Swain Aishwarya, Senapati Smruti Sikha, Pan Archana
Department of Bioinformatics, School of Life Sciences, Pondicherry University, R.V. Nagar, Kalapet, Puducherry, 605014, India.
Mol Divers. 2025 Feb 7. doi: 10.1007/s11030-024-11097-z.
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.
SecA蛋白是细菌蛋白质转运系统中的一种重要蛋白质,据报道,它是包括多重耐药鲍曼不动杆菌在内的多种细菌中有前景的药物靶点,针对该菌迫切需要开发新型药物。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。最初,对SecA蛋白进行结构建模以生成多个模型,并使用各种标准对其进行评估。选择最可靠的模型,即来自AlphaFold2的Rank3模型,进行分子动力学(MD)模拟研究以获得能量最小化结构。针对天然化合物数据库(LOTUS和CMNPD)对该能量最小化结构进行虚拟筛选,鉴定出五种天然化合物,即TCC、TMX、DDA、PF和DOP,其对接分数分别为-9.801 kcal/mol、-9.565 kcal/mol、-9.092 kcal/mol、-8.862 kcal/mol和-8.7五8 kcal/mol,这些分数明显优于已知的SecA抑制剂CJ-21058(-3.92 kcal/mol)、泛霉素(-3.234 kcal/mol)和孟加拉玫瑰红(-2.608 kcal/mol)。MD模拟研究证实了所有五种化合物的蛋白质-配体复合物的稳定性。尽管DOP表现出最强的结合能(ΔG = -46.93±6.11 kcal/mol),但由于它可能导致呼吸道毒性和眼睛刺激而被排除。另一方面,TMX表现出显著的结合能(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SecA蛋白的潜在抑制剂。因此,我们的研究发现一种天然化合物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,以开发针对由鲍曼不动杆菌/其他相关临床重要病原体引起的传染病的新型药物。