揭示肝细胞癌的关键驱动因素:网络药理学,机器学习驱动配体发现和动态模拟的协同方法。

IF 2.3 3区 环境科学与生态学 Q3 CHEMISTRY, MULTIDISCIPLINARY SAR and QSAR in Environmental Research Pub Date : 2024-11-01 Epub Date: 2025-01-03 DOI:10.1080/1062936X.2024.2434577
D K Sabir, J A Bin Jumah, I Ancy
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引用次数: 0

摘要

肝细胞癌(HCC)在全球癌症相关死亡率中排名第四。本研究旨在通过网络药理学(network pharmacology, NP)揭示参与HCC的基因和途径,并通过基于机器学习(machine learning, ML)的配体筛选发现潜在的药物。此外,还进行了毒性预测、分子对接和分子动力学(MD)模拟。NP研究发现了与HCC相关的关键基因,特别是AKT1和GSK3β酶。通路分析显示,PI3K-AKT和WNT信号通路等关键通路在HCC进展中发挥关键作用。使用ML,鉴定出AKT1和GSK3β的潜在抑制剂,包括AKT1的CHEMBL2177361和CHEMBL403354,以及GSK3β的CHEMBL3652546和CHEMBL4641631。md后分析包括RMSD、2D-RMSD、RMSD聚类、RMSF、PCA、DCCM、停留时间分析、扩散系数、基于自编码器的降维、FEL和MM/GBSA来了解蛋白质与配体的相互作用。本研究揭示了抑制剂与AKT1和GSK3β的稳定相互作用。4种配合物的结合自由能分别为-39.9、-46.8、-41.6和-45.9 kcal/mol。本研究利用生物信息学工具对参与HCC进展和发病机制的基因和途径提供了新的见解。此外,基于ml的虚拟筛选发现了针对HCC靶蛋白(如AKT1和GSK3β)的有效抑制剂。
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Unveiling key drivers of hepatocellular carcinoma: a synergistic approach with network pharmacology, machine learning-driven ligand discovery and dynamic simulations.

Hepatocellular carcinoma (HCC) ranks fourth in cancer-related mortality worldwide. This study aims to uncover the genes and pathways involved in HCC through network pharmacology (NP) and to discover potential drugs via machine learning (ML)-based ligand screening. Additionally, toxicity prediction, molecular docking, and molecular dynamics (MD) simulations were conducted. NP study identified key genes related to HCC, particularly the enzymes AKT1 and GSK3β. Pathway analysis revealed that crucial pathways like PI3K-AKT and WNT signalling play pivotal roles in HCC progression. Using ML, potential inhibitors for AKT1 and GSK3β were identified, including CHEMBL2177361 and CHEMBL403354 for AKT1, and CHEMBL3652546 and CHEMBL4641631 for GSK3β. post-MD analyses, including RMSD, 2D-RMSD, RMSD cluster, RMSF, PCA, DCCM, residence time analysis, diffusion coefficient, autoencoder-based dimensionality reduction, FEL and MM/GBSA were performed to understand the protein-ligand interactions. The present study reveals the stable interactions of the inhibitors with AKT1 and GSK3β. The binding free energies of all the four complexes were -39.9, -46.8, -41.6, and -45.9 kcal/mol, respectively. This research provides novel insights into the genes and pathways involved in the progression and pathogenesis of HCC using bioinformatics tools. Furthermore, ML-based virtual screening identified potent inhibitors against the target proteins of HCC, such as AKT1 and GSK3β.

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来源期刊
CiteScore
5.20
自引率
20.00%
发文量
78
审稿时长
>24 weeks
期刊介绍: SAR and QSAR in Environmental Research is an international journal welcoming papers on the fundamental and practical aspects of the structure-activity and structure-property relationships in the fields of environmental science, agrochemistry, toxicology, pharmacology and applied chemistry. A unique aspect of the journal is the focus on emerging techniques for the building of SAR and QSAR models in these widely varying fields. The scope of the journal includes, but is not limited to, the topics of topological and physicochemical descriptors, mathematical, statistical and graphical methods for data analysis, computer methods and programs, original applications and comparative studies. In addition to primary scientific papers, the journal contains reviews of books and software and news of conferences. Special issues on topics of current and widespread interest to the SAR and QSAR community will be published from time to time.
期刊最新文献
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