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GDP-曼酸酸酶是Xanthomonas citri中一个有效的标,用于控制类癌症

André Vessoni Alexandrino^1,2, Mariana Pegrucci Barcelos³, Leonardo Bruno Federico³

¹Laboratório de Bioquímica e Biologia Molecular Aplicada (LBBMA), Departamento de Genética e Evolução, Universidade Federal de São Carlos, São Carlos, São Paulo, Brazil.

Microbiology spectrum

|May 9, 2024

概括

桑托蒙纳斯 (Xanthomonas citri) 下属物种. (Xcc) 导致类的癌症. 一个关键的酶,XanB,对于Xcc的致病性至关重要. 针对XanBB的抑制剂

科学领域:

植物病理学植物病理学
细菌学细菌学是一门学科.
生物化学生物化学
药物发现药物发现药物发现

背景情况:

类,是由Xanthomonas citri亚种引起的. (Xcc) 是一个重要的农业疾病.
目前的管理依赖于基于铜的处理方法,需要可持续的替代方案.
具有二异相酶 (PMI) 和瓜诺辛二酸-二酸酸酶 (GMP) 活性的酶XanB是Xcc的表面蛋白质,参与宿主相互作用.

研究的目的:

阐明XanB在Xcc致病性中的作用及其作为药物点的潜力.
为了识别和评估XanB抑制剂用于类瘤控制.

主要方法:

构建和分析XanB删除突变及其补充.
对XanB的同质建模和化学数据库的in silico虚拟选.
试验室酶分析测试以评估XanB对GMP和PMI活动的抑制剂有效性.
在体内评估抑制剂在降低类瘤严重性的有效性.

主要成果:

这种XanB删除突变在运动性,生物膜生成和紫外线抵抗方面表现出缺陷,并且是非致病的.
突变的补充恢复了野生类型的表型.
在体选中,发现了具有有利ADME/毒素特性的三种化合物.
这些化合物抑制了XanB的GMP活性超过50%,并将类瘤的严重程度降低了高达95%.

结论:

XanB对于Xcc的致病性至关重要,其GMP活性起着关键作用.
XanB 抑制剂显示出可持续类瘤控制的显著潜力.
对于开发针对与Xanthomonas相关的疾病的新型治疗策略,XanB是一个有前途的目标.

关键词:

国内生产总值 - - 曼诺酸铁酸酶克桑托蒙纳斯 (Xanthomonas) 是一种类植物的癌症.保护果的保护抑制剂抑制剂抑制剂创新创新创新创新创新光曼诺酶异构酶是一种

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