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Literature summary for 3.4.22.26 extracted from

  • Kee, N.L.; Krause, J.; Blatch, G.L.; Muramoto, K.; Sakka, K.; Sakka, M.; Naude, R.J.; Wagner, L.; Wolf, R.; Rahfeld, J.U.; Demuth, H.U.; Mielicki, W.P.; Frost, C.L.
    The proteolytic profile of human cancer procoagulant suggests that it promotes cancer metastasis at the level of activation rather than degradation (2015), Protein J., 34, 338-348 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(NH4)2SO4 76% inhibition at about 40 mM Homo sapiens
benzamidine strong inhibition Homo sapiens
CaCl2 91% inhibition at about 40 mM Homo sapiens
EDTA low inhibition Homo sapiens
HgCl2 complete inhibition at about 40 mM Homo sapiens
MgCl2 81% inhibition at about 40 mM Homo sapiens
MgSO4 68% inhibition at about 40 mM Homo sapiens
additional information no or poor inhibition by iodoacetamide and E-64 Homo sapiens
NaCl 12-21% inhibition, respectively Homo sapiens
pepstatin A low inhibition Homo sapiens
Phenylmethylsulfonylfluoride strong inhibition Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.01182
-
tert-benzyloxycarbonyl-QVR-7-amido-4-methylcoumarin pH 7.4, 37°C Homo sapiens
0.2265
-
PQVR-7-amido-4-methylcoumarin pH 7.4, 37°C Homo sapiens
0.2675
-
QVR-7-amido-4-methylcoumarin pH 7.4, 37°C Homo sapiens
0.3463
-
QSPVR-7-amido-4-methylcoumarin pH 7.4, 37°C Homo sapiens
0.3933
-
LPAPR-7-amido-4-methylcoumarin pH 7.4, 37°C Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular
-
Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
inactive factor X + H2O Homo sapiens activation of blood coagulation factor X, degradation of factor X during 24 h active factor Xa + ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
native enzyme from human placental membranes Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
additional information tumor cell Homo sapiens
-
placental membrane
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7-methoxycoumarin-4-acetyl-GYPGQV + H2O
-
Homo sapiens 7-methoxycoumarin-4-acetate + GYPGQV
-
?
7-methoxycoumarin-4-acetyl-IVGGQE + H2O
-
Homo sapiens 7-methoxycoumarin-4-acetate + IVGGQE
-
?
7-methoxycoumarin-4-acetyl-SFLLRN + H2O
-
Homo sapiens 7-methoxycoumarin-4-acetate + SFLLRN
-
?
7-methoxycoumarin-4-acetyl-VSQKSP + H2O
-
Homo sapiens 7-methoxycoumarin-4-acetate + VSQKSP
-
?
7-methoxycoumarin-4-acetyl-VYQPQP + H2O
-
Homo sapiens 7-methoxycoumarin-4-acetate + VYQPQP
-
?
collagen type IV + H2O
-
Homo sapiens ?
-
?
Fibronectin + H2O enzyme CP cleaves fibronectin between Ala and Val residues, in regions rich in Pro and Gln residues. The 45 and 60 kDa fragments have the same N-terminal sequence, generated by cleavage of the bond between Ala292 and Val293 Homo sapiens ?
-
?
inactive factor X + H2O activation of blood coagulation factor X, degradation of factor X during 24 h Homo sapiens active factor Xa + ?
-
?
inactive factor X + H2O activation of blood coagulation factor X (57.3 kDa), cleavage of factor X at the conventional activation site, i.e. between Arg52 and Ile53, in the heavy chain Homo sapiens active factor Xa + ?
-
?
Laminin + H2O
-
Homo sapiens ?
-
?
LPAPR-7-amido-4-methylcoumarin + H2O
-
Homo sapiens LPAPR + 7-amino-4-methylcoumarin
-
?
additional information substrate specificity analysis, mass spectrometric detection of cleavage products. No activity with tert-benzyloxycarbonyl-QSPVR-7-amido-4-methylcoumarin and TLDPR-7-amido-4-methylcoumarin. Enzyme CP shows very little cysteine protease activity, it appears to exhibit mixed protease activity, but acts predominantly as a serine protease Homo sapiens ?
-
?
PQVR-7-amido-4-methylcoumarin + H2O
-
Homo sapiens PQVR + 7-amino-4-methylcoumarin
-
?
QSPVR-7-amido-4-methylcoumarin + H2O
-
Homo sapiens QSPVR + 7-amino-4-methylcoumarin
-
?
QVR-7-amido-4-methylcoumarin + H2O
-
Homo sapiens QVR + 7-amino-4-methylcoumarin
-
?
tert-butoxycarbonyl-QVR-7-amido-4-methylcoumarin + H2O best synthetic substrate Homo sapiens tert-butoxycarbonyl-QVR + 7-amino-4-methylcoumarin
-
?

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.989
-
tert-benzyloxycarbonyl-QVR-7-amido-4-methylcoumarin pH 7.4, 37°C Homo sapiens
1.147
-
QVR-7-amido-4-methylcoumarin pH 7.4, 37°C Homo sapiens
2.496
-
QSPVR-7-amido-4-methylcoumarin pH 7.4, 37°C Homo sapiens
3.942
-
LPAPR-7-amido-4-methylcoumarin pH 7.4, 37°C Homo sapiens
4.578
-
PQVR-7-amido-4-methylcoumarin pH 7.4, 37°C Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

General Information

General Information Comment Organism
physiological function cancer procoagulant (CP) is a protease present in malignant tumours, but not normal tissue, is a known activator of coagulation factor X (FX). degradation of FX by CP occurs at a much slower rate than degradation by conventional activators. Cancer procoagulant has a function in cancer progression. The enzyme is not essential for either cancer-associated blood coagulation or the degradation of extracellular matrix proteins. The protease may be required for the proteolytic activation of membrane receptors Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
4.288
-
QVR-7-amido-4-methylcoumarin pH 7.4, 37°C Homo sapiens
7.208
-
QSPVR-7-amido-4-methylcoumarin pH 7.4, 37°C Homo sapiens
10.02
-
LPAPR-7-amido-4-methylcoumarin pH 7.4, 37°C Homo sapiens
20.21
-
PQVR-7-amido-4-methylcoumarin pH 7.4, 37°C Homo sapiens
83.67
-
tert-benzyloxycarbonyl-QVR-7-amido-4-methylcoumarin pH 7.4, 37°C Homo sapiens