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Literature summary for 3.2.1.166 extracted from
- Mechanisms of heparanase inhibition by the heparan sulfate mimetic PG545 and three structural analogues (2013), FEBS Open Bio, 3, 346-351.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| recombinant expression in insect cells | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| PG545 | a heparan sulfate mimetic tetrasaccharide, competitive inhibition | Homo sapiens |  |
| PG545 cholestanol aglycon | the cholestanol aglycon of PG545 significantly increased affinity for heparanase and also modified the inhibition mode, parabolic competition | Homo sapiens | |
| PG545 trisaccharide derivative | - |
Homo sapiens | |
| sulfated PG545 | competitive inhibition | Homo sapiens | |
| sulfated trisaccharide from PG545 | partial competitive inhibition | Homo sapiens | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | Michaelis-Menten kinetics | Homo sapiens | |
| 0.0036 | - |
fondaparinux | pH 5.0, 37°C | Homo sapiens | |
| 0.0124 | - |
sulfated PG545 | pH 5.0, 37°C | Homo sapiens | |
| 0.197 | - |
sulfated trisaccharide from PG545 | pH 5.0, 37°C | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| fondaparinux + H2O | - |
Homo sapiens | ? | - |
? | |
| sulfated PG545 + H2O | - |
Homo sapiens | ? | - |
? | |
| sulfated trisaccharide from PG545 + H2O | - |
Homo sapiens | ? | - |
? | |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 5 | - |
assay at | Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.00444 | - |
PG545 | pH 5.0, 37°C | Homo sapiens | |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.012 | - |
pH 5.0, 37°C | Homo sapiens | PG545 | |
| 0.416 | - |
pH 5.0, 37°C | Homo sapiens | sulfated PG545 | |
| 4.82 | - |
pH 5.0, 37°C | Homo sapiens | sulfated trisaccharide from PG545 | |
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