Application | Comment | Organism |
---|---|---|
drug development | the enzyme is a potential target in anti-cancer therapy | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
additional information | enzyme overexpressions and clinical outcome, overview | Homo sapiens |
additional information | matriptase depletion results in postnatal death of the mice due to dehydration which is caused by a lack of epithelial barrier function in the skin of newborns, these matriptase knockout mice also have abnormal hair follicle development and disturbed thymic homeostasis showing increased lymphocyte apoptosis in the thymuses and profilaggrin accumulation in epidermal tissue, transgenic mice with increased expression of matriptase in the epidermis show induction of spontaneous squamous cell carcinomas and strongly potentiated chemical skin carcinogenesis, possibly through activation of the tumor-promoting PI3K-Akt pathway, while double transgenic mice co-expressing matriptase and its cognate inhibitor HAI-1 do not develop spontaneous skin cancers and do not show increased susceptibility to chemical carcinogenesis | Mus musculus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
3-[(2R)-3-[4-(2-carbamimidamidoethyl)piperidin-1-yl]-2-[(naphthalen-2-ylsulfonyl)amino]propyl]benzenecarboximidamide | - |
Homo sapiens | |
hepatocyte growth factor activator inhibitor-1 | HAI-1 | Homo sapiens | |
hepatocyte growth factor activator inhibitor-1 | HAI-1, the cognate matriptase inhibitor is able to compensate for the effect of augmented matriptase activity, providing a rationale for the inhibition of matriptase to prevent tumor growth in vivo | Mus musculus | |
N-(3-[[(1R)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)ethyl]sulfamoyl]phenyl)-beta-alaninamide | - |
Homo sapiens | |
sulfonylated 3-amidino-phenylalanine inhibitors | - |
Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
cell surface | the catalytic domain of matriptase is located in the extracellular space | Mus musculus | 9986 | - |
cell surface | the catalytic domain of matriptase is located in the extracellular space | Homo sapiens | 9986 | - |
plasma membrane | matriptase is a type II transmembrane trypsin-like serine protease | Mus musculus | 5886 | - |
plasma membrane | matriptase is a type II transmembrane trypsin-like serine protease | Homo sapiens | 5886 | - |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
collagen type IV + H2O | Mus musculus | involved in ECM degradation/remodeling | ? | - |
? | |
collagen type IV + H2O | Homo sapiens | involved in ECM degradation/remodeling | ? | - |
? | |
Fibronectin + H2O | Mus musculus | involved in adhesion and migration/invasiveness | ? | - |
? | |
Fibronectin + H2O | Homo sapiens | involved in adhesion and migration/invasiveness | ? | - |
? | |
Gelatin + H2O | Mus musculus | involved in ECM degradation/remodeling | ? | - |
? | |
Gelatin + H2O | Homo sapiens | involved in ECM degradation/remodeling | ? | - |
? | |
hepatocyte growth factor/scatter factor + H2O | Mus musculus | seven proteases are involved in the activation of HGF/SF, involved in cell proliferation and adhesion, ECM degradation/remodeling, and migration/invasiveness, overview | activated hepatocyte growth factor/scatter factor + ? | - |
? | |
hepatocyte growth factor/scatter factor + H2O | Homo sapiens | seven proteases are involved in the activation of HGF/SF, involved in cell proliferation and adhesion, ECM degradation/remodeling, and migration/invasiveness, overview | activated hepatocyte growth factor/scatter factor + ? | - |
? | |
IGFBP-rP1 + H2O | Mus musculus | involved in involved in cell proliferation and adhesion | ? | - |
? | |
IGFBP-rP1 + H2O | Homo sapiens | involved in involved in cell proliferation and adhesion | ? | - |
? | |
Laminin + H2O | Mus musculus | involved in adhesion and migration/invasiveness | ? | - |
? | |
Laminin + H2O | Homo sapiens | involved in adhesion and migration/invasiveness | ? | - |
? | |
additional information | Homo sapiens | enzyme regulation and deregulation in cancer, overview, matriptase is involved in cancer initiation and progression, it not only facilitates cellular invasiveness but may also activate oncogenic pathways, overview | ? | - |
? | |
additional information | Mus musculus | enzyme regulation and deregulation in cancer, overview, matriptase is involved in cancer initiation and progression, it not only facilitates cellular invasiveness but may also activate oncogenic pathways, the protease is essential for postnatal survival, matriptase has pleiotropic functions in the development of the epidermis, hair follicles, and cellular immune system, the protease is essential for postnatal survival, overview | ? | - |
? | |
PAR-2 + H2O | Mus musculus | involved in involved in cell adhesion | ? | - |
? | |
PAR-2 + H2O | Homo sapiens | involved in involved in cell adhesion | ? | - |
? | |
pro-urokinase plasminogen activator + H2O | Mus musculus | activation at the cell surface, where uPA and matriptase co-localize, involved in cell proliferation and adhesion, ECM degradation/remodeling, and migration/invasiveness | urokinase plasminogen activator + propeptide of urokinase plasminogen activator | - |
? | |
pro-urokinase plasminogen activator + H2O | Homo sapiens | activation at the cell surface, where uPA and matriptase co-localize, involved in cell proliferation and adhesion, ECM degradation/remodeling, and migration/invasiveness | urokinase plasminogen activator + propeptide of urokinase plasminogen activator | - |
? | |
profilaggrin + H2O | Mus musculus | involved in terminal epithelial cell differentiation, mechanism of enzyme access for direct cleavage in vivo, overview | filaggrin + propeptide of filaggrin | - |
? | |
profilaggrin + H2O | Homo sapiens | involved in terminal epithelial cell differentiation, mechanism of enzyme access for direct cleavage in vivo, overview | filaggrin + propeptide of filaggrin | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Mus musculus | - |
- |
- |
Posttranslational Modification | Comment | Organism |
---|---|---|
proteolytic modification | matriptase is activated by cleavage at the activation sequence RQAR-/-V | Mus musculus |
proteolytic modification | matriptase is activated by cleavage at the activation sequence RQAR-/-V | Homo sapiens |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
carcinoma cell | high enzyme expression level | Mus musculus | - |
carcinoma cell | high enzyme expression level | Homo sapiens | - |
epithelial cell | - |
Mus musculus | - |
epithelial cell | - |
Homo sapiens | - |
keratinocyte | - |
Mus musculus | - |
keratinocyte | - |
Homo sapiens | - |
PC-3 cell | - |
Homo sapiens | - |
skin | - |
Mus musculus | - |
skin | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
collagen type IV + H2O | - |
Mus musculus | ? | - |
? | |
collagen type IV + H2O | - |
Homo sapiens | ? | - |
? | |
collagen type IV + H2O | involved in ECM degradation/remodeling | Mus musculus | ? | - |
? | |
collagen type IV + H2O | involved in ECM degradation/remodeling | Homo sapiens | ? | - |
? | |
Fibronectin + H2O | - |
Mus musculus | ? | - |
? | |
Fibronectin + H2O | - |
Homo sapiens | ? | - |
? | |
Fibronectin + H2O | involved in adhesion and migration/invasiveness | Mus musculus | ? | - |
? | |
Fibronectin + H2O | involved in adhesion and migration/invasiveness | Homo sapiens | ? | - |
? | |
Gelatin + H2O | - |
Mus musculus | ? | - |
? | |
Gelatin + H2O | - |
Homo sapiens | ? | - |
? | |
Gelatin + H2O | involved in ECM degradation/remodeling | Mus musculus | ? | - |
? | |
Gelatin + H2O | involved in ECM degradation/remodeling | Homo sapiens | ? | - |
? | |
hepatocyte growth factor/scatter factor + H2O | - |
Mus musculus | activated hepatocyte growth factor/scatter factor + ? | - |
? | |
hepatocyte growth factor/scatter factor + H2O | - |
Homo sapiens | activated hepatocyte growth factor/scatter factor + ? | - |
? | |
hepatocyte growth factor/scatter factor + H2O | seven proteases are involved in the activation of HGF/SF, involved in cell proliferation and adhesion, ECM degradation/remodeling, and migration/invasiveness, overview | Mus musculus | activated hepatocyte growth factor/scatter factor + ? | - |
? | |
hepatocyte growth factor/scatter factor + H2O | seven proteases are involved in the activation of HGF/SF, involved in cell proliferation and adhesion, ECM degradation/remodeling, and migration/invasiveness, overview | Homo sapiens | activated hepatocyte growth factor/scatter factor + ? | - |
? | |
IGFBP-rP1 + H2O | - |
Mus musculus | ? | - |
? | |
IGFBP-rP1 + H2O | - |
Homo sapiens | ? | - |
? | |
IGFBP-rP1 + H2O | involved in involved in cell proliferation and adhesion | Mus musculus | ? | - |
? | |
IGFBP-rP1 + H2O | involved in involved in cell proliferation and adhesion | Homo sapiens | ? | - |
? | |
Laminin + H2O | - |
Mus musculus | ? | - |
? | |
Laminin + H2O | - |
Homo sapiens | ? | - |
? | |
Laminin + H2O | involved in adhesion and migration/invasiveness | Mus musculus | ? | - |
? | |
Laminin + H2O | involved in adhesion and migration/invasiveness | Homo sapiens | ? | - |
? | |
additional information | enzyme regulation and deregulation in cancer, overview, matriptase is involved in cancer initiation and progression, it not only facilitates cellular invasiveness but may also activate oncogenic pathways, overview | Homo sapiens | ? | - |
? | |
additional information | enzyme regulation and deregulation in cancer, overview, matriptase is involved in cancer initiation and progression, it not only facilitates cellular invasiveness but may also activate oncogenic pathways, the protease is essential for postnatal survival, matriptase has pleiotropic functions in the development of the epidermis, hair follicles, and cellular immune system, the protease is essential for postnatal survival, overview | Mus musculus | ? | - |
? | |
additional information | R/KXSR-/-A is the cleavage sequence of matriptase | Mus musculus | ? | - |
? | |
additional information | R/KXSR-/-A is the cleavage sequence of matriptase | Homo sapiens | ? | - |
? | |
PAR-2 + H2O | - |
Mus musculus | ? | - |
? | |
PAR-2 + H2O | - |
Homo sapiens | ? | - |
? | |
PAR-2 + H2O | involved in involved in cell adhesion | Mus musculus | ? | - |
? | |
PAR-2 + H2O | involved in involved in cell adhesion | Homo sapiens | ? | - |
? | |
pro-urokinase plasminogen activator + H2O | - |
Mus musculus | urokinase plasminogen activator + propeptide of urokinase plasminogen activator | - |
? | |
pro-urokinase plasminogen activator + H2O | - |
Homo sapiens | urokinase plasminogen activator + propeptide of urokinase plasminogen activator | - |
? | |
pro-urokinase plasminogen activator + H2O | activation at the cell surface, where uPA and matriptase co-localize, involved in cell proliferation and adhesion, ECM degradation/remodeling, and migration/invasiveness | Mus musculus | urokinase plasminogen activator + propeptide of urokinase plasminogen activator | - |
? | |
pro-urokinase plasminogen activator + H2O | activation at the cell surface, where uPA and matriptase co-localize, involved in cell proliferation and adhesion, ECM degradation/remodeling, and migration/invasiveness | Homo sapiens | urokinase plasminogen activator + propeptide of urokinase plasminogen activator | - |
? | |
profilaggrin + H2O | - |
Mus musculus | filaggrin + propeptide of filaggrin | - |
? | |
profilaggrin + H2O | - |
Homo sapiens | filaggrin + propeptide of filaggrin | - |
? | |
profilaggrin + H2O | involved in terminal epithelial cell differentiation, mechanism of enzyme access for direct cleavage in vivo, overview | Mus musculus | filaggrin + propeptide of filaggrin | - |
? | |
profilaggrin + H2O | involved in terminal epithelial cell differentiation, mechanism of enzyme access for direct cleavage in vivo, overview | Homo sapiens | filaggrin + propeptide of filaggrin | - |
? |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0000067 | - |
N-(3-[[(1R)-2-[4-(2-aminoethyl)piperidin-1-yl]-1-(3-carbamimidoylbenzyl)ethyl]sulfamoyl]phenyl)-beta-alaninamide | - |
Homo sapiens | |
0.0000067 | 0.000046 | sulfonylated 3-amidino-phenylalanines | - |
Homo sapiens | |
0.000046 | - |
3-[(2R)-3-[4-(2-carbamimidamidoethyl)piperidin-1-yl]-2-[(naphthalen-2-ylsulfonyl)amino]propyl]benzenecarboximidamide | - |
Homo sapiens |