Tafenoquine and its derivatives as inhibitors for the severe acute respiratory syndrome coronavirus 2
Yeh Chen, Wenhao Yang, Hsiao‐Fan Chen, Li‐Min Huang, Jing-Yan Gao, Cheng‐Wen Lin, Yuchuan Wang, Chia‐Shin Yang, Yiliang Liu, Mei‐Hui Hou, Chia-Ling Tsai, Yi-Zhen Chou, Bao‐Yue Huang, Chian-Fang Hung, Yu-Lin Hung, Wei‐Jan Wang, Wen‐Chi Su, Vathan Kumar, Yu‐Chieh Wu, Shih-Wei Chao, Chih‐Shiang Chang, Jin‐Shing Chen, Yu-Ping Chiang, Der‐Yang Cho, Long‐Bin Jeng, Chang‐Hai Tsai, Mien‐Chie Hung
Abstract
by altering the loop region (residues 139-144) near the catalytic Cys145, which could block the catalysis of its peptide substrates. We also found that TFQ inhibited human transmembrane protease serine 2 (TMPRSS2). Furthermore, one TFQ derivative, compound 7, showed a better therapeutic index than TFQ on TMPRSS2 and may therefore inhibit the infectibility of SARS-CoV-2, including that of several mutant variants. These results suggest new potential strategies to block infection of SARS-CoV-2 and rising variants.