Research Article

Superior Silencing by 2′,4′-BNANC-Based Short Antisense Oligonucleotides Compared to 2′,4′-BNA/LNA-Based Apolipoprotein B Antisense Inhibitors

Table 1

Oligonucleotides used in this study.

IDSequence (°C)IC50 (nM)

ApoB-LNA-205′-TTCAGcattggtattCAGTG-3′75 ± 0.87.9 ± 1.7
ApoB-LNA-165′-CAGcattggtatTCAG-3′64 ± 0.82.9 ± 0.4a
ApoB-LNA-145′-AGCattggtatTCA-3′61 ± 0.21.4 ± 0.5b
ApoB-LNA-135′-GCattggtatTCA-3′58 ± 0.22.8 ± 0.8a
ApoB-LNA-105′-CattggtatT-3′25 ± 1.4N.D.
ApoB-NC-205′-TTCAGcattggtattCAGTG-3′79 ± 1.011.4 ± 3.0
ApoB-NC-165′-CAGcattggtatTCAG-3′69 ± 0.81.3 ± 0.3b
ApoB-NC-145′-AGCattggtatTCA-3′64 ± 0.30.6 ± 0.1
ApoB-NC-135′-GCattggtatTCA-3′61 ± 0.10.9 ± 0.1
ApoB-NC-105′-CattggtatT-3′32 ± 0.4N.D.

2′,4′-BNA/LNA was shown in uppercase and 2′,4′-BNANC  was in italic. Natural DNA was shown in lowercase. All the linkages are phosphorothioated. We measured and IC50 values of all entries. values were determined in three independent experiments (±SD). Nondetectable IC50 values, due to low potency, were marked ND. a,bPairs of two IC50 values with superscript letters are NOT statistically significant.