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Literature summary extracted from

  • Novinec, M.; Kovacic, L.; Lenarcic, B.; Baici, A.
    Conformational flexibility and allosteric regulation of cathepsin K (2010), Biochem. J., 429, 379-389.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
3.4.22.38 chondroitin sulfate non-essential activator in assays using low-molecular-mass substrates, 4fold stimulation of activity at 0.2 mM Homo sapiens
3.4.22.38 dermatan sulfate non-essential activator in assays using low-molecular-mass substrates, 4fold stimulation of activity at 0.2 mM Homo sapiens
3.4.22.38 heparin 12fold stimulation of activity at 0.2 mM Homo sapiens
3.4.22.38 additional information hyaluronan has no effect on activity Homo sapiens
3.4.22.38 NaCl 300 mM NaCl stimulates enzyme activity Homo sapiens

General Stability

EC Number General Stability Organism
3.4.22.38 the activity of cathepsin K alone is relatively unstable in aqueous solution, having a half-life of approx. 7 min at pH 7.4 and 37°C. Increasing the ionic strength of the incubation mixture to 300 mM with NaCl decreases the half-life by 7fold. The presence of chondrotin sulfate and dermatan sulfate slightly reduces the stability of cathepsin K (half lives of 5.5 and 6.0 min respectively), whereas heparin has a strong stabilizing effect and increases the enzyme's half-life by more than 5fold (38 min) Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.38 N2TY slow-binding inhibitor of cathepsin K Homo sapiens
3.4.22.38 Stefin A slow-binding inhibitor of cathepsin K Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.22.38 0.0032
-
 benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin enzyme in the presence of 300 mM NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C Homo sapiens
3.4.22.38 0.0051
-
 benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin enzyme in the presence of 300 mM NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C Homo sapiens
3.4.22.38 0.0077
-
 benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin enzyme in the absence of NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C Homo sapiens
3.4.22.38 0.021
-
 benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin enzyme in the absence of NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.22.38 Homo sapiens
-
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
3.4.22.38 glycoprotein
-
 Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.22.38 benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens ?
-
 ?
3.4.22.38 benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens benzyloxycarbonyl-Val-Val-Arg + 7-amino-4-methylcoumarin
-
 ?
3.4.22.38 Elastin + H2O the elastinolytic activity of cathepsin K at pH 7.4 is 60% of that observed at pH 6.2 Homo sapiens ?
-
 ?
3.4.22.38 soluble calf-skin collagen + H2O
-
 Homo sapiens ?
-
 ?

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.4.22.38 0.19
-
 benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin enzyme in the presence of 300 mM NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C Homo sapiens
3.4.22.38 0.37
-
 benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin enzyme in the absence of NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C Homo sapiens
3.4.22.38 39
-
 benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin enzyme in the presence of 300 mM NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C Homo sapiens
3.4.22.38 91
-
 benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin enzyme in the absence of NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C Homo sapiens

kcat/KM [mM/s]

EC Number kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
3.4.22.38 48
-
 benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin enzyme in the absence of NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C Homo sapiens
3.4.22.38 59
-
 benzyloxycarbonyl-Val-Val-Arg-7-amido-4-methylcoumarin enzyme in the presence of 300 mM NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C Homo sapiens
3.4.22.38 4300
-
 benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin enzyme in the absence of NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C Homo sapiens
3.4.22.38 7600
-
 benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin enzyme in the presence of 300 mM NaCl, in 50 mM HEPES, pH 7.4, containing 1 mM EDTA and 2.5 mM dithiothreitol, at 25°C Homo sapiens