Application | Comment | Organism |
---|---|---|
drug development | uPA is a potential therapeutic target in a variety of pathological conditions, including cancer | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
expression of mutant enzymes in HEK-293T cells | Homo sapiens |
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 | 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 Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | kinetics | Mus musculus | |
additional information | - |
additional information | kinetics | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
plasminogen + H2O | Mus musculus | - |
plasmin + ? | - |
? | |
plasminogen + H2O | Homo sapiens | - |
plasmin + ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Mus musculus | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
commercial preparation | purified enzyme | Mus musculus | - |
commercial preparation | purified enzyme | Homo sapiens | - |
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 | 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 Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Mus musculus |
37 | - |
assay at | Homo sapiens |
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 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 |