Precise Enzymatic Cleavage Sites for Improved Bioactivity of siRNA Lipo-Polyplexes
نویسندگان
چکیده
منابع مشابه
Precise redox-sensitive cleavage sites for improved bioactivity of siRNA lipopolyplexes.
Lipo-oligomers have been proven as potent siRNA carriers based on stable electrostatic and hydrophobic complex formation and endosomal membrane destabilization. Although high stability of siRNA polyplexes is desirable in the extracellular space and cellular uptake, intracellular disassembly is important for the cytosolic release of siRNA and RNA-induced silencing complex formation. To improve t...
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Although our understanding of RNAi and our knowledge on designing and synthesizing active and safe siRNAs significantly increased during the past decade, targeted delivery remains the major limitation in the development of siRNA therapeutics. On one hand, practical considerations dictate robust chemistry reproducibly providing precise carrier molecules. On the other hand, the multistep delivery...
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Many previous non–viral siRNA vector development efforts have yielded reagents effective for in vitro transfection but that have poor in vivo pharmacokinetics and bioactivity. The current work focuses on development of a siRNA nanocarrier optimized to overcome both cell–level barriers (uptake/endosomal escape) and systemic barriers following intravenous delivery (stability for long circulation ...
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RNA interference (RNAi) is a powerful tool to treat diseases and elucidate target gene function. Prior to clinical implementation, however, challenges including the safe, efficient and targeted delivery of siRNA must be addressed. Here, we report cationic nanogel nanostructured polymers (NSPs) prepared by atom transfer radical polymerization (ATRP) for in vitro and in vivo siRNA delivery in mam...
متن کاملRole of clathrin- and caveolae-mediated endocytosis in gene transfer mediated by lipo- and polyplexes.
We investigated the effects of inhibitors of clathrin-mediated endocytosis (chlorpromazine and K(+) depletion) and of caveolae-mediated uptake (filipin and genistein) on internalization of FITC-poly-l-lysine-labeled DOTAP/DNA lipoplexes and PEI/DNA polyplexes by A549 pneumocytes and HeLa cells and on the transfection efficiencies of these complexes with the luciferase gene. Uptake of the comple...
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ژورنال
عنوان ژورنال: Bioconjugate Chemistry
سال: 2018
ISSN: 1043-1802,1520-4812
DOI: 10.1021/acs.bioconjchem.8b00585