Lipophilic 2'-O-Acetalester RNAs:Synthesis, Thermal Duplex Stability, Nuclease Resistance, Cellular Uptake and siRNA Activity after Spontaneous Naked Delivery.

We report synthesis, biochemical and biophysical characteristics of 2'-O-phenylisobutyryloxymethyl (PiBuOM)-modified siRNA and their impact on biological activity. In case of spontaneous cellular uptake of naked PiBuOM-modified siRNA, we observe increased target suppression in human cells versus unmodified or pivaloyloxymethyl (PivOM)-modified siRNA. We provide evidence for improved spontaneous cellular uptake of naked PiBuOM-modified siRNA and for substantial target suppression in human cells in serum-containing medium.
PMID: 27569765 [PubMed - as supplied by publisher]

Source: Chembiochem - August 28, 2016 Category: Biochemistry Authors: Biscans A, Bertrand JR, Dubois J, Rüger J, Vasseur JJ, Sczakiel G, Dupouy C, Debart F Tags: Chembiochem Source Type: research