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

BRENDA support

Literature summary extracted from

  • Zavyalova, E.; Kopylov, A.
    Multiple inhibitory kinetics reveal an allosteric interplay among thrombin functional sites (2015), Thromb. Res., 135, 212-216.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.4.21.5
-
 Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.5 antithrombin III pseudo-complete inhibition, noncompetitive Homo sapiens
3.4.21.5 argatroban complete inhibition, noncompetitive Homo sapiens
3.4.21.5 bivalirudin complete inhibition, noncompetitive Homo sapiens
3.4.21.5 GPRP pseudo-complete inhibition, noncompetitive Homo sapiens
3.4.21.5 heparin partial inhibition, noncompetitive Homo sapiens
3.4.21.5 hirugen complete inhibition, noncompetitive Homo sapiens
3.4.21.5 additional information investigation on the effect of thrombin inhibitors on fibrinogen hydrolysis using a turbidimetric assay. There is a close relation between binding and inhibitory modes of the thrombin ligands. Active site- and exosite I-targeted ligands are able to inhibit fibrinogen hydrolysis completely. Macromolecular ligands affect fibrinogen hydrolysis in a competitive manner due to creation of the interacting area comparable to the thrombin-fibrinogen one. Low-molecular ligands probably form nonproductive complex interfering the appropriate orientation of substrate on the thrombin. Exosite II-targeted ligands are capable for only partial inhibition, indicating the fine tuning of the thrombin enzymatic activity via allosteric effects Homo sapiens
3.4.21.5 Phe-Pro-Arg-chloromethyl ketone complete inhibition, noncompetitive Homo sapiens
3.4.21.5 Toggle-25 t partial inhibition, noncompetitive Homo sapiens

Organism

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

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.5 commercial preparation
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.5 fibrinogen + H2O
-
 Homo sapiens fibrin + fibrinopeptide A + fibrinopeptide B
-
 ?

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.5 0.0000014
-
 antithrombin III pH 7.4, 37°C Homo sapiens
3.4.21.5 0.00000175
-
 bivalirudin pH 7.4, 37°C Homo sapiens
3.4.21.5 0.0000064
-
 argatroban pH 7.4, 37°C Homo sapiens
3.4.21.5 0.00001
-
 Toggle-25 t pH 7.4, 37°C Homo sapiens
3.4.21.5 0.0000208
-
 Phe-Pro-Arg-chloromethyl ketone pH 7.4, 37°C Homo sapiens
3.4.21.5 0.0015
-
 hirugen pH 7.4, 37°C Homo sapiens
3.4.21.5 0.00265
-
 heparin pH 7.4, 37°C Homo sapiens
3.4.21.5 0.027
-
 GPRP pH 7.4, 37°C Homo sapiens