针对登革热病毒 NS1 蛋白寡聚结构域的 FDA 批准药物的再利用:一种计算方法。

IF 3.9 2区 化学 Q2 CHEMISTRY, APPLIED Molecular Diversity Pub Date : 2024-07-17 DOI:10.1007/s11030-024-10936-3
Dwaipayan Chaudhuri, Medha Ghosh, Satyabrata Majumder, Kalyan Giri
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引用次数: 0

摘要

登革热是一种严重危害全球健康的疾病,其主要病原体是登革热病毒(DENV)。登革热病毒的非结构蛋白 1(NS1)在发病机制中起着关键作用。它与多种自身免疫事件、内皮细胞凋亡和血管渗漏有关,主要在感染的临界期增加。本研究通过文献检索确定了 NS1 蛋白寡聚化结构域的重要残基。利用 DrugBank 数据库的整个数据集进行了虚拟筛选,并根据结合能值选出了针对 NS1 蛋白的潜在小分子抑制剂。随后对入围化合物进行了分子动力学(MD)模拟,最终确定了五种化合物。对这五种化合物进一步进行 RAMD 模拟,在配体质心上施加特定大小的随机方向力,以将配体推出蛋白质结合口袋,从而定量估算其结合能值,确定蛋白质与配体之间阻止配体从其结合位点解除结合的相互作用强度、最终选择了 DB00826(纳他霉素)、DB11274(二氢-α-麦角隐亭)和 DB11275(表隐亭)这三种主要化合物,其中 DB11274 具有防治特发性帕金森病的作用,因此可能在预防登革热相关帕金森病方面发挥重要作用。这些化合物通过阻止 NS1 蛋白的寡聚化,从而防止疾病的发展和发病机制,可作为预防登革热的前瞻性药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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

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.

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来源期刊
Molecular Diversity
Molecular Diversity 化学-化学综合
CiteScore
7.30
自引率
7.90%
发文量
219
审稿时长
2.7 months
期刊介绍: Molecular Diversity is a new publication forum for the rapid publication of refereed papers dedicated to describing the development, application and theory of molecular diversity and combinatorial chemistry in basic and applied research and drug discovery. The journal publishes both short and full papers, perspectives, news and reviews dealing with all aspects of the generation of molecular diversity, application of diversity for screening against alternative targets of all types (biological, biophysical, technological), analysis of results obtained and their application in various scientific disciplines/approaches including: combinatorial chemistry and parallel synthesis; small molecule libraries; microwave synthesis; flow synthesis; fluorous synthesis; diversity oriented synthesis (DOS); nanoreactors; click chemistry; multiplex technologies; fragment- and ligand-based design; structure/function/SAR; computational chemistry and molecular design; chemoinformatics; screening techniques and screening interfaces; analytical and purification methods; robotics, automation and miniaturization; targeted libraries; display libraries; peptides and peptoids; proteins; oligonucleotides; carbohydrates; natural diversity; new methods of library formulation and deconvolution; directed evolution, origin of life and recombination; search techniques, landscapes, random chemistry and more;
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