Table 1.
CPI-17 derived peptides tested *.
| No. | Peptide sequence | Efficacy |
|---|---|---|
| 600 | NH2-RRVTVKYDRR-NH2 | No |
| 605 | NH2-RRVpTVKYDRR-NH2 | No |
| 610 | NH2-RRVTVKYKRR-NH2 | No |
| 615 | NH2-RRVpTVKYKRR-NH2 | No |
| 620 | NH2-RRKTVKYDRR-NH2 | No |
| 630 | NH2-RRVEVKYDRR-NH2 | Yes |
*R36VTVKYDRR44 was selected as the starting sequence (peptide 600). Residues were varied in test series as indicated (bold, underlined). Efficacy was determined by TEER reduction following apical application of 5 mM to Caco-2 cell monolayers with a two-fold increase in 4 kDa dextran flux as the efficacy threshold. Peptide 630 (NH2-RRVEVKYDRR-NH2) was synthesized in the retro-inverso form with d-amino acids as PIP peptide 640 (NH2-rrdykvevrr-NH2).