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Literature summary for 3.4.21.109 extracted from

  • Owen, K.A.; Qiu, D.; Alves, J.; Schumacher, A.M.; Kilpatrick, L.M.; Li, J.; Harris, J.L.; Ellis, V.
    Pericellular activation of hepatocyte growth factor by the transmembrane serine proteases matriptase and hepsin, but not by the membrane-associated protease uPA (2010), Biochem. J., 426, 219-228.
    View publication on PubMed
Search for more literature for 3.4.21.109

Cloned(Commentary)

Cloned (Comment) Organism
recombinant human matriptase protease domain is expressed in Escherichia coli and Saccharomyces cerevisiae Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
CJ-730 3-amidinophenylalanine-based inhibitor CJ-730, completely inhibits pro-HGF activation in PC3 cells Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
pro-HGF + H2O Homo sapiens matriptase is an efficient activator of hepatocyte growth factor ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
DU-145 cell expression determined by quantitative RT-PCR Homo sapiens
-
LNCaP cell expression determined by quantitative RT-PCR Homo sapiens
-
PC-3 cell expression determined by quantitative RT-PCR, highest expression among different prostate cancer cell lines Homo sapiens
-
PNT-1A cell expression determined by quantitative RT-PCR Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
pro-HGF + H2O matriptase is an efficient activator of hepatocyte growth factor Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
matriptase
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00004
-
 CJ-730 3-amidinophenylalanine-based inhibitor CJ-730 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5
-
 3-amidinophenylalanine-based inhibitor CJ-730: although CJ-730 completely inhibits pro-HGF activation in PC3 cells, the IC50 value is determined to be 100fold above the Ki value. This discrepancy suggests that the inhibitory effect is possibly due to non-specific inhibition of proteases other than matriptase Homo sapiens CJ-730

General Information

General Information Comment Organism
malfunction matriptase expression down-regulated with matriptase-targeting siRNA effectively abolishes pro-HGF activation Homo sapiens
physiological function matriptase efficiently activates hepatocyte growth factor Homo sapiens