Title: Biological effects of hexitol and altritol-modified siRNAs targeting B-Raf
Authors: Fisher, Michael
Abramov, Mikhail
Van Aerschot, Arthur
Rozenski, Jef
Dixit, Vidula
Juliano, Rudy L ×
Herdewijn, Piet #
Issue Date: Mar-2009
Publisher: Elsevier science bv
Series Title: European journal of pharmacology vol:606 issue:1-3 pages:38-44
Abstract: increasing the effectiveness of siRNAs through chemical modification is an important task. Here we describe altritol and hexitol modified oligonucleotides targeting the B-Raf oncogene that is critical for the growth and survival of melanoma cells. Using assays for apoptosis, DNA synthesis, colony formation and B-Raf protein and message levels, we demonstrate that certain hexitol modifications can improve the effectiveness of B-Raf siRNAs and also increase duration of action. Altritol modified siRNAs were similar to or slightly less effective than unmodified B-Raf siRNA. Modifications at the 3' or 5' end of the sense strand, at the 3' end of the antisense strand, or within either strand were well tolerated. The basis for the increased effectiveness of the hexitol-modified siRNAs is not fully understood but may be partly due to increased stability to nucleases. (C) 2009 Elsevier B.V. All rights reserved.
ISSN: 0014-2999
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Medicinal Chemistry (Rega Institute)
× corresponding author
# (joint) last author

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