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Literature summary for 3.4.21.73 extracted from
- Synthesis and activity of amides of tripeptides as potential urokinase inhibitors (2010), J. Enzyme Inhib. Med. Chem., 25, 139-142.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 2-phenethyl-SO2-D-Ser-Ala-Arg-al | is an irreversible urokinase inhibitor, and an alkylating agent forming a covalent adduct with an active site of the enzyme | Homo sapiens |  |
| D-Ser-Ala-Arg-NH-(CH2)5-NH2 | competitive inhibition | Homo sapiens | |
| D-Ser-Ala-Arg-NH-(CH2)7-NH2 | - |
Homo sapiens | |
| D-Ser-Ala-Arg-NH-(CH2)8-NH2 | - |
Homo sapiens | |
| D-Ser-Ala-Arg-NH-(CH2)9-NH2 | - |
Homo sapiens | |
| i-Boc-D-Ser-Ala-Arg-al | is an alkylating agent, and irreversibly inhibits urokinase by forming a covalent adduct with an active site of the enzyme | Homo sapiens | |
| additional information | synthesis and inhibitory potencies of d-Ser-Ala-Arg-NH-X peptides, overview. All compounds with a hydroxyl residue of an amide group do not inhibit urokinase, no inhibition by D-Ser-Ala-Arg-NH | Homo sapiens |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| plasminogen + H2O | Homo sapiens | - |
plasmin + ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| commercial preparation | - |
Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| plasminogen + H2O | - |
Homo sapiens | plasmin + ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Urokinase | - |
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 |
|---|---|---|---|
| 8.8 | - |
assay at | Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0063 | - |
D-Ser-Ala-Arg-NH-(CH2)5-NH2 | pH 8.8, 37°C | Homo sapiens | |
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Release 2023.1 (January 2023)
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