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Literature summary for 3.4.17.20 extracted from

  • Do, Y.H.; Gifford-Moore, D.S.; Beight, D.W.; Rathnachalam, R.; Klimkowski, V.J.; Warshawsky, A.M.; Lu, D.
    Inhibition of thrombin activatable fibrinolysis inhibitor by cysteine derivatives (2005), Thromb. Res., 116, 265-271.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
DL-mercaptomethyl-3-guanidinoethylthiopropanoic acid i.e. Plummer's inhibitor, IC50: 0.029 mM Homo sapiens
glycyl-glycyl-L-cysteine
-
Homo sapiens
glycyl-L-cysteine
-
Homo sapiens
guanidinyl-L-cysteine IC50: 0.0094 mM in inhibition of plasma fibrin clot lysis Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
fibrin + H2O Homo sapiens partially degraded fibrin in fibrin clots, cleavage of C-terminal Lys fibrin + Lys
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
proteolytic modification Ca2+-dependent activation by thrombin at room temperature Homo sapiens

Reaction

Reaction Comment Organism Reaction ID
release of C-terminal Arg and Lys from a polypeptide catalytically important residues are G207, I243, I247, S254, and I255, catalytic mechanism and substrate binding Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
fibrin + H2O partially degraded fibrin in fibrin clots, cleavage of C-terminal Lys Homo sapiens fibrin + Lys
-
?
[3-(2-furylacryloyl)]-L-alanyl-L-arginine + H2O
-
Homo sapiens [3-(2-furylacryloyl)]-L-alanine + L-arginine
-
?
[3-(2-furylacryloyl)]-L-phenylalanyl-L-phenylalanine + H2O
-
Homo sapiens [3-(2-furylacryloyl)]-L-phenylalanine + L-phenylalanine
-
?

Subunits

Subunits Comment Organism
More active site ligand complex model building using D-Cys, guanidinyl-L-cysteine, glycyl-glycyl-L-cysteine, and glycyl-L-cysteine Homo sapiens

Synonyms

Synonyms Comment Organism
TAFI
-
Homo sapiens
thrombin activatable fibrinolysis inhibitor
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
assay at room temperatur Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
additional information inhibition kinetics Homo sapiens
0.00008
-
guanidinyl-L-cysteine 22°C Homo sapiens
0.0001
-
DL-mercaptomethyl-3-guanidinoethylthiopropanoic acid 22°C Homo sapiens
0.00014
-
glycyl-L-cysteine 22°C Homo sapiens
0.00099
-
glycyl-glycyl-L-cysteine 22°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0094
-
IC50: 0.0094 mM in inhibition of plasma fibrin clot lysis Homo sapiens guanidinyl-L-cysteine
0.029
-
i.e. Plummer's inhibitor, IC50: 0.029 mM Homo sapiens DL-mercaptomethyl-3-guanidinoethylthiopropanoic acid