3.4.21.106: hepsin
This is an abbreviated version!
For detailed information about hepsin, go to the full flat file.
Word Map on EC 3.4.21.106
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3.4.21.106
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prostate
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matriptase
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medicine
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hai-1
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prostasin
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trypsin-like
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ttsps
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pro-hgf
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amacr
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tmprss3
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uromodulin
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biotechnology
- 3.4.21.106
- prostate
- matriptase
- medicine
- hai-1
- prostasin
-
trypsin-like
-
ttsps
- pro-hgf
- amacr
-
tmprss3
-
uromodulin
- biotechnology
Reaction
cleavage after basic amino-acid residues, with Arg strongly preferred to Lys =
Synonyms
hepsin, S01.224, TMPRSS1, transmembrane serine protease 1, type II transmembrane serine protease
ECTree
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Substrates Products
Substrates Products on EC 3.4.21.106 - hepsin
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REACTION DIAGRAM
Abz-KQSRKFVPY(3-NO2) + H2O
Abz-KQSR + KFVPY(3-NO2)
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peptide sequence from trask
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?
Abz-RKRRGSRGY(3-NO2) + H2O
Abz-RKRR + GSRGY(3-NO2)
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peptide sequence from filaggrin
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-
?
Abz-RQRRALEKY(3-NO2) + H2O
Abz-RQRR + ALEKY(3-NO2)
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peptide sequence from alphaEbeta7 integrin
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-
?
Abz-SKGRSLIGY(3-NO2) + H2O
Abz-SKGR + SLIGY(3-NO2)
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peptide sequence from PAR-2
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-
?
Abz-SKLRVVGGY(3-NO2) + H2O
Abz-SKLR + VVGGY(3-NO2)
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peptide sequence from proMSP-1
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?
acetyl-KQLR-7-amido-4-methylcoumarin + H2O
?
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most active tetrapeptide substrate
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?
acetyl-PVDR-7-amido-4-methylcoumarin + H2O
?
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least active tetrapeptide substrate
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?
Boc-QAR-7-amido-4-methylcoumarin + H2O
Boc-QAR + 7-amino-4-methylcoumarin
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-
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?
epidermal growth factor receptor + H2O
?
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hepsin cleavage of epidermal growth factor receptor is not dependent on receptor tyrosine phosphorylation
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?
L-Asp-L-Ala-L-Ala-L-Arg-4-nitroanilide + H2O
L-Asp-L-Ala-L-Ala-L-Arg + 4-nitroaniline
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-
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?
L-Asp-L-Lys-(gamma-Cbo)-L-Pro-L-Arg-4-nitroanilide + H2O
L-Asp-L-Lys-(gamma-Cbo)-L-Pro-L-Arg + 4-nitroaniline
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-
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?
laminin-332 + H2O
?
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by Western blotting and mass spectrometry, it is shown that hepsin cleaves the beta3 chain of rat Laminin-332. N-terminal sequencing identifies the cleavage site at beta3 Arg245, in a sequence context (SQLR245 cleavage LQGSCFC) conserved among species and in remarkable agreement with reported consensus target sequences for hepsin activity
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?
microsomal glutathione S-transferase 1 + H2O
active microsomal glutathione S-transferase
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hepsin seems to activate through microsomal glutathione S-transferase 1 dimer formation
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?
N-acetyl-KQLR-7-amido-4-methylcoumarin + H2O
N-acetyl-KQLR + 7-amino-4-methylcoumarin
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?
N-acetyl-L-Lys-L-Arg-L-Leu-L-Arg-7-amido-4-carbamoylmethylcoumarin + H2O
?
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?
N-benzyloxycarbonyl-Ala-Arg-Arg 4-methylcoumarin 7-amide + H2O
N-benzyloxycarbonyl-Ala-Arg-Arg + 7-amino-4-methylcoumarin
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weak substrate
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?
N-tert-butyloxycarbonyl-Gly-Lys-Arg 4-methylcoumarin 7-amide + H2O
N-tert-butyloxycarbonyl-Gly-Lys-Arg + 7-amino-4-methylcoumarin
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weak substrate
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?
pro-macrophage-stimulating protein + H2O
?
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the cleavage site is between Arg(483) and Val(484). At least 50% of the substrate is processed within 1 h at a hepsin concentration of 2.4 nM and at a molar enzyme to substrate ratio of 1:500
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?
pro-urokinase-type plasminogen activator + H2O
active high molecular weight urokinase-type plasminogen activator
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cleavage at the Lys158-Ile159 (P1-P1') peptide bond
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?
prostasin pro-peptide + H2O
prostasin
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hepsin activates prostasin, cleavage occurs at Arg44
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?
single-chain hepatocyte growth factor + H2O
two-chain hepatocyte growth factor
efficiently converted by soluble form of hepsin comprising the entire extracellular domain
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?
Suc-Leu-Leu-Val-Tyr-4-methylcoumaryl-7-amide + H2O
?
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2% active with the purifed enzyme
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?
t-butyloxycarbonyl-Ala-Gly-Pro-Arg-4-methylcoumaryl-7-amide + H2O
?
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12% active with the purifed enzyme
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?
t-butyloxycarbonyl-Gln-Ala-Arg-7-amido-4-methylcoumaryl-7-amide + H2O
t-butyloxycarbonyl-Gln-Ala-Arg + 7-amino-4-methylcoumarin
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?
t-butyloxycarbonyl-Gln-Arg-Arg-4-methylcoumaryl-7-amide + H2O
?
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100% active with the purifed enzyme
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?
t-butyloxycarbonyl-Gln-Gly-Arg-4-methylcoumaryl-7-amide + H2O
?
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58% active with the purifed enzyme
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?
t-butyloxycarbonyl-Glu-Ala-Arg-4-methylcoumaryl-7-amide + H2O
?
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41% active with the purifed enzyme
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?
t-butyloxycarbonyl-Glu-Lys-Lys-4-methylcoumaryl-7-amide + H2O
?
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8% active with the purifed enzyme
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?
t-butyloxycarbonyl-Gly-Lys-Arg-4-methylcoumaryl-7-amide + H2O
?
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25% active with the purifed enzyme
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?
t-butyloxycarbonyl-Leu-Lys-Arg-4-methylcoumaryl-7-amide + H2O
?
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19% active with the purifed enzyme
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?
t-butyloxycarbonyl-Leu-Ser-Thr-Arg-4-methylcoumaryl-7-amide + H2O
?
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13% active with the purifed enzyme
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?
t-butyloxycarbonyl-Val-Pro-Arg-4-methylcoumaryl-7-amide + H2O
?
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20% active with the purifed enzyme
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?
tert-butyloxycarbonyl-Gln-Ala-Arg 4-methylcoumarin 7-amide + H2O
tert-butyloxycarbonyl-Gln-Ala-Arg + 7-amino-4-methylcoumarin
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weak substrate
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?
tert-butyloxycarbonyl-Gln-Arg-Arg 4-methylcoumarin 7-amide + H2O
tert-butyloxycarbonyl-Gln-Arg-Arg + 7-amino-4-methylcoumarin
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?
tert-Butyloxycarbonyl-Val-Pro-Arg 4-methylcoumarin 7-amide + H2O
tert-Butyloxycarbonyl-Val-Pro-Arg + 7-amino-4-methylcoumarin
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weak substrate
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?
Z-Phe-Arg-4-methylcoumaryl-7-amide + H2O
?
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9% active with the purifed enzyme
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?
zymogen factor VII + H2O
factor VIIa
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cleaves between Arg152 and Ile153
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?
Abz-RQARVVGGY(3-NO2) + H2O
Abz-RQAR + VVGGY(3-NO2)
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peptide sequence from matriptase
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?
hepatocyte growth factor precursor + H2O
?
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potential substrate for hepsin in vivo
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?
hepatocyte growth factor precursor + H2O
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the catalytic domain of hepsin is a highly efficient activator (50% activation at 3.4 nM) of hepatocyte growth factor, the optimal P4-P1 substrate preference for hepsin sequence is Lys-Gln-Leu-Arg which exactly matches the activation sequence of hepatocyte growth factor precursor
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?
active hepatocyte growth factor
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hepsin-mediated pro-HGF activation may be critical in the pathogenesis of human prostate cancer
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?
additional information
?
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enzyme does not cleave factor VII R152E mutant
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?
additional information
?
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hepsin reduces cell growth, cell invation and soft agar colony formation after expression in PC-3, LNCaP and DU145 cells
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?
additional information
?
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P1-P4 substrate specificity, hepsin exhibits strong preference at the P1 position for arginine over lysine, favours theonine, leucine or asparagine at the P2, glutamine or lysine at the P3, and proline or lysine at the P4 position
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?
additional information
?
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does not cleave pro-tissue-type plasminogen activator
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?
additional information
?
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hepsin exhibits trypsin-like catalytic activity that favores Arg at the P1, Thr/Leu/Asn at the P2, Gln/Lys at the P3, and Pro/Lys at the P4 positions
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?
additional information
?
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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
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?
additional information
?
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cleaves after basic amino acid residues, Arg being preferable to Lys
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?
additional information
?
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hepsin stimulates disulfide-linked microsomal glutathione transferase 1 dimer formation resulting in activation of microsomal glutathione transferase 1 and preferential degradation of microsomal glutathione transferase 1 dimer
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?