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Literature summary for 3.4.21.59 extracted from

  • Hallgren, J.; Estrada, S.; Karlson, U.; Alving, K.; Pejler, G.
    Heparin antagonists are potent inhibitors of mast cell tryptase (2001), Biochemistry, 40, 7342-7349.
    View publication on PubMed
Search for more literature for 3.4.21.59

Application

Application Comment Organism
medicine heparin antagonists potentially may be used in treatment of mast cell-mediated diseases, potent and selective inhibitor of tryptase will be an essential tool to determine the role of tryptase in inflammation and other processes, tryptase plays a role in asthma and other allergic and inflammatory skin diseases like psoriasis and atopic dermatitis Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
recombinant tryptase expressed in human 293 cells Mus musculus

General Stability

General Stability Organism
stabilized by heparin proteoglycans Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
APC-366 low molecular weight active site-directed competitive tryptase inhibitor Homo sapiens
polybrene heparin antagonist, potent inhibitor, noncompetitive inhibition Homo sapiens
polybrene heparin antagonist, potent inhibitor, noncompetitive inhibition, recombinant tryptase Mus musculus
protamine heparin antagonist, potent inhibitor, competitive inhibition Homo sapiens
protamine heparin antagonist, potent inhibitor, competitive inhibition, recombinant tryptase Mus musculus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.19
-
 N-p-tosyl-Gly-Pro-Lys-p-nitroanilide pH 6.0, 25°C, 1200 ng polybrene Mus musculus
0.2
-
 N-p-tosyl-Gly-Pro-Lys-p-nitroanilide pH 6.0, 25°C, 600 ng polybrene Mus musculus
0.21
-
 N-p-tosyl-Gly-Pro-Lys-p-nitroanilide pH 6.0, 25°C, 800 ng or 1000 ng polybrene Mus musculus
0.27
-
 N-p-tosyl-Gly-Pro-Lys-p-nitroanilide pH 6.0, 25°C Mus musculus
0.4
-
 D-Ile-Pro-Arg-p-nitroanilide pH 6.0, 25°C, 60 ng polybrene Homo sapiens
0.41
-
 N-p-tosyl-Gly-Pro-Lys-p-nitroanilide pH 6.0, 25°C, 0.001 mg protamine Mus musculus
0.43
-
 D-Ile-Pro-Arg-p-nitroanilide pH 6.0, 25°C, 80 ng polybrene Homo sapiens
0.44
-
 D-Ile-Pro-Arg-p-nitroanilide pH 6.0, 25°C, 100 ng polybrene Homo sapiens
0.46
-
 D-Ile-Pro-Arg-p-nitroanilide pH 6.0, 25°C Homo sapiens
0.53
-
 N-p-tosyl-Gly-Pro-Lys-p-nitroanilide pH 6.0, 25°C, 0.0015 mg protamine Mus musculus
0.64
-
 N-p-tosyl-Gly-Pro-Lys-p-nitroanilide pH 6.0, 25°C, 0.002 mg protamine Mus musculus
1.7
-
 D-Ile-Pro-Arg-p-nitroanilide pH 6.0, 25°C, 100 ng protamine Homo sapiens
6.7
-
 D-Ile-Pro-Arg-p-nitroanilide pH 6.0, 25°C, 800 ng protamine Homo sapiens
7.4
-
 D-Ile-Pro-Arg-p-nitroanilide pH 6.0, 25°C, 400 ng protamine Homo sapiens
8.2
-
 D-Ile-Pro-Arg-p-nitroanilide pH 6.0, 25°C, 200 ng protamine Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
200000
-
 gel filtration Mus musculus
200000
-
 gel filtration Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
 mouse
-

Purification (Commentary)

Purification (Comment) Organism
recombinant enzyme Mus musculus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-Ile-Pro-Arg-p-nitroanilide + H2O
-
 Homo sapiens ?
-
 ?
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide + H2O
-
 Mus musculus ?
-
 ?
N-p-tosyl-Gly-Pro-Lys-p-nitroanilide + H2O
-
 Homo sapiens ?
-
 ?

Subunits

Subunits Comment Organism
tetramer
-
 Homo sapiens

Synonyms

Synonyms Comment Organism
Mast cell tryptase
-
 Mus musculus
Mast cell tryptase
-
 Homo sapiens
mMCP-6
-
 Mus musculus
mouse mast cell protease 6
-
 Mus musculus

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.74
-
 N-p-tosyl-Gly-Pro-Lys-p-nitroanilide pH 6.0, 25°C, 1200 ng polybrene Mus musculus
1.5
-
 N-p-tosyl-Gly-Pro-Lys-p-nitroanilide pH 6.0, 25°C, 1000 ng polybrene Mus musculus
2.6
-
 N-p-tosyl-Gly-Pro-Lys-p-nitroanilide pH 6.0, 25°C, 800 ng polybrene Mus musculus
3 6 D-Ile-Pro-Arg-p-nitroanilide pH 6.0, 25°C, 200 ng protamine Homo sapiens
3.6
-
 N-p-tosyl-Gly-Pro-Lys-p-nitroanilide pH 6.0, 25°C, 600 ng polybrene Mus musculus
3.9
-
 N-p-tosyl-Gly-Pro-Lys-p-nitroanilide pH 6.0, 25°C, 0.002 mg protamine Mus musculus
4.3
-
 N-p-tosyl-Gly-Pro-Lys-p-nitroanilide pH 6.0, 25°C Mus musculus
5
-
 D-Ile-Pro-Arg-p-nitroanilide pH 6.0, 25°C, 150 ng polybrene Homo sapiens
5.1
-
 N-p-tosyl-Gly-Pro-Lys-p-nitroanilide pH 6.0, 25°C, 0.0015 mg protamine Mus musculus
5.8
-
 N-p-tosyl-Gly-Pro-Lys-p-nitroanilide pH 6.0, 25°C, 0.001 mg protamine Mus musculus
6.08
-
 N-p-tosyl-Gly-Pro-Lys-p-nitroanilide pH 6.0, 25°C, 1200 ng polybrene Mus musculus
8
-
 D-Ile-Pro-Arg-p-nitroanilide pH 6.0, 25°C, 100 ng polybrene Homo sapiens
9.9
-
 D-Ile-Pro-Arg-p-nitroanilide pH 6.0, 25°C, 80 ng polybrene Homo sapiens
14
-
 D-Ile-Pro-Arg-p-nitroanilide pH 6.0, 25°C Homo sapiens
16
-
 D-Ile-Pro-Arg-p-nitroanilide pH 6.0, 25°C, 100 ng protamine Homo sapiens
17
-
 D-Ile-Pro-Arg-p-nitroanilide pH 6.0, 25°C, 60 ng polybrene Homo sapiens
26
-
 D-Ile-Pro-Arg-p-nitroanilide pH 6.0, 25°C, 800 ng protamine Homo sapiens
40
-
 D-Ile-Pro-Arg-p-nitroanilide pH 6.0, 25°C, 400 ng protamine Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00053
-
 APC-366 pH 6.0, 25°C, 4 h incubation Homo sapiens
0.25
-
 APC-366 pH 6.0, 25°C, 40 min incubation Homo sapiens