Silvas Jesus A, Jureka Alexander S, Nicolini Anthony M, Chvatal Stacie A, Basler Christopher F
Center for Microbial Pathogenesis, Institute for Biomedical Sciences, Georgia State University, Atlanta, GA, 30303.
Equal contribution.
bioRxiv. 2020 Jul 20:2020.07.18.210211. doi: 10.1101/2020.07.18.210211.
Therapeutics targeting replication of SARS coronavirus 2 (SARS-CoV-2) are urgently needed. Coronaviruses rely on host membranes for entry, establishment of replication centers and egress. Compounds targeting cellular membrane biology and lipid biosynthetic pathways have previously shown promise as antivirals and are actively being pursued as treatments for other conditions. Here, we tested small molecule inhibitors that target membrane dynamics or lipid metabolism. Included were inhibitors of the PI3 kinase VPS34, which functions in autophagy, endocytosis and other processes; Orlistat, an inhibitor of lipases and fatty acid synthetase, is approved by the FDA as a treatment for obesity; and Triacsin C which inhibits long chain fatty acyl-CoA synthetases. VPS34 inhibitors, Orlistat and Triacsin C inhibited virus growth in Vero E6 cells and in the human airway epithelial cell line Calu-3, acting at a post-entry step in the virus replication cycle. Of these the VPS34 inhibitors exhibit the most potent activity.
迫切需要针对严重急性呼吸综合征冠状病毒2(SARS-CoV-2)复制的治疗方法。冠状病毒依靠宿主膜进行进入、建立复制中心和释放。靶向细胞膜生物学和脂质生物合成途径的化合物此前已显示出作为抗病毒药物的潜力,并且正在积极探索将其作为其他病症的治疗方法。在此,我们测试了靶向膜动力学或脂质代谢的小分子抑制剂。其中包括参与自噬、内吞作用和其他过程的PI3激酶VPS34的抑制剂;奥利司他,一种脂肪酶和脂肪酸合成酶的抑制剂,已被美国食品药品监督管理局(FDA)批准用于治疗肥胖症;以及抑制长链脂肪酰辅酶A合成酶的三辛环素C。VPS34抑制剂、奥利司他和三辛环素C在Vero E6细胞和人气道上皮细胞系Calu-3中抑制病毒生长,作用于病毒复制周期的进入后阶段。其中,VPS34抑制剂表现出最有效的活性。