文章基本信息

标题：Application of Acoustic Ejection MS System to High-Throughput Screening for SARS-CoV-2 3CL Protease Inhibitors
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作者：Tsukasa Hasegawa ; Riyo M. Imamura ; Tateki Suzuki 等
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