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Identification and Characterization of Zika Virus NS5 Methyltransferase Inhibitors

Front Cell Infect Microbiol. 2021-04; 
Weibao Song, Hongjuan Zhang, Yu Zhang, Ying Chen, Yuan Lin, Yanxing Han, Jiandong Jiang
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Recombinant Proteins … The ZIKV RNA sequence for methyltransferase reaction was synthesized de novo by Genscript (Nanjing, Jiangsu, CHN)?… The screening library was a natural product library provided by MedChem Express (Monmouth Junction, NJ, USA)?… Get A Quote

摘要

The recurring outbreak of Zika virus (ZIKV) worldwide makes an emergent demand for novel, safe and efficacious anti-ZIKV agents. ZIKV non-structural protein 5 (NS5) methyltransferase (MTase), which is essential for viral replication, is regarded as a potential drug target. In our study, a luminescence-based methyltransferase assay was used to establish the ZIKV NS5 MTase inhibitor screening model. Through screening a natural product library, we found theaflavin, a polyphenol derived from tea, could inhibit ZIKV NS5 MTase activity with a 50% inhibitory concentration (IC) of 10.10 μM. Molecular docking and site-directed mutagenesis analyses identified D146 as the key amino acid in the interaction between ZIKV NS... More

關(guān)鍵詞

NS5, Zika virus, inhibitors, methyltransferase, theaflavin
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