Activating Compound | Comment | Organism | Structure |
---|---|---|---|
chondroitin 4-sulfate | required for gelatinolytic activity | Homo sapiens | |
Pepsin | - |
Homo sapiens |
Cloned (Comment) | Organism |
---|---|
mutant enzymes are expressed in Pichia pastoris | Homo sapiens |
Crystallization (Comment) | Organism |
---|---|
mutant K9E/I171E/Q172S/N190M/K191G/L195K (E-64 inhibited) in complex with the 17000 Da fraction of chondroitin 4-sulfate, hanging drop vapor diffusion method, using 30% (v/v) 2-methyl-2,4-pentanediol, 0.1 M sodium acetate buffer, pH 4.5, and 20 mM CaCl2 | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
K9E | the mutant shows decreased catalytic efficiencies towards Z-Leu-Arg-7-amido-4-methylcoumarin and Z-Gly-Pro-Arg-7-amido-4-methylcoumarin compared to the wild type enzyme | Homo sapiens |
K9E/I171E/Q172S | the mutant shows decreased catalytic efficiency towards Z-Leu-Arg-7-amido-4-methylcoumarin and increased catalytic efficiency towards Z-Gly-Pro-Arg-7-amido-4-methylcoumarin compared to the wild type enzyme | Homo sapiens |
K9E/I171E/Q172S/N190M/K191G/L195K | the mutant shows decreased catalytic efficiency towards Z-Leu-Arg-7-amido-4-methylcoumarin and increased catalytic efficiency towards Z-Gly-Pro-Arg-7-amido-4-methylcoumarin compared to the wild type enzyme | Homo sapiens |
K9E/N190M/K191G/L195K | the mutant shows increased catalytic efficiency towards Z-Leu-Arg-7-amido-4-methylcoumarin and decreased catalytic efficiency towards Z-Gly-Pro-Arg-7-amido-4-methylcoumarin compared to the wild type enzyme | Homo sapiens |
N190M/K191G/L195K | the mutant shows increased catalytic efficiencies towards Z-Leu-Arg-7-amido-4-methylcoumarin and Z-Gly-Pro-Arg-7-amido-4-methylcoumarin compared to the wild type enzyme | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
E-64 | i.e. L-3-carboxy-trans-2,3-epoxypropionylleucylamido-(4-guanidino)butane | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0024 | - |
Z-Leu-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E/I171E/Q172S, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
0.0033 | - |
Z-Leu-Arg-7-amido-4-methylcoumarin | wild type enzyme, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
0.0034 | - |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
0.0035 | - |
Z-Leu-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
0.0037 | - |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E/I171E/Q172S, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
0.0037 | - |
Z-Leu-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E/I171E/Q172S/N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
0.0037 | - |
Z-Leu-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E/N190M/K191G/L195K , in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
0.0038 | - |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin | mutant enzyme N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
0.0043 | - |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E/N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
0.0046 | - |
Z-Leu-Arg-7-amido-4-methylcoumarin | mutant enzyme N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
0.0058 | - |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E/I171E/Q172S/N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
0.048 | - |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin | wild type enzyme, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
Collagen type I + H2O | Homo sapiens | - |
? | - |
? | |
Gelatin + H2O | Homo sapiens | distinct cathepsin K/chondroitin 4-sulfate interactions are necessary for the collagenolytic activity of the enzyme | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P43235 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
osteoclast | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
Collagen type I + H2O | - |
Homo sapiens | ? | - |
? | |
Gelatin + H2O | distinct cathepsin K/chondroitin 4-sulfate interactions are necessary for the collagenolytic activity of the enzyme | Homo sapiens | ? | - |
? | |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin + H2O | - |
Homo sapiens | Z-Gly-Pro-Arg + 7-amino-4-methylcoumarin | - |
? | |
Z-Leu-Arg-7-amido-4-methylcoumarin + H2O | - |
Homo sapiens | Z-Leu-Arg + 7-amino-4-methylcoumarin | - |
? |
Synonyms | Comment | Organism |
---|---|---|
catK | - |
Homo sapiens |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
1.9 | - |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E/N190M/K191G/L195K , in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
2 | - |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
2.1 | - |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E/I171E/Q172S, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
2.9 | - |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin | wild type enzyme, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
3.6 | - |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E/I171E/Q172S/N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
3.7 | - |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin | mutant enzyme N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
5.6 | - |
Z-Leu-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E/I171E/Q172S/N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
5.7 | - |
Z-Leu-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
6.2 | - |
Z-Leu-Arg-7-amido-4-methylcoumarin | wild type enzyme, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
6.4 | - |
Z-Leu-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E/I171E/Q172S, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
7.6 | - |
Z-Leu-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E/N190M/K191G/L195K , in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
9.1 | - |
Z-Leu-Arg-7-amido-4-methylcoumarin | mutant enzyme N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens |
kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
1500 | - |
Z-Leu-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E/I171E/Q172S/N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
1600 | - |
Z-Leu-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
1900 | - |
Z-Leu-Arg-7-amido-4-methylcoumarin | wild type enzyme, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
2000 | - |
Z-Leu-Arg-7-amido-4-methylcoumarin | mutant enzyme N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
2100 | - |
Z-Leu-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E/N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
2700 | - |
Z-Leu-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E/I171E/Q172S, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
4400 | - |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E/N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
5700 | - |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E/I171E/Q172S, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
5900 | - |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
6000 | - |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin | wild type enzyme, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
6200 | - |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin | mutant enzyme K9E/I171E/Q172S/N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens | |
9700 | - |
Z-Gly-Pro-Arg-7-amido-4-methylcoumarin | mutant enzyme N190M/K191G/L195K, in 100 mM sodium acetate buffer, pH 5.5, containing 2.5 mM dithiothreitol, and 2.5 mM EDTA, at 28°C | Homo sapiens |