Identification of a novel small molecule inhibitor against SARS coronavirus helicase

Jin Beom Cho; Jin Moo Lee; Hee Chul Ahn; Yong Joo Jeong

doi:10.4014/jmb.1507.07078

Identification of a novel small molecule inhibitor against SARS coronavirus helicase

Jin Beom Cho, Jin Moo Lee, Hee Chul Ahn, Yong Joo Jeong

Department of Pharmacy

Kookmin University

Research output: Contribution to journal › Article › peer-review

21 Scopus citations

Abstract

A new chemical inhibitor against severe acute respiratory syndrome (SARS) coronavirus helicase, 7-ethyl-8-mercapto-3-methyl-3,7-dihydro-1H-purine-2,6-dione, was identified. We investigated the inhibitory effect of the compound by conducting colorimetry-based ATP hydrolysis assay and fluorescence resonance energy transfer-based double-stranded DNA unwinding assay. The compound suppressed both ATP hydrolysis and double-stranded DNA unwinding activities of helicase with IC₅₀ values of 8.66 ± 0.26 μM and 41.6 ± 2.3 μM, respectively. Moreover, we observed that the compound did not show cytotoxicity up to 80 μM concentration. Our results suggest that the compound might serve as a SARS coronavirus inhibitor.

Original language	English
Pages (from-to)	2007-2010
Number of pages	4
Journal	Journal of Microbiology and Biotechnology
Volume	25
Issue number	12
DOIs	https://doi.org/10.4014/jmb.1507.07078
State	Published - 18 Sep 2015

Keywords

ATP hydrolysis
DsDNA unwinding
Helicase
Inhibitor
SARS

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10.4014/jmb.1507.07078

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title = "Identification of a novel small molecule inhibitor against SARS coronavirus helicase",

abstract = "A new chemical inhibitor against severe acute respiratory syndrome (SARS) coronavirus helicase, 7-ethyl-8-mercapto-3-methyl-3,7-dihydro-1H-purine-2,6-dione, was identified. We investigated the inhibitory effect of the compound by conducting colorimetry-based ATP hydrolysis assay and fluorescence resonance energy transfer-based double-stranded DNA unwinding assay. The compound suppressed both ATP hydrolysis and double-stranded DNA unwinding activities of helicase with IC50 values of 8.66 ± 0.26 μM and 41.6 ± 2.3 μM, respectively. Moreover, we observed that the compound did not show cytotoxicity up to 80 μM concentration. Our results suggest that the compound might serve as a SARS coronavirus inhibitor.",

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AU - Lee, Jin Moo

AU - Ahn, Hee Chul

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AB - A new chemical inhibitor against severe acute respiratory syndrome (SARS) coronavirus helicase, 7-ethyl-8-mercapto-3-methyl-3,7-dihydro-1H-purine-2,6-dione, was identified. We investigated the inhibitory effect of the compound by conducting colorimetry-based ATP hydrolysis assay and fluorescence resonance energy transfer-based double-stranded DNA unwinding assay. The compound suppressed both ATP hydrolysis and double-stranded DNA unwinding activities of helicase with IC50 values of 8.66 ± 0.26 μM and 41.6 ± 2.3 μM, respectively. Moreover, we observed that the compound did not show cytotoxicity up to 80 μM concentration. Our results suggest that the compound might serve as a SARS coronavirus inhibitor.

KW - ATP hydrolysis

KW - DsDNA unwinding

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Identification of a novel small molecule inhibitor against SARS coronavirus helicase

Abstract

Keywords

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