通过机器学习、分子对接和动力学模拟鉴定痴呆中FUS蛋白的天然抑制剂。

IF 2.5 4区 医学 Q2 MATHEMATICAL & COMPUTATIONAL BIOLOGY
Frontiers in Neuroinformatics Pub Date : 2025-02-05 eCollection Date: 2024-01-01 DOI:10.3389/fninf.2024.1439090
Darwin Li
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引用次数: 0

摘要

痴呆症是一种复杂的、使人衰弱的神经退行性疾病,对寻求有效治疗提出了深刻的挑战。FUS蛋白是这个问题的核心,因为它在各种疾病中经常失调。我们选择了一条计算工作路线,包括靶向FUS蛋白的天然抑制剂,提供了一种新的治疗策略。我们首先回顾了FUS蛋白的结构;使用AlphaFold2和SwissModel算法的早期预测模型显示了一种富含环的蛋白质-一种与灵活性相关的结构成分。然而,这些模型显示出局限性,ERRAT和Verify3D评分不足。为了提高准确性,我们转向I-TASSER套件,该套件提供了经过稳健验证指标确认的精致结构模型。有了一个可靠的模型,我们的研究利用机器学习技术,特别是随机森林算法,来浏览大量的植物化学物质数据集。这导致了nimbinin, dehydroxymethylflazine和其他几种化合物作为潜在的FUS抑制剂的鉴定。值得注意的是,在AutoDock vina的分子对接分析中,dehydroxymethylflazine和cleroindicin C被鉴定出具有高结合亲和力和与FUS蛋白相互作用的稳定性,这一点得到了广泛的分子动力学模拟的证实。这些化合物来源于药用植物,不仅在结构上与靶蛋白相容,而且具有适合药物开发的药代动力学特征,包括有利于穿透血脑屏障的最佳分子量和LogP值。这一计算探索为随后的实验验证铺平了道路,并强调了这些天然化合物作为治疗痴呆症的创新药物的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Identifying natural inhibitors against FUS protein in dementia through machine learning, molecular docking, and dynamics simulation.

Dementia, a complex and debilitating spectrum of neurodegenerative diseases, presents a profound challenge in the quest for effective treatments. The FUS protein is well at the center of this problem, as it is frequently dysregulated in the various disorders. We chose a route of computational work that involves targeting natural inhibitors of the FUS protein, offering a novel treatment strategy. We first reviewed the FUS protein's framework; early forecasting models using the AlphaFold2 and SwissModel algorithms indicated a loop-rich protein-a structure component correlating with flexibility. However, these models showed limitations, as reflected by inadequate ERRAT and Verify3D scores. Seeking enhanced accuracy, we turned to the I-TASSER suite, which delivered a refined structural model affirmed by robust validation metrics. With a reliable model in hand, our study utilized machine learning techniques, particularly the Random Forest algorithm, to navigate through a vast dataset of phytochemicals. This led to the identification of nimbinin, dehydroxymethylflazine, and several other compounds as potential FUS inhibitors. Notably, dehydroxymethylflazine and cleroindicin C identified during molecular docking analyses-facilitated by AutoDock Vina-for their high binding affinities and stability in interaction with the FUS protein, as corroborated by extensive molecular dynamics simulations. Originating from medicinal plants, these compounds are not only structurally compatible with the target protein but also adhere to pharmacokinetic profiles suitable for drug development, including optimal molecular weight and LogP values conducive to blood-brain barrier penetration. This computational exploration paves the way for subsequent experimental validation and highlights the potential of these natural compounds as innovative agents in the treatment of dementia.

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来源期刊
Frontiers in Neuroinformatics
Frontiers in Neuroinformatics MATHEMATICAL & COMPUTATIONAL BIOLOGY-NEUROSCIENCES
CiteScore
4.80
自引率
5.70%
发文量
132
审稿时长
14 weeks
期刊介绍: Frontiers in Neuroinformatics publishes rigorously peer-reviewed research on the development and implementation of numerical/computational models and analytical tools used to share, integrate and analyze experimental data and advance theories of the nervous system functions. Specialty Chief Editors Jan G. Bjaalie at the University of Oslo and Sean L. Hill at the École Polytechnique Fédérale de Lausanne are supported by an outstanding Editorial Board of international experts. This multidisciplinary open-access journal is at the forefront of disseminating and communicating scientific knowledge and impactful discoveries to researchers, academics and the public worldwide. Neuroscience is being propelled into the information age as the volume of information explodes, demanding organization and synthesis. Novel synthesis approaches are opening up a new dimension for the exploration of the components of brain elements and systems and the vast number of variables that underlie their functions. Neural data is highly heterogeneous with complex inter-relations across multiple levels, driving the need for innovative organizing and synthesizing approaches from genes to cognition, and covering a range of species and disease states. Frontiers in Neuroinformatics therefore welcomes submissions on existing neuroscience databases, development of data and knowledge bases for all levels of neuroscience, applications and technologies that can facilitate data sharing (interoperability, formats, terminologies, and ontologies), and novel tools for data acquisition, analyses, visualization, and dissemination of nervous system data. Our journal welcomes submissions on new tools (software and hardware) that support brain modeling, and the merging of neuroscience databases with brain models used for simulation and visualization.
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