PKC β pseudosubstrate
Biological ActivityPKC β pseudosubstrate is a selective cell-permeable peptide inhibitor of protein kinase C (IC50 ~ 0.5 μM). 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.
(Modifications: Disulfide bridge between 17 -1*)
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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.
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