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通过基于结构的设计获得的抗结核化合物的P型ATPase膜载体 (CtpF) 针对Mycobacterium tuberculosis的特定向

Paola Santos¹, Luz M Salazar², Milena Maya-Hoyos²

¹Programa Maestría en Microbiología, Facultad Ciencias de la Salud, Universidad Colegio Mayor de Cundinamarca, Calle 28 N° 5B-02; Departamento de Química, Facultad de Ciencias, Universidad Nacional de Colombia, Carrera 30 N° 45-03, Bogotá, Colombia.

International journal of mycobacteriology

|December 27, 2023

概括

确定了针对Mycobacterium结核病CtpF蛋白的新型抗结核病 (抗结核病) 候选药物. ZINC14541509显著增加了CtpF转录,这表明它有可能成为一种新的抗结核药物标.

科学领域:

微生物学微生物学
药物发现药物发现药物发现
分子生物学分子生物学

背景情况:

越来越多的抗药性Mycobacterium结核病 (Mtb) 需要新的抗结核病 (抗结核病) 药物.
Mtb等离子膜P型ATPases是潜在的抗结核病点,因为它们在离子稳态和毒性中的作用.
运输Ca2+的P2型ATPaseCtpF与Mtb氧化应激反应和持久性有关.

研究的目的:

评估两种新型抗Mtb化合物对Mtb ctpF基因和其他P2型ATPases的转录的影响.
评估这些化合物的抗菌活性对抗Mycobacterium bovis.

主要方法:

使用定量逆转录聚合酶链反应 (qRT-PCR) 来测量基因转录水平.
通过虚拟查识别的两个化合物ZINC14541509和ZINC63908257进行了测试.
对Mycobacterium bovis的细菌活性进行了评估.

主要成果:

这两种化合物都显著增加了ctpF基因转录.
ZINC14541509对ctpF转录产生了特别强烈的影响.
这些化合物对Mycobacterium bovis.表现出活性.

结论:

Mtb CtpF 蛋白可能是 ZINC14541509.9 的特定标.
ZINC14541509代表了基于结构的新抗结核药物设计的有希望的头.

关键词:

针对抗结核病的目标.P型的ATP酶是一种P型的ATP酶.转录模式的转录模式结核病是一种肺结核病.

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