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Literature summary for 3.4.21.20 extracted from

  • Sambrano, G.R.; Huang, W.; Faruqi, T.; Mahrus, S.; Craik, C.; Coughlin, S.R.
    Cathepsin G activates protease-activated receptor-4 in human platelets (2000), J. Biol. Chem., 275, 6819-6823.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
N-formylmethionyl-leucyl-phenylalanine induces release of enzyme from neutrophils Homo sapiens
platelet-activating factor induces release of enzyme from neutrophils Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
ecotin
-
Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ enzyme triggers calcium mobilization Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens enzyme causes platelet secretion and aggregation mediated by protease-activated receptor-4, i.e. PAR4, triggers calcium mobilization in PAR4-transfected fibroblasts, PAR4-expressing Xenopus oocytes, and washed human platelets, enzyme might mediate platelet-neutrophil interaction at sites of vascular injury or inflammation, regulation of enzyme activity on platelets and protease-activated receptors-1 and -4 ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
neutrophil azurophilic granule Homo sapiens
-
platelet
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Fibronectin + H2O hydrolysis after methionine, leucine, phenylalanine, lysine, or arginine residues Homo sapiens ?
-
?
Laminin + H2O hydrolysis after methionine, leucine, phenylalanine, lysine, or arginine residues Homo sapiens ?
-
?
additional information no activity with PAR1-mutant A2F and PAR4 mutant G1P Homo sapiens ?
-
?
additional information enzyme causes platelet secretion and aggregation mediated by protease-activated receptor-4, i.e. PAR4, triggers calcium mobilization in PAR4-transfected fibroblasts, PAR4-expressing Xenopus oocytes, and washed human platelets, enzyme might mediate platelet-neutrophil interaction at sites of vascular injury or inflammation, regulation of enzyme activity on platelets and protease-activated receptors-1 and -4 Homo sapiens ?
-
?
N-succinyl-Ala-Ala-Pro-Phe-thiobenzyl ester + H2O chromogenic substrate Homo sapiens ?
-
?
protease-activated receptor-1 + H2O i.e. PAR1, activation of platelets by hydrolysis of the receptor protein Homo sapiens ?
-
?
protease-activated receptor-4 + H2O i.e. PAR4, activation of platelets by hydrolysis of the receptor protein Homo sapiens ?
-
?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000000015
-
ecotin
-
Homo sapiens