Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.21.109 extracted from

  • Uhland, K.
    Matriptase and its putative role in cancer (2006), Cell. Mol. Life Sci., 63, 2968-2978.
    View publication on PubMed

Application

Application Comment Organism
drug development the enzyme is a potential target in anti-cancer therapy Homo sapiens

Protein Variants

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

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

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/ Products (Substrates)

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

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-

Posttranslational Modification

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

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 and Products (Substrate)

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 [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