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 µMconcentration. Our results suggest that the compound might serve as a SARS coronavirus inhibitor.
authors.affiliation: Department of Bio and Nanochemistry, Kookmin University, Seoul 136-702, Republic of Korea.
authors.forename: Jin-Beom
authors.initials: JB
authors.lastname: Cho
authors.affiliation: Department of Bio and Nanochemistry, Kookmin University, Seoul 136-702, Republic of Korea.
authors.forename: Jin-Moo
authors.initials: JM
authors.lastname: Lee
authors.affiliation: Department of Pharmacy, Dongguk University-Seoul, Goyang 410-820, Republic of Korea.
authors.forename: Hee-Chul
authors.initials: HC
authors.lastname: Ahn
authors.affiliation: Department of Bio and Nanochemistry, Kookmin University, Seoul 136-702, Republic of Korea.
authors.forename: Yong-Joo
authors.initials: YJ
authors.lastname: Jeong
mesh_terms: D000255:Adenosine Triphosphate / Q000378:metabolism; D000998:Antiviral Agents / Q000302:isolation & purification / Q000494:pharmacology*; D004265:DNA Helicases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D006868:Hydrolysis; D020128:Inhibitory Concentration 50; D045473:Severe acute respiratory syndrome-related coronavirus / Q000201:enzymology*
chemical_list: D000998:Antiviral Agents; D004791:Enzyme Inhibitors; D000255:Adenosine Triphosphate; D004265:DNA Helicases
keywords: ATP hydrolysis; SARS; dsDNA unwinding; helicase