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 | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
commercial preparation | recombinant enzyme | Homo sapiens | - |
liver | - |
Homo sapiens | - |
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 | Comment | Organism |
---|---|---|
More | cathepsin B possesses A and B chains | Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
More | cathepsin B is a cysteine peptidase of the papain family | Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
25 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
4.5 | 6 | assay at | Homo sapiens |
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 |