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Literature summary extracted from

  • Fukumizu, A.; Tsuda, Y.; Wanaka, K.; Tada, M.; Okamoto, S.; Hijikata-Okunomiya, A.; Okada, Y.
    Amino acids and peptides. LIII. Synthesis and biological activities of some pseudo-peptide analogs of PKSI-527, a plasma kallikrein selective inhibitor: the importance of the peptide backbone (1999), Chem. Pharm. Bull., 47, 1141-1144.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
3.4.21.34 factor XIIa activation of prekallikrein Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.34 trans-4-aminomethylcyclohexanecarbonyl-D-phenylalanyl-PSI(CH2-NH)-4-aminophenyl acetic acid PKSI-527 pseudo-peptide analogue, 5% inhibition at 1 mM Homo sapiens
3.4.21.34 trans-4-aminomethylcyclohexanecarbonyl-L-phenylalanyl-4-aminophenyl acetic acid i.e. PKSI-527, selective inhibitor, both carbonyl groups of the structure are required Homo sapiens
3.4.21.34 trans-4-aminomethylcyclohexanecarbonyl-L-phenylalanyl-PSI(CH2-NH)-4-aminophenyl acetic acid PKSI-527 pseudo-peptide analogue, 7% inhibition at 1 mM Homo sapiens
3.4.21.34 trans-4-aminomethylcyclohexanecarbonyl-PSI(CH2-NH)-L-phenylalanyl-4-aminophenyl acetic acid PKSI-527 pseudo-peptide analogue, 20% inhibition at 1 mM Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.4.21.34 soluble in the blood, prekallikrein Homo sapiens
-
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.4.21.34 kininogen + H2O Homo sapiens
-
bradykinin + fragment of kininogen
-
ir

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.34 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.34 plasma
-
Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.34 D-Pro-Phe-Arg-4-nitroanilide + H2O
-
Homo sapiens D-Pro-Phe-Arg + 4-nitroaniline
-
ir
3.4.21.34 factor XII + H2O activation of factor XII Homo sapiens ?
-
?
3.4.21.34 kininogen + H2O
-
Homo sapiens bradykinin + fragment of kininogen
-
?
3.4.21.34 kininogen + H2O
-
Homo sapiens bradykinin + fragment of kininogen
-
ir
3.4.21.34 plasminogen + H2O activation of plasminogen Homo sapiens plasmin + ?
-
ir
3.4.21.34 pro-urokinase + H2O activation of pro-urokinase Homo sapiens urokinase + ?
-
?

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.4.21.34 37
-
assay at Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.34 0.00081
-
trans-4-aminomethylcyclohexanecarbonyl-L-phenylalanyl-4-aminophenyl acetic acid 37°C Homo sapiens