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  • 标题:Application of Acoustic Ejection MS System to High-Throughput Screening for SARS-CoV-2 3CL Protease Inhibitors
  • 本地全文:下载
  • 作者:Tsukasa Hasegawa ; Riyo M. Imamura ; Tateki Suzuki
  • 期刊名称:Chemical and Pharmaceutical Bulletin
  • 印刷版ISSN:0009-2363
  • 电子版ISSN:1347-5223
  • 出版年度:2022
  • 卷号:70
  • 期号:3
  • 页码:199-201
  • DOI:10.1248/cpb.c21-01003
  • 语种:English
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:MS is a powerful methodology for chemical screening to directly quantify substrates and products of enzymes, but its low throughput has been an issue. Recently, an acoustic liquid-handling apparatus (Echo®) used for rapid nano-dispensing has been coupled to a high-sensitivity mass spectrometer to create the Echo® MS system, and we applied this system to screening of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) 3CL protease inhibitors. Primary screening of 32033 chemical samples was completed in 12 h. Among the hits showing selective, dose-dependent 3CL-inhibitory activity, 8 compounds showed antiviral activity in cell-based assay.
  • 关键词:severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) 3CL protease;main protease;acoustic ejection MS;high-throughput screening;label-free
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