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Literature summary extracted from

  • Hoang, V.L.; Li, Y.; Kim, S.K.
    Cathepsin B inhibitory activities of phthalates isolated from a marine Pseudomonas strain (2008), Bioorg. Med. Chem. Lett., 18, 2083-2088.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.4.22.1 expressed in murine melanoma cell line B16-F10 Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.1 CA030
-
 Homo sapiens
3.4.22.1 di-(2-ethylhexyl)phthalate non-competitive inhibitor Homo sapiens
3.4.22.1 dibutyl phthalate non-competitive inhibitor Homo sapiens
3.4.22.1 E-64
-
 Homo sapiens
3.4.22.1 leupeptin
-
 Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.4.22.1 lysosome
-
 Homo sapiens 5764
-

Organism

EC Number Organism UniProt Comment Textmining
3.4.22.1 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.
3.4.22.1 benzyloxycarbonyl-L-Arg-Arg-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens benzyloxycarbonyl-L-Arg-Arg + 7-amino-4-methylcoumarin
-
 ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.22.1 0.42
-
 di-(2-ethylhexyl)phthalate wild type enzyme, in 0.4 M sodium potassium phosphate buffer (pH 6.0) containing 8 mM dithiothreitol and 4 mM EDTA, at 37°C Homo sapiens
3.4.22.1 0.64
-
 dibutyl phthalate wild type enzyme, in 0.4 M sodium potassium phosphate buffer (pH 6.0) containing 8 mM dithiothreitol and 4 mM EDTA, at 37°C Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.22.1 0.14
-
 recombinant enzyme, in Hank's balanced salt solution containing 2 mM L-cysteine, pH 7.0, at 37°C Homo sapiens di-(2-ethylhexyl)phthalate
3.4.22.1 0.23
-
 recombinant enzyme, in Hank's balanced salt solution containing 2 mM L-cysteine, pH 7.0, at 37°C Homo sapiens dibutyl phthalate
3.4.22.1 0.38
-
 wild type enzyme, in 0.4 M sodium potassium phosphate buffer (pH 6.0) containing 8 mM dithiothreitol and 4 mM EDTA, at 37°C Homo sapiens di-(2-ethylhexyl)phthalate
3.4.22.1 0.42
-
 wild type enzyme, in 0.4 M sodium potassium phosphate buffer (pH 6.0) containing 8 mM dithiothreitol and 4 mM EDTA, at 37°C Homo sapiens dibutyl phthalate