Estoppey David, Lee Chia Min, Janoschke Marco, Lee Boon Heng, Wan Kah Fei, Dong Hongping, Mathys Philippe, Filipuzzi Ireos, Schuhmann Tim, Riedl Ralph, Aust Thomas, Galuba Olaf, McAllister Gregory, Russ Carsten, Spiess Martin, Bouwmeester Tewis, Bonamy Ghislain M C, Hoepfner Dominic
Novartis Institutes for BioMedical Research, Novartis Pharma AG, Forum 1 Novartis Campus, 4056 Basel, Switzerland.
Novartis Institute for Tropical Diseases, 10 Biopolis Road, Chromos #05-01, 138670 Singapore, Singapore.
Cell Rep. 2017 Apr 18;19(3):451-460. doi: 10.1016/j.celrep.2017.03.071.
Flavivirus infections by Zika and dengue virus impose a significant global healthcare threat with no US Food and Drug Administration (FDA)-approved vaccination or specific antiviral treatment available. Here, we present the discovery of an anti-flaviviral natural product named cavinafungin. Cavinafungin is a potent and selectively active compound against Zika and all four dengue virus serotypes. Unbiased, genome-wide genomic profiling in human cells using a novel CRISPR/Cas9 protocol identified the endoplasmic-reticulum-localized signal peptidase as the efficacy target of cavinafungin. Orthogonal profiling in S. cerevisiae followed by the selection of resistant mutants pinpointed the catalytic subunit of the signal peptidase SEC11 as the evolutionary conserved target. Biochemical analysis confirmed a rapid block of signal sequence cleavage of both host and viral proteins by cavinafungin. This study provides an effective compound against the eukaryotic signal peptidase and independent confirmation of the recently identified critical role of the signal peptidase in the replicative cycle of flaviviruses.
寨卡病毒和登革热病毒引起的黄病毒感染对全球医疗保健构成了重大威胁,目前尚无美国食品药品监督管理局(FDA)批准的疫苗或特定的抗病毒治疗方法。在此,我们报告了一种名为卡维那芬净的抗黄病毒天然产物的发现。卡维那芬净是一种对寨卡病毒和所有四种登革热病毒血清型均具有强效且选择性活性的化合物。使用一种新型的CRISPR/Cas9方案在人类细胞中进行的无偏向全基因组分析确定,内质网定位的信号肽酶是卡维那芬净的作用靶点。在酿酒酵母中进行正交分析,随后选择抗性突变体,确定信号肽酶SEC11的催化亚基为进化保守靶点。生化分析证实,卡维那芬净可迅速阻断宿主蛋白和病毒蛋白的信号序列切割。这项研究提供了一种针对真核信号肽酶的有效化合物,并独立证实了信号肽酶在黄病毒复制周期中最近确定的关键作用。