Table 2.
Inhibitory Activities (IC50 Values) of the Stapled and Linear Peptides toward the 3′-End Processing and Strand Transfer Reactions Catalyzed by HIV-1 IN
| peptide | I50
μM)> |
|
|---|---|---|
| 3′-end processing | strand transfer | |
| 3S (stapled) | 5.8 ± 0.8 | 3.8 ± 0.7 |
| 4S (stapled) | 2.5 ± 0.4 | 1.1 ± 0.08 |
| 5S (stapled) | 2.8 ± 0.3 | 1.2 ± 0.09 |
| 6S (stapled) | 2.4 ± 0.4 | 0.84 ± 0.07 |
| 7S (stapled) | >111 | 54.4 ± 9.6 |
| 8S (stapled) | 5.6 ± 0.7 | 4.1 ± 0.6 |
| 9S (stapled) | 4.9 ± 0.6 | 1.9 ± 0.2 |
| 4L (linear) | 5.2 ± 0.5 | 1.7 ± 0.3 |
| 5L (linear) | 9.6 ± 0.6 | 4.4 ± 0.4 |
| 6L (linear) | 2.6 ± 0.4 | 1.2 ± 0.09 |
| 8L (linear) | 2.5 ± 0.3 | 1.0 ± 0.07 |
| 9L (linear) | 2.1 ± 0.2 | 0.9 ± 0.06 |
| 11S (stapled) | 4.2 ± 0.7 | 0.7 ± 0.08 |
| 11L (linear) | 3.5 ± 0.3 | 1.7 ± 0.3 |
| 1 | 2.6 ± 0.2 | 1.1 ± 0.08 |
| 2 | 0.079 ± 0.007 | 0.036 ± 0.008 |