Enhanced Cellular Uptake of G-Rich Oligonucleotides

A. Peyman Hoechst Aktiengesellschaft, G 838, D-65926, Frankfurt, am Main, Germany

A. Ryte Hoechst Aktiengesellschaft, G 838, D-65926, Frankfurt, am Main, Germany

M. Helsberg Hoechst Aktiengesellschaft, G 838, D-65926, Frankfurt, am Main, Germany

G. Kretzschmar Hoechst Aktiengesellschaft, G 838, D-65926, Frankfurt, am Main, Germany

M. Mag Hoechst Aktiengesellschaft, G 838, D-65926, Frankfurt, am Main, Germany

E. Uhlmann Hoechst Aktiengesellschaft, G 838, D-65926, Frankfurt, am Main, Germany

Abstract

Sequence-dependency of cellular uptake of oligonucleotides into Vero cells has been studied. Cellular uptake of 5′-[³⁵S]-labelled homopolymers decreased in the order (dG)₁₆ >> (dT)₁₆> (dA)₁₆ > (dC)₁₆. The change of two base-pairs (dG → dA) in a dG-rich antisense oligonucleotide with good antiviral activity dramatically decreased cellular uptake and abolished antiviral activity.

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Enhanced Cellular Uptake of G-Rich Oligonucleotides

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Enhanced Cellular Uptake of G-Rich Oligonucleotides

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