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Literature summary for 3.4.17.20 extracted from

  • Suzuki, K.; Muto, Y.; Fushihara, K.; Kanemoto, K.; Iida, H.; Sato, E.; Kikuchi, C.; Matsushima, T.; Kato, E.; Nomoto, M.; Yoshioka, S.; Ishii, H.
    Enhancement of fibrinolysis by EF6265 [(S)-7-amino-2-[[[(R)-2-methyl-1-(3-phenylpropanoylamino)propyl]hydroxypho sphinoyl] methyl]heptanoic acid], a specific inhibitor of plasma carboxypeptidase B (2004), J. Pharmacol. Exp. Ther., 309, 607-615.
    View publication on PubMed
Search for more literature for 3.4.17.20

Application

Application Comment Organism
pharmacology enzyme inhibitors are valid as enhancer of physiological fibrinolysis in microcirculation and as adjunctive agent to tissue-type plasminogen activator for thromboembolic diseases in humans while maintaining a small effect on primary hemostasis Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
EF6265 i.e. (S)-7-amino-2-[([(R)-2-methyl-1-(3-phenylpropanoylamino)propyl]hydroxyphosphinoyl)methyl]heptanoic acid, IC50: 0.00000826 mM, inhibitory effect in vivo, overview Homo sapiens
EF6265 i.e. (S)-7-amino-2-[([(R)-2-methyl-1-(3-phenylpropanoylamino)propyl]hydroxyphosphinoyl)methyl]heptanoic acid, IC50: 0.00000389 mM, inhibitory effect in vivo, overview Rattus norvegicus
[(S)-7-amino-2-[[[(R)-2-methyl-1-(3-phenylpropanoylamino)propyl]hydroxyphosphinoyl]methyl]heptanoic acid] IC50: 8.3 nM, potent and highly selective inhibitor. Systemically administered inhibitor enhances fibrinolysis in a dose- and time-dependent manner Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular
-
 Homo sapiens
-
-
extracellular
-
 Rattus norvegicus
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens the enzyme down-regulates fibrinolysis by removing carboxy-terminal lysine residues, which are ligands for plasminogen and tissue-type plasminogen activator, from partially degraded fibrin, pharmacological profile and pathphysiological role of the enzyme in rat thrombolysis ?
-
 ?
additional information Rattus norvegicus the enzyme down-regulates fibrinolysis by removing carboxy-terminal lysine residues, which are ligands for plasminogen and tissue-type plasminogen activator, from partially degraded fibrin, pharmacological profile and pathphysiological role of the enzyme in rat thrombolysis ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Rattus norvegicus
-
 male Wistar rats
-

Posttranslational Modification

Posttranslational Modification Comment Organism
proteolytic modification the enzyme is activated by thrombin Homo sapiens
proteolytic modification the enzyme is activated by thrombin Rattus norvegicus

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
 Homo sapiens
-
blood plasma
-
 Rattus norvegicus
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
-
 Homo sapiens
additional information
-
 in vivo arteriovenous shunt thrombosis model, ex vivo clot lysis assay Rattus norvegicus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information the enzyme down-regulates fibrinolysis by removing carboxy-terminal lysine residues, which are ligands for plasminogen and tissue-type plasminogen activator, from partially degraded fibrin, pharmacological profile and pathphysiological role of the enzyme in rat thrombolysis Homo sapiens ?
-
 ?
additional information the enzyme down-regulates fibrinolysis by removing carboxy-terminal lysine residues, which are ligands for plasminogen and tissue-type plasminogen activator, from partially degraded fibrin, pharmacological profile and pathphysiological role of the enzyme in rat thrombolysis Rattus norvegicus ?
-
 ?

Synonyms

Synonyms Comment Organism
Plasma carboxypeptidase B
-
 Homo sapiens
Plasma carboxypeptidase B
-
 Rattus norvegicus
plasma CPB
-
 Homo sapiens
plasma CPB
-
 Rattus norvegicus
TAFI
-
 Homo sapiens
TAFI
-
 Rattus norvegicus
thrombin-activatable fibrinolysis inhibitor
-
 Homo sapiens
thrombin-activatable fibrinolysis inhibitor
-
 Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
 assay at Homo sapiens
25
-
 assay at Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.6
-
 assay at Homo sapiens
7.6
-
 assay at Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000389
-
 i.e. (S)-7-amino-2-[([(R)-2-methyl-1-(3-phenylpropanoylamino)propyl]hydroxyphosphinoyl)methyl]heptanoic acid, IC50: 0.00000389 mM, inhibitory effect in vivo, overview Rattus norvegicus EF6265
0.00000826
-
 i.e. (S)-7-amino-2-[([(R)-2-methyl-1-(3-phenylpropanoylamino)propyl]hydroxyphosphinoyl)methyl]heptanoic acid, IC50: 0.00000826 mM, inhibitory effect in vivo, overview Homo sapiens EF6265
0.0000083
-
 IC50: 8.3 nM, potent and highly selective inhibitor. Systemically administered inhibitor enhances fibrinolysis in a dose- and time-dependent manner Homo sapiens [(S)-7-amino-2-[[[(R)-2-methyl-1-(3-phenylpropanoylamino)propyl]hydroxyphosphinoyl]methyl]heptanoic acid]