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Literature summary for 3.4.21.6 extracted from

  • Kroh, H.K.; Panizzi, P.; Tchaikovski, S.; Baird, T.R.; Wei, N.; Krishnaswamy, S.; Tans, G.; Rosing, J.; Furie, B.; Furie, B.C.; Bock, P.E.
    Active site-labeled prothrombin inhibits prothrombinase in vitro and thrombosis in vivo (2011), J. Biol. Chem., 286, 23345-23356.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.6

Activating Compound

Activating Compound Comment Organism Structure
Factor Va
-
 Mus musculus
Factor Va
-
 Homo sapiens
phospholipid vesicle
-
 Mus musculus
phospholipid vesicle
-
 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
FPR-prothrombin i.e. prothrombin specifically active site-labeled with D-Phe-Pro-Arg-CH2Cl, acts as a competitive inhibitor of prothrombin activation. The inhibitory effect of FPR-ProT increases with decreasing phospholipid concentration, with a 5fold decrease in the FPR-ProT concentration required for 50% inhibition at 0.002 mM phospholipid compared with that at 0.030 mM Homo sapiens
ProTS195A the prothrombin mutant also does inhibit thrombin generation, but with a much smaller effect compared to that with FPR-ProT Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.000071
-
 ProTS195A pH 7.7, 37°C, versus prothrombin, in absence of phospholipid Homo sapiens
0.000079
-
 prothrombin pH 7.7, 37°C Homo sapiens
0.00016
-
 FPR-prothrombin pH 7.7, 37°C, in presence of phospholipid at 0.025 mM Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane
-
 Mus musculus 16020
-

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ required Mus musculus
Ca2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
prothrombin + H2O Mus musculus
-
 thrombin + ?
-
 ?
prothrombin + H2O Homo sapiens
-
 thrombin + ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood vessel wall
-
 Mus musculus
-
fibroblast
-
 Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
FPR-prothrombin + H2O i.e. prothrombin specifically active site-labeled with D-Phe-Pro-Arg-CH2Cl is cleaved by prothrombinase to intermediate meizothrombin, but the reaction is then directed to formation of a different FPR-prothrombin 2 intermediate product Homo sapiens meizothrombin
-
 ?
FPR-prothrombin + H2O i.e. prothrombin specifically active site-labeled with D-Phe-Pro-Arg-CH2Cl and AF660-labeled, is cleaved by prothrombinase to intermediate meizothrombin, but the reaction is then directed to formation of a different FPR-prothrombin 2 intermediate product Mus musculus meizothrombin + ?
-
 ?
prothrombin + H2O
-
 Mus musculus thrombin + ?
-
 ?
prothrombin + H2O
-
 Homo sapiens thrombin + ?
-
 ?
ProTS195A + H2O the mutant protein also acts as competitive inhibitor of prothrombin activation Homo sapiens ?
-
 ?
Z-D-Arg-Gly-L-Arg-4-nitroanilide + H2O
-
 Homo sapiens Z-D-Arg-Gly-L-Arg + 4-nitroaniline
-
 ?

Synonyms

Synonyms Comment Organism
factor Xa
-
 Mus musculus
factor Xa
-
 Homo sapiens
FXa
-
 Mus musculus
FXa
-
 Homo sapiens
prothrombinase
-
 Mus musculus
prothrombinase
-
 Homo sapiens

Temperature Optimum [°C]

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

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
81
-
 prothrombin pH 7.7, 37°C Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.7
-
 assay at Mus musculus
7.7
-
 assay at Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000057
-
 FPR-prothrombin pH 7.7, 37°C, versus prothrombin, in absence of phospholipid Homo sapiens
0.000098
-
 ProTS195A pH 7.7, 37°C, versus prothrombin, in absence of phospholipid Homo sapiens
0.00028
-
 FPR-prothrombin pH 7.7, 37°C, versus prothrombin, in presence of phospholipid at 0.025 mM Homo sapiens

General Information

General Information Comment Organism
additional information prothrombin specifically active site-labeled with D-Phe-Pro-Arg-CH2Cl shows altered activity in vitro and in vivo compared to the wild-type protein, overview Homo sapiens
additional information prothrombin specifically active site-labeled with D-Phe-Pro-Arg-CH2Cl shows altered activity in vitro and in vivo compared to the wild-type protein. [AF660]FPR-mouse ProT binds to fibroblast membranes in mouse plasma, overview Mus musculus
physiological function the final serine proteinase zymogen activation step of the blood coagulation pathway is the proteolytic activation of prothrombin to thrombin by prothrombinase. Prothrombinase consists of the proteinase, factor Xa, bound to its protein cofactor, factor Va, assembled in the presence of calcium on phospholipid membranes containing phosphatidylserine Mus musculus
physiological function the final serine proteinase zymogen activation step of the blood coagulation pathway is the proteolytic activation of prothrombin to thrombin by prothrombinase. Prothrombinase consists of the proteinase, factor Xa, bound to its protein cofactor, factor Va, assembled in the presence of calcium on phospholipid membranes containing phosphatidylserine Homo sapiens