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Literature summary for 3.4.21.B43 extracted from

  • Memari, N.; Jiang, W.; Diamandis, E.P.; Luo, L.Y.
    Enzymatic properties of human kallikrein-related peptidase 12 (KLK12) (2007), Biol. Chem., 388, 427-435.
    View publication on PubMed
Search for more literature for 3.4.21.B43

Cloned(Commentary)

Cloned (Comment) Organism
expressed in NS0 myeloma cell line Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3,4-dichloroisocoumarin strong inhibitor at 0.25 mM Homo sapiens
Aprotinin weak inhibition at 0.02 mM Homo sapiens
benzamidine strong inhibitor at 5 mM Homo sapiens
additional information no inhibition is observed for soybean trypsin inhibitor at concentrations up to 500 nM, alpha1-antichymotrypsin, kallistatin, plasminogen activator inhibitor-1, and alpha2-macroglobulin Homo sapiens
NaCl activity is reduced by approximately 30% in the presence of 0.8 M NaCl Homo sapiens
Zn2+ 10 mM Zn2+ is sufficient to inhibit 50% of the KLK12 enzyme activity, more than 95% suppression can be achieved by 0.2 mM Zn2+ Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0294
-
 D-Val-Leu-Lys-thiobenzyl ester in 0.1 M Tris, 10 mM CaCl2, 0.15 M NaCl, pH 8.0, at 37°C Homo sapiens
0.0686
-
 tert-butyloxycarbonyl-QAR-7-amido-4-methylcoumarin in 0.1 M Tris, 10 mM CaCl2, 0.15 M NaCl, pH 8.0, at 37°C Homo sapiens
0.2
-
 tert-butyloxycarbonyl-VPR-7-amido-4-methylcoumarin in 0.1 M Tris, 10 mM CaCl2, 0.15 M NaCl, pH 8.0, at 37°C Homo sapiens
0.35
-
 tert-butyloxycarbonyl-DPR-7-amido-4-methylcoumarin in 0.1 M Tris, 10 mM CaCl2, 0.15 M NaCl, pH 8.0, at 37°C Homo sapiens
0.565
-
 tert-butyloxycarbonyl-FSR-7-amido-4-methylcoumarin in 0.1 M Tris, 10 mM CaCl2, 0.15 M NaCl, pH 8.0, at 37°C Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ compared to the absence of calcium, a 2fold, 2.5fold, and 3fold increase in activity could be obtained by adding Ca2+ concentration of 0.1, 1, and 10 mM, respectively, however, it is not increased further by higher concentrations of Ca2+ Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
38000
-
 SDS-PAGE Homo sapiens

Organic Solvent Stability

Organic Solvent Comment Organism
Brij-35 adding 10-20% glycerol and 0.05% Brij-35 to the KLK12 autoactivation mixture can slow down activation Homo sapiens
Glycerol adding 10-20% glycerol and 0.05% Brij-35 to the KLK12 autoactivation mixture can slow down activation Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Purification (Commentary)

Purification (Comment) Organism
affinity chromatography and gel filtration Homo sapiens

Storage Stability

Storage Stability Organism
37°C, 12.5 mM MES, 75 mM NaCl, after 16 h, 24 h, 48 h, and 72 h only 50%, 35%, 20%, and 10% of the initial activity is detected Homo sapiens
37°C, in the presence of 10-20% glycerol and 0.05% Brij-35, 72 h, 10% loss of activity Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
alpha2-antiplasmin + H2O
-
 Homo sapiens ?
-
 ?
Antithrombin III + H2O
-
 Homo sapiens ?
-
 ?
C1 inhibitor + H2O
-
 Homo sapiens ?
-
 ?
D-Val-Leu-Lys-thiobenzyl ester + H2O 100% activity Homo sapiens D-Val-Leu-Lys + thiobenzyl alcohol
-
 ?
additional information no cleavage is observed for tert-butyloxycarbonyl-QGR-7-amido-4-methylcoumarin, benzyloxycarbonyl-GGR-7-amido-4-methylcoumarin, L-Pro-Phe-Arg-7-amido-4-methylcoumarin, succinyl-AFK-7-amido-4-methylcoumarin, succinyl-AAPF-7-amido-4-methylcoumarin, succinyl-ALPF-7-amido-4-methylcoumarin, succinyl-LLVY-7-amido-4-methylcoumarin, L-Tyr-7-amido-4-methylcoumarin, and S2586 Homo sapiens ?
-
 ?
additional information pro-KLK12 can undergo autoactivation Homo sapiens ?
-
 ?
protein C inhibitor + H2O
-
 Homo sapiens ?
-
 ?
tert-butyloxycarbonyl-DPR-7-amido-4-methylcoumarin + H2O 55% activity compared to D-Val-Leu-Lys-thiobenzyl ester Homo sapiens tert-butyloxycarbonyl-DPR + 7-amino-4-methylcoumarin
-
 ?
tert-butyloxycarbonyl-FSR-7-amido-4-methylcoumarin + H2O 13% activity compared to D-Val-Leu-Lys-thiobenzyl ester Homo sapiens tert-butyloxycarbonyl-FSR + 7-amino-4-methylcoumarin
-
 ?
tert-butyloxycarbonyl-QAR-7-amido-4-methylcoumarin + H2O 98% activity compared to D-Val-Leu-Lys-thiobenzyl ester Homo sapiens tert-butyloxycarbonyl-QAR + 7-amino-4-methylcoumarin
-
 ?
tert-butyloxycarbonyl-VPR-7-amido-4-methylcoumarin + H2O 85% activity compared to D-Val-Leu-Lys-thiobenzyl ester Homo sapiens tert-butyloxycarbonyl-VPR + 7-amino-4-methylcoumarin
-
 ?

Synonyms

Synonyms Comment Organism
kallikrein-related peptidase 12
-
 Homo sapiens
KLK12
-
 Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.017
-
 tert-butyloxycarbonyl-DPR-7-amido-4-methylcoumarin in 0.1 M Tris, 10 mM CaCl2, 0.15 M NaCl, pH 8.0, at 37°C Homo sapiens
0.052 2.1 tert-butyloxycarbonyl-FSR-7-amido-4-methylcoumarin in 0.1 M Tris, 10 mM CaCl2, 0.15 M NaCl, pH 8.0, at 37°C Homo sapiens
0.97
-
 tert-butyloxycarbonyl-QAR-7-amido-4-methylcoumarin in 0.1 M Tris, 10 mM CaCl2, 0.15 M NaCl, pH 8.0, at 37°C Homo sapiens
8.1
-
 tert-butyloxycarbonyl-VPR-7-amido-4-methylcoumarin in 0.1 M Tris, 10 mM CaCl2, 0.15 M NaCl, pH 8.0, at 37°C Homo sapiens
10.06
-
 tert-butyloxycarbonyl-FSR-7-amido-4-methylcoumarin in 0.1 M Tris, 10 mM CaCl2, 0.15 M NaCl, pH 8.0, at 37°C Homo sapiens
12.42
-
 D-Val-Leu-Lys-thiobenzyl ester in 0.1 M Tris, 10 mM CaCl2, 0.15 M NaCl, pH 8.0, at 37°C Homo sapiens
17.26
-
 tert-butyloxycarbonyl-QAR-7-amido-4-methylcoumarin in 0.1 M Tris, 10 mM CaCl2, 0.15 M NaCl, pH 8.0, at 37°C Homo sapiens
25.81
-
 tert-butyloxycarbonyl-VPR-7-amido-4-methylcoumarin in 0.1 M Tris, 10 mM CaCl2, 0.15 M NaCl, pH 8.0, at 37°C Homo sapiens
32.65
-
 tert-butyloxycarbonyl-DPR-7-amido-4-methylcoumarin in 0.1 M Tris, 10 mM CaCl2, 0.15 M NaCl, pH 8.0, at 37°C Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5 8
-
 Homo sapiens

pH Stability

pH Stability pH Stability Maximum Comment Organism
5 7 when the pH is decreased to less than 5.0, KLK12 enzyme activity becomes undetectable, KLK12 activity is very sensitive to pH changes in the range 6.5-7.0 (within this range, a decrease of 0.5 pH units results in a more than 60% reduction in activity) Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.011
-
-
 Homo sapiens 3,4-dichloroisocoumarin
0.28
-
-
 Homo sapiens benzamidine