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Literature summary for 3.4.22.38 extracted from

  • Cherney, M.M.; Lecaille, F.; Kienitz, M.; Nallaseth, F.S.; Li, Z.; James, M.N.; Broemme, D.
    Structure-activity analysis of cathepsin K/chondroitin 4-sulfate interactions (2011), J. Biol. Chem., 286, 8988-8998.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.22.38

Activating Compound

Activating Compound Comment Organism Structure
chondroitin 4-sulfate required for gelatinolytic activity Homo sapiens
Pepsin
-
 Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
mutant enzymes are expressed in Pichia pastoris Homo sapiens

Crystallization (Commentary)

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

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

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 [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/ Products (Substrates)

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

Organism UniProt Comment Textmining
Homo sapiens P43235
-
-

Source Tissue

Source Tissue Comment Organism Textmining
osteoclast
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms Comment Organism
catK
-
 Homo sapiens

Turnover Number [1/s]

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 [mM/s]

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