Application of Acoustic Ejection MS System to High-Throughput Screening for SARS-CoV-2 3CL Protease Inhibitors

Tsukasa Hasegawa; Riyo M. Imamura; Tateki Suzuki; Takao Hashiguchi; Takao Nomura; Satoko Otsuguro; Katsumi Maenaka; Michihito Sasaki; Yasuko Orba; Hirofumi Sawa; Akihiko Sato; Takayoshi Okabe; Tetsuo Nagano; Hirotatsu Kojima

doi:10.1248/cpb.c21-01003

This article has now been updated. Please use the final version.

Application of Acoustic Ejection MS System to High-Throughput Screening for SARS-CoV-2 3CL Protease Inhibitors

Tsukasa Hasegawa, Riyo M. Imamura, Tateki Suzuki, Takao Hashiguchi, Takao Nomura, Satoko Otsuguro, Katsumi Maenaka, Michihito Sasaki, Yasuko Orba, Hirofumi Sawa, Akihiko Sato, Takayoshi Okabe, Tetsuo Nagano, Hirotatsu Kojima

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Keywords: SARS-CoV-2 3CL protease, Main protease, acoustic ejection mass spectrometry, high-throughput screening, label-free

JOURNAL FREE ACCESS Advance online publication

Article ID: c21-01003

DOI https://doi.org/10.1248/cpb.c21-01003

The final version of this article is now available: Vol. 70 (2022), No. 3 pp. 199-201

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Abstract

Mass spectrometry 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 SARS-CoV-2 3CL protease inhibitors. Primary screening of 32,033 chemical samples was completed in 12 hours. Among the hits showing selective, dose-dependent 3CL-inhibitory activity, 8 compounds showed antiviral activity in cell-based assay.

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