equal to or stronger than their parental isolates, which suggests that the resistance risk of to Y18501 is high. The consecutive applications of Y18501 in the field resulted in the rapid resistance of and decreased control efficacy of cucumber downy mildew (CDM), which could be alleviated by compounding with mancozeb. A positive cross-resistance was detected between Y18501 and oxathiapiprolin. The amino acid substitutions G705V, L798W, and I812F in PscORP1 conferred resistance to Y18501 in , which was validated by molecular docking and molecular dynamics simulations.
Y18501是一种新型氧化甾醇结合蛋白抑制剂（OSBPI），对……显示出强烈的抑制活性。在本研究中，测定了159株……分离株对Y18501的敏感性，其EC值范围为0.001至11.785μg/mL，表明田间已出现对Y18501耐药的亚群体。通过杀菌剂适应性处理获得了10个对Y18501耐药的突变体，其适应性与其亲本分离株相当或更强，这表明……对Y18501的耐药风险很高。在田间连续施用Y18501导致……迅速产生抗性，黄瓜霜霉病（CDM）的防治效果下降，与代森锰锌复配可缓解这种情况。在Y18501和恶唑菌酰胺之间检测到正向交叉抗性。PscORP1中的氨基酸取代G705V、L798W和I812F赋予……对Y18501的抗性，这通过分子对接和分子动力学模拟得到验证。
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