| abstract |
In accordance with the present invention, antisense oligonucleotides are provided with enhanced membrane permeability and stability. This is accomplished in accordance with the invention through conjugating oligoribonucleotides with a hydrophobic carrier agent at the 2'-O position of the oligonucleotides. The hydrophobic carrier agent comprises a compound of the following general structure: <IMAGE> wherein R1, R2, R3, R4, and R5 are independently H, NO2, halide, linear or branched alkyl, linear or branched acyl, linear or branched alkylene, linear or branched O-alkyl, linear or branched amido, linear or branched S-alkyl, mono or disubstituted amine, linear or branched thioamido, phosphothionate, or phosphothioate. In a preferred embodiment, R1 and R3 are NO2. In such embodiment, it will be appreciated that when R2, R4, and R5 are H, the compound is DNP and when R4 is F, the compound is FDNP. |