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Literature summary for 3.4.22.1 extracted from

  • Mirkovic, B.; Premzl, A.; Hodnik, V.; Doljak, B.; Jevnikar, Z.; Anderluh, G.; Kos, J.
    Regulation of cathepsin B activity by 2A2 monoclonal antibody (2009), FEBS J., 276, 4739-4751.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2A2 monoclonal antibody binds to the epitope EPGYSP sequence, i.e. in the nonapeptide CIAEPGYSP, that is located between amino acid residues 133-138 of cathepsin B in the proximity of the occluding loop, surface plasmon resonance analysis, overview. Binding of 2A2 monoclonal antibody to the cathepsin B/cystatin C complex causes the dissociation of cystatin C from the complex, and binding of the antibody induces a conformational change in cathepsin B, stabilizing its exopeptidase conformation and thus disabling its harmful action associated with its endopeptidase activity Homo sapiens

Localization

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
BODIPY FL casein + H2O
-
Homo sapiens ?
-
?
DQ-collagen IV + H2O
-
Homo sapiens ?
-
?
additional information cathepsin B is a cysteine protease with both endopeptidase and exopeptidase activity Homo sapiens ?
-
?

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
5
-
exopeptidase activity assay at Homo sapiens
6
-
endopeptidase activity assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
702
-
pH 6.0, 37°C, versus substrate DQ-collagen IV Homo sapiens 2A2 monoclonal antibody
761
-
pH 6.0, 37°C, versus substrate BODIPY FL casein Homo sapiens 2A2 monoclonal antibody

General Information

General Information Comment Organism
physiological function the endopeptidase activity of cathepsin B is associated with the degradation of the extracellular matrix proteins, which is a process required for tumor cell invasion and metastasis, the activity can be inhibited by the 2A2 monoclonal antibody Homo sapiens