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猴痘病毒甲基转移酶的结构与计算分析:动态抑制机制及其对抗病毒设计的意义

Structural and computational analysis of monkeypox virus methyltransferase: dynamic inhibition mechanisms and their implications for antiviral design.

作者信息

Waqas Muhammad, Shahid Syed Ahsan, Shahab Muhammad, Zhu Yongkun, Fahira Aamir, Huang Zunnan

机构信息

The Affiliated Dongguan Songshan Lake Central Hospital, Guangdong Medical University, Dongguan, 523326, Guangdong, People's Republic of China.

Guangdong Medical University Key Laboratory of Big Data Mining and Precision Drug Design, Dongguan Key Laboratory of Computer-Aided Drug Design, Guangdong Provincial Key Laboratory for Research and Development of Natural Drugs, School of Pharmacy, Guangdong Medical University, Dongguan, 523808, Guangdong, People's Republic of China.

出版信息

Mol Divers. 2025 Aug 13. doi: 10.1007/s11030-025-11258-8.

Abstract

Monkeypox (Mpox), an emerging global health threat, necessitates the development of effective antiviral agents. In our study, we selected the Mpox virus methyltransferase VP39 (MTase) protein due to its role in viral replication and immune evasion. The MTase protein is essential in Mpox and is associated with similar replication mechanisms in other viruses like COVID-19, making it a broad-spectrum target for antiviral therapy. We screened the ZINC20 in-stock compounds against the MTase protein, utilizing molecular docking, accompanied by pharmacokinetic analysis to assess their binding affinity and drug-like properties, and conducted molecular dynamic simulations to observe the stability and conformational changes of the protein-ligand complexes over time. The docking results revealed that the highest binding energy was exhibited by ZINC257233856, with a value of - 7.68 kcal/mol, indicating a strong interaction with the MTase protein followed by the other compounds. All the compounds selected for the study showed consistently acceptable safety profiles. Molecular dynamics simulations demonstrated that the selected compounds, specifically ZINC257233856, showed significant stability within the MTase binding pocket. Additionally, solvation thermodynamics were investigated using Grid Inhomogeneous Solvation Theory (GIST), revealing key hydration patterns and thermodynamic hotspots that further support the binding stability of top-ranked inhibitors. Thus, our study demonstrates the promising potential of selected compounds as therapeutic options against Mpox. Our findings lay a foundational basis for further clinical investigation and the development of effective treatments.

摘要

猴痘是一种新出现的全球健康威胁,因此需要开发有效的抗病毒药物。在我们的研究中,我们选择了猴痘病毒甲基转移酶VP39(MTase)蛋白,因为它在病毒复制和免疫逃避中发挥作用。MTase蛋白在猴痘中至关重要,并且与其他病毒(如COVID-19)的类似复制机制相关,使其成为抗病毒治疗的广谱靶点。我们利用分子对接技术,对ZINC20库存化合物针对MTase蛋白进行筛选,并通过药代动力学分析评估它们的结合亲和力和类药性质,还进行了分子动力学模拟,以观察蛋白质-配体复合物随时间的稳定性和构象变化。对接结果显示,ZINC257233856表现出最高的结合能,值为-7.68 kcal/mol,表明它与MTase蛋白有很强的相互作用,其次是其他化合物。本研究中选择的所有化合物都显示出一致的可接受的安全性。分子动力学模拟表明,所选化合物,特别是ZINC257233856,在MTase结合口袋内表现出显著的稳定性。此外,使用网格非均匀溶剂化理论(GIST)研究了溶剂化热力学,揭示了关键的水合模式和热力学热点,进一步支持了排名靠前的抑制剂的结合稳定性。因此,我们的研究证明了所选化合物作为抗猴痘治疗选择的潜在前景。我们的发现为进一步的临床研究和有效治疗方法的开发奠定了基础。

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