CELL PERMEABLE CONJUGATES OF PEPTIDES FOR INHIBITION OF PROTEIN KINASES

摘要

The present invention provides inhibitors of protein kinases comprising a molecule having at least a first moiety competent for penetration of said molecule into cells, and a second moiety for having a protein kinase inhibiting effect within said cells, said first moiety being joined to said second moiety through a linker or a spacer. The complex molecules of the invention are preferably peptide conjugates having improved cell-permeabilit y, serum stability and kinase selectivity compared to known protein kinase inhibitors. Pharmaceutical compositions comprising these protein kinase inhibitors, and methods of using such compositions for treatment of cancers and other diseases associated with protein kinase activity are also disclose d.