Table 2.
Sequences and Ki values of inhibiting uPAs of mupain-1 variants.
| Peptide code | Sequence* | Ki values (μM) | ||
|---|---|---|---|---|
| muPA | huPA | huPA H99Y | ||
| mupain-1 | CPAYSRYLDC | 0.55 ± 0.08 (5) | > 1000 | 15.3 ± 0.2 (3) |
| mupain-1-12 | CPAYS[12]YLDC | 0.28 ± 0.02 (3) | 93 ± 19 (3) | 0.34 ± 0.06 (3) |
| mupain-1-16 | CPAYS[16]YLDC | 0.045 ± 0.01 (3) | 93 ± 18 (3) | 1.86 ± 0.74 (3) |
| mupain-1-IG | CPAYSRYIGC | 0.020 ± 0.004 (3) | 38 ± 23 (3) | 0.01 ± 0.001 (3) |
| mupain-1-12-IG | CPAYS[12]YIGC | 0.010 ± 0.002 (3) | 0.56 ± 0.12 (3) | 2.48 ± 0.07 (3) |
| mupain-1-16-IG | CPAYS[16]YIGC | 0.002 ± 0.0005 (3) | 0.53 ± 0.07 (3) | 0.01 ± 0.002 (3) |
| mupain-1-D9A | CPAYSRYLAC | 0.89 ± 0.02 (3) | > 1000 | 5.99 ± 0.43 (3) |
| mupain-1-12-D9A | CPAYS[12]YLAC | 0.19 ± 0.01 (3) | 11.7 ± 0.36 (3) | 0.19 ± 0.04 (3) |
| mupain-1-16-D9A | CPAYS[16]YLAC | 0.076 ± 0.003 (3) | 16.9 ± 1.8 (3) | 0.31 ± 0.01 (3) |
*All synthetic peptides are of an acetylated N-terminus and an amidated C-terminus, and are cyclized through the underlined residues.