Multifunctional CPP polymer system for tumor-targeted pDNA and siRNA delivery.
Cell-penetrating peptides (CPPs) are a very interesting class of molecules to be introduced in gene and siRNA vectors. They can be used to overcome one of the biggest hurdles in gene and siRNA delivery in vitro and in vivo, the transfer across cell membranes. This chapter describes protocols for the synthesis and biological evaluation of a polylysine-based polymer. In this carrier system, melittin is used as CPP with a high activity to disrupt membranes. pH-Labile masking is applied to render the lytic activity specific for intracellular acidic endolysosomal organelles.
Department of Pharmacy, Pharmaceutical Biotechnology, Centre for Drug Research, Ludwig-Maximilians-Universität, Munich, Germany.
Christian
C
Dohmen
Ernst
E
Wagner
D000595:Amino Acid Sequence; D000818:Animals; D001483:Base Sequence; D002460:Cell Line; D057846:Cell-Penetrating Peptides / Q000737:chemistry* / Q000378:metabolism* / Q000633:toxicity; D004247:DNA / Q000235:genetics / Q000378:metabolism*; D004337:Drug Carriers / Q000737:chemistry / Q000378:metabolism / Q000633:toxicity; D004912:Erythrocytes / Q000187:drug effects / Q000378:metabolism; D017930:Genes, Reporter / Q000235:genetics; D008156:Luciferases / Q000235:genetics; D008555:Melitten / Q000737:chemistry / Q000378:metabolism / Q000633:toxicity; D051379:Mice; D008969:Molecular Sequence Data; D009369:Neoplasms / Q000235:genetics / Q000378:metabolism*; D010957:Plasmids / Q000235:genetics; D011107:Polylysine / Q000737:chemistry*; D034741:RNA, Small Interfering / Q000235:genetics / Q000378:metabolism*; D014162:Transfection / Q000379:methods*; D014302:Trinitrobenzenesulfonic Acid / Q000378:metabolism
D057846:Cell-Penetrating Peptides; D004337:Drug Carriers; D034741:RNA, Small Interfering; D008555:Melitten; D011107:Polylysine; D014302:Trinitrobenzenesulfonic Acid; D004247:DNA; D008156:Luciferases