Mondal Shakhinur Islam, Ferdous Sabiha, Jewel Nurnabi Azad, Akter Arzuba, Mahmud Zabed, Islam Md Muzahidul, Afrin Tanzila, Karim Nurul
Genetic Engineering and Biotechnology Department, Shahjalal University of Science and Technology, Sylhet, Bangladesh ; Division of Microbiology, Department of Infectious Diseases, Faculty of Medicine, University of Miyazaki, Miyazaki, Japan.
Genetic Engineering and Biotechnology Department, Shahjalal University of Science and Technology, Sylhet, Bangladesh.
Adv Appl Bioinform Chem. 2015 Dec 8;8:49-63. doi: 10.2147/AABC.S88522. eCollection 2015.
Bacterial enteric infections resulting in diarrhea, dysentery, or enteric fever constitute a huge public health problem, with more than a billion episodes of disease annually in developing and developed countries. In this study, the deadly agent of hemorrhagic diarrhea and hemolytic uremic syndrome, Escherichia coli O157:H7 was investigated with extensive computational approaches aimed at identifying novel and broad-spectrum antibiotic targets. A systematic in silico workflow consisting of comparative genomics, metabolic pathways analysis, and additional drug prioritizing parameters was used to identify novel drug targets that were essential for the pathogen's survival but absent in its human host. Comparative genomic analysis of Kyoto Encyclopedia of Genes and Genomes annotated metabolic pathways identified 350 putative target proteins in E. coli O157:H7 which showed no similarity to human proteins. Further bio-informatic approaches including prediction of subcellular localization, calculation of molecular weight, and web-based investigation of 3D structural characteristics greatly aided in filtering the potential drug targets from 350 to 120. Ultimately, 44 non-homologous essential proteins of E. coli O157:H7 were prioritized and proved to have the eligibility to become novel broad-spectrum antibiotic targets and DNA polymerase III alpha (dnaE) was the top-ranked among these targets. Moreover, druggability of each of the identified drug targets was evaluated by the DrugBank database. In addition, 3D structure of the dnaE was modeled and explored further for in silico docking with ligands having potential druggability. Finally, we confirmed that the compounds N-coeleneterazine and N-(1,4-dihydro-5H-tetrazol-5-ylidene)-9-oxo-9H-xanthene-2-sulfon-amide were the most suitable ligands of dnaE and hence proposed as the potential inhibitors of this target protein. The results of this study could facilitate the discovery and release of new and effective drugs against E. coli O157:H7 and other deadly human bacterial pathogens.
导致腹泻、痢疾或伤寒的细菌性肠道感染构成了一个巨大的公共卫生问题,在发展中国家和发达国家,每年发病超过10亿例。在本研究中,利用广泛的计算方法对出血性腹泻和溶血尿毒综合征的致命病原体大肠杆菌O157:H7进行了研究,旨在确定新的广谱抗生素靶点。采用了一种系统的计算机模拟工作流程,包括比较基因组学、代谢途径分析和其他药物优先排序参数,以识别对病原体生存至关重要但在其人类宿主中不存在的新药物靶点。对京都基因与基因组百科全书注释的代谢途径进行比较基因组分析,在大肠杆菌O157:H7中鉴定出350个假定的靶蛋白,这些蛋白与人类蛋白没有相似性。进一步的生物信息学方法,包括亚细胞定位预测、分子量计算以及基于网络的三维结构特征研究,极大地有助于将潜在药物靶点从350个筛选到120个。最终,对大肠杆菌O157:H7的44个非同源必需蛋白进行了优先排序,并证明它们有资格成为新的广谱抗生素靶点,其中DNA聚合酶IIIα(dnaE)在这些靶点中排名第一。此外,通过药物银行数据库评估了每个已鉴定药物靶点的成药性。此外,对dnaE的三维结构进行了建模,并进一步探索了与具有潜在成药性的配体进行计算机模拟对接。最后,我们证实化合物N-腔肠素和N-(1,4-二氢-5H-四唑-5-亚基)-9-氧代-9H-呫吨-2-磺酰胺是dnaE最合适的配体,因此被提议作为该靶蛋白的潜在抑制剂。本研究结果有助于发现和推出针对大肠杆菌O157:H7和其他致命人类细菌病原体的新型有效药物。