Table 2.
Sequence, analytical data, and effect of peptides 19–28 on HIV-1 IN activities.
| Peptide | Sequence | HPLC | ESI-MS | IN inhibition |
|---|---|---|---|---|
| k' | Found | IC50(μM) | ||
| 18 | VVAKEIVAH | 3.50 | 1007 | 4.5 ± 0.9 |
| 19 | FVAKEIVAH | 4.40 | 1054.4 | NA |
| 20 | VFAKEIVAH | 4.50 | 1054.5 | 375 ± 19 |
| 21 | VVAKEIFAH | 4.20 | 1054.2 | 504 ± 22 |
| 22 | AVAKEIVAH | 3.90 | 978.6 | NA |
| 23 | VAAKEIVAH | 4.20 | 978.4 | NA |
| 24 | VVAAEIVAH | 4.84 | 949.5 | 20.8 ± 1.3 |
| 25 | VVAKAIVAH | 4.05 | 948.6 | 13.0 ± 1.0 |
| 26 | VVAKEAVAH | 1.39 | 964.5 | NA |
| 27 | VVAKEIAAH | 3.90 | 978.5 | NA |
| 28 | VVAKEIVAA | 4.89 | 939.5 | NA |
| Raltegravir | 0.24 ± 0.02 |
All peptide are acetylated and amidate at C terminal and N terminal respectively.
k' [(peptide retention time – solvent retention time)/solvent retention time]. Peptide concentration μM.
NA = Not Applicable, 50% inhibition by the compound was not achieved (as example see the dose-response curve of peptide 19 in Supplementary Material).