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Literature summary for 3.4.22.1 extracted from

  • Schenker, P.; Alfarano, P.; Kolb, P.; Caflisch, A.; Baici, A.
    A double-headed cathepsin B inhibitor devoid of warhead (2008), Protein Sci., 17, 2145-2155.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
additional information inhibitor screening, overview Homo sapiens
[2-[2-(2,4-dioxo-1,3-thiazolidin-3-yl)ethylamino]-2-oxoethyl] 2-(furan-2-carbonylamino) acetate i.e. DOFA, a reversible, double-headed competitive inhibitor of cathepsin B, the dioxothiazolidine head of the compound sterically hinders binding of the C-terminal residue of substrates resulting in inhibition of the exopeptidase activity of cathepsin B in a physiopathologically relevant pH range, competitive versus substrates ortho-aminobenzoyl-Gly-Ile-Val-Arg-Ala-Lys-Nepsilon-2,4-dinitrophenyl-OH and carbobenzoxy-Arg-Arg-7-amido-4-methylcoumarin, structure and enzyme docking, overview Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation recombinant enzyme Homo sapiens
-
liver
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-aminobenzoyl-Gly-Ile-Val-Arg-Ala-(Nepsilon-2,4-dinitrophenyl)Lys + H2O an exoproteolytic substrate Homo sapiens 2-aminobenzoyl-Gly-Ile-Val-Arg + Ala-(Nepsilon-2,4-dinitrophenyl)Lys
-
?
carbobenzoxy-Arg-Arg-7-amido-4-methylcoumarin + H2O an endoproteolytic substrate Homo sapiens carbobenzoxy-Arg-Arg + 7-amino-4-methylcoumarin
-
?

Subunits

Subunits Comment Organism
More cathepsin B possesses A and B chains Homo sapiens

Synonyms

Synonyms Comment Organism
More cathepsin B is a cysteine peptidase of the papain family Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
4.5 6 assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information kinetic mechanism of inhibition by [2-[2-(2,4-dioxo-1,3-thiazolidin-3-yl)ethylamino]-2-oxoethyl] 2-(furan-2-carbonylamino) acetate Homo sapiens
0.0048
-
[2-[2-(2,4-dioxo-1,3-thiazolidin-3-yl)ethylamino]-2-oxoethyl] 2-(furan-2-carbonylamino) acetate pH 4.5, 25°C, competitive versus carbobenzoxy-Arg-Arg-7-amido-4-methylcoumarin Homo sapiens
0.0067
-
[2-[2-(2,4-dioxo-1,3-thiazolidin-3-yl)ethylamino]-2-oxoethyl] 2-(furan-2-carbonylamino) acetate pH 4.5, 25°C, competitive versus ortho-aminobenzoyl-Gly-Ile-Val-Arg-Ala-Lys-Nepsilon-2,4-dinitrophenyl-OH Homo sapiens
0.0113
-
[2-[2-(2,4-dioxo-1,3-thiazolidin-3-yl)ethylamino]-2-oxoethyl] 2-(furan-2-carbonylamino) acetate pH 6.0, 25°C, competitive versus carbobenzoxy-Arg-Arg-7-amido-4-methylcoumarin Homo sapiens