Activating Compound | Comment | Organism | Structure |
---|---|---|---|
NaCl | the enzyme requires a physiological concentration of NaCl (150 mM) for optimal activity | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
expressed in Escherichia coli JM109 cells | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
F297A | the mutant shows no activity with kallidin or [Arg0]-Met-enkephalin | Homo sapiens |
F297Y | the mutation causes a significant decrease in hydrolytic activity toward synthetic and peptide substrates (13fold and 15fold lower catalytic efficiencies with L-Arg-7-amido-4-methylcoumarin and L-Lys-7-amido-4-methylcoumarin, respectively. No activity with kallidin or [Arg0]-Met-enkephalin) as well as chloride anion sensitivity | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
arphamenine A | - |
Homo sapiens | |
Arphamenine B | - |
Homo sapiens | |
bestatin | - |
Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.0529 | - |
L-Arg-7-amido-4-methylcoumarin | wild type enzyme, at pH 7.4 and 37°C | Homo sapiens | |
0.208 | - |
L-Arg-7-amido-4-methylcoumarin | mutant enzyme F297Y, at pH 7.4 and 37°C | Homo sapiens | |
0.323 | - |
L-Lys-7-amido-4-methylcoumarin | wild type enzyme, at pH 7.4 and 37°C | Homo sapiens | |
0.598 | - |
L-Lys-7-amido-4-methylcoumarin | mutant enzyme F297Y, at pH 7.4 and 37°C | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q9H4A4 | - |
- |
Purification (Comment) | Organism |
---|---|
DEAE Toyopearl column chromatography and TALON column chromatography | Homo sapiens |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
kallidin + H2O | i.e. KRPPGFSPFR | Homo sapiens | bradykinin + ? | - |
? | |
L-Ala-7-amido-4-methylcoumarin + H2O | about 2% activity compared to L-Arg-7-amido-4-methylcoumarin | Homo sapiens | L-Ala + 7-amino-4-methylcoumarin | - |
? | |
L-Arg-7-amido-4-methylcoumarin + H2O | 100% activity | Homo sapiens | L-Arg + 7-amino-4-methylcoumarin | - |
? | |
L-Gln-7-amido-4-methylcoumarin + H2O | about 1% activity compared to L-Arg-7-amido-4-methylcoumarin | Homo sapiens | L-Gln + 7-amino-4-methylcoumarin | - |
? | |
L-Ile-7-amido-4-methylcoumarin + H2O | about 1% activity compared to L-Arg-7-amido-4-methylcoumarin | Homo sapiens | L-Ile + 7-amino-4-methylcoumarin | - |
? | |
L-Leu-7-amido-4-methylcoumarin + H2O | about 1% activity compared to L-Arg-7-amido-4-methylcoumarin | Homo sapiens | L-Leu + 7-amino-4-methylcoumarin | - |
? | |
L-Lys-7-amido-4-methylcoumarin + H2O | about 45% activity compared to L-Arg-7-amido-4-methylcoumarin | Homo sapiens | L-Lys + 7-amino-4-methylcoumarin | - |
? | |
L-Met-7-amido-4-methylcoumarin + H2O | about 1% activity compared to L-Arg-7-amido-4-methylcoumarin | Homo sapiens | L-Met + 7-amino-4-methylcoumarin | - |
? | |
L-Phe-7-amido-4-methylcoumarin + H2O | about 5% activity compared to L-Arg-7-amido-4-methylcoumarin | Homo sapiens | L-Phe + 7-amino-4-methylcoumarin | - |
? | |
L-Tyr-7-amido-4-methylcoumarin + H2O | about 7% activity compared to L-Arg-7-amido-4-methylcoumarin | Homo sapiens | L-Tyr + 7-amino-4-methylcoumarin | - |
? | |
L-Val-7-amido-4-methylcoumarin + H2O | about 1% activity compared to L-Arg-7-amido-4-methylcoumarin | Homo sapiens | L-Val + 7-amino-4-methylcoumarin | - |
? | |
additional information | no activity with L-Cys-7-amido-4-methylcoumarin, L-Asp-7-amido-4-methylcoumarin, and L-Glu-7-amido-4-methylcoumarin | Homo sapiens | ? | - |
? | |
[Arg0]-Met-enkephalin + H2O | i.e. RYGGFM | Homo sapiens | Met-enkephalin + de-[Tyr]-Met-enkephalin | - |
? |
Subunits | Comment | Organism |
---|---|---|
? | x * 74000, SDS-PAGE | Homo sapiens |
Synonyms | Comment | Organism |
---|---|---|
APB | - |
Homo sapiens |
Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
1.56 | - |
L-Lys-7-amido-4-methylcoumarin | mutant enzyme F297Y, at pH 7.4 and 37°C | Homo sapiens | |
2.95 | - |
L-Arg-7-amido-4-methylcoumarin | mutant enzyme F297Y, at pH 7.4 and 37°C | Homo sapiens | |
9.64 | - |
L-Arg-7-amido-4-methylcoumarin | wild type enzyme, at pH 7.4 and 37°C | Homo sapiens | |
12.9 | - |
L-Lys-7-amido-4-methylcoumarin | wild type enzyme, at pH 7.4 and 37°C | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000007 | - |
wild type enzyme, at pH 7.4 and 37°C | Homo sapiens | Arphamenine B | |
0.00000382 | - |
wild type enzyme, at pH 7.4 and 37°C | Homo sapiens | bestatin | |
0.00000402 | - |
wild type enzyme, at pH 7.4 and 37°C | Homo sapiens | arphamenine A |
kcat/KM Value [1/mMs-1] | kcat/KM Value Maximum [1/mMs-1] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
2.61 | - |
L-Lys-7-amido-4-methylcoumarin | mutant enzyme F297Y, at pH 7.4 and 37°C | Homo sapiens | |
14.2 | - |
L-Arg-7-amido-4-methylcoumarin | mutant enzyme F297Y, at pH 7.4 and 37°C | Homo sapiens | |
39.9 | - |
L-Lys-7-amido-4-methylcoumarin | wild type enzyme, at pH 7.4 and 37°C | Homo sapiens | |
182 | - |
L-Arg-7-amido-4-methylcoumarin | wild type enzyme, at pH 7.4 and 37°C | Homo sapiens |