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US 2009/0215101 A1Published application
HCV Protease substrates
AssigneeMerck Sharp & Dohme Corp.
InventorsShi-Shan Mao, S. Dale Lewis
Life of this patent
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Abstract
The present invention features HCV NS3 protease substrates containing a europium label and a quenching group. The europium label and quenching group are located on different sides of an ester HCV NS3 protease cleavage site. The substrate can be used in a time-resolved fluorescence (TRF) assay to measure HCV protease activity.
Claims7
A hepatitis C virus NS3 protease substrate comprising the following structure:
- (B)n-X1-X2-X3-X4-X5-X6-X7-X8-X9-(Z)m
- wherein each B is an independently selected amino acid;
- X1 is either aspartic acid or glutamic acid;
- X2 is aspartic acid;
- X3 is methionine;
- X4 is glutamic acid;
- X5 is glutamic acid;
- X6 is 2-aminobutyric acid;
- X7 is alanine;
- X8 is serine;
- X9 is either lysine, histidine, cysteine or arginine;
- each Z is an independently selected amino acid;
- n is 0 to 10;
- m is 0 to 10;
- provided that X6 is joined to X7 by an ester linkage;
- further provided that either:
- (a) at least one of a (B)n amino acid or X1 is labeled with europium, and at least one of X9 or an (Z)m amino acid is labeled with a quenching group;
- or (b) at least one of a (B)n amino acid or X1 is labeled with a quenching group, and at least one of X9 or an (Z)m amino acid is labeled with europium;
- and
- further provided that the amino terminus amino acid is optionally modified with an amino terminus protecting group and the carboxyl terminus amino acid is optionally modified with a carboxyl terminus protecting group.
17 more elements
Dependencies are inferred from the claim text.