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重新利用美国食品药品监督管理局(FDA)批准的药物对抗登革病毒NS1蛋白的寡聚化结构域:一种计算方法。

Repurposing of FDA-approved drugs against oligomerization domain of dengue virus NS1 protein: a computational approach.

作者信息

Chaudhuri Dwaipayan, Ghosh Medha, Majumder Satyabrata, Giri Kalyan

机构信息

Department of Life Sciences, Presidency University, 86/1 College Street, Kolkata, 700073, India.

出版信息

Mol Divers. 2025 Apr;29(2):1619-1639. doi: 10.1007/s11030-024-10936-3. Epub 2024 Jul 17.

Abstract

Dengue fever is a serious health hazard on a global scale and its primary causative agent is the dengue virus (DENV). The non-structural protein 1 (NS1) of DENV plays a pivotal role in pathogenesis. It is associated with several autoimmune events, endothelial cell apoptosis, and vascular leakage, which increase mainly during the critical phase of infection. In this study, important residues of the oligomerization domain of NS1 protein were identified by literature searches. Virtual screening has been conducted using the entire dataset of the DrugBank database and the potential small-molecule inhibitors against the NS1 protein have been chosen on the basis of binding energy values. This is succeeded by molecular dynamics (MD) simulations of the shortlisted compounds, ultimately giving rise to five compounds. These five compounds were further subjected to RAMD simulations by applying a random direction force of specific magnitude on the ligand center of mass in order to push the ligand out of the protein-binding pocket, for the quantitative estimation of their binding energy values to determine the interaction strength between protein and ligand which prevents ligand unbinding from its binding site, ultimately leading to the selection of three major compounds, DB00826 (Natamycin), DB11274 (Dihydro-alphaergocryptine), and DB11275 (Epicriptine), with the DB11274 having a role against idiopathic Parkinson's disease, and thus may have possible important roles in the prevention of dengue-associated Parkinsonism. These compounds may act as prospective drugs against dengue, by preventing the oligomerization of the NS1 protein, thereby preventing disease progression and pathogenesis.

摘要

登革热在全球范围内是一种严重的健康危害,其主要病原体是登革热病毒(DENV)。DENV的非结构蛋白1(NS1)在发病机制中起关键作用。它与多种自身免疫事件、内皮细胞凋亡和血管渗漏有关,这些主要在感染的关键阶段增加。在本研究中,通过文献检索确定了NS1蛋白寡聚化结构域的重要残基。使用DrugBank数据库的整个数据集进行了虚拟筛选,并根据结合能值选择了针对NS1蛋白的潜在小分子抑制剂。通过对入围化合物进行分子动力学(MD)模拟成功实现了这一点,最终产生了五种化合物。通过对配体质心施加特定大小的随机方向力,对这五种化合物进一步进行随机加速分子动力学(RAMD)模拟,以将配体推出蛋白质结合口袋,用于定量估计它们的结合能值,以确定蛋白质与配体之间的相互作用强度,从而防止配体从其结合位点解离,最终筛选出三种主要化合物,即DB00826(游霉素)、DB11274(二氢-α-麦角隐亭)和DB11275(表隐亭),其中DB11274对特发性帕金森病有作用,因此可能在预防登革热相关帕金森综合征中发挥重要作用。这些化合物可能通过阻止NS1蛋白的寡聚化,从而预防疾病进展和发病机制,成为抗登革热的潜在药物。

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