期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 6, 页码 1636-1638出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.02.010
关键词
SARS-CoV; Helicase; Aryl diketoacid (ADK); Duplex DNA-unwinding activity
资金
- Rural Development Administration, Republic of Korea [11-30-68]
- Korean Government [KRF-2007-313-C00451, 10580]
- Kookmin University in Korea
As anti-HCV aryl diketoacids (ADK) are good metal chelators, we anticipated that ADKs might serve as potential inhibitors of SARS CoV (SCV) NTPase/helicase (Hel) by mimicking the binding modes of the bismuth complexes which effectively competes for the Zn2+ ion binding sites in SCV Hel thereby disrupting and inhibiting both the NTPase and helicase activities. Phosphate release assay and FRET-based assay of the ADK analogues showed that the ADKs selectively inhibit the duplex DNA-unwinding activity without significant impact on the helicase ATPase activity. Also, antiviral activities of the ADKs were shown dependent upon the substituent. Taken together, these results suggest that there might be ADK-specific binding site in the SCV Hel, which warrants further investigations with diverse ADKs to provide valuable insights into rational design of specific SCV Hel inhibitors. (C) 2009 Elsevier Ltd. All rights reserved.
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