Table 2.
Inhibition activities of Cmpd8, Cmpd21, and truncated analogs. Inhibitory effect of compounds on sPLA2-IIA-integrin interaction was assessed in adhesion assays using αvβ3-K562 cells and immobilized sPLA2-IIA. The IC50 and maximum inhibition was calculated with adhesion without inhibitors as 100% and adhesion to BSA only as 0%. Data are shown as means ± S.E. (n=3).
| Compound | Structural Formulaa | Activity (IC50, μM) |
Maximum Inhibition (%) |
|---|---|---|---|
| Cmpd8-1 | R-OH | - | N/A |
| Cmpd8-2 | R-Ala | - | N/A |
| Cmpd8-3 | R-Ala-Trp | - | N/A |
| Cmpd8-4 | R-Ala-Trp-Asp* | - | N/A |
| Cmpd8-5 | Ala-Trp-Asp*-Ile | - | N/A |
| Cmpd8 | R-Ala-Trp-Asp*-Ile | 20±1.3 | 85±1.5 |
| Cmpd21-1 | R-Gly | 241±33 | 98±2.4 |
| Cmpd21-2 | R-Gly-Arg* | 262±6.8 | 77±1.8 |
| Cmpd21-3 | R-Gly-Arg*-Gly | 217±14 | 81±3.0 |
| Cmpd21-4 | R-Gly-Arg*-Gly-Asp* | 155±3.8 | 87±1.7 |
| Cmpd21-5 | R-Gly-Arg*-Gly-Asp*-Asp* | - | N/A |
| Cmpd21-6 | Gly-Arg*-Gly-Asp*-Asp*-Asp* | - | N/A |
| Cmpd21 | R-Gly-Arg*-Gly-Asp*-Asp*-Asp* | 71±18 | 93±10 |
|
A terminal residue has an ending NH2 group replacing the OH group of its carboxylic acid functionality. Amino acids with an asterisk stand for D-amino acids.