Selective cell-permeable peptide inhibitor of protein kinase C (IC50
~ 0.5 μ
M). Consists of amino acids 19 - 31 of PKC pseudosubstrate domain linked by a disulphide bridge to a cell permeabilisation Antennapedia domain vector peptide. The Antennapedia peptide is actively taken up by intact cells, at 4 or 37°C, ensuring rapid and effective uptake of the inhibitor peptide. Once inside the cell, the disulphide bonds are subjected to reduction in the cytoplasm leading to release of the inhibitor peptide.
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The third helix of the Antennapedia homeodomain translocates through biological membranes.
Derossi D, Joliot AH, Chassaing G, Prochiantz A.
J Biol Chem.
Protein kinase C contains a pseudosubstrate prototope in its regulatory domain.
House and Kemp
Intraneuronal delivery of protein kinase C pseudosubstrate leads to growth cone collapse.
Theodore et al.