Department of Chemistry, University of Illinois at Chicago, Chicago, Illinois 60607, United States.
Departments of Chemistry, California State University Sacramento, 6000 J Street, Sacramento, California 95819-6057, United States.
J Chem Inf Model. 2024 Sep 23;64(18):7141-7151. doi: 10.1021/acs.jcim.4c00541. Epub 2024 Sep 4.
Many viruses initiate their cell-entry by binding their multisubunit receptors to human heparan sulfate proteoglycans (HSPG) and other molecular components present on cellular membranes. These viral interactions could be blocked and the whole viruses could be eliminated by suitable HSPG-mimetics providing multivalent binding to viral protein receptors. Here, large sulfoglycodendron HSPG-mimetics of different topologies, structures, and sizes were designed to this purpose. Atomistic molecular dynamics simulations were used to examine the ability of these broad-spectrum antivirals to block multiprotein HSPG-receptors in HIV, SARS-CoV-2, HPV, and dengue viruses. To characterize the inhibitory potential of these mimetics, their binding to individual and multiple protein receptors was examined. In particular, vectorial distributions of binding energies between the mimetics and viral protein receptors were introduced and calculated along the simulated trajectories. Space-dependent residual analysis of the mimetic-receptor binding was also performed. This analysis revealed the detailed nature of binding between these antivirals and viral protein receptors and provided evidence that large inhibitors with multivalent binding might act like a molecular glue initiating the self-assembly of protein receptors in enveloped viruses.
许多病毒通过将其多亚基受体与人类硫酸乙酰肝素蛋白聚糖 (HSPG) 和细胞膜上存在的其他分子成分结合来启动细胞进入。这些病毒相互作用可以被合适的 HSPG 模拟物阻断,这些模拟物可以对病毒蛋白受体进行多价结合,从而消除整个病毒。为此,设计了具有不同拓扑结构、结构和大小的大型硫酸化糖萜 HSPG 模拟物。原子分子动力学模拟用于研究这些广谱抗病毒药物阻断 HIV、SARS-CoV-2、HPV 和登革热病毒中多蛋白 HSPG 受体的能力。为了表征这些模拟物的抑制潜力,研究了它们与单个和多个蛋白受体的结合。特别地,引入并计算了模拟轨迹上模拟物和病毒蛋白受体之间结合能的向量分布。还对模拟物-受体结合的空间相关残差进行了分析。该分析揭示了这些抗病毒药物与病毒蛋白受体之间结合的详细性质,并提供了证据表明,具有多价结合的大型抑制剂可能充当分子胶,启动包膜病毒中蛋白受体的自组装。