Computational Biology Lab, National Center for Bioinformatics, Quaid-i-Azam University, Islamabad, 45320, Pakistan.
Computational Biology Lab, National Center for Bioinformatics, Quaid-i-Azam University, Islamabad, 45320, Pakistan.
J Mol Graph Model. 2023 May;120:108425. doi: 10.1016/j.jmgm.2023.108425. Epub 2023 Feb 6.
Orientia tsutsugamushi, the causative agent of scrub typhus has been found resistant to various classes of antibiotics such as penicillins, gentamycin and cephalosporins. Review of current literature suggests that the prevalence of scrub typhus has increased globally. Therefore, the current study has aimed at exploring the genome of O. tsutsugamushi to identify potential drug target proteins that can be used for developing novel antibiotics against the pathogen. Subtractive proteomics approach has revealed FIS as a potential drug target protein involved in two component system (TCS), a signaling pathway crucial for bacteria to survive and adjust in changing environmental conditions. Molecular docking studies have revealed compound-356 (CHEMBRIDGE-10040641-3710.356) as a potential inhibitor in both chains A and B of the FIS protein. Simulation results suggest that the docked complex has remained stable and compact throughout the 200 ns run. Significant conformational changes including the hinge motion was observed in the DNA binding domain. Furthermore, the presence of salt bridge between GLU910 and ARG417, rearrangement of interaction residues and displacement of ATP in the central AAA + domain upon binding to the inhibitor were also observed playing a role in stabilizing the protein structure.
恙虫病东方体是恙虫病的病原体,已发现其对各种类别的抗生素(如青霉素、庆大霉素和头孢菌素)具有耐药性。对现有文献的综述表明,恙虫病的流行范围在全球范围内有所扩大。因此,本研究旨在探索恙虫病东方体的基因组,以鉴定潜在的药物靶标蛋白,用于开发针对病原体的新型抗生素。消减蛋白质组学方法揭示了 FIS 作为参与双组分系统(TCS)的潜在药物靶标蛋白,该系统是细菌在不断变化的环境条件下生存和适应的关键信号通路。分子对接研究表明,化合物 356(CHEMBRIDGE-10040641-3710.356)可作为 FIS 蛋白的两个亚基 A 和 B 中的潜在抑制剂。模拟结果表明,对接复合物在 200 ns 的运行过程中保持稳定和紧凑。在 DNA 结合域中观察到显著的构象变化,包括铰链运动。此外,在与抑制剂结合时,还观察到 GLU910 和 ARG417 之间形成盐桥、相互作用残基的重排以及中央 AAA+ 域中 ATP 的位移,这些都对稳定蛋白质结构起到了作用。