The Effect of INA [(R)-1-O-(1-Pyrenylmethyl)Glycerol] Insertions on the Structure and Biological Activity of a G-Quadruplex from a Critical Kras G-Rich Sequence

Susanna Cogoi Department of Biomedical Science and Technology, University of Udine, Udine, Italy

Manikandan Paramasivan Department of Biomedical Science and Technology, University of Udine, Udine, Italy

L. E. Xodo Department of Biomedical Science and Technology, University of Udine, Udine, Italy

Vyacheslav V. Filichev Department of Chemistry, Nucleic Acid Center, University of Southern Denmark, Odense, M, Denmark

Erik B. Pedersen Department of Chemistry, Nucleic Acid Center, University of Southern Denmark, Odense, M, Denmark

Abstract

Quadruplex-forming oligonucleotides containing INA [(R)-1-O-(1-pyrenylmethyl)glycerol] insertions have been designed and studied for their capacity to inhibit the expression of the KRAS oncogene in pancreatic adenocarcinoma cells. It is found that INA can influence the folding topology of the G-quadruplex. The oligonucleotides forming the most stable G-quadruplex (ODN-637) is found to exhibit the highest bioactivity.

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The Effect of INA [(R)-1-O-(1-Pyrenylmethyl)Glycerol] Insertions on the Structure and Biological Activity of a G-Quadruplex from a Critical Kras G-Rich Sequence

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The Effect of INA [(R)-1-O-(1-Pyrenylmethyl)Glycerol] Insertions on the Structure and Biological Activity of a G-Quadruplex from a Critical Kras G-Rich Sequence

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