D-RECS (2) novel drug or gene delivery system based on responses to PKC alpha intracellular signals (D-RECS)

We propose a novel method for gene therapy using drug or gene delivery system based on responses to intracellular signals, especially to the phosphorylation of protein kinase C (PKC) alpha. A cationic peptide that has high phosphoarylation sensitivity for PKC alpha was designed, and then a polymer with these peptides was synthesized. In the electrophoresis examination, the polymer containing the cationic peptide formed a stable complex with anionic DNA, but free DNA was found after phosphorylation by PKC alpha. In the intratumor delivery of polymer/DNA complex, the luciferase activity in the positive polymer for PKC alpha at charge ratios of 0.1 and 0.3 was 10- to 20-fold higher than that in the negative control polymer with a peptide which the phosphorylated site Serine was substituted by Alanine. These results indicate that the D-RECS is applicable to gene therapy in vivo.