Activation of peptide prodrugs by hk2
AssigneeGenspera, Inc.
InventorsSamuel Denmeade, John Isaacs, Hans Lilja
Life of this patent
Estimating the term…
Abstract
The invention provides novel peptide prodrugs that contain cleavage sites specifically cleaved by human kallikrein 2 (hK2). These prodrugs are useful for substantially inhibiting the non-specific toxicity of a variety of therapeutic drugs. Upon cleavage of the prodrug by hK2, the therapeutic drugs are activated and exert their toxicity. Methods for treating cell proliferative disorders are also featured in the invention.
Claims76
A peptide comprising an amino acid sequence having a cleavage site specific for an enzyme having a proteolytic activity of human kallikrein 2 (hK2), wherein the peptide comprises the sequence G-K-A-X1-X2-X3, wherein at least one of X1, X2, and X3 is arginine, and wherein the other two amino acid residues at X1, X2, and X3 are each any amino acid residue.
A peptide composition comprising a plurality of peptides, each peptide comprising an amino acid sequence having a cleavage site specific for an enzyme having a proteolytic activity of human kallikrein 2 (hK2), wherein each peptide comprises the sequence G-K-A-X1-X2-X3, wherein at least one of X1, X2, and X3 is arginine, and wherein the other two amino acid residues at X1, X2, and X3 are each any amino acid residue.
Dependencies are inferred from the claim text.