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US 2007/0166778 A1Published application
Substrates and methods for assaying deubiquitinating enzymes
OwnerXavier Jacq, Jean-Christophe Raininventors
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Abstract
The invention relates to substrates and methods suitable for assaying deubiquitinating enzyme activity, and in particular for screening inhibitors of enzymes involved in removal of mono or poly-ubiquitin chains from a target protein as well as inhibitors of ubiquitin precursors. Such inhibitors may have utility in the treatment of disease states associated with ubiquitin processing as well as proteolysis.
Claims25
A deubiquitinating enzyme substrate which comprises the amino acid chain:
- R1-ubiquitin-ribosomal protein-R2
- in which:
- R1 and R2 are each independently selected from the group consisting of a member of a donor/acceptor pair and a member of a ligand/receptor pair, and R1 is different from R2.
A deubiquitinating enzyme substrate which comprises the amino acid chain
- R1 and R2 are each independently selected from the group consisting of a member of a donor/acceptor pair and a member of a ligand/receptor pair, and R1 is different from R2;
- n is an integer which is at least 1;
- m is an integer which is at least 1;
- and
- K(y) is an isopeptide linkage between a lysine of first ubiquitin and C-terminal glycine of a second ubiquitin.
2 more elements
Dependencies are inferred from the claim text.