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金属β-乳糖酶对taniborbactam耐药性的结构基础

Salvador I Drusin¹, Christophe Le Terrier^2,3, Laurent Poirel^2,4

¹Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Rosario, Argentina.

Antimicrobial agents and chemotherapy

|December 8, 2023

概括

新的双循环酸盐抑制剂,如taniborbactam,可以对抗抗卡巴耐药的细菌. 然而,金属β-乳糖酶中的单个突变可以通过破坏抑制剂结合来引起耐药性,这对新型抗菌疗法构成了挑战.

科学领域:

微生物学微生物学
药用化学医学化学
计算生物学计算生物学

背景情况:

金属β-乳酸酶 (MBLs) 是一种主要的威胁,在耐卡巴胺的格拉姆阴性病原体.
双循环酸盐,包括taniborbactam,代表了对抗MBLs的有希望的策略.
新兴的耐药性,如NDM-9逃离taniborbactam,需要了解耐药性机制.

研究的目的:

调查金属β-乳酸酶中对双循环酸盐抑制剂的耐药性的分子基础.
确定单个氨基酸替代物赋予对taniborbactam的耐药性的机制.
为设计下一代不太容易产生抗性的MBL抑制剂提供见解.

主要方法:

对接分析对接分析
蛋白质 - 配体相互作用的计算分析.
分析MBL活性部位的静电相互作用.

主要成果:

对taniborbactam的耐药性可能是由于抑制剂的侧链和MBL活性位点循环之间的静电相互作用被破坏而产生的.
在非必需的MBL残留物中单个氨基酸的替代可以导致taniborbactam的非生产性结合模式.
这种抵抗机制不仅仅局限于NDM-9,而且可以影响其他MBL变体.

结论:

在MBL中单点突变可能会意外导致对高级抑制剂如taniborbactam的耐药性.
了解这些耐药性机制对于持续开发有效的抗微生物疗法至关重要.
需要进一步的研究来设计规避常见抗药途径的MBL抑制剂.

关键词:

在NDM-9中,它是NDM-9.金属-β-乳酸的存在.坦尼博巴克坦的抗药性

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