Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.21.68 extracted from

  • Li, C.Y.; de Veer, S.J.; Law, R.H.P.; Whisstock, J.C.; Craik, D.J.; Swedberg, J.E.
    Characterising the subsite specificity of urokinase-type plasminogen activator and tissue-type plasminogen activator using a sequence-defined peptide aldehyde library (2019), ChemBioChem, 20, 46-50 .
    View publication on PubMed
Search for more literature for 3.4.21.68

Cloned(Commentary)

Cloned (Comment) Organism
gene PLAT, recombinant human tPA (residue 297-562) is expressed in Expi293 cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information screening of a peptide aldehyde library against tPA, inhibitory potencies of compounds at 0.01 mM, analysis of effects of different amino acids on positions P4, P3, P2, and P1, overview Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
 additional information Michaelis-Menten kinetics Homo sapiens
0.48
-
 acetyl-FTAR-4-nitroanilide pH and temperature not specified in the publication Homo sapiens
0.59
-
 acetyl-FYAR-4-nitroanilide pH and temperature not specified in the publication Homo sapiens
0.76
-
 acetyl-GTGR-4-nitroanilide pH and temperature not specified in the publication Homo sapiens
1.1
-
 acetyl-GTAR-4-nitroanilide pH and temperature not specified in the publication Homo sapiens
1.3
-
 acetyl-QYAR-4-nitroanilide pH and temperature not specified in the publication Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P00750
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-FTAR-4-nitroanilide + H2O
-
 Homo sapiens acetyl-FTAR + 4-nitroaniline
-
 ?
acetyl-FYAR-4-nitroanilide + H2O
-
 Homo sapiens acetyl-FYAR + 4-nitroaniline
-
 ?
acetyl-GTAR-4-nitroanilide + H2O
-
 Homo sapiens acetyl-GTAR + 4-nitroaniline
-
 ?
acetyl-GTGR-4-nitroanilide + H2O
-
 Homo sapiens acetyl-GTGR + 4-nitroaniline
-
 ?
acetyl-QYAR-4-nitroanilide + H2O
-
 Homo sapiens acetyl-QYAR + 4-nitroaniline
-
 ?
benzyl-TAR-4-nitroanilide + H2O
-
 Homo sapiens benzyl-TAR + 4-nitroaniline
-
 ?
additional information substrate specificity of enzyme tissue-type plasminogen activator, comparison with urokinase-type plasminogen activator, EC 3.4.21.73. The urokinase-type plasminogen activator shows much higher activity towards the peptide substrates Homo sapiens ?
-
 ?
Z-Pyr-Gly-Arg-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens Z-Pyr-Gly-Arg + 7-amino-4-methylcoumarin
-
 ?

Synonyms

Synonyms Comment Organism
PLAT
-
 Homo sapiens
Tissue-type plasminogen activator
-
 Homo sapiens
tPA
-
 Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.21
-
 acetyl-GTGR-4-nitroanilide pH and temperature not specified in the publication Homo sapiens
0.24
-
 acetyl-FTAR-4-nitroanilide pH and temperature not specified in the publication Homo sapiens
0.36
-
 acetyl-GTAR-4-nitroanilide pH and temperature not specified in the publication Homo sapiens
0.46
-
 acetyl-QYAR-4-nitroanilide pH and temperature not specified in the publication Homo sapiens
0.86
-
 acetyl-FYAR-4-nitroanilide pH and temperature not specified in the publication Homo sapiens

General Information

General Information Comment Organism
metabolism urokinase-type plasminogen activator (uPA) and tissue-type plasminogen activator (tPA) are two serine proteases that contribute to initiating fibrinolysis by activating plasminogen. uPA is also an important tumour-associated protease due to its role in extracellular matrix remodelling Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
0.28
-
 acetyl-GTGR-4-nitroanilide pH and temperature not specified in the publication Homo sapiens
0.33
-
 acetyl-GTAR-4-nitroanilide pH and temperature not specified in the publication Homo sapiens
0.35
-
 acetyl-QYAR-4-nitroanilide pH and temperature not specified in the publication Homo sapiens
0.5
-
 acetyl-FTAR-4-nitroanilide pH and temperature not specified in the publication Homo sapiens
1.46
-
 acetyl-FYAR-4-nitroanilide pH and temperature not specified in the publication Homo sapiens