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Literature summary for 3.4.21.73 extracted from
- A cyclic peptidylic inhibitor of murine urokinase-type plasminogen activator: changing species specificity by substitution of a single residue (2008), Biochem. J., 15, 447-457.
Application
| Application | Comment | Organism |
|---|---|---|
| drug development | uPA is a potential therapeutic target in a variety of pathological conditions, including cancer | Homo sapiens |
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expression of mutant enzymes in HEK-293T cells | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| H99Y | site-directed mutagenesis, the mutation exchanges the human residue H99 for the murine equivalent Y99, rendering the mutant enzyme susceptible for inhibition by the murine peptide sequence mupain-1, overview | Homo sapiens |
| H99Y/Q192K | site-directed mutagenesis, the mutations exchanges the human residues for the murine equivalents, rendering the mutant enzyme susceptible for inhibition by the murine peptide sequence mupain-1, overview | Homo sapiens |
| V41K/H99Y | site-directed mutagenesis, the mutations exchanges the human residues for the murine equivalents, rendering the mutant enzyme susceptible for inhibition by the murine peptide sequence mupain-1, overview | Homo sapiens |
| V41K/H99Y/Q192K | site-directed mutagenesis, the mutations exchanges the human residues for the murine equivalents, rendering the mutant enzyme susceptible for inhibition by the murine peptide sequence mupain-1, overview | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| additional information | phage-displayed peptide library screening for murine uPA-binding peptide sequences, overview | Mus musculus | |
| mupain-1 | i.e. CPAYSRYLDC, isolated from a murine peptide library and reconstructed, no inhibition of wild-type human enzyme, since the inhibitor is highly specific for the murine enzyme, but inhibition by the human enzyme mutant H99Y, overview, expression of mupain-1 peptide sequence in fusion with the N-terminal domains of the phage coat protein g3p in Escherichia coli | Homo sapiens |  |
| mupain-1 | i.e. CPAYSRYLDC, isolated from a murine peptide library and reconstructed, competitive and highly selective inhibitor, R6 of mupain-1 is the P1 residue, extended binding interaction including the P5, P3, P2, P1, and P1' residues of mupain-1 and the specificity pocket, the catalytic triad, and the amino acids 41, 99 and 192 located in and around the active site of murine uPA, overview, expression of mupain-1 peptide sequence in fusion with the two N-terminal domains of g3p, D1 and D2 in Escherichia coli | Mus musculus | |
KM Value [mM]
| KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | kinetics | Mus musculus | |
| additional information | - |
additional information | kinetics | Homo sapiens |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| plasminogen + H2O | Mus musculus | - |
plasmin + ? | - |
? | |
| plasminogen + H2O | Homo sapiens | - |
plasmin + ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Mus musculus | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| commercial preparation | purified enzyme | Mus musculus | - |
| commercial preparation | purified enzyme | Homo sapiens | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| plasminogen + H2O | - |
Mus musculus | plasmin + ? | - |
? | |
| plasminogen + H2O | - |
Homo sapiens | plasmin + ? | - |
? | |
| plasminogen + H2O | human Glu-plasminogen | Mus musculus | plasmin + ? | - |
? | |
| plasminogen + H2O | human Glu-plasminogen | Homo sapiens | plasmin + ? | - |
? | |
| S-2444 + H2O | chromogenic substrate | Mus musculus | pyroGlu-Gly-Arg + 4-nitroaniline | - |
? | |
| S-2444 + H2O | chromogenic substrate | Homo sapiens | pyroGlu-Gly-Arg + 4-nitroaniline | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| uPA | - |
Mus musculus |
| uPA | - |
Homo sapiens |
| Urokinase-type plasminogen activator | - |
Mus musculus |
| Urokinase-type plasminogen activator | - |
Homo sapiens |
Temperature Optimum [°C]
| Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|
| 37 | - |
assay at | Mus musculus |
| 37 | - |
assay at | Homo sapiens |
pH Optimum
| pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|
| 7.4 | - |
assay at | Mus musculus |
| 7.4 | - |
assay at | Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| additional information | - |
additional information | inhibition kinetics | Mus musculus | |
| additional information | - |
additional information | inhibition kinetics | Homo sapiens | |
| 0.0004 | - |
mupain-1 | pH 7.4, 37°C | Mus musculus | |
| 0.0036 | - |
mupain-1 | pH 7.4, 37°C, mutant V41K/H99Y/Q192K | Homo sapiens | |
| 0.0069 | - |
mupain-1 | pH 7.4, 37°C, mutant V41K/H99Y | Homo sapiens | |
| 0.0153 | - |
mupain-1 | pH 7.4, 37°C, mutant H99Y | Homo sapiens | |
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