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Screening of drugs by FRET analysis identifies inhibitors of SARS-CoV 3CL protease.

Abstract：

:SARS-CoV 3CL protease is essential for viral protein processing and is regarded as a good drug target to prevent SARS-CoV replication. In the present study, we established a high-throughput FRET technique for screening for anti-SARS-CoV 3CL protease drugs. Of a thousand existing drugs examined, hexachlorophene was identified as the most potent in inhibiting SARS-CoV 3CL protease. Further characterization showed that it was effective at micromolar concentrations (K(i) = 4 microM). The binding mode was competitive, and the inhibitory effect was dependent on preincubation time. Two other drugs, triclosan and nelfinavir, were about 10 times less potent. The structure-based search and biological evaluation of various hexachlorophene analogues were described. These analogues gave optimal inhibitory activity against SARS-CoV 3CL protease with IC(50) values ranging from 7.6 to 84.5 microM. Optimization of hexachlorophene analogues was shown to provide several active 3CL protease inhibitors that function as potential anti-SARS agents.

journal_name

Biochem Biophys Res Commun

journal_title

Biochemical and biophysical research communications

authors

Liu YC,Huang V,Chao TC,Hsiao CD,Lin A,Chang MF,Chow LP

doi

10.1016/j.bbrc.2005.05.095

subject

Has Abstract

pub_date

2005-07-22 00:00:00

pages

194-9

issue

1

eissn

0006-291X

issn

1090-2104

pii

S0006-291X(05)01051-X

journal_volume

333

pub_type

杂志文章

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