通过抑制囊膜蛋白和阻断 RNA 封装来破坏登革热病毒组装的小分子研究。

IF 3.9 2区 化学 Q2 CHEMISTRY, APPLIED
Hrithika Panday, Abhimanyu Kumar Jha, Vivek Dhar Dwivedi
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引用次数: 0

摘要

登革热是一个重大的全球公共卫生问题,在全世界造成大量的发病和死亡。这种疾病有多种表现形式,从轻微发热到可能危及生命的并发症。开发有效的治疗方法仍然是医疗保健系统面临的严峻挑战。尽管进行了广泛的研究,但目前还没有抗病毒药物获准用于登革热的预防或治疗。在病毒附着的早期阶段锁定目标对于抑制病毒复制至关重要。囊壳蛋白在病毒的结构完整性、组装和病毒基因组释放中起着至关重要的作用。在本研究中,我们采用了一种以囊膜蛋白为重点的计算方法,从美国食品药物管理局批准的药物库中找出可能的登革热病毒强效抑制剂。我们对美国 FDA 批准的药物进行了高通量虚拟筛选,以确定有可能抗击登革热的药物分子,同时节省成本和时间。筛选过程确定了四个药物分子(Nordihydroguaiaretic acid、Ifenprodil tartrate、Lathyrol 和 Safinamide Mesylate),依据是它们的最高结合亲和力和 MM/GBSA 分数。其中,去甲二氢愈创木脂酸的结合亲和力比参照分子高,为-11.66 kcal/mol。相比之下,酒石酸艾芬地尔和 Lathyrol 的结果与参考分子相似,其结合能分别为 - 9.42 kcal/mol 和 - 9.29 kcal/mol。筛选结束后,进行了分子动力学模拟,以探索分子的稳定性和构象的可能性。后分子模拟分析进一步支持了药物分子。此外,还利用 MM/GBSA 方法计算了结合能,并利用自由能谱计算了不同的过渡态,结果表明药物表现出显著的过渡态。具体来说,去甲二氢愈创木酸和酒石酸艾芬地尔显示出更高的灵活性,而Lathyrol和甲磺酸沙芬那胺则显示出更可预测和更一致的蛋白质折叠。这一重大突破为防治登革热带来了新希望,彰显了计算药物发现在确定强效抑制剂方面的力量,并为新型治疗方法铺平了道路。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Investigation of small molecules disrupting dengue virus assembly by inhibiting capsid protein and blocking RNA encapsulation.

Dengue fever is a significant global public health concern, causing substantial morbidity and mortality worldwide. The disease can manifest in various forms, from mild fever to potentially life-threatening complications. Developing effective treatments remains a critical challenge to healthcare systems. Despite extensive research, no antiviral drugs have been approved for either the prevention or treatment of dengue. Targeting the virus during its early phase of attachment is essential to inhibit viral replication. The capsid protein plays a crucial role in the virus's structural integrity, assembly, and viral genome release. In the present study, we employed a computational approach focused on the capsid protein to identify possible potent inhibitors against the dengue virus from a library of FDA-approved drugs. We employed high-throughput virtual screening on FDA-approved drugs to identify drug molecules that could potentially combat the disease and save both cost and time. The screening process identified four drug molecules (Nordihydroguaiaretic acid, Ifenprodil tartrate, Lathyrol, and Safinamide Mesylate) based on their highest binding affinity and MM/GBSA scores. Among these, Nordihydroguaiaretic acid showed higher binding affinity than the reference molecule with - 11.66 kcal/mol. In contrast, Ifenprodil tartrate and Lathyrol showed similar results to the reference molecule, with binding energies of - 9.42 kcal/mol and - 9.29 kcal/mol, respectively. Following the screening, molecular dynamic simulations were performed to explore the molecular stability and conformational possibilities. The drug molecules were further supported by post-molecular simulation analysis. Furthermore, binding energies were also computed using the MM/GBSA approach, and the free energy landscape was used to calculate the different transition states, revealing that the drugs exhibited significant transition states. Specifically, Nordihydroguaiaretic acid and Ifenprodil tartrate displayed higher flexibility, while Lathyrol and Safinamide Mesylate showed more predictable and consistent protein folding. This significant breakthrough offers new hope against dengue, highlighting the power of computational drug discovery in identifying potent inhibitors and paving the way for novel treatment approaches.

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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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