Self-aggregates of oligoarginine-conjugated poly(amino acid) derivatives as a carrier for intracellular drug delivery.
N(omega)-2,2,4,6,7-Pentamethyldihydrobenzofuran-5-sulfonyl (N(omega)-Pbf)-protected oligoarginine was directly conjugated to poly(amino acid) derivatives modified with a long alkyl chain. The final concentration of conjugated peptides was easily controlled by the feed ratio of oligoarginine to polymer backbone and a final soluble polymeric system was obtained by the deprotection of N(omega)-Pbf groups. The polymeric conjugates formed stable self-aggregates of size range of 8-40 nm in aqueous solution and effectively internalized into HeLa cells by adsorptive endocytosis.
Yang
Seung Rim
SR
Department of Chemical and Biomolecular Engineering, Korea Advanced Institute of Science and Technology, 305-701, Guseong-dong, Yuseong-gu, Daejeon, Republic of Korea.
Kim
Seung Beom
SB
Joe
Cheol O
CO
Kim
Jong-Duk
JD
D016503:Drug Delivery Systems; D004705:Endocytosis / Q000187:drug effects; D006367:HeLa Cells; D006801:Humans; D010455:Peptides / Q000737:chemistry / Q000494:pharmacology*
D010455:Peptides; C015462:polyarginine