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Literature summary for 3.4.21.34 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
Search for more literature for 3.4.21.34

Activating Compound

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

Inhibitors

Inhibitors Comment Organism Structure
trans-4-aminomethylcyclohexanecarbonyl-D-phenylalanyl-PSI(CH2-NH)-4-aminophenyl acetic acid PKSI-527 pseudo-peptide analogue, 5% inhibition at 1 mM Homo sapiens
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
trans-4-aminomethylcyclohexanecarbonyl-L-phenylalanyl-PSI(CH2-NH)-4-aminophenyl acetic acid PKSI-527 pseudo-peptide analogue, 7% inhibition at 1 mM Homo sapiens
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

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
plasma
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Temperature Optimum [°C]

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

Ki Value [mM]

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