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双特异性抑制剂向了三糖生物合成途径中的酶

Yitong Chen¹, Liu Tang¹, Zhiyang Jiang²

¹Ministry of Agriculture Key Laboratory for Crop Pest Monitoring and Green Control, College of Plant Protection, China Agricultural University, Beijing 100193, China.

Journal of agricultural and food chemistry

|December 21, 2023

概括

研究人员在Magnaporthe oryzae中发现了A1-4,一种新型的双重特异性杀菌剂,向三六酸盐合成酶 (TPS) 和三六酸盐酸酶 (TPP). 这种抑制剂显示出开发更安全的杀菌剂来对抗抗性的前景.

科学领域:

生物化学生物化学
植物病理学植物病理学
药用化学医学化学

背景情况:

抗真菌杀菌剂耐药性需要具有独特作用模式的新型化合物.
动物中没有三糖生物合成酶,三糖-6-酸盐合成酶 (TPS) 和三糖-6-酸盐酸酶 (TPP),这使得它们成为安全的杀菌剂标.
麦格纳波特 (Magnaporthe oryzae) 对农业构成重大威胁,需要有效的控制策略.

研究的目的:

发现和描述一种新的双特异性抑制剂,针对Magnaporthe oryzae中的TPS和TPP酶.
评估已识别的抑制剂对M. oryzae毒性的有效性,并了解其作用机制.

主要方法:

使用虚拟查和表面等离子体共振 (SPR) 来识别潜在的抑制剂.
在体外酶抑制试验中,使用纯化的MoTps1和MoTps2-TPP进行了测试.
生物活性测定评估了M. oryzae的毒性和虫形态.
用/交换质谱法 (HDX-MS) 来研究抑制剂-对象相互作用.

主要成果:

鉴定出A1-4是一种双特异性抑制剂,与MoTps1和MoTps2-TPP相互作用.
在体外,A1-4有效抑制了TPS和TPP的酶活性.
生物测试表明,A1-4抑制了M. oryzae的毒性,并诱导状细胞醇聚合,这是MoTps2相关的表型.
HDX-MS数据表明A1-4与TPS和TPP的基质结合口袋结合.

结论:

A1-4是一种强大的打击化合物,在M. oryzae的三糖生物合成途径中对关键酶具有双重目标特异性.
发现A1-4为开发新型,更安全的杀菌剂提供了有希望的基础,降低了耐药性发展风险.
针对TPS和TPP同时提供了一种强大的策略来控制M. oryzae和潜在的其他真菌病原体.

关键词:

马格纳波特花 (Magnaporthe oryzae) 是一个很大的植物.具有双重的特异性.抑制剂抑制剂的使用三糖的生物合成

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