qsar驱动的潜在抗h1n1抑制剂的发现和排序

IF 3.3 Q2 MULTIDISCIPLINARY SCIENCES
Imad Hammoudan , Nouh Mounadi , Meriem Khedraoui , Imane Yamari , Samir Chtita , Adil Touimi Benjelloun
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引用次数: 0

摘要

甲型流感病毒(IAV)是对人类的主要呼吸道威胁,其大流行的潜力在于其基因重组的高发生率和能力。神经氨酸酶(NA)是一种介导新合成病毒颗粒释放的表面糖蛋白,是其繁殖的关键因素。在这项工作中,我们对168个靶向NA的候选分子进行了全面的计算机研究,整合了定量构效关系(QSAR)建模、分子对接和分子动力学(MD)模拟。基于机制相关性和计算简单性选择的二维描述符构建的QSAR模型显示出强大的预测能力(R²= 0.82;Q²= 0.81),符合OECD验证标准。根据对接分数排名靠前的化合物进行ADMET筛选,然后进行MD模拟以评估复合物的稳定性。随后,使用MM/PBSA方法进行自由能计算,以估计最有希望的配体-蛋白质复合物的结合亲和力,为其相互作用谱提供更深入的热力学见解。在测试的分子中,一些候选分子因其良好的结合行为和药代动力学特性而脱颖而出,为未来抗流感药物的开发提供了有希望的基础。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
QSAR-driven discovery and ranking of potential anti-H1N1 inhibitors
The Influenza A virus (IAV), a major respiratory threat to humans, owes its pandemic potential to a high rate and capacity for genetic reassortment. A pivotal factor in its propagation is neuraminidase (NA), a surface glycoprotein that mediates the release of newly synthesized viral particles. In this work, we undertook a comprehensive in silico investigation of 168 candidate molecules targeting NA, integrating quantitative structure-activity relationship (QSAR) modeling, molecular docking, and molecular dynamics (MD) simulations. The QSAR model, constructed using 2D descriptors selected for their mechanistic relevance and computational simplicity, showed strong predictive power (R² = 0.82; Q² = 0.81), in line with OECD validation standards. Top-ranking compounds based on docking scores underwent ADMET screening, followed by MD simulations to evaluate complex stability. Subsequently, free energy calculations using the MM/PBSA approach were performed to estimate the binding affinities of the most promising ligand–protein complexes, providing deeper thermodynamic insight into their interaction profiles. Among the molecules tested, several candidates stood out for their favorable binding behavior and pharmacokinetic properties, offering a promising basis for the future development of anti-influenza drugs.
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来源期刊
Scientific African
Scientific African Multidisciplinary-Multidisciplinary
CiteScore
5.60
自引率
3.40%
发文量
332
审稿时长
10 weeks
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