Effect of peptide content on the regulation of transgene expression by protein kinase Cα-responsive linear polyethylenimine-peptide conjugates

Riki Toita, Jeong Hun Kang, Chan Woo Kim, Shujiro Shiosaki, Takeshi Mori, Takuro Niidome, Yoshiki Katayama

Research output: Contribution to journalArticlepeer-review

3 Citations (Scopus)

Abstract

We examined a series of linear polyethylenimine (LPEI)-based nanocarriers that activate transgene expression in response to cancer-specific protein kinase Cα (PKCα). Eight types of LPEI-peptide conjugate differing in peptide content and number were synthesized using click chemistry. The conjugates could form polyplexes with pDNA through electrostatic interaction, but the degree of pDNA condensation, sizes, and surface charges of the resulting polyplexes depended on the pendant-peptide content and number. None of the polyplexes showed significant cytotoxicity toward human hepatoma cells (HepG2). Furthermore, pendant peptide content and number markedly affected transgene activation in response to PKCα. To achieve an all-or-none response to PKCα, we determined the optimum peptide content and number in LPEI-peptide conjugates as ≈6. mol% and ≈40. peptides/conjugate.

Original languageEnglish
Pages (from-to)123-129
Number of pages7
JournalColloids and Surfaces B: Biointerfaces
Volume123
DOIs
Publication statusPublished - Nov 1 2014

All Science Journal Classification (ASJC) codes

  • Biotechnology
  • Surfaces and Interfaces
  • Physical and Theoretical Chemistry
  • Colloid and Surface Chemistry

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