Activating Compound | Comment | Organism | Structure |
---|---|---|---|
additional information | recombinant CatS is activated in 100 mM sodium acetate, pH 5.5 containing 1 mM EDTA and 2 mM dithiothreitol for 30 min at 37°C | Homo sapiens |
Application | Comment | Organism |
---|---|---|
drug development | CatS is involved in the pathogenesis of autoimmune disorders, atherosclerosis and obesity, therefore, it represents a promising pharmacological target for drug development | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
human recombinant CatS expressed in Escherichia coli | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(2Z)-3-(4-[[5-(3,5-dimethylisoxazol-4-yl)-1,2,4-oxadiazol-3-yl]methoxy]phenyl)-2-(methylsulfonyl)prop-2-enenitrile | - |
Homo sapiens | |
(3S)-N-[2-(1H-indol-3-yl)ethyl]-3-[[(4-methylphenyl)sulfonyl]amino]-2-oxo-4-phenylbutanamide | - |
Homo sapiens | |
1,1-bis(cyanomethyl)-3-[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]urea | - |
Homo sapiens | |
2,2'-[[3-(trifluoromethyl)phenyl]imino]bis[N-(4-methylphenyl)acetamide] | - |
Homo sapiens | |
2-(4-tert-butylphenyl)-5-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-1,3-oxazole-4-carbonitrile | - |
Homo sapiens | |
2-hydroxy-N'-[1H-indol-3-yl(oxo)acetyl]-2,2-diphenylacetohydrazide | - |
Homo sapiens | |
2-{[3-(4-chloro-5-hydroxy-2-methoxyphenyl)-4-oxo-3,4-dihydroquinazolin-2-yl]sulfanyl}-N-[(1S)-1-cyano-1,2-dimethylpropyl]acetamide | - |
Homo sapiens | |
4-[(4-[(E)-[(cyanoacetyl)hydrazono]methyl]phenoxy)methyl]benzoic acid | - |
Homo sapiens | |
methyl (2Z)-4-[4-(dimethylamino)phenyl]-4-oxo-2-[(phenylcarbonyl)hydrazono]butanoate | - |
Homo sapiens | |
methyl 4-[(E)-[[(3-[2-[(2-chlorobenzyl)oxy]phenyl]-1H-pyrazol-5-yl)carbonyl]hydrazono]methyl]benzoate | - |
Homo sapiens | |
N-(4-cyano-1-phenyl-1H-pyrazol-5-yl)-2-[(4-ethyl-5-thiophen-2-yl-4H-1,2,4-triazol-3-yl)sulfanyl]acetamide | - |
Homo sapiens | |
N-[(1R)-1-([2-[(1,3-benzoxazol-2-ylsulfanyl)acetyl]hydrazino]carbonyl)propyl]-2-[(phenylcarbonyl)amino]benzamide | - |
Homo sapiens | |
N-[2-(1-methylethyl)phenyl]-Na-(phenoxycarbonyl)-L-tryptophanamide | - |
Homo sapiens | |
N-[2-oxo-2-[(2Z)-2-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)hydrazino]ethyl]-2-pyridin-2-yl-1H-benzimidazole-1-carboxamide | - |
Homo sapiens | |
[2-[[(4-chlorophenyl)sulfanyl]methyl]-4-hydroxy-6,7-dimethoxyquinazolin-3(4H)-yl]acetonitrile | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
invariant chain + H2O | Homo sapiens | invariant chain li is degraded by CatS to the class II-associated invariant chain peptide which dissociates from the MHC-II molecule by forming a complex with the human leucocyte antigen-DM | ? | - |
? | |
additional information | Homo sapiens | in the case of atherosclerotic lesions, the local extracellular matrix is degraded either by CatS secreted by smooth muscle cells and macrophages or by circulating CatS produced by adipose tissue, this elastolytic activity of CatS causes the migration of blood monocytes and smooth muscle cells into the vascular wall which leads to the progression of atherosclerotic lesions | ? | - |
? | |
additional information | Homo sapiens | the cysteine protease cathepsin S is involved in the pathogenesis of autoimmune disorders, atherosclerosis and obesity | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
adipocyte | - |
Homo sapiens | - |
B-lymphocyte | - |
Homo sapiens | - |
dendritic cell | - |
Homo sapiens | - |
macrophage | - |
Homo sapiens | - |
smooth muscle | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
Cbz-Val-Val-Arg-7-amido-4-methylcoumarin + H2O | - |
Homo sapiens | Cbz-Val-Val-Arg + 7-amino-4-methylcoumarin | - |
? | |
invariant chain + H2O | invariant chain li is degraded by CatS to the class II-associated invariant chain peptide which dissociates from the MHC-II molecule by forming a complex with the human leucocyte antigen-DM | Homo sapiens | ? | - |
? | |
additional information | in the case of atherosclerotic lesions, the local extracellular matrix is degraded either by CatS secreted by smooth muscle cells and macrophages or by circulating CatS produced by adipose tissue, this elastolytic activity of CatS causes the migration of blood monocytes and smooth muscle cells into the vascular wall which leads to the progression of atherosclerotic lesions | Homo sapiens | ? | - |
? | |
additional information | the cysteine protease cathepsin S is involved in the pathogenesis of autoimmune disorders, atherosclerosis and obesity | Homo sapiens | ? | - |
? |
Subunits | Comment | Organism |
---|---|---|
monomer | enzyme has 217 amino acids, the structure of CatS is composed of 2 domains | Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
cathepsin S | - |
Homo sapiens |
CatS | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00278 | - |
methyl 4-[(E)-[[(3-[2-[(2-chlorobenzyl)oxy]phenyl]-1H-pyrazol-5-yl)carbonyl]hydrazono]methyl]benzoate | in 0.5 M MES, 2 mM DTT at pH 6.0 | Homo sapiens | |
0.00298 | - |
(3S)-N-[2-(1H-indol-3-yl)ethyl]-3-[[(4-methylphenyl)sulfonyl]amino]-2-oxo-4-phenylbutanamide | in 0.5 M MES, 2 mM DTT at pH 6.0 | Homo sapiens | |
0.00844 | - |
(2Z)-3-(4-[[5-(3,5-dimethylisoxazol-4-yl)-1,2,4-oxadiazol-3-yl]methoxy]phenyl)-2-(methylsulfonyl)prop-2-enenitrile | in 0.5 M MES, 2 mM DTT at pH 6.0 | Homo sapiens | |
0.00889 | - |
N-[(1R)-1-([2-[(1,3-benzoxazol-2-ylsulfanyl)acetyl]hydrazino]carbonyl)propyl]-2-[(phenylcarbonyl)amino]benzamide | in 0.5 M MES, 2 mM DTT at pH 6.0 | Homo sapiens | |
0.0109 | - |
2-[[3-(4-chloro-5-hydroxy-2-methoxyphenyl)-4-oxo-3,4-dihydroquinazolin-2-yl]sulfanyl]-N-[(1S)-1-cyano-1,2-dimethylpropyl]acetamide | in 0.5 M MES, 2 mM DTT at pH 6.0 | Homo sapiens | |
0.01458 | - |
2,2'-[[3-(trifluoromethyl)phenyl]imino]bis[N-(4-methylphenyl)acetamide] | in 0.5 M MES, 2 mM DTT at pH 6.0 | Homo sapiens | |
0.01527 | - |
N-[2-oxo-2-[(2Z)-2-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)hydrazino]ethyl]-2-pyridin-2-yl-1H-benzimidazole-1-carboxamide | in 0.5 M MES, 2 mM DTT at pH 6.0 | Homo sapiens | |
0.01663 | - |
methyl (2Z)-4-[4-(dimethylamino)phenyl]-4-oxo-2-[(phenylcarbonyl)hydrazono]butanoate | in 0.5 M MES, 2 mM DTT at pH 6.0 | Homo sapiens | |
0.01948 | - |
N-[2-(1-methylethyl)phenyl]-Na-(phenoxycarbonyl)-L-tryptophanamide | in 0.5 M MES, 2 mM DTT at pH 6.0 | Homo sapiens | |
0.02817 | - |
[2-[[(4-chlorophenyl)sulfanyl]methyl]-4-hydroxy-6,7-dimethoxyquinazolin-3(4H)-yl]acetonitrile | in 0.5 M MES, 2 mM DTT at pH 6.0 | Homo sapiens | |
0.05686 | - |
2-hydroxy-N'-[1H-indol-3-yl(oxo)acetyl]-2,2-diphenylacetohydrazide | in 0.5 M MES, 2 mM DTT at pH 6.0 | Homo sapiens | |
0.1982 | - |
N-(4-cyano-1-phenyl-1H-pyrazol-5-yl)-2-[(4-ethyl-5-thiophen-2-yl-4H-1,2,4-triazol-3-yl)sulfanyl]acetamide | in 0.5 M MES, 2 mM DTT at pH 6.0 | Homo sapiens | |
0.4377 | - |
1,1-bis(cyanomethyl)-3-[1-methyl-1-[3-(1-methylethenyl)phenyl]ethyl]urea | in 0.5 M MES, 2 mM DTT at pH 6.0 | Homo sapiens | |
3.39 | - |
4-[(4-[(E)-[(cyanoacetyl)hydrazono]methyl]phenoxy)methyl]benzoic acid | in 0.5 M MES, 2 mM DTT at pH 6.0 | Homo sapiens | |
146.3 | - |
2-(4-tert-butylphenyl)-5-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-1,3-oxazole-4-carbonitrile | in 0.5 M MES, 2 mM DTT at pH 6.0 | Homo sapiens |