Table 3.
ASO Modification | Modification Type | Nuclease Resistance | RNAse H Cleavage | Target Affinity | Toxicity |
---|---|---|---|---|---|
Phosphorothioate (PS) | Phosphate | + | Yes | - | ++ |
Phosphoramidate (NP) | Phosphate | + | No | + | + |
Methyl-phosphonate (MP) | Phosphate | + | No | - | + |
2′-O-methyl (2′-OMe) | Ribose | ++ | No | ++ | + Reduced immune activation; less toxic than PS |
2′-O-methoxyethyl (2′-MOE) | Ribose | ++ | No | ++ | + Reduced immune activation; Less than 2′-OMe; less toxic than PS |
Phosphorodiamidate morpholino (PMO) | Ribose phosphate | ++ | No | ++ | Safer |
Locked nucleic acid (LNA) | Ribose | ++ | No | +++ | +++ |
Constrained ethyl (cEt) | Ribose | +++ | No | +++ | ++ |
Peptide nucleic acid (PNA) | Ribose phosphate | ++ | No | ++ | ++ No immune activation |