Evaluation of the transfection property of a peptide ligand for the fibroblast growth factor receptor as part of PEGylated polyethylenimine polyplex

Gene therapy progress and prospects: synthetic polymer-based systems

“…Recent concepts include peptide-based targeting ligands, and new strategies for simultaneous and defined incorporation of targeting and shielding functions into polyplexes. 44,[47][48][49] For example, the cyclic pentapeptide CNGRC conjugated with PEG, and attached to PEI through noncovalent phenyldiboronic acid/salicylhydroxamic acid bridges, was used for polyplex formation targeting CD13 of tumor and tumor endothelial cells. Intravenous application of such polyplexes delivering p53-encoding pDNA in tumor-bearing mice showed encouraging therapeutic antitumoral effects.…”

“…47 A 7-mer peptide (MQLPLAT) targeting the fibroblast growth factor 2 receptor was incorporated into PEGylated PEI polyplexes. 48 Two approaches were compared, conjugating the peptide to PEI through a PEG spacer either before (premodified) or after (postmodified) complexation of PEI with DNA. Both approaches led to similar biophysical properties, but only the postmodification approach resulted in increased cell uptake and transfection, presumably because of better accessibility of the peptide ligand to the fibroblast growth factor receptor.…”

The mechanism of selective transfection mediated by pentablock copolymers; Part I: Investigation of cellular uptake

“…There may be two reasons: PB-PLE has better accessibility of EGF to EGF receptors on the cell surface; EGF will not affect the complexation between PB and DNA, since the PLE was added after the formation of DNA condensates. This greatest effectiveness of incorporating a ligand on the most accessible position has been reported by attaching a peptide or EGF to PEGylated PEI polyplexes [5,6,30]. Thus, it is not surprising that PBE-PL showed the most inefficient transfection, owing to the smaller chance of EGF being exposed to the cell surface receptors and the potential interference with DNA condensation by conjugating EGF to the pentablock copolymer.…”

Enhanced lentiviral vector production in 293FT cells expressing Siglec-9

“…Several studies reported that EGFmodified lipid vesicles were constructed for effective delivery to tumor cells expressing high levels of the EGF receptor (Kikuchi et al 1996). A similar approach has been used for transferrin or lactoferrin with their receptors, and the RGD peptide with integrins (Cheng 1996;Elfinger et al 2007;Kunath et al 2003;Rao et al 2008;Scott et al 2001). In this regard, Siglecs also exhibited enhanced efficiency of uptake of binding substances.…”