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Literature summary for 3.4.22.26 extracted from
- In vitro screening of synthetic fluorogenic substrates for detection of cancer procoagulant activity (2018), Protein J., 37, 151-163 .
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | Michaelis-Menten kinetics, Km calculated using different plots, kinetic analysis, overview | Rattus norvegicus |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Ca2+ | required for activity, activates | Rattus norvegicus |  |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| inactive factor X + H2O | Rattus norvegicus | activation of blood coagulation factor X | active factor Xa + ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Rattus norvegicus | - |
- |
- |
Purification (Commentary)
| Purification (Comment) | Organism |
|---|---|
| native enzyme from human amnion-chorion membranes by two steps of anion exchange chromatography and lyophilisation | Rattus norvegicus |
Specific Activity [micromol/min/mg]
| Specific Activity Minimum [µmol/min/mg] | Specific Activity Maximum [µmol/min/mg] | Comment | Organism |
|---|---|---|---|
| 0.16 | - |
substrate GDR-7-amido-4-methylcoumarin, pH and temperature not specified in the publication | Rattus norvegicus |
| 0.65 | - |
substrate PQPQYVA-7-amido-4-methylcoumarin, pH and temperature not specified in the publication | Rattus norvegicus |
| 0.98 | - |
substrate tert-benzyloxycarbonyl-PKSQSVA-7-amido-4-methylcoumarin, pH and temperature not specified in the publication | Rattus norvegicus |
| 1.47 | - |
substrate PKSQSVA-7-amido-4-methylcoumarin, pH and temperature not specified in the publication | Rattus norvegicus |
| 1.63 | - |
substrate tert-benzyloxycarbonyl-PQPQYVA-7-amido-4-methylcoumarin, pH and temperature not specified in the publication | Rattus norvegicus |
| 1.95 | - |
substrate tert-benzyloxycarbonyl-RGD-7-amido-4-methylcoumarin, pH and temperature not specified in the publication | Rattus norvegicus |
| 2.93 | - |
substrate AVSQSKP-7-amido-4-methylcoumarin, pH and temperature not specified in the publication | Rattus norvegicus |
| 3.09 | - |
substrate PQVR-7-amido-4-methylcoumarin, pH and temperature not specified in the publication | Rattus norvegicus |
| 6.67 | - |
substrate tert-benzyloxycarbonyl-GDR-7-amido-4-methylcoumarin, pH and temperature not specified in the publication | Rattus norvegicus |
| 9.44 | - |
substrate AVYQPQP-7-amido-4-methylcoumarin, pH and temperature not specified in the publication | Rattus norvegicus |
| 17.58 | - |
substrate RGD-7-amido-4-methylcoumarin, pH and temperature not specified in the publication | Rattus norvegicus |
| 66.91 | - |
substrate tert-benzyloxycarbonyl-AVYQPQP-7-amido-4-methylcoumarin, pH and temperature not specified in the publication | Rattus norvegicus |
| 99.79 | - |
substrate tert-benzyloxycarbonyl-QVR-7-amido-4-methylcoumarin, pH and temperature not specified in the publication | Rattus norvegicus |
| 163.28 | - |
substrate tert-benzyloxycarbonyl-AVR-7-amido-4-methylcoumarin, pH and temperature not specified in the publication | Rattus norvegicus |
| 332.25 | - |
substrate tert-benzyloxycarbonyl-PQVR-7-amido-4-methylcoumarin, pH and temperature not specified in the publication | Rattus norvegicus |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| AVSQSKP-7-amido-4-methylcoumarin + H2O | low activity | Rattus norvegicus | AVSQSKP + 7-amino-4-methylcoumarin | - |
? | |
| AVYQPQP-7-amido-4-methylcoumarin + H2O | low activity | Rattus norvegicus | AVYQPQP + 7-amino-4-methylcoumarin | - |
? | |
| GDR-7-amido-4-methylcoumarin + H2O | low activity | Rattus norvegicus | GDR + 7-amino-4-methylcoumarin | - |
? | |
| inactive factor X + H2O | activation of blood coagulation factor X | Rattus norvegicus | active factor Xa + ? | - |
? | |
| additional information | in vitro screening of synthetic fluorogenic substrates for detection of cancer procoagulant activity, substrate design, synthesis, and evaluation, e.g. based on the RGD motif of fibronectin, overview. The most reliable assay for the quantification of cancer procoagulant activity is the three-stage chromogenic assay which utilises the ability of cancer procoagulant to activate factor X. In this assay, the activation of factor X leads to the formation of activated thrombin from prothrombin and the eventual hydrolyses of a thrombin chromogenic substrate which contains a p nitroaniline leaving group. No activity with tert-benzyloxycarbonyl-AVSQSKP-7-amido-4-methylcoumarin | Rattus norvegicus | ? | - |
? | |
| PKSQSVA-7-amido-4-methylcoumarin + H2O | low activity | Rattus norvegicus | PKSQSVA + 7-amino-4-methylcoumarin | - |
? | |
| PQPQYVA-7-amido-4-methylcoumarin + H2O | low activity | Rattus norvegicus | PQPQYVA + 7-amino-4-methylcoumarin | - |
? | |
| PQVR-7-amido-4-methylcoumarin + H2O | - |
Rattus norvegicus | PQVR + 7-amino-4-methylcoumarin | - |
? | |
| RGD-7-amido-4-methylcoumarin + H2O | low activity | Rattus norvegicus | RGD + 7-amino-4-methylcoumarin | - |
? | |
| tert-butoxycarbonyl-AVR-7-amido-4-methylcoumarin + H2O | high activity | Rattus norvegicus | tert-butoxycarbonyl-AVR + 7-amino-4-methylcoumarin | - |
? | |
| tert-butoxycarbonyl-AVYQPQP-7-amido-4-methylcoumarin + H2O | high activity | Rattus norvegicus | tert-butoxycarbonyl-AVYQPQP + 7-amino-4-methylcoumarin | - |
? | |
| tert-butoxycarbonyl-GDR-7-amido-4-methylcoumarin + H2O | - |
Rattus norvegicus | tert-butoxycarbonyl-GDR + 7-amino-4-methylcoumarin | - |
? | |
| tert-butoxycarbonyl-PKSQSVA-7-amido-4-methylcoumarin + H2O | low activity | Rattus norvegicus | tert-butoxycarbonyl-PKSQSVA + 7-amino-4-methylcoumarin | - |
? | |
| tert-butoxycarbonyl-PQPQYVA-7-amido-4-methylcoumarin + H2O | - |
Rattus norvegicus | tert-butoxycarbonyl-PQPQYVA + 7-amino-4-methylcoumarin | - |
? | |
| tert-butoxycarbonyl-PQVR-7-amido-4-methylcoumarin + H2O | best substrate, this substrate is also cleaved by collagenase | Rattus norvegicus | tert-butoxycarbonyl-PQVR + 7-amino-4-methylcoumarin | - |
? | |
| tert-butoxycarbonyl-QVR-7-amido-4-methylcoumarin + H2O | high activity | Rattus norvegicus | tert-butoxycarbonyl-QVR + 7-amino-4-methylcoumarin | - |
? | |
| tert-butoxycarbonyl-RGD-7-amido-4-methylcoumarin + H2O | - |
Rattus norvegicus | tert-butoxycarbonyl-RGD + 7-amino-4-methylcoumarin | - |
? | |
Subunits
| Subunits | Comment | Organism |
|---|---|---|
| ? | x * 68000, SDS-PAGE | Rattus norvegicus |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7 | - |
optimum pH 8.0 with substrate tert-benzyloxycarbonyl-QVR-7-amido-4-methylcoumarin | Rattus norvegicus |
| 8 | - |
optimum pH 8.0 with substrate PQVR-7-amido-4-methylcoumarin | Rattus norvegicus |
General Information
| General Information | Comment | Organism |
|---|---|---|
| physiological function | cancer procoagulant is a direct activator of coagulation factor X, itt is among one of the tumour cell products or activities which may promote fibrin formation and is suggested to be selectively associated with the malignant phenotype | Rattus norvegicus |
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Release 2023.1 (January 2023)
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