Lee Kong Chian School of Medicine, Nanyang Technological University, Singapore, Singapore; NTU Institute of Structural Biology, Nanyang Technological University, Singapore, Singapore.
Department of Molecular Medicine, The Herbert Wertheim UF Scripps Institute for Biomedical Innovation & Technology, FL, United States.
SLAS Discov. 2024 Jul;29(5):100164. doi: 10.1016/j.slasd.2024.100164. Epub 2024 May 24.
Zika virus (ZIKV) continues to pose a significant global public health threat, with recurring regional outbreaks and potential for pandemic spread. Despite often being asymptomatic, ZIKV infections can have severe consequences, including neurological disorders and congenital abnormalities. Unfortunately, there are currently no approved vaccines or antiviral drugs for the prevention or treatment of ZIKV. One promising target for drug development is the ZIKV NS2B-NS3 protease due to its crucial role in the virus life cycle. In this study, we established a cell-based ZIKV protease inhibition assay designed for high-throughput screening (HTS). Our assay relies on the ZIKV protease's ability to cleave a cyclised firefly luciferase fused to a natural cleavage sequence between NS2B and NS3 protease within living cells. We evaluated the performance of our assay in HTS setting using the pharmacologic controls (JNJ-40418677 and MK-591) and by screening a Library of Pharmacologically Active Compounds (LOPAC). The results confirmed the feasibility of our assay for compound library screening to identify potential ZIKV protease inhibitors.
寨卡病毒(ZIKV)仍然构成重大的全球公共卫生威胁,存在区域性反复暴发和潜在大流行传播的风险。尽管通常无症状,但寨卡病毒感染可能会产生严重后果,包括神经紊乱和先天异常。不幸的是,目前尚无预防或治疗寨卡病毒的批准疫苗或抗病毒药物。寨卡病毒 NS2B-NS3 蛋白酶是药物开发的一个有前途的靶点,因为它在病毒生命周期中起着至关重要的作用。在这项研究中,我们建立了一种基于细胞的寨卡病毒蛋白酶抑制测定法,旨在进行高通量筛选(HTS)。我们的测定法依赖于寨卡病毒蛋白酶切割活细胞内 NS2B 和 NS3 蛋白酶之间天然切割序列融合的环化萤火虫荧光素酶的能力。我们使用药理学对照(JNJ-40418677 和 MK-591)和药理学活性化合物库(LOPAC)筛选来评估我们在 HTS 环境中测定法的性能。结果证实了我们的测定法在化合物库筛选中用于鉴定潜在寨卡病毒蛋白酶抑制剂的可行性。