Table 1.
Sequences and Ki values of inhibiting huPA of upain-1 variants.
| Peptide code | Sequence* | Ki values of inhibiting huPA (μM) |
|---|---|---|
| upain-1 | CSWRGLENHRMC | 30 ± 1 (3) |
| D1D2-upain-1 | CSWRGLENHRMC-D1D2 | 2.2 ± 0.1 (3) |
| upain-2 | CSWRGLENHAAC | 35 ± 8 (3) |
| MGSADGA-upain-1-GAAG | MGSADGA-CSWRGLENHRMC-GAAG | 4.5 ± 0.8 (3) |
| MGSADGA-upain-2-GAAG | MGSADGA-CSWRGLENHAAC-GAAG | 3.5 ± 0.1 (3) |
| DGA-upain-2 | DGA-CSWRGLENHAAC | 4.6 ± 0.6 (3) |
| bicyclic peptide 24 | CSWRGCENHAAPA | 26 ± 13 (6) |
| bicyclic peptide 29 | CSWRGCENHAAAP | 32 ± 14 (6) |
| upain-1 W3A | CSARGLENHRMC | 313 ± 8 (3) |
*All synthetic peptides are of an acetylated N-terminus and an amidated C-terminus, and are cyclized through the underlined residues.