Beilstein J. Org. Chem.2015,11, 763–772, doi:10.3762/bjoc.11.86
-2025, USA 10.3762/bjoc.11.86 Abstract The success of siRNA-based therapeutics highly depends on a safe and efficient delivery of siRNA into the cytosol. In this study, we post-modified the primary amines on dendriticpolyglycerolamine (dPG-NH2) with different ratios of two relevant amino acids, namely
residues (His) are important for safe and efficient siRNA transfection, this study indicates that AAdPGs containing higher degrees of His display lower cytotoxicity and more efficient endosomal escape.
Keywords: arginine; dendriticpolyglycerolamine; histidine; multivalent vector; siRNA delivery
negative phosphates groups of the DNA [21]. Here, we chose dendriticpolyglycerolamine (dPG-NH2) with moderate amine loading (50% of all hydroxy groups on a 10 kDa dPG core) and introduced both amino acids via amide coupling to mimic DNA histones interactions.
In a recent study, our group demonstrated the
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Graphical Abstract
Scheme 1:
Synthesis of multivalent arginine and histidine functionalized dPG-NH2 50%. The depicted dPG-NH2 re...