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通过抑制衣壳蛋白和阻断RNA封装来研究破坏登革病毒组装的小分子。

Investigation of small molecules disrupting dengue virus assembly by inhibiting capsid protein and blocking RNA encapsulation.

作者信息

Panday Hrithika, Jha Abhimanyu Kumar, Dwivedi Vivek Dhar

机构信息

Department of Biotechnology, Sharda University, Greater Noida, UP, India.

Department of Biotechnology, School of Biosciences and Technology, Galgotias University, Greater Noida, India.

出版信息

Mol Divers. 2024 Sep 20. doi: 10.1007/s11030-024-10980-z.

Abstract

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.

摘要

登革热是一个重大的全球公共卫生问题,在全球范围内导致大量发病和死亡。该疾病可表现为多种形式,从轻度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系统面临的一项严峻挑战。尽管进行了广泛研究,但尚无抗病毒药物被批准用于预防或治疗登革热。在病毒早期附着阶段对其进行靶向作用对于抑制病毒复制至关重要。衣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关键作用。在本研究中,我们采用了一种针对衣壳蛋白的计算方法,从美国食品药品监督管理局(FDA)批准的药物库中识别可能有效的登革热病毒抑制剂。我们对FDA批准的药物进行了高通量虚拟筛选,以确定可能对抗该疾病的药物分子,从而节省成本和时间。筛选过程基于四种药物分子(去甲二氢愈创木酸、酒石酸艾芬地尔、千金子醇和甲磺酸沙芬酰胺)的最高结合亲和力和MM/GBSA评分进行确定。其中,去甲二氢愈创木酸的结合亲和力高于参考分子,为 -11.66千卡/摩尔。相比之下,酒石酸艾芬地尔和千金子醇与参考分子的结果相似,结合能分别为 -9.42千卡/摩尔和 -9.29千卡/摩尔。筛选后,进行了分子动力学模拟以探索分子稳定性和构象可能性。分子模拟后的分析进一步支持了这些药物分子。此外,还使用MM/GBSA方法计算了结合能,并利用自由能景观计算了不同的过渡态,结果表明这些药物表现出显著的过渡态。具体而言,去甲二氢愈创木酸和酒石酸艾芬地尔表现出更高的灵活性,而千金子醇和甲磺酸沙芬酰胺则显示出更可预测和一致的蛋白质折叠。这一重大突破为对抗登革热带来了新希望,凸显了计算药物发现技术在识别有效抑制剂方面的强大作用,并为新型治疗方法铺平了道路。

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