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吡唑 - 苯衍生物对基孔肯雅病毒进入的强效抑制作用:针对E1 - E2糖蛋白复合物的计算研究

Potent Inhibition of Chikungunya Virus Entry by a Pyrazole-Benzene Derivative: A Computational Study Targeting the E1-E2 Glycoprotein Complex.

作者信息

Rahman Md Mohibur, Limon Md Belayet Hasan, Saikat Tanvir Ahmed, Saha Poulomi, Nahid Abdul Hadi, Alam Mohammad Mamun, Rahman Mohammed Ziaur

机构信息

One Health Laboratory, Infectious Diseases Division, International Centre for Diarrhoeal Disease Research, Mohakhali, Dhaka 1212, Bangladesh.

Department of Microbiology and Immunology, University of Louisville, Louisville, KY 40202, USA.

出版信息

Int J Mol Sci. 2025 Jul 5;26(13):6480. doi: 10.3390/ijms26136480.

Abstract

The Chikungunya virus (CHIKV) continues to pose a significant global health challenge due to the absence of effective antiviral treatments and limited vaccine availability. This study employed a comprehensive in silico workflow, incorporating high-throughput virtual screening, binding free-energy calculations, ADMET (absorption, distribution, metabolism, excretion, and toxicity) analysis, and 200 ns molecular dynamics (MD) simulations, to identify new inhibitors targeting the E1-E2 glycoprotein complex, crucial for CHIKV entry and membrane fusion. Four promising candidates were identified from a library of 20,000 compounds, with CID 136801451 showing the most potent binding (docking score: -10.227; ΔG_bind: -51.53 kcal/mol). The top four compounds exhibited favorable ADMET profiles, meeting nearly all criteria. MD simulations confirmed stable binding and strong interactions between CID 136801451 and the E1-E2 complex, evidenced by consistently low RMSD values. These findings highlight CID 136801451 as a promising CHIKV entry inhibitor, warranting further in vitro and in vivo evaluation to advance the development of effective anti-CHIKV therapeutics.

摘要

由于缺乏有效的抗病毒治疗方法且疫苗供应有限,基孔肯雅病毒(CHIKV)仍然是一项重大的全球卫生挑战。本研究采用了全面的计算机模拟工作流程,包括高通量虚拟筛选、结合自由能计算、ADMET(吸收、分布、代谢、排泄和毒性)分析以及200纳秒分子动力学(MD)模拟,以确定针对E1-E2糖蛋白复合体的新型抑制剂,该复合体对CHIKV进入和膜融合至关重要。从20000种化合物库中鉴定出四种有前景的候选物,其中CID 136801451表现出最强的结合能力(对接分数:-10.227;ΔG_bind:-51.53千卡/摩尔)。排名前四的化合物表现出良好的ADMET特性,几乎满足所有标准。MD模拟证实了CID 136801451与E1-E2复合体之间的稳定结合和强相互作用,持续较低的均方根偏差(RMSD)值证明了这一点。这些发现突出了CID 136801451作为一种有前景的CHIKV进入抑制剂,值得进一步进行体外和体内评估,以推动有效的抗CHIKV治疗药物的开发。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ab6b/12250591/9a5d714c6bc5/ijms-26-06480-g001a.jpg

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