Table 1.
Ki values of the catechol containing compounds for TLN, PLN, ALN, MMP-14, and MMP-9(T).
| Compound |
Ki ± sd (μM) |
||||
|---|---|---|---|---|---|
| McaRPPGFSAFK(Dnp)-OH |
McaPLGL(Dpa)AR-NH2 |
||||
| TLN | PLN | ALN | MMP-14 | MMP-9(T) | |
| ML32 | N.D. | 38 ± 8 | N.D. | 19 ± 0.8 | 51 ± 17 |
| BF471 | 13 ± 2 | 9 ± 3 | 49 ± 5 | 6.6 ± 0. 6 | 13 ± 2 |
| BF489 | 14 ± 5 | 16 ± 3 | N.D. | 8.3 ± 0.6 | 12.6 ± 0.6 |
| MT336 | N.D. | N.D. | N.D. | 12 ± 1 | 13 ± 1 |
Ki values determined for both bacterial and human metalloproteases using two different fluorescence quenched peptide substrates, McaRPPGFSAFK(Dnp)-OH (for TLN, PLN, and ALN) and McaPLGL(Dpa)AR-NH2 (for MMP-9(T) and MMP-14). The concentration of the substrates used was 4 µM and the highest concentration of tested inhibitors was 100 µM. Compounds included are only those where 100 µM of the compound reduced the enzymatic activity by 60% or more as described in the text. The Ki values are based on 4–6 experiments.
N.D.: not determined.