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Literature summary for 3.4.21.109 extracted from

  • Farady, C.J.; Sun, J.; Darragh, M.R.; Miller, S.M.; Craik, C.S.
    The mechanism of inhibition of antibody-based inhibitors of membrane-type serine protease 1 (MT-SP1) (2007), J. Mol. Biol., 369, 1041-1051.
    View publication on PubMedView publication on EuropePMC

Protein Variants

Protein Variants Comment Organism
D217A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
D60A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
D96A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
E169A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
F94A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
F97A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
F99A site-directed mutagenesis, inactive mutant Homo sapiens
H143A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
I41A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
I60A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
K224A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
L153A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
N95A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
Q145A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
Q174A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
Q175A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
Q192A site-directed mutagenesis, inactive mutant Homo sapiens
Q221A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
Q38A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
R222A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
R60A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
R87A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
T150A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
T98A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens
W215A site-directed mutagenesis, inactive mutant Homo sapiens
Y146A site-directed mutagenesis, the mutant shows altered inhibition kinetics with different inhibitors, overview Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
4-aminobenzamidine weak competitive inhibition, competition assay with antibody inhibitors, overview Homo sapiens
Bovine pancreatic trypsin inhibitor BPTI Homo sapiens
scFv antibody E2 competitive mechanism of inhibition of the scFv antibody enzyme inhibitors, which competes with substrate binding in the S1 site, the antibody binds to a number of residues flanking the active site, forming a unique three-dimensional binding epitope Homo sapiens
scFv antibody S4 competitive mechanism of inhibition of the scFv antibody enzyme inhibitors, which competes with substrate binding in the S1 site, the antibody binds to a number of residues flanking the active site, forming a unique three-dimensional binding epitope Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information pre-steady-state and steady-state kinetics, stopped-flow, overview Homo sapiens
0.0017
-
pro-urokinase plasminogen activator
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
pro-urokinase plasminogen activator + H2O Homo sapiens
-
urokinase plasminogen activator + propeptide of urokinase plasminogen activator
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
pro-urokinase plasminogen activator + H2O
-
Homo sapiens urokinase plasminogen activator + propeptide of urokinase plasminogen activator
-
?

Synonyms

Synonyms Comment Organism
membrane-type serine protease 1
-
Homo sapiens
MT-SP1
-
Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.89
-
pro-urokinase plasminogen activator
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information inhibition kinetics with antobodies E2 and S4 and point mutants thereof, overview Homo sapiens
0.0000000123
-
scFv antibody E2
-
Homo sapiens
0.0000000497
-
Bovine pancreatic trypsin inhibitor
-
Homo sapiens
0.0000000704
-
scFv antibody S4
-
Homo sapiens
0.0288
-
4-aminobenzamidine
-
Homo sapiens