Thaikkad Amritha, Henna Fathimath, Thomas Sonet Daniel, John Levin, Raju Rajesh, Jayanandan Abhithaj
Centre for Integrative Omics Data Science, Yenepoya (Deemed to Be University), Mangalore, Karnataka, 575018, India.
Institute of Regeneration and Repair (IRR), The University of Edinburgh, 4-5 Little France Dr, Edinburgh EH16 4UU, United Kingdom, Edinburgh, Scotland.
Mol Divers. 2025 May 2. doi: 10.1007/s11030-025-11206-6.
Human metapneumovirus (hMPV) primarily causes respiratory tract infections in young children and older adults. According to the 2024 Human Pneumonia Etiology Research for Child Health (PERCH) study, hMPV is the second leading common cause of pneumonia in children under five in Asia and Africa. The virus encodes nine proteins, including the essential Fusion (F) and G glycoproteins, which facilitate entry to the host cells. Currently, there are no approved vaccines or antiviral treatments for hMPV; supportive care is the primary way it is managed. Hence, this study focuses on the F protein as a therapeutic target to find a repurposable drug to fight hMPV. Refolding of the F protein and its binding to heparan sulfate enable hMPV infection. Heparin sulfate is important for hMPV binding, and we have found that cangrelor and AVN 944 can prevent the fusion of membranes. We developed a deep learning-based pharmacophore to identify potential drugs targeting hMPV, from which we could narrowed a list of 2400 FDA-approved drugs and 255 antiviral drugs to 792 and 72 drugs, respectively. We then conducted quantitative validation using the ROC curve. Further virtual screening of the drugs was performed, leading us to select the one with the highest docking score. The validation of the deep learning prediction in virtual screening Pearson correlation was done. Further, the MD simulation of these drugs confirmed that the protein-drug complex stability remained in dynamic condition. Further, the stability of protein-drug complexes than unbound protein was confirmed by Free Energy Landscape and Dynamic Cross Correlation Matrices. Further in vitro and in vivo experiments need to determine the efficacy of the identified candidates.
人偏肺病毒(hMPV)主要引起幼儿和老年人的呼吸道感染。根据2024年儿童健康人类肺炎病因研究(PERCH),hMPV是亚洲和非洲五岁以下儿童肺炎的第二大常见病因。该病毒编码九种蛋白质,包括必需的融合(F)糖蛋白和G糖蛋白,它们有助于进入宿主细胞。目前,尚无批准用于hMPV的疫苗或抗病毒治疗方法;支持性护理是其主要治疗方式。因此,本研究聚焦于F蛋白作为治疗靶点,以寻找一种可重新利用的抗hMPV药物。F蛋白的重折叠及其与硫酸乙酰肝素的结合促成hMPV感染。硫酸乙酰肝素对hMPV结合很重要,我们发现坎格雷洛和AVN 944可以阻止膜融合。我们开发了一种基于深度学习的药效团来识别靶向hMPV的潜在药物,据此我们可以将2400种FDA批准的药物和255种抗病毒药物的列表分别缩小到792种和72种。然后我们使用ROC曲线进行定量验证。对这些药物进行了进一步的虚拟筛选,从而使我们选择了对接分数最高的药物。完成了虚拟筛选中深度学习预测的Pearson相关性验证。此外,这些药物的分子动力学模拟证实蛋白质-药物复合物的稳定性处于动态状态。此外,通过自由能景观和动态交叉相关矩阵证实了蛋白质-药物复合物比未结合的蛋白质更稳定。还需要进一步的体外和体内实验来确定所鉴定候选药物的疗效。