Isozyme-specific antagonists of protein kinase C
AssigneeThe Board of Trustees of the Leland Stanford Junior University
InventorDaria Mochly-Rosen
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Abstract
A method of changing or otherwise converting the biological activity of a PKC peptide agonist to a peptide antagonist is described. The method involves substituting one or more amino acid residues so as to effect a change in charge in the peptide and/or to otherwise make the sequence similar to a sequence derived from the PKC binding site on the RACK protein for the respective PKC enzyme. Methods of inhibiting the activity of a PKC enzyme, and various peptide antagonists of εPKC are also disclosed.
Claims5
A composition comprising a peptide consisting of an amino acid sequence selected from the group consisting of SEQ ID NO:50;
- SEQ ID NO:51;
- SEQ ID NO:52;
- SEQ ID NO:53;
- SEQ ID NO:54;
- SEQ ID NO:55;
- SEQ ID NO:56;
- and SEQ ID NO:57, crosslinked via an N-terminal Cys-Cys bond to a peptide to facilitate transport cellular uptake.
A composition comprising a peptide consisting of SEQ ID NO:
- 55, crosslinked via an N-terminal Cys-Cys bond to a Tat-derived peptide or to a polyarginine peptide.
Dependencies are inferred from the claim text.