Table 2. Effect of the Oligonucleotide Structure on the Inhibition of 3′-Processing by the Conjugate.
| modification | oligonucleotide 5′ → 3′ | 3′-processing IC50 (nM) |
|---|---|---|
| 11D-E | GGTTTTTGTGT-E | 50 ± 7 |
| 11DX-E-1 | GGTTTTTxGTxGTx-E | 100 ± 15 |
| 11DX-E-2 | GGTxTxTxTTGTGT-E | 110 ± 20 |
| 11DX-E-3 | GGTxTTxTTGTxGT-E | 100 ± 15 |
| 11DS-E-1 | GsGsTsTsTsTsTsGsTsGsTs-E | 18 ± 4 |
| 11DS-E-2 | GGTTTTTsGTsGTs-E | 20 ± 2 |
| 11DS-E-3 | GGTsTsTsTTGTGT-E | 22 ± 6 |
| 11DS-E-4 | GGTsTTTsTGTsGT-E | 24 ± 7 |
| HEX-11D | HEX-GGTTTTTGTGT | 55 ± 10 |
| HEX-11-ddR | HEX-(ddR)10T | 1200 ± 70 |
| HEX-11D-ddR-1 | HEX-(ddR)6TGTGT | 280 ± 35 |
| HEX-11D-ddR-2 | HEX-GGTT(ddR)6T | 250 ± 30 |
| HEX-11-PD | HEX-(PD)10T | 1300 ± 90 |
| HEX-11D-PD-1 | HEX-(PD)6TGTGT | 250 ± 25 |
| HEX-11D-PD-2 | HEX-GGTT(PD)6T | 310 ± 45 |
| 11M-E | mGmGmUmUmUm-UmUmGmUmGmU-E | 48 ± 8 |
| HEX-11M | HEX-mGmGmUmUmUm-UmUmGmUmGmU | 52 ± 10 |
| HEX-11MS | HEX-mGsmGsmUsmUsm-UsmUsmUsmGsmUsmGsmUs | 19 ± 4 |
| HEX-11MS-Ole | HEX-mGsmGsmUsmUsm-UsmUsmUsmGsmUsmGsmUs-Ole | 20 ± 3 |