Literature summary for 3.4.22.38 extracted from

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

Search for more literature for 3.4.22.38

Activating Compound

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

General Stability

General Stability	Organism
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

Organism

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

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

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism
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
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
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
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

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-

Posttranslational Modification

Posttranslational Modification	Comment	Organism
glycoprotein	-	Homo sapiens

Source Tissue

Source Tissue	Comment	Organism	Textmining

Substrates and Products (Substrate)

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

Turnover Number [1/s]

Turnover Number Minimum [1/s]	Turnover Number Maximum [1/s]	Substrate	Comment	Organism
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
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
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
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]

kcat/KM Value [1/mMs^-1]	kcat/KM Value Maximum [1/mMs^-1]	Substrate	Comment	Organism
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
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
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
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