以肺炎克雷伯氏菌中的 MurG 酶为靶标:新型抗菌药发现的硅学方法。

IF 2.5 4区 生物学 Q3 MICROBIOLOGY
Pragati Mahur, Amit Kumar Singh, Jayaraman Muthukumaran, Monika Jain
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引用次数: 0

摘要

抗生素的广泛使用引发了抗生素耐药性这一全球性危机,尤其是针对肺炎克雷伯氏菌等革兰氏阴性菌的耐药性,肺炎克雷伯氏菌是医院感染的主要病因,死亡率很高。当务之急是确定有效的药物靶点,重点是抑制细菌生长的代谢途径。针对肺炎克雷伯菌的关键代谢途径将是防止其生长和引发疾病的更有效方法。本研究的重点是抑制 UDP-N-acetylglucosamine--N-acetylmuramyl-(pentapeptide)pyrophosphoryl-undecaprenol N-acetylglucosamine transferase (MurG) 酶,它是肽聚糖生物合成途径中的一个关键酶。研究人员利用高通量虚拟筛选技术,从 Enamine 高通量筛选中心库中寻找可能的先导分子。对筛选出的高结合亲和力配体进一步评估了其药物相似性和其他药代动力学特性。在这些分析的基础上,选择了 Z95813755_1、Z324718246_1 和 Z324718246_2 这三种配体进行进一步的分子动力学模拟研究。分子动力学模拟结果和 MM/PBSA 分析表明,Z95813755_1 和 Z324718246_2 分子对 MurG 有更高的结合亲和力。我们首次报告了针对肺炎克雷伯菌 MurG 的潜在候选抑制剂,为治疗多重耐药肺炎克雷伯菌感染提供了新的思路。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Targeting MurG enzyme in Klebsiella pneumoniae: An in silico approach to novel antimicrobial discovery.

Antibiotic resistance poses a global crisis fuelled by widespread antibiotic use, particularly against Gram-negative bacteria like Klebsiella pneumoniae, a leading cause of hospital-acquired infections with high mortality rates. Urgent identification of effective drug targets is imperative, with a focus on metabolic pathways to inhibit bacterial growth. Targeting the crucial metabolic pathways of K. pneumoniae would be a more efficient way to prevent its growth and the diseases that it causes. The present study focused on inhibiting the UDP-N-acetylglucosamine--N-acetylmuramyl-(pentapeptide)pyrophosphoryl-undecaprenol N-acetylglucosamine transferase (MurG) enzyme, which is a key enzyme in peptidoglycan biosynthesis pathway. A high throughput virtual screening was used to find possible lead molecules from Enamine -High-Throughput Screening Center library. The resulting high binding affinity ligands were further assessed for their drug-likeness and other pharmacokinetic properties. Based on these analyses, the three ligands Z95813755_1, Z324718246_1 and Z324718246_2 were selected for further molecular dynamic simulation studies. The molecular dynamic simulation results and MM/PBSA analysis predicted that both Z95813755_1 and Z324718246_2, molecules show higher binding affinity towards MurG. For the first time we are reporting potential candidate inhibitors against MurG from K. pneumoniae, providing new insights in management of multi drug resistant K. pneumoniae infections.

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来源期刊
Research in microbiology
Research in microbiology 生物-微生物学
CiteScore
4.10
自引率
3.80%
发文量
54
审稿时长
16 days
期刊介绍: Research in Microbiology is the direct descendant of the original Pasteur periodical entitled Annales de l''Institut Pasteur, created in 1887 by Emile Duclaux under the patronage of Louis Pasteur. The Editorial Committee included Chamberland, Grancher, Nocard, Roux and Straus, and the first issue began with Louis Pasteur''s "Lettre sur la Rage" which clearly defines the spirit of the journal:"You have informed me, my dear Duclaux, that you intend to start a monthly collection of articles entitled "Annales de l''Institut Pasteur". You will be rendering a service that will be appreciated by the ever increasing number of young scientists who are attracted to microbiological studies. In your Annales, our laboratory research will of course occupy a central position, but the work from outside groups that you intend to publish will be a source of competitive stimulation for all of us."That first volume included 53 articles as well as critical reviews and book reviews. From that time on, the Annales appeared regularly every month, without interruption, even during the two world wars. Although the journal has undergone many changes over the past 100 years (in the title, the format, the language) reflecting the evolution in scientific publishing, it has consistently maintained the Pasteur tradition by publishing original reports on all aspects of microbiology.
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