Suppr超能文献

基于药效团模型的虚拟筛选和分子动力学鉴定了针对沃氏衣原体的新型抑制剂和药物靶标。

Pharmacophore modelling based virtual screening and molecular dynamics identified the novel inhibitors and drug targets against Waddlia chondrophila.

机构信息

Banner Sun Health Research Institute, Sun City, AZ, USA.

Department of Zoology, College of Science, King Saud University, P.O. Box 2455, 11451, Riyadh, Saudi Arabia.

出版信息

Sci Rep. 2024 Jun 12;14(1):13472. doi: 10.1038/s41598-024-63555-1.

Abstract

Waddlia chondrophila is a possible cause of fetal death in humans. This Chlamydia-related bacterium is an emergent pathogen that causes human miscarriages and ruminant abortions, which results in financial losses. Despite the years of efforts, the underlying mechanism behind the pathogenesis of W. chondrophila is little known which hindered the development of novel treatment options. In the framework of current study, computational approaches were used to identify novel inhibitors (phytocompounds) and drug targets against W. chondrophila. At first, RNA polymerase sigma factor SigA and 3-deoxy-D-manno-octulosonic acid transferase were identified through subtractive proteomics pipeline. Afterwards, extensive docking and simulation analyses were conducted to optimize potentially novel phytocompounds by assessing their binding affinity to target proteins. A 100ns molecular dynamics simulation well complimented the compound's binding affinity and indicated strong stability of predicted compounds at the docked site. The calculation of binding free energies with MMGBSA corroborated the significant binding affinity between phytocompounds and target protein binding sites. The proposed phytocompounds may be a viable treatment option for patients infected with W. chondrophila; however, further research is required to ensure their safety.

摘要

软骨弯杆菌可能是导致人类胎儿死亡的原因。这种与衣原体相关的细菌是一种新兴病原体,可导致人类流产和反刍动物流产,造成经济损失。尽管多年来努力研究,软骨弯杆菌发病机制的潜在机制仍知之甚少,这阻碍了新型治疗方法的开发。在当前研究框架中,使用计算方法来鉴定针对软骨弯杆菌的新型抑制剂(植物化合物)和药物靶点。首先,通过消减蛋白质组学管道鉴定 RNA 聚合酶 sigma 因子 SigA 和 3-脱氧-D-甘露庚酮糖酸转移酶。然后,通过评估它们与靶蛋白的结合亲和力,进行广泛的对接和模拟分析,以优化潜在的新型植物化合物。100ns 分子动力学模拟很好地补充了化合物的结合亲和力,并表明预测化合物在对接位点具有很强的稳定性。用 MMGBSA 计算结合自由能证实了植物化合物与靶蛋白结合位点之间的显著结合亲和力。所提出的植物化合物可能是治疗感染软骨弯杆菌患者的可行方法;但是,需要进一步的研究以确保其安全性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7aa5/11169463/66afe11fda65/41598_2024_63555_Fig1_HTML.jpg

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验