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利用虚拟筛选、分子对接和动力学模拟发现耐多药铜绿假单胞菌中的新型DdlA抑制剂。

Discovery of novel DdlA inhibitors in multidrug-resistant Pseudomonas aeruginosa using virtual screening, molecular docking, and dynamics simulations.

作者信息

Aldakheel Fahad M, Alduraywish Shatha A

机构信息

Department of Clinical Laboratory Sciences, College of Applied Medical Sciences, King Saud University, 11433, Riyadh, Saudi Arabia.

Department of Family and Community Medicine, College of Medicine, King Saud University, Riyadh, Saudi Arabia.

出版信息

Sci Rep. 2025 May 1;15(1):15290. doi: 10.1038/s41598-025-97698-6.

Abstract

Pseudomonas aeruginosa is a gram-negative, opportunistic pathogen that represents a serious risk factor in healthcare services due to its natural resistance mechanisms and the increasing prevalence of multi-drug resistant strains. This study utilized in silico computational approaches to identify the novel inhibitors for D-alanine-D-alanine ligase A (DdlA), an essential enzyme for the bacterial peptidoglycan biosynthesis pathway necessary for cell wall integrity. A structure-based virtual screening of The Medicinal Fungi Secondary Metabolites and Therapeutics (MeFSAT) chemical library was conducted, followed by molecular docking to evaluate the binding affinity of small molecules to the DdlA active site. MSID000191, MSID000200, and MSID000102 were recognized as the leading candidates in the preliminary docking data due to their low binding energy values. These compounds exhibited binding energies markedly superior to the control drug (D-cycloserine), suggesting a substantial potential for inhibiting the DdlA enzyme. Detailed interaction analyses revealed significant salt bridges and hydrogen bonds with active site residues, which enhance the stability of the complex. Density Functional Theory (DFT) analysis and MMPBSA calculations also provided insights into electronic properties and binding free energy, respectively. These findings highlight the potential of these inhibitors as therapeutic candidates and showcase the effectiveness of computational methods in accelerating drug discovery against multidrug-resistant P. aeruginosa. Future research should incorporate more in-silico techniques and experimental validations to confirm these results.

摘要

铜绿假单胞菌是一种革兰氏阴性机会致病菌,由于其天然耐药机制以及多重耐药菌株的日益流行,它在医疗服务中是一个严重的风险因素。本研究利用计算机计算方法来鉴定D-丙氨酸-D-丙氨酸连接酶A(DdlA)的新型抑制剂,DdlA是细菌肽聚糖生物合成途径中对细胞壁完整性至关重要的一种必需酶。对药用真菌次生代谢产物与治疗学(MeFSAT)化学库进行了基于结构的虚拟筛选,随后进行分子对接以评估小分子与DdlA活性位点的结合亲和力。由于其低结合能值,MSID000191、MSID000200和MSID000102在初步对接数据中被识别为主要候选物。这些化合物表现出明显优于对照药物(D-环丝氨酸)的结合能,表明其具有抑制DdlA酶的巨大潜力。详细的相互作用分析揭示了与活性位点残基形成的显著盐桥和氢键,这增强了复合物的稳定性。密度泛函理论(DFT)分析和MMPBSA计算分别提供了对电子性质和结合自由能的见解。这些发现突出了这些抑制剂作为治疗候选物的潜力,并展示了计算方法在加速针对多重耐药铜绿假单胞菌的药物发现中的有效性。未来的研究应纳入更多的计算机技术和实验验证来证实这些结果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/26c8/12046020/53916f7fb5ab/41598_2025_97698_Fig1_HTML.jpg

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