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Literature summary for 3.4.22.15 extracted from

  • Lecaille, F.; Chowdhury, S.; Purisima, E.; Broemme, D.; Lalmanach, G.
    The S2 subsites of cathepsins K and L and their contribution to collagen degradation (2007), Protein Sci., 16, 662-670.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
mutants expressed in Pichia pastoris Homo sapiens

Protein Variants

Protein Variants Comment Organism
A205L mutant shows an effective cathepsin K-like preference for Leu and Pro Homo sapiens
L67Y/A205L mutation induces a switch of the enzymatic specificity toward small selective inhibitors and peptidyl substrates Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
E-64
-
Homo sapiens
N-(4-biphenylacetyl)-S-methylcysteine-(D)-Arg-Phe-beta-phenethylamide also called Cat L inhibitor 7, specific inhibitor Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0011
-
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin mutant enzyme L67Y/A205L Homo sapiens
0.0013
-
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin wild type enzyme Homo sapiens
0.0087
-
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin wild type enzyme Homo sapiens
0.0098
-
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin mutant enzyme L67Y/A205L Homo sapiens
0.014
-
benzyloxycarbonyl-Gly-Pro-Arg-7-amido-4-methylcoumarin mutant enzyme L67Y/A205L Homo sapiens
0.081
-
benzyloxycarbonyl-Gly-Pro-Arg-7-amido-4-methylcoumarin wild type enzyme Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
butyl-Sepharose column chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-Gly-Pro-Arg-7-amido-4-methylcoumarin + H2O
-
Homo sapiens benzyloxycarbonyl-Gly-Pro-Arg + 7-amino-4-methylcoumarin
-
?
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin + H2O
-
Homo sapiens benzyloxycarbonyl-Leu-Arg + 7-amino-4-methylcoumarin
-
?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
Homo sapiens benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
?
Collagen + H2O substrate for cathepsin L mutant A205L Homo sapiens ?
-
?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.01
-
benzyloxycarbonyl-Gly-Pro-Arg-7-amido-4-methylcoumarin wild type enzyme Homo sapiens
0.5
-
benzyloxycarbonyl-Gly-Pro-Arg-7-amido-4-methylcoumarin mutant enzyme L67Y/A205L Homo sapiens
5.4
-
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin wild type enzyme Homo sapiens
17.6
-
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin wild type enzyme Homo sapiens
20.5
-
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin mutant enzyme L67Y/A205L Homo sapiens
27.2
-
benzyloxycarbonyl-Leu-Arg-7-amido-4-methylcoumarin mutant enzyme L67Y/A205L Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0043
-
N-(4-biphenylacetyl)-S-methylcysteine-(D)-Arg-Phe-beta-phenethylamide wild type enzyme Homo sapiens