天然化合物对鲍曼不动杆菌SecA蛋白潜在抑制剂的筛选。

IF 3.9 2区 化学 Q2 CHEMISTRY, APPLIED
Aishwarya Swain, Smruti Sikha Senapati, Archana Pan
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引用次数: 0

摘要

SecA蛋白是细菌蛋白质转运系统中的重要蛋白,已被报道为多种细菌的有希望的药物靶点,包括多药耐药鲍曼不动杆菌,迫切需要开发新药。为此,本研究旨在筛选天然化合物作为该病原体SecA蛋白的潜在抑制剂。首先,对SecA蛋白进行结构建模,生成多个模型,并使用各种标准对其进行评估。选择最可靠的模型AlphaFold2中的Rank3进行分子动力学(MD)模拟研究,以获得能量最小化的结构。利用天然化合物数据库(LOTUS和CMNPD)对该结构进行虚拟筛选,鉴定出TCC、TMX、DDA、PF和DOP 5种天然化合物,对接分数分别为- 9.801 kcal/mol、- 9.565 kcal/mol、- 9.092 kcal/mol、- 8.862 kcal/mol和- 8.758 kcal/mol,显著优于已知的SecA抑制剂jc -21058 (- 3.92 kcal/mol)、Pannomycin (- 3.234 kcal/mol)和Rose Bengal (- 2.608 kcal/mol)。MD模拟研究证实了这五种化合物的蛋白质配体复合物的稳定性。虽然DOP的结合能最强(ΔG = - 46.93±6.11 kcal/mol),但由于其可引起呼吸毒性和眼睛刺激而被排除。另一方面,TMX显示出显著的结合能(ΔG = - 38.23±2.97 kcal/mol),复合物稳定性,良好的生物利用度和可接受的安全性,表明它是一种潜在的SecA蛋白抑制剂。因此,我们的研究揭示了一种天然化合物TMX作为针对特定靶蛋白的潜在抑制剂。这可以进一步进行实验验证,开发针对鲍曼不动杆菌/其他相关临床重要病原体引起的传染病的新药。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
In silico screening of natural compounds as potential inhibitors against SecA protein of Acinetobacter baumannii.

SecA protein is a vital protein in bacterial protein transport systems and has been reported as a promising drug target in various bacteria, including the multidrug-resistant Acinetobacter baumannii for which development of novel drugs are urgently needed. To this end, the present study aims to screen natural compounds as potential inhibitors against SecA protein of this pathogen. Initially, structural modeling of SecA protein was performed to generate multiple models, which were assessed using various criteria. The most reliable model, Rank3 from AlphaFold2, was selected for molecular dynamics (MD) simulation study to obtain an energy-minimized structure. Virtual screening of this energy-minimized structure against the natural compound databases (LOTUS and CMNPD) identified five natural compounds, namely TCC, TMX, DDA, PF, and DOP with docking scores of - 9.801 kcal/mol, - 9.565 kcal/mol, - 9.092 kcal/mol, - 8.862 kcal/mol, and - 8.758 kcal/mol, respectively, which were significantly better than those of known SecA inhibitors CJ-21058 (- 3.92 kcal/mol), Pannomycin (- 3.234 kcal/mol), and Rose Bengal (- 2.608 kcal/mol). MD simulation studies confirmed the stability of protein-ligand complexes for all five compounds. Although DOP demonstrated the strongest binding energy (ΔG = - 46.93 ± 6.11 kcal/mol), it was excluded as it could cause respiratory toxicity and eye irritation. TMX, on the other hand, showed significant binding energy (ΔG = - 38.23 ± 2.97 kcal/mol), complex stability, good bioavailability, and an acceptable safety profile, indicating it as a potential inhibitor against SecA protein. Thus, our study uncovers a natural compound TMX as a potential inhibitor against a specific target protein. This can be further explored for experimental validation to develop novel drugs against the infectious diseases caused by A. baumannii/other related clinically important pathogens.

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来源期刊
Molecular Diversity
Molecular Diversity 化学-化学综合
CiteScore
7.30
自引率
7.90%
发文量
219
审稿时长
2.7 months
期刊介绍: Molecular Diversity is a new publication forum for the rapid publication of refereed papers dedicated to describing the development, application and theory of molecular diversity and combinatorial chemistry in basic and applied research and drug discovery. The journal publishes both short and full papers, perspectives, news and reviews dealing with all aspects of the generation of molecular diversity, application of diversity for screening against alternative targets of all types (biological, biophysical, technological), analysis of results obtained and their application in various scientific disciplines/approaches including: combinatorial chemistry and parallel synthesis; small molecule libraries; microwave synthesis; flow synthesis; fluorous synthesis; diversity oriented synthesis (DOS); nanoreactors; click chemistry; multiplex technologies; fragment- and ligand-based design; structure/function/SAR; computational chemistry and molecular design; chemoinformatics; screening techniques and screening interfaces; analytical and purification methods; robotics, automation and miniaturization; targeted libraries; display libraries; peptides and peptoids; proteins; oligonucleotides; carbohydrates; natural diversity; new methods of library formulation and deconvolution; directed evolution, origin of life and recombination; search techniques, landscapes, random chemistry and more;
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