TY - JOUR
T1 - Effect of peptide content on the regulation of transgene expression by protein kinase Cα-responsive linear polyethylenimine-peptide conjugates
AU - Toita, Riki
AU - Kang, Jeong Hun
AU - Kim, Chan Woo
AU - Shiosaki, Shujiro
AU - Mori, Takeshi
AU - Niidome, Takuro
AU - Katayama, Yoshiki
N1 - Funding Information:
This work was financially supported in-part by a Grant-in-aid for Scientific Research from Ministry of Education, Culture, Sports, Science & Technology (MEXT) in Japan. R.T. is grateful to Japan Society for the Promotion of Science (JSPS) for the doctoral scholarship.
Publisher Copyright:
© 2014 Elsevier B.V.
PY - 2014/11/1
Y1 - 2014/11/1
N2 - 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.
AB - 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.
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U2 - 10.1016/j.colsurfb.2014.09.004
DO - 10.1016/j.colsurfb.2014.09.004
M3 - Article
AN - SCOPUS:84915803545
SN - 0927-7765
VL - 123
SP - 123
EP - 129
JO - Colloids and Surfaces B: Biointerfaces
JF - Colloids and Surfaces B: Biointerfaces
ER -
