Table 1.
Sequence, analytical data and effect of peptides 1–18 on HIV-1 IN activities.
| Peptide | Sequence | HPLC | ESI MS | IN inhibition |
|---|---|---|---|---|
| k' | Found | IC50(μM) ±SD | ||
| 1 | 1FLDGIDKAQD | 4.70 | 1163.1 | NA |
| 2 | 4GIDKAQDEHE | 5.03 | 1182.5 | 162±9 |
| 3 | 7KAQDEHEKYH | 4.63 | 1326.7 | NE |
| 4 | 10DEHEKYHSNW | 4.75 | 1385.5 | NA |
| 5 | 13EKYHSNWRA | 5.02 | 1363.7 | NE |
| 6 | 16HSNWRAMASD | 2.94 | 1215.5 | NE |
| 7 | 19WRAMASDFNL | 2.30 | 1251.7 | NE |
| 8 | 22MASDFNLPPV | 1.30 | 1131.6 | NA |
| 9 | 25DFNLPPVVAK | 3.70 | 1140.6 | 213 ± 12 |
| 10 | 28LPPVVAKEIV | 4.40 | 1105.8 | NA |
| 11 | 31VVAKEIVASC | 2.12 | 1059.7 | NA |
| 12 | 34KEIVASCDKC | 3.06 | 1136.5 | 477 ± 23 |
| 13 | 37VASCDKCQLK | 2.80 | 1135.5 | NA |
| 14 | 40CDKCQLKGEA | 2.60 | 1135.4 | NA |
| 15 | 43CQLKGEAM | 3.70 | 920.3 | NA |
| 16 | 31VVAKEIVAS | 2.50 | 956.5 | NA |
| 17 | VVAKEIVASH VVAKEIVAH | 5.22 | 1094.0 | NA |
| 18 | VVAKEIVAH | 3.50 | 1007.0 | 4.5 ± 0.9 |
| Raltegravir | 0.18 ± 0.01 |
All peptide are acetylated and amidate at N terminal and C terminal respectively.
k' [(peptide retention time – solvent retention time)/solvent retention time]. Peptide concentration μM.
NE, No effect. The peptide demonstrated no significant effect in the IN assay, where the percent activity for the compounds was found to be 100 ± 7% (As example see the dose-response curve of peptide 5 in Supplementary Material).
NA, Not Applicable, 50% inhibition by the compound was not achieved (As example see the dose-response curve of peptide 8 in Supplementary Material).