猴痘病毒甲基转移酶的结构和计算分析:动态抑制机制及其对抗病毒设计的意义。

IF 3.8 2区 化学 Q2 CHEMISTRY, APPLIED
Muhammad Waqas, Syed Ahsan Shahid, Muhammad Shahab, Yongkun Zhu, Aamir Fahira, Zunnan Huang
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引用次数: 0

摘要

猴痘是一种新出现的全球健康威胁,需要开发有效的抗病毒药物。在我们的研究中,我们选择了m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起作用。MTase蛋白在m痘中是必不可少的,并且与COVID-19等其他病毒的类似复制机制相关,使其成为抗病毒治疗的广谱靶标。我们通过分子对接,结合药代动力学分析,筛选库存中针对MTase蛋白的ZINC20化合物,评估其结合亲和力和药物样性质,并进行分子动力学模拟,观察蛋白-配体复合物的稳定性和随时间的构象变化。对接结果显示,ZINC257233856的结合能最高,为- 7.68 kcal/mol,表明其与MTase蛋白的相互作用较强,其次为其他化合物。所有为研究选择的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,所选择的化合物,特别是ZINC257233856,在MTase结合口袋中表现出显著的稳定性。此外,利用网格不均匀溶剂化理论(GIST)研究了溶剂化热力学,揭示了关键的水化模式和热力学热点,进一步支持了顶级抑制剂的结合稳定性。因此,我们的研究表明,选定的化合物作为治疗m痘的选择有很大的潜力。我们的发现为进一步的临床研究和开发有效的治疗方法奠定了基础。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Structural and computational analysis of monkeypox virus methyltransferase: dynamic inhibition mechanisms and their implications for antiviral design.

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.

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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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