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Literature summary extracted from
- Probing the substrate specificities of matriptase, matriptase-2, hepsin and DESC1 with internally quenched fluorescent peptides (2009), FEBS J., 276, 2213-2226.
Cloned(Commentary)
| EC Number | Cloned (Comment) | Organism |
|---|---|---|
| 3.4.21.106 | fragment containing amino acids 45-417 is expressed as a C-terminal His-tagged fusion protein in Drosophila S2 cells | Homo sapiens |
| 3.4.21.109 | amino acids 596-855 are expressed in Escherichia coli cells | Homo sapiens |
| 3.4.21.109 | for expression in Drosophila S2 cells | Homo sapiens |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 3.4.21.106 | 4-(2-aminoethyl)-benzenesulfonylfluoride hydrochloride | residual hepsin activity: 0% | Homo sapiens |  |
| 3.4.21.106 | 4-methylumbelliferyl p-guanidinobenzoate | irreversible inhibitor | Homo sapiens | |
| 3.4.21.106 | alpha1-Aantichymotrypsin | residual hepsin activity: 88% | Homo sapiens | |
| 3.4.21.106 | alpha1-antitrypsin | residual hepsin activity: 67% | Homo sapiens | |
| 3.4.21.106 | alpha2-antiplasmin | residual hepsin activity: 1% | Homo sapiens | |
| 3.4.21.106 | antithrombin III | residual hepsin activity: 0% | Homo sapiens | |
| 3.4.21.106 | Aprotinin | residual hepsin activity: 1% | Homo sapiens | |
| 3.4.21.106 | leupeptin | residual hepsin activity: 4% | Homo sapiens | |
| 3.4.21.106 | plasminogen activator inhibitor-1 | residual hepsin activity: 0% | Homo sapiens | |
| 3.4.21.106 | Soybean trypsin inhibitor | residual hepsin activity: 78% | Homo sapiens | |
| 3.4.21.109 | 4-(2-aminoethyl)-benzenesulfonylfluoride hydrochloride | AEBSF | Homo sapiens | |
| 3.4.21.109 | alpha2-antiplasmin | - |
Homo sapiens | |
| 3.4.21.109 | antithrombin III | - |
Homo sapiens | |
| 3.4.21.109 | Aprotinin | - |
Homo sapiens | |
| 3.4.21.109 | leupeptin | - |
Homo sapiens | |
| 3.4.21.109 | plasminogen activator inhibitor I | - |
Homo sapiens |
KM Value [mM]
| EC Number | KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 3.4.21.106 | 0.068 | - |
Abz-RQLRVVGGY(3-NO2) | - |
Homo sapiens | |
| 3.4.21.106 | 0.07 | - |
Abz-RQRRVVGGY(3-NO2) | - |
Homo sapiens | |
| 3.4.21.106 | 0.072 | - |
Abz-RRARVVGGY(3-NO2) | - |
Homo sapiens | |
| 3.4.21.106 | 0.085 | - |
Abz-RQRRALEKY(3-NO2) | peptide sequence from alphaEbeta7 integrin | Homo sapiens | |
| 3.4.21.106 | 0.109 | - |
Abz-RQYRVVGGY(3-NO2) | - |
Homo sapiens | |
| 3.4.21.106 | 0.114 | - |
Abz-KQSRKFVPY(3-NO2) | peptide sequence from trask | Homo sapiens | |
| 3.4.21.106 | 0.14 | - |
Abz-SKLRVVGGY(3-NO2) | peptide sequence from proMSP-1 | Homo sapiens | |
| 3.4.21.106 | 0.175 | - |
Abz-RQARYVGGY(3-NO2) | - |
Homo sapiens | |
| 3.4.21.106 | 0.189 | - |
Abz-RKRRGSRGY(3-NO2) | peptide sequence from filaggrin | Homo sapiens | |
| 3.4.21.106 | 0.191 | - |
Abz-RQARAVGGY(3-NO2) | - |
Homo sapiens | |
| 3.4.21.106 | 0.22 | - |
Abz-RAARVVGGY(3-NO2) | - |
Homo sapiens | |
| 3.4.21.106 | 0.29 | - |
Abz-RLARVVGGY(3-NO2) | - |
Homo sapiens | |
| 3.4.21.106 | 0.369 | - |
Abz-RQARVVGGY(3-NO2) | - |
Homo sapiens | |
| 3.4.21.106 | 0.369 | - |
Abz-RQARVVGGY(3-NO2) | peptide sequence from matriptase | Homo sapiens | |
| 3.4.21.106 | 0.373 | - |
Abz-SKGRSLIGY(3-NO2) | peptide sequence from PAR-2 | Homo sapiens | |
| 3.4.21.109 | 0.0033 | - |
RRARVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.012 | - |
RRARVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.018 | - |
RQARAVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.03 | - |
filaggrin | - |
Homo sapiens | |
| 3.4.21.109 | 0.046 | - |
filaggrin | - |
Homo sapiens | |
| 3.4.21.109 | 0.05 | - |
RQRRVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.05 | - |
RQYRVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.052 | - |
trask | - |
Homo sapiens | |
| 3.4.21.109 | 0.065 | - |
RQARQVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.07 | - |
trask | - |
Homo sapiens | |
| 3.4.21.109 | 0.088 | - |
RLARVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.1 | - |
alphaEbeta7 integrin | - |
Homo sapiens | |
| 3.4.21.109 | 0.104 | - |
matriptase | - |
Homo sapiens | |
| 3.4.21.109 | 0.104 | - |
RQARVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.111 | - |
alphaEbeta7 integrin | - |
Homo sapiens | |
| 3.4.21.109 | 0.124 | - |
RQLRVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.126 | - |
matriptase | - |
Homo sapiens | |
| 3.4.21.109 | 0.126 | - |
RQARVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.128 | - |
RQARAVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.137 | - |
RYARVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.142 | - |
protease-activated receptor-2 | - |
Homo sapiens | |
| 3.4.21.109 | 0.159 | - |
RAARVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.197 | - |
protease-activated receptor-2 | - |
Homo sapiens | |
| 3.4.21.109 | 0.869 | - |
RQARYVGG | - |
Homo sapiens | |
Molecular Weight [Da]
| EC Number | Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
|---|---|---|---|---|
| 3.4.21.106 | 30000 | - |
SDS-PAGE, autocatalytically processed form consisting of amino acids 163-417 | Homo sapiens |
| 3.4.21.106 | 45000 | - |
SDS-PAGE, molecular weight of used fragment containing amino acids 45-417 | Homo sapiens |
| 3.4.21.109 | 29000 | - |
amino acids 596-855, theoretical molecular mass | Homo sapiens |
| 3.4.21.109 | 84000 | - |
calculated molecular mass | Homo sapiens |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 3.4.21.106 | Homo sapiens | - |
- |
- |
| 3.4.21.109 | Homo sapiens | - |
- |
- |
Purification (Commentary)
| EC Number | Purification (Comment) | Organism |
|---|---|---|
| 3.4.21.106 | using HisTrap FF columns | Homo sapiens |
| 3.4.21.109 | - |
Homo sapiens |
| 3.4.21.109 | by immobilized metal-chelate affinity chromatography | Homo sapiens |
Source Tissue
| EC Number | Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|---|
| 3.4.21.106 | liver | hepsin is cloned from a liver cDNA | Homo sapiens | - |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.4.21.106 | Abz-KQSRKFVPY(3-NO2) + H2O | peptide sequence from trask | Homo sapiens | Abz-KQSR + KFVPY(3-NO2) | - |
? | |
| 3.4.21.106 | Abz-RAARVVGGY(3-NO2) + H2O | - |
Homo sapiens | Abz-RAAR + VVGGY(3-NO2) | - |
? | |
| 3.4.21.106 | Abz-RKRRGSRGY(3-NO2) + H2O | peptide sequence from filaggrin | Homo sapiens | Abz-RKRR + GSRGY(3-NO2) | - |
? | |
| 3.4.21.106 | Abz-RLARVVGGY(3-NO2) + H2O | - |
Homo sapiens | Abz-RLAR + VVGGY(3-NO2) | - |
? | |
| 3.4.21.106 | Abz-RQARAVGGY(3-NO2) + H2O | - |
Homo sapiens | Abz-RQAR + AVGGY(3-NO2) | - |
? | |
| 3.4.21.106 | Abz-RQARVVGGY(3-NO2) + H2O | - |
Homo sapiens | Abz-RQAR + VVGGY(3-NO2) | - |
? | |
| 3.4.21.106 | Abz-RQARVVGGY(3-NO2) + H2O | peptide sequence from matriptase | Homo sapiens | Abz-RQAR + VVGGY(3-NO2) | - |
? | |
| 3.4.21.106 | Abz-RQARYVGGY(3-NO2) + H2O | - |
Homo sapiens | Abz-RQAR + YVGGY(3-NO2) | - |
? | |
| 3.4.21.106 | Abz-RQLRVVGGY(3-NO2) + H2O | - |
Homo sapiens | Abz-RQLR + VVGGY(3-NO2) | - |
? | |
| 3.4.21.106 | Abz-RQRRALEKY(3-NO2) + H2O | peptide sequence from alphaEbeta7 integrin | Homo sapiens | Abz-RQRR + ALEKY(3-NO2) | - |
? | |
| 3.4.21.106 | Abz-RQRRVVGGY(3-NO2) + H2O | - |
Homo sapiens | Abz-RQRR + VVGGY(3-NO2) | - |
? | |
| 3.4.21.106 | Abz-RQYRVVGGY(3-NO2) + H2O | - |
Homo sapiens | Abz-RQYR + VVGGY(3-NO2) | - |
? | |
| 3.4.21.106 | Abz-RRARVVGGY(3-NO2) + H2O | - |
Homo sapiens | Abz-RRAR + VVGGY(3-NO2) | - |
? | |
| 3.4.21.106 | Abz-SKGRSLIGY(3-NO2) + H2O | peptide sequence from PAR-2 | Homo sapiens | Abz-SKGR + SLIGY(3-NO2) | - |
? | |
| 3.4.21.106 | Abz-SKLRVVGGY(3-NO2) + H2O | peptide sequence from proMSP-1 | Homo sapiens | Abz-SKLR + VVGGY(3-NO2) | - |
? | |
| 3.4.21.106 | Boc-Gln-Ala-Arg-AMC + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.21.106 | additional information | to study the substrate specificity of type II transmembrane serine proteases internally quenched fluorogenic peptide substrates are used based on the autoactivation sequence of matriptase (RQARVVGG). Positions P4, P3, P2 and P1 are substituted with nonpolar (Ala, Leu), aromatic (Tyr), acid (Glu) and basic (Arg) amino acids, whereas P1 is fixed to Arg. Hepsin shares similarities with matriptase and DESC1, but is markedly more permissive at P2 | Homo sapiens | ? | - |
? | |
| 3.4.21.109 | alphaEbeta7 integrin + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.21.109 | filaggrin + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.21.109 | matriptase + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.21.109 | protease-activated receptor-2 + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.4.21.109 | RAARVVGG + H2O | - |
Homo sapiens | RAAR + VVGG | - |
? | |
| 3.4.21.109 | RLARVVGG + H2O | - |
Homo sapiens | RLAR + VVGG | - |
? | |
| 3.4.21.109 | RQARAVGG + H2O | - |
Homo sapiens | RQAR + AVGG | - |
? | |
| 3.4.21.109 | RQARQVGG + H2O | - |
Homo sapiens | RQAR + QVGG | - |
? | |
| 3.4.21.109 | RQARVVGG + H2O | - |
Homo sapiens | RQAR + VVGG | - |
? | |
| 3.4.21.109 | RQARYVGG + H2O | - |
Homo sapiens | RQAR + YVGG | - |
? | |
| 3.4.21.109 | RQLRVVGG + H2O | - |
Homo sapiens | RQLR + VVGG | - |
? | |
| 3.4.21.109 | RQRRVVGG + H2O | - |
Homo sapiens | RQRR + VVGG | - |
? | |
| 3.4.21.109 | RQYRVVGG + H2O | - |
Homo sapiens | RQYR + VVGG | - |
? | |
| 3.4.21.109 | RRARVVGG + H2O | - |
Homo sapiens | RRAR + VVGG | - |
? | |
| 3.4.21.109 | RYARVVGG + H2O | - |
Homo sapiens | RYAR + VVGG | - |
? | |
| 3.4.21.109 | trask + H2O | - |
Homo sapiens | ? | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 3.4.21.106 | hepsin | - |
Homo sapiens |
| 3.4.21.109 | matriptase | - |
Homo sapiens |
| 3.4.21.109 | matriptase-2 | - |
Homo sapiens |
| 3.4.21.109 | type II transmembrane serine protease | - |
Homo sapiens |
Temperature Optimum [°C]
| EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|---|
| 3.4.21.106 | 37 | - |
assay at | Homo sapiens |
Turnover Number [1/s]
| EC Number | Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 3.4.21.106 | 0.5 | - |
Abz-RAARVVGGY(3-NO2) | - |
Homo sapiens | |
| 3.4.21.106 | 0.5 | - |
Abz-RRARVVGGY(3-NO2) | - |
Homo sapiens | |
| 3.4.21.106 | 0.5 | - |
Abz-RQARAVGGY(3-NO2) | - |
Homo sapiens | |
| 3.4.21.106 | 0.5 | - |
Abz-RQARYVGGY(3-NO2) | - |
Homo sapiens | |
| 3.4.21.106 | 0.6 | - |
Abz-RLARVVGGY(3-NO2) | - |
Homo sapiens | |
| 3.4.21.106 | 1.1 | - |
Abz-RQYRVVGGY(3-NO2) | - |
Homo sapiens | |
| 3.4.21.106 | 1.4 | - |
Abz-RQARVVGGY(3-NO2) | - |
Homo sapiens | |
| 3.4.21.106 | 1.4 | - |
Abz-RQRRVVGGY(3-NO2) | - |
Homo sapiens | |
| 3.4.21.106 | 1.4 | - |
Abz-RQARVVGGY(3-NO2) | peptide sequence from matriptase | Homo sapiens | |
| 3.4.21.106 | 1.5 | - |
Abz-RQLRVVGGY(3-NO2) | - |
Homo sapiens | |
| 3.4.21.106 | 12 | - |
Abz-KQSRKFVPY(3-NO2) | peptide sequence from trask | Homo sapiens | |
| 3.4.21.106 | 15 | - |
Abz-SKGRSLIGY(3-NO2) | peptide sequence from PAR-2 | Homo sapiens | |
| 3.4.21.106 | 16 | - |
Abz-SKLRVVGGY(3-NO2) | peptide sequence from proMSP-1 | Homo sapiens | |
| 3.4.21.106 | 39 | - |
Abz-RQRRALEKY(3-NO2) | peptide sequence from alphaEbeta7 integrin | Homo sapiens | |
| 3.4.21.106 | 66 | - |
Abz-RKRRGSRGY(3-NO2) | peptide sequence from filaggrin | Homo sapiens | |
| 3.4.21.109 | 0.3 | - |
RRARVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.3 | - |
RQARAVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.3 | - |
RAARVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.3 | - |
RLARVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.5 | - |
RQLRVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.6 | - |
RYARVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.7 | - |
RQYRVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.8 | - |
RQARQVGG | - |
Homo sapiens | |
| 3.4.21.109 | 0.9 | - |
RRARVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 1 | - |
matriptase | - |
Homo sapiens | |
| 3.4.21.109 | 1 | - |
RQARVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 1.5 | - |
matriptase | - |
Homo sapiens | |
| 3.4.21.109 | 1.5 | - |
RQARVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 2 | - |
RQARYVGG | - |
Homo sapiens | |
| 3.4.21.109 | 2.2 | - |
protease-activated receptor-2 | - |
Homo sapiens | |
| 3.4.21.109 | 5.5 | - |
RQARAVGG | - |
Homo sapiens | |
| 3.4.21.109 | 6.8 | - |
filaggrin | - |
Homo sapiens | |
| 3.4.21.109 | 7.2 | - |
trask | - |
Homo sapiens | |
| 3.4.21.109 | 7.2 | - |
alphaEbeta7 integrin | - |
Homo sapiens | |
| 3.4.21.109 | 26 | - |
RQRRVVGG | - |
Homo sapiens | |
| 3.4.21.109 | 32 | - |
filaggrin | - |
Homo sapiens | |
| 3.4.21.109 | 45 | - |
alphaEbeta7 integrin | - |
Homo sapiens | |
| 3.4.21.109 | 46 | - |
trask | - |
Homo sapiens | |
| 3.4.21.109 | 61 | - |
protease-activated receptor-2 | - |
Homo sapiens |
pH Optimum
| EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|---|
| 3.4.21.106 | 8.5 | - |
- |
Homo sapiens |
| 3.4.21.109 | 7.5 | - |
- |
Homo sapiens |
| 3.4.21.109 | 8.5 | - |
activity assay | Homo sapiens |
| 3.4.21.109 | 8.5 | - |
acivity assay | Homo sapiens |
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