Non-peptide inhibitors of HCV serine proteinase

被引：29

作者：

Kakiuchi, N

Komoda, Y

Komoda, K

Takeshita, N

Okada, S

Tani, T

Shimotohno, K

机构：

[1] Kyoto Univ, Inst Virus Res, Sakyo Ku, Kyoto 60601, Japan

[2] Sumitomo Met Ind Ltd, HQL Res Labs, Kyoto 61902, Japan

来源：

FEBS LETTERS | 1998年 / 421卷 / 03期

关键词：

hepatitis C virus; proteinase inhibitor; non-peptide compound;

D O I：

10.1016/S0014-5793(97)01566-4

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

We screened a chemical Library of 2000 compounds for inhibitors of hepatitis C virus (HCV) serine proteinase using an in vitro screening method measuring the hydrolysis of the peptide substrate. Three compounds sere found to be the most potent inhibitors (IC50 < 10(-5) M). Two of them had a similar structure, that of halogenated benzanilide, and were not inhibitory for common serine proteinases, They inhibited the enzyme non-competitively with the substrate, Together with the result of the analogous compounds in the chemical library, the presumed structural requirements of the inhibition are pointed out. (C) 1998 Federation of European Biochemical Societies.

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页码：217 / 220

页数：4

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