Institute of Pharmaceutical Biology and Phytochemistry, University of Münster, Corrensstr. 48, 48149 Münster, Germany.
Institute of Virology-Clinical Virology, University of Münster and University Hospital Münster, Von-Stauffenberg-Str. 36, 48151 Münster, Germany.
Viruses. 2022 Jun 21;14(7):1354. doi: 10.3390/v14071354.
Membrane fusion constitutes an essential step in the replication cycle of numerous viral pathogens, hence it represents an important druggable target. In the present study, we established a virus-free, stable reporter fusion inhibition assay (SRFIA) specifically designed to identify compounds interfering with virus-induced membrane fusion. The dual reporter assay is based on two stable Vero cell lines harboring the third-generation tetracycline (Tet3G) transactivator and a bicistronic reporter gene cassette under the control of the tetracycline responsive element (TRE3G), respectively. Cell-cell fusion by the transient transfection of viral fusogens in the presence of doxycycline results in the expression of the reporter enzyme secreted alkaline phosphatase (SEAP) and the fluorescent nuclear localization marker EYFPNuc. A constitutively expressed, secreted form of nanoluciferase (secNLuc) functioned as the internal control. The performance of the SRFIA was tested for the quantification of SARS-CoV-2- and HSV-1-induced cell-cell fusion, respectively, showing high sensitivity and specificity, as well as the reliable identification of known fusion inhibitors. Parallel quantification of secNLuc enabled the detection of cytotoxic compounds or insufficient transfection efficacy. In conclusion, the SRFIA reported here is well suited for high-throughput screening for new antiviral agents and essentially will be applicable to all viral fusogens causing cell-cell fusion in Vero cells.
膜融合是许多病毒病原体复制周期中的一个基本步骤,因此它是一个重要的可药物靶标。在本研究中,我们建立了一种无病毒、稳定的报告融合抑制测定法(SRFIA),专门用于鉴定干扰病毒诱导的膜融合的化合物。该双报告测定法基于两个稳定的 Vero 细胞系,分别携带第三代四环素(Tet3G)转录激活剂和双顺反子报告基因盒,受四环素反应元件(TRE3G)的控制。在存在强力霉素的情况下,通过瞬时转染病毒融合剂,导致报告酶分泌碱性磷酸酶(SEAP)和荧光核定位标记 EYFPNuc 的表达。稳定表达的分泌型纳米荧光素酶(secNLuc)作为内参。SRFIA 的性能已通过 SARS-CoV-2 和 HSV-1 诱导的细胞-细胞融合的定量测试进行了测试,显示出高灵敏度和特异性,以及对已知融合抑制剂的可靠鉴定。secNLuc 的平行定量能够检测到细胞毒性化合物或转染效率不足。总之,本报告的 SRFIA 非常适合用于高通量筛选新的抗病毒药物,并且基本上适用于在 Vero 细胞中引起细胞-细胞融合的所有病毒融合剂。