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Application of Acoustic Ejection MS System to High-Throughput Screening for SARS-CoV-2 3CL Protease Inhibitors.
Hasegawa, Tsukasa; Imamura, Riyo M; Suzuki, Tateki; Hashiguchi, Takao; Nomura, Takao; Otsuguro, Satoko; Maenaka, Katsumi; Sasaki, Michihito; Orba, Yasuko; Sawa, Hirofumi; Sato, Akihiko; Okabe, Takayoshi; Nagano, Tetsuo; Kojima, Hirotatsu.
  • Hasegawa T; Drug Discovery Initiative, The University of Tokyo.
  • Imamura RM; Drug Discovery Initiative, The University of Tokyo.
  • Suzuki T; Institute for Frontier Life and Medical Sciences, Kyoto University.
  • Hashiguchi T; Institute for Frontier Life and Medical Sciences, Kyoto University.
  • Nomura T; Faculty of Pharmaceutical Sciences, Hokkaido University.
  • Otsuguro S; Faculty of Pharmaceutical Sciences, Hokkaido University.
  • Maenaka K; Faculty of Pharmaceutical Sciences, Hokkaido University.
  • Sasaki M; International Institute for Zoonosis Control, Hokkaido University.
  • Orba Y; International Institute for Zoonosis Control, Hokkaido University.
  • Sawa H; International Institute for Zoonosis Control, Hokkaido University.
  • Sato A; International Institute for Zoonosis Control, Hokkaido University.
  • Okabe T; Drug Discovery and Disease Research Laboratory, Shionogi & Co., Ltd.
  • Nagano T; Drug Discovery Initiative, The University of Tokyo.
  • Kojima H; Drug Discovery Initiative, The University of Tokyo.
Chem Pharm Bull (Tokyo) ; 70(3): 199-201, 2022 Mar 01.
Article in English | MEDLINE | ID: covidwho-1714684
ABSTRACT
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.
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Full text: Available Collection: International databases Database: MEDLINE Main subject: Protease Inhibitors / COVID-19 Type of study: Diagnostic study / Screening study Limits: Humans Language: English Journal: Chem Pharm Bull (Tokyo) Year: 2022 Document Type: Article

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Full text: Available Collection: International databases Database: MEDLINE Main subject: Protease Inhibitors / COVID-19 Type of study: Diagnostic study / Screening study Limits: Humans Language: English Journal: Chem Pharm Bull (Tokyo) Year: 2022 Document Type: Article