BRENDA - Enzyme Database
show all sequences of 3.4.21.B12

Characterization of hK4 (prostase), a prostate-specific serine protease: activation of the precursor of prostate specific antigen (pro-PSA) and single-chain urokinase-type plasminogen activator and degradation of prostatic acid phosphatase

Takayama, T.K.; McMullen, B.A.; Nelson, P.S.; Matsumura, M.; Fujikawa, K.; Biochemistry 40, 15341-15348 (2001)

Data extracted from this reference:

Cloned(Commentary)
Cloned (Commentary)
Organism
construction of a chimeric enzyme with exchange of the pro-piece of the zymogen for that of prostate-specific antigen PSA to create an activation site suceptible for trypsin-type proteases, expression in Escherichia coli strain BL21(DE3)
Homo sapiens
Inhibitors
Inhibitors
Commentary
Organism
Structure
Aprotinin
complex formation with the self-activated recombinant, chimeric enzyme
Homo sapiens
benzamidine
93% inhibition at 10 mM
Homo sapiens
Nalpha-p-tosyl-L-lysine chloromethyl ketone
85% inhibition at 1 mM; i.e. TLCK
Homo sapiens
Soybean trypsin inhibitor
99% inhibition at 1 mg/ml
Homo sapiens
Molecular Weight [Da]
Molecular Weight [Da]
Molecular Weight Maximum [Da]
Commentary
Organism
21000
-
x * 21000, self-activated recombinant, chimeric enzyme, SDS-PAGE
Homo sapiens
Natural Substrates/ Products (Substrates)
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
ID
52 kDa prostatic acid phosphatase + H2O
Homo sapiens
enzyme may be involved in the physiological clearance of prostatic acid phosphatase
33 kDa prostatic acid phosphatase + 19 kDa fragment
-
Homo sapiens
?
polypeptide + H2O
Homo sapiens
enzyme plays a role in the physiologic processing of seminal plasma proteins , e.g. pro-PSA, as well as in the pathogenesis of prostate cancer through the activation of pro-PSA
peptides
-
Homo sapiens
?
pro-prostate-specific antigen + H2O
Homo sapiens
i.e. PSA
activated prostate-specific antigen
-
Homo sapiens
?
pro-prostate-specific antigen + H2O
Homo sapiens
activation of PSA
activated prostate-specific antigen
-
Homo sapiens
?
Organism
Organism
UniProt
Commentary
Textmining
Homo sapiens
-
-
-
Posttranslational Modification
Posttranslational Modification
Commentary
Organism
proteolytic modification
recombinant chimeric enzyme with exchange of the pro-piece of the zymogen for that of prostate-specific antigen PSA to create an activation site suceptible for trypsin-type proteases proteolytically activates itself
Homo sapiens
Purification (Commentary)
Purification (Commentary)
Organism
recombinant chimeric enzyme after isolation from inclusion bodies and refolding
Homo sapiens
Renatured (Commentary)
Renatured (Commentary)
Organism
isolation from inclusion bodies after recombinant expression in Escherichia coli, refolding with self-activation during the process
Homo sapiens
Source Tissue
Source Tissue
Commentary
Organism
Textmining
prostate
specific
Homo sapiens
-
Specific Activity [micromol/min/mg]
Specific Activity Minimum [µmol/min/mg]
Specific Activity Maximum [µmol/min/mg]
Commentary
Organism
0.31
-
purified recombinant enzyme, substrate H-D-Val-L-Leu-L-Lys-4-nitroanilide
Homo sapiens
0.67
-
purified recombinant enzyme, substrate N-benzoyl-L-Ile-L-Glu-Gly-L-Arg-4-nitroanilide
Homo sapiens
1.12
-
purified recombinant enzyme, substrate H-D-Pro-L-Phe-L-Arg-4-nitroanilide
Homo sapiens
1.42
-
purified recombinant enzyme, substrate H-D-Val-Leu-Arg-4-nitroanilide
Homo sapiens
Substrates and Products (Substrate)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
Substrate Product ID
52 kDa prostatic acid phosphatase + H2O
recombinant self-activated, chimeric enzyme
647338
Homo sapiens
33 kDa prostatic acid phosphatase + 19 kDa fragment
products contain 256 and 73 amino acid residues, respectively
647338
Homo sapiens
?
52 kDa prostatic acid phosphatase + H2O
primary cleavage site is the Arg73-Ser74 bond
647338
Homo sapiens
33 kDa prostatic acid phosphatase + 19 kDa fragment
products contain 256 and 73 amino acid residues, respectively
647338
Homo sapiens
?
52 kDa prostatic acid phosphatase + H2O
inactivation of substrate
647338
Homo sapiens
33 kDa prostatic acid phosphatase + 19 kDa fragment
products contain 256 and 73 amino acid residues, respectively
647338
Homo sapiens
?
52 kDa prostatic acid phosphatase + H2O
enzyme may be involved in the physiological clearance of prostatic acid phosphatase
647338
Homo sapiens
33 kDa prostatic acid phosphatase + 19 kDa fragment
-
647338
Homo sapiens
?
benzoyl-L-Ile-L-Glu-Gly-L-Arg-4-nitroanilide + H2O
recombinant self-activated, chimeric enzyme
647338
Homo sapiens
benzoyl-L-Ile-L-Glu-Gly-L-Arg + 4-nitroaniline
-
-
-
?
benzoyl-L-Ile-L-Glu-Gly-L-Arg-4-nitroanilide + H2O
fluorogenic substrate, i.e. S-2222
647338
Homo sapiens
benzoyl-L-Ile-L-Glu-Gly-L-Arg + 4-nitroaniline
-
-
-
?
D-Pro-L-Phe-L-Arg-4-nitroanilide + H2O
recombinant self-activated, chimeric enzyme
647338
Homo sapiens
D-Pro-L-Phe-L-Arg + 4-nitroaniline
-
-
-
?
D-Pro-L-Phe-L-Arg-4-nitroanilide + H2O
fluorogenic substrate, i.e. S-2302
647338
Homo sapiens
D-Pro-L-Phe-L-Arg + 4-nitroaniline
-
-
-
?
D-Val-L-Leu-L-Lys-4-nitroanilide + H2O
recombinant self-activated, chimeric enzyme
647338
Homo sapiens
D-Val-L-Leu-L-Lys + 4-nitroaniline
-
-
-
?
D-Val-L-Leu-L-Lys-4-nitroanilide + H2O
fluorogenic substrate, i.e. S-2251
647338
Homo sapiens
D-Val-L-Leu-L-Lys + 4-nitroaniline
-
-
-
?
D-Val-Leu-Arg-4-nitroanilide + H2O
recombinant self-activated, chimeric enzyme
647338
Homo sapiens
D-Val-Leu-Arg + 4-nitroaniline
-
-
-
?
D-Val-Leu-Arg-4-nitroanilide + H2O
fluorogenic substrate, i.e. S-2266
647338
Homo sapiens
D-Val-Leu-Arg + 4-nitroaniline
-
-
-
?
additional information
no activity with serum albumin from human seminal plasma
647338
Homo sapiens
?
-
-
-
-
additional information
enzyme has a trypsin-type substrate specificty
647338
Homo sapiens
?
-
-
-
-
additional information
no activity with pyroglu-Gly-Arg-4-nitroanilide, i.e. S-2444, and with 3-carbomethoxypropionyl-L-Arg-L-Pro-L-Tyr-4-nitroanilide, i.e. S-2586
647338
Homo sapiens
?
-
-
-
-
polypeptide + H2O
-
647338
Homo sapiens
peptides
-
647338
Homo sapiens
?
polypeptide + H2O
enzyme plays a role in the physiologic processing of seminal plasma proteins , e.g. pro-PSA, as well as in the pathogenesis of prostate cancer through the activation of pro-PSA
647338
Homo sapiens
peptides
-
647338
Homo sapiens
?
pro-prostate-specific antigen + H2O
activation of substrate
647338
Homo sapiens
activated prostate-specific antigen
-
647338
Homo sapiens
?
pro-prostate-specific antigen + H2O
recombinant self-activated, chimeric enzyme
647338
Homo sapiens
activated prostate-specific antigen
-
647338
Homo sapiens
?
pro-prostate-specific antigen + H2O
i.e. PSA
647338
Homo sapiens
activated prostate-specific antigen
-
647338
Homo sapiens
?
pro-prostate-specific antigen + H2O
activation of PSA
647338
Homo sapiens
activated prostate-specific antigen
-
647338
Homo sapiens
?
pro-urokinase-type plasminogen activator + H2O
activation of substrate
647338
Homo sapiens
activated urokinase-type plasminogen activator
-
647338
Homo sapiens
?
pro-urokinase-type plasminogen activator + H2O
recombinant self-activated, chimeric enzyme
647338
Homo sapiens
activated urokinase-type plasminogen activator
-
647338
Homo sapiens
?
pro-urokinase-type plasminogen activator + H2O
i.e. pro-uPA
647338
Homo sapiens
activated urokinase-type plasminogen activator
-
647338
Homo sapiens
?
Subunits
Subunits
Commentary
Organism
?
x * 21000, self-activated recombinant, chimeric enzyme, SDS-PAGE
Homo sapiens
Synonyms
Synonyms
Commentary
Organism
K4
-
Homo sapiens
Temperature Optimum [°C]
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
37
-
assay at
Homo sapiens
pH Optimum
pH Optimum Minimum
pH Optimum Maximum
Commentary
Organism
7.5
-
-
Homo sapiens
pH Range
pH Minimum
pH Maximum
Commentary
Organism
5
10.3
7% of maximal activity at ph 5.0, 32% at pH 5.5, and 40% at pH 10.3
Homo sapiens
Cloned(Commentary) (protein specific)
Commentary
Organism
construction of a chimeric enzyme with exchange of the pro-piece of the zymogen for that of prostate-specific antigen PSA to create an activation site suceptible for trypsin-type proteases, expression in Escherichia coli strain BL21(DE3)
Homo sapiens
Inhibitors (protein specific)
Inhibitors
Commentary
Organism
Structure
Aprotinin
complex formation with the self-activated recombinant, chimeric enzyme
Homo sapiens
benzamidine
93% inhibition at 10 mM
Homo sapiens
Nalpha-p-tosyl-L-lysine chloromethyl ketone
85% inhibition at 1 mM; i.e. TLCK
Homo sapiens
Soybean trypsin inhibitor
99% inhibition at 1 mg/ml
Homo sapiens
Molecular Weight [Da] (protein specific)
Molecular Weight [Da]
Molecular Weight Maximum [Da]
Commentary
Organism
21000
-
x * 21000, self-activated recombinant, chimeric enzyme, SDS-PAGE
Homo sapiens
Natural Substrates/ Products (Substrates) (protein specific)
Natural Substrates
Organism
Commentary (Nat. Sub.)
Natural Products
Commentary (Nat. Pro.)
Organism (Nat. Pro.)
Reversibility
ID
52 kDa prostatic acid phosphatase + H2O
Homo sapiens
enzyme may be involved in the physiological clearance of prostatic acid phosphatase
33 kDa prostatic acid phosphatase + 19 kDa fragment
-
Homo sapiens
?
polypeptide + H2O
Homo sapiens
enzyme plays a role in the physiologic processing of seminal plasma proteins , e.g. pro-PSA, as well as in the pathogenesis of prostate cancer through the activation of pro-PSA
peptides
-
Homo sapiens
?
pro-prostate-specific antigen + H2O
Homo sapiens
i.e. PSA
activated prostate-specific antigen
-
Homo sapiens
?
pro-prostate-specific antigen + H2O
Homo sapiens
activation of PSA
activated prostate-specific antigen
-
Homo sapiens
?
Posttranslational Modification (protein specific)
Posttranslational Modification
Commentary
Organism
proteolytic modification
recombinant chimeric enzyme with exchange of the pro-piece of the zymogen for that of prostate-specific antigen PSA to create an activation site suceptible for trypsin-type proteases proteolytically activates itself
Homo sapiens
Purification (Commentary) (protein specific)
Commentary
Organism
recombinant chimeric enzyme after isolation from inclusion bodies and refolding
Homo sapiens
Renatured (Commentary) (protein specific)
Commentary
Organism
isolation from inclusion bodies after recombinant expression in Escherichia coli, refolding with self-activation during the process
Homo sapiens
Source Tissue (protein specific)
Source Tissue
Commentary
Organism
Textmining
prostate
specific
Homo sapiens
-
Specific Activity [micromol/min/mg] (protein specific)
Specific Activity Minimum [µmol/min/mg]
Specific Activity Maximum [µmol/min/mg]
Commentary
Organism
0.31
-
purified recombinant enzyme, substrate H-D-Val-L-Leu-L-Lys-4-nitroanilide
Homo sapiens
0.67
-
purified recombinant enzyme, substrate N-benzoyl-L-Ile-L-Glu-Gly-L-Arg-4-nitroanilide
Homo sapiens
1.12
-
purified recombinant enzyme, substrate H-D-Pro-L-Phe-L-Arg-4-nitroanilide
Homo sapiens
1.42
-
purified recombinant enzyme, substrate H-D-Val-Leu-Arg-4-nitroanilide
Homo sapiens
Substrates and Products (Substrate) (protein specific)
Substrates
Commentary Substrates
Literature (Substrates)
Organism
Products
Commentary (Products)
Literature (Products)
Organism (Products)
Reversibility
ID
52 kDa prostatic acid phosphatase + H2O
recombinant self-activated, chimeric enzyme
647338
Homo sapiens
33 kDa prostatic acid phosphatase + 19 kDa fragment
products contain 256 and 73 amino acid residues, respectively
647338
Homo sapiens
?
52 kDa prostatic acid phosphatase + H2O
primary cleavage site is the Arg73-Ser74 bond
647338
Homo sapiens
33 kDa prostatic acid phosphatase + 19 kDa fragment
products contain 256 and 73 amino acid residues, respectively
647338
Homo sapiens
?
52 kDa prostatic acid phosphatase + H2O
inactivation of substrate
647338
Homo sapiens
33 kDa prostatic acid phosphatase + 19 kDa fragment
products contain 256 and 73 amino acid residues, respectively
647338
Homo sapiens
?
52 kDa prostatic acid phosphatase + H2O
enzyme may be involved in the physiological clearance of prostatic acid phosphatase
647338
Homo sapiens
33 kDa prostatic acid phosphatase + 19 kDa fragment
-
647338
Homo sapiens
?
benzoyl-L-Ile-L-Glu-Gly-L-Arg-4-nitroanilide + H2O
recombinant self-activated, chimeric enzyme
647338
Homo sapiens
benzoyl-L-Ile-L-Glu-Gly-L-Arg + 4-nitroaniline
-
-
-
?
benzoyl-L-Ile-L-Glu-Gly-L-Arg-4-nitroanilide + H2O
fluorogenic substrate, i.e. S-2222
647338
Homo sapiens
benzoyl-L-Ile-L-Glu-Gly-L-Arg + 4-nitroaniline
-
-
-
?
D-Pro-L-Phe-L-Arg-4-nitroanilide + H2O
recombinant self-activated, chimeric enzyme
647338
Homo sapiens
D-Pro-L-Phe-L-Arg + 4-nitroaniline
-
-
-
?
D-Pro-L-Phe-L-Arg-4-nitroanilide + H2O
fluorogenic substrate, i.e. S-2302
647338
Homo sapiens
D-Pro-L-Phe-L-Arg + 4-nitroaniline
-
-
-
?
D-Val-L-Leu-L-Lys-4-nitroanilide + H2O
recombinant self-activated, chimeric enzyme
647338
Homo sapiens
D-Val-L-Leu-L-Lys + 4-nitroaniline
-
-
-
?
D-Val-L-Leu-L-Lys-4-nitroanilide + H2O
fluorogenic substrate, i.e. S-2251
647338
Homo sapiens
D-Val-L-Leu-L-Lys + 4-nitroaniline
-
-
-
?
D-Val-Leu-Arg-4-nitroanilide + H2O
recombinant self-activated, chimeric enzyme
647338
Homo sapiens
D-Val-Leu-Arg + 4-nitroaniline
-
-
-
?
D-Val-Leu-Arg-4-nitroanilide + H2O
fluorogenic substrate, i.e. S-2266
647338
Homo sapiens
D-Val-Leu-Arg + 4-nitroaniline
-
-
-
?
additional information
no activity with serum albumin from human seminal plasma
647338
Homo sapiens
?
-
-
-
-
additional information
enzyme has a trypsin-type substrate specificty
647338
Homo sapiens
?
-
-
-
-
additional information
no activity with pyroglu-Gly-Arg-4-nitroanilide, i.e. S-2444, and with 3-carbomethoxypropionyl-L-Arg-L-Pro-L-Tyr-4-nitroanilide, i.e. S-2586
647338
Homo sapiens
?
-
-
-
-
polypeptide + H2O
-
647338
Homo sapiens
peptides
-
647338
Homo sapiens
?
polypeptide + H2O
enzyme plays a role in the physiologic processing of seminal plasma proteins , e.g. pro-PSA, as well as in the pathogenesis of prostate cancer through the activation of pro-PSA
647338
Homo sapiens
peptides
-
647338
Homo sapiens
?
pro-prostate-specific antigen + H2O
activation of substrate
647338
Homo sapiens
activated prostate-specific antigen
-
647338
Homo sapiens
?
pro-prostate-specific antigen + H2O
recombinant self-activated, chimeric enzyme
647338
Homo sapiens
activated prostate-specific antigen
-
647338
Homo sapiens
?
pro-prostate-specific antigen + H2O
i.e. PSA
647338
Homo sapiens
activated prostate-specific antigen
-
647338
Homo sapiens
?
pro-prostate-specific antigen + H2O
activation of PSA
647338
Homo sapiens
activated prostate-specific antigen
-
647338
Homo sapiens
?
pro-urokinase-type plasminogen activator + H2O
activation of substrate
647338
Homo sapiens
activated urokinase-type plasminogen activator
-
647338
Homo sapiens
?
pro-urokinase-type plasminogen activator + H2O
recombinant self-activated, chimeric enzyme
647338
Homo sapiens
activated urokinase-type plasminogen activator
-
647338
Homo sapiens
?
pro-urokinase-type plasminogen activator + H2O
i.e. pro-uPA
647338
Homo sapiens
activated urokinase-type plasminogen activator
-
647338
Homo sapiens
?
Subunits (protein specific)
Subunits
Commentary
Organism
?
x * 21000, self-activated recombinant, chimeric enzyme, SDS-PAGE
Homo sapiens
Temperature Optimum [°C] (protein specific)
Temperature Optimum [°C]
Temperature Optimum Maximum [°C]
Commentary
Organism
37
-
assay at
Homo sapiens
pH Optimum (protein specific)
pH Optimum Minimum
pH Optimum Maximum
Commentary
Organism
7.5
-
-
Homo sapiens
pH Range (protein specific)
pH Minimum
pH Maximum
Commentary
Organism
5
10.3
7% of maximal activity at ph 5.0, 32% at pH 5.5, and 40% at pH 10.3
Homo sapiens
Other publictions for EC 3.4.21.B12
No.
1st author
Pub Med
title
organims
journal
volume
pages
year
Activating Compound
Application
Cloned(Commentary)
Crystallization (Commentary)
Engineering
General Stability
Inhibitors
KM Value [mM]
Localization
Metals/Ions
Molecular Weight [Da]
Natural Substrates/ Products (Substrates)
Organic Solvent Stability
Organism
Oxidation Stability
Posttranslational Modification
Purification (Commentary)
Reaction
Renatured (Commentary)
Source Tissue
Specific Activity [micromol/min/mg]
Storage Stability
Substrates and Products (Substrate)
Subunits
Synonyms
Temperature Optimum [°C]
Temperature Range [°C]
Temperature Stability [°C]
Turnover Number [1/s]
pH Optimum
pH Range
pH Stability
Cofactor
Ki Value [mM]
pI Value
IC50 Value
Activating Compound (protein specific)
Application (protein specific)
Cloned(Commentary) (protein specific)
Cofactor (protein specific)
Crystallization (Commentary) (protein specific)
Engineering (protein specific)
General Stability (protein specific)
IC50 Value (protein specific)
Inhibitors (protein specific)
Ki Value [mM] (protein specific)
KM Value [mM] (protein specific)
Localization (protein specific)
Metals/Ions (protein specific)
Molecular Weight [Da] (protein specific)
Natural Substrates/ Products (Substrates) (protein specific)
Organic Solvent Stability (protein specific)
Oxidation Stability (protein specific)
Posttranslational Modification (protein specific)
Purification (Commentary) (protein specific)
Renatured (Commentary) (protein specific)
Source Tissue (protein specific)
Specific Activity [micromol/min/mg] (protein specific)
Storage Stability (protein specific)
Substrates and Products (Substrate) (protein specific)
Subunits (protein specific)
Temperature Optimum [°C] (protein specific)
Temperature Range [°C] (protein specific)
Temperature Stability [°C] (protein specific)
Turnover Number [1/s] (protein specific)
pH Optimum (protein specific)
pH Range (protein specific)
pH Stability (protein specific)
pI Value (protein specific)
Expression
General Information
General Information (protein specific)
Expression (protein specific)
KCat/KM [mM/s]
KCat/KM [mM/s] (protein specific)
752370
Swedberg
Potent, selective, and cell-p ...
Homo sapiens
ACS Med. Chem. Lett.
9
1258-1262
2018
-
-
-
-
-
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1
1
-
-
-
-
-
2
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1
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1
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1
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2
-
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1
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1
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1
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1
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1
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752672
Perez
Direct evidence that KLK4 is ...
Homo sapiens
Biochem. Biophys. Res. Commun.
495
1896-1900
2017
-
-
-
-
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-
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1
-
1
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2
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1
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2
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-
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2
2
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-
752888
Yang
Tissue kallikrein-related pep ...
Homo sapiens
Biol. Chem.
398
1151-1164
2017
-
1
-
-
-
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-
1
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2
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2
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1
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753881
Wang
-
KLK4 is synchronically expres ...
Mus musculus
Int. J. Clin. Exp. Pathol.
10
5751-5757
2017
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1
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1
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1
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2
2
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754526
Vickers
Properties of the 4-kallikrei ...
Homo sapiens
J. Urol.
197
607-613
2017
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1
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1
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682813
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How do enamelysin and kallikre ...
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Davidson
Kallikrein 4 expression is up- ...
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668285
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Xi
Kallikrein 4 is a predominantl ...
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647339
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Porcine kallikrein-4 activatio ...
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647338
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Characterization of hK4 (prost ...
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Biochemistry
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