Table 7.
Sequences of CatS1–2 and CatK1–2 and their reported biological properties [99].
Comp. | Sequence a | Ki for CatS, pH 5.5 [nM] b | Ki for CatS, pH 7.4 [nM] b | Ki for CatK, pH 5.5 [nM] b | Ki for CatL, pH 5.5 [nM] b |
---|---|---|---|---|---|
CatS1 | Ac-Gly-Arg-Trp-His-Pro-Met-GlyΨ[Tz]Ala-Pro-Trp-Glu-D-Ala-D-Arg-NH2 | 15,000 ± 5000 | 42,000 ± 8000 | 10,000 ± 3600 | 30,000 ± 3200 |
CatS2 | Ac-Gly-Arg-Trp-His-Pro-Met-azaGly-Ala-Pro-Trp-Glu-D-Ala-D-Arg-NH2 | 26 ± 5 | 17 ± 3 | 3 ± 0.8 | 5 ± 0.5 |
CatK1 | Abz-Arg-Pro-Pro-GlyΨ[Tz]Phe-Ser-Pro-Phe-Arg-Tyr(3-NO2)-NH2 | n.o. | n.o. | 800 ± 330 | 22,000 ± 2000 |
CatK2 | Abz-Arg-Pro-Pro-azaGly-Phe-Ser-Pro-Phe-Arg-Tyr(3-NO2)-NH2 | n.o. | n.o. | 9 ± 0.7 | 2000 ± 400 |
a Abz: o-Aminobenzoic acid b Ki values were determined by measuring residual peptidase activity after incubation with the peptidomimetics at 37 °C using Z-Leu-Arg-AMC (Cathepsin S) or Z-Phe-Arg-AMC (Cathepsin K and L) as substrate. Data expressed as the means ± SEM of three individual experiments. n.o.: not observed.