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Literature summary for 3.4.17.20 extracted from
- Thrombin-activatable fibrinolysis inhibitor (2004), Curr. Med. Chem., 11, 2335-2348.
Activating Compound
| Activating Compound | Comment | Organism | Structure |
|---|---|---|---|
| activation peptide | the activated TAFIa acts in complex with the activation peptide, enzyme regulation overview | Mus musculus | |
| activation peptide | the activated TAFIa acts in complex with the activation peptide, enzyme regulation overview | Homo sapiens | |
| additional information | dexamethasone induces expression of the enzyme 2fold | Homo sapiens |
Protein Variants
| Protein Variants | Comment | Organism |
|---|---|---|
| moe | construction of enzyme-deficient mice by gene disruption, which is not lethal and does not cause a pathogenic phenotype, the mice show delayed wound healing, overview | Mus musculus |
| additional information | the enzyme shows polymorphisms, e.g. at residue 325, genotypes, correlated diseases, overview | Homo sapiens |
General Stability
| General Stability | Organism |
|---|---|
| the enzyme is spontaneously inactivated by conformational changes | Mus musculus |
| the enzyme is spontaneously inactivated by conformational changes | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 2-mercaptoethanol | - |
Homo sapiens |  |
| 4-chloromercuribenzoate | - |
Homo sapiens | |
| DTT | - |
Homo sapiens | |
| epsilon-amino caproic acid | - |
Homo sapiens | |
| GEMSA | reversible, mechanism, reduces enzyme activity 10fold | Homo sapiens | |
| Hirudo medicinalis peptide inhibitor | - |
Homo sapiens | |
| MERGEPTA | - |
Homo sapiens | |
| additional information | the enzyme is spontaneously inactivated by conformational changes | Homo sapiens | |
| additional information | the enzyme is spontaneously inactivated by conformational changes | Mus musculus | |
| o-phenanthroline | - |
Homo sapiens | |
| potato carboxypeptidase inhibitor | inhibition mechanism | Homo sapiens |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| extracellular | - |
Mus musculus | - |
- |
| extracellular | - |
Homo sapiens | - |
- |
Metals/Ions
| Metals/Ions | Comment | Organism | Structure |
|---|---|---|---|
| Zn2+ | bound by residues His159, Glu162, and His288 | Mus musculus | |
| Zn2+ | bound by residues His159, Glu162, and His288, Zn2+ is important in the catalytic mechanism | Homo sapiens | |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| Glu-plasminogen + H2O | Homo sapiens | - |
Glu + plasmin | - |
? | |
| Lys-plasminogen + H2O | Homo sapiens | - |
Lys + plasmin | - |
? | |
| additional information | Mus musculus | the enzyme circulates as inactive zymogen in the blood stream becoming activated upon blood clotting, the enzyme inhibits fibrinolysis by cleaving C-terminal lysine from the surface of partially degraded fibrin, which stimulates the tissue-type plasminogen activator-mediated conversion of plasminogen to plasmin, the enzyme might also be involved in regulation of inflammation and tissue repair, enzyme regulation overview | ? | - |
? | |
| additional information | Homo sapiens | the enzyme circulates as inactive zymogen in the blood stream becoming activated upon blood clotting, the enzyme inhibits fibrinolysis by cleaving C-terminal lysine from the surface of partially degraded fibrin, which stimulates the tissue-type plasminogen activator-mediated conversion of plasminogen to plasmin, the enzyme might also be involved in regulation of inflammation and tissue repair, enzyme regulation overview | ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Mus musculus | - |
- |
- |
Posttranslational Modification
| Posttranslational Modification | Comment | Organism |
|---|---|---|
| glycoprotein | the enzyme contains 4 potential N-glycosylation sites at Asn22, Asn51, Asn63, and Asn96, carbohydrates account for 20% of total mass of TAFI and are responsable for stabilization | Homo sapiens |
| proteolytic modification | the enzyme is synthesized as zymogen TAFI, activation by the thrombin to the active form TAFIa | Mus musculus |
| proteolytic modification | the enzyme is synthesized as zymogen TAFI, activation by the thrombin/thrombomodulin or by plasmin to the active form TAFIa, cleavage patterns, overview | Homo sapiens |
Reaction
| Reaction | Comment | Organism | Reaction ID |
|---|---|---|---|
| release of C-terminal Arg and Lys from a polypeptide | substrate binding involves residues ARg235, Tyr341, and Asn234, while catalysis involves residues Glu363 and ARg217, mechanism of action of TAFI, overview | Mus musculus | |
| release of C-terminal Arg and Lys from a polypeptide | substrate binding involves residues ARg235, Tyr341, and Asn234, while catalysis involves residues Glu363 and ARg217, mechanism of action of TAFI, overview, Zn2+ is important in the catalytic mechanism | Homo sapiens |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| blood | the enzyme circulates as inactive zymogen in the blood stream becoming activated upon blood clotting | Mus musculus | - |
| blood | the enzyme circulates as inactive zymogen in the blood stream becoming activated upon blood clotting | Homo sapiens | - |
| liver | - |
Mus musculus | - |
| additional information | no enzyme expression in kidney and testis | Mus musculus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| Glu-plasminogen + H2O | - |
Homo sapiens | Glu + plasmin | - |
? | |
| Lys-plasminogen + H2O | - |
Homo sapiens | Lys + plasmin | - |
? | |
| Lys-plasminogen + H2O | preferred substrate | Homo sapiens | Lys + plasmin | - |
? | |
| additional information | the enzyme circulates as inactive zymogen in the blood stream becoming activated upon blood clotting, the enzyme inhibits fibrinolysis by cleaving C-terminal lysine from the surface of partially degraded fibrin, which stimulates the tissue-type plasminogen activator-mediated conversion of plasminogen to plasmin, the enzyme might also be involved in regulation of inflammation and tissue repair, enzyme regulation overview | Mus musculus | ? | - |
? | |
| additional information | the enzyme circulates as inactive zymogen in the blood stream becoming activated upon blood clotting, the enzyme inhibits fibrinolysis by cleaving C-terminal lysine from the surface of partially degraded fibrin, which stimulates the tissue-type plasminogen activator-mediated conversion of plasminogen to plasmin, the enzyme might also be involved in regulation of inflammation and tissue repair, enzyme regulation overview | Homo sapiens | ? | - |
? | |
| additional information | the enzyme binds alpha2-macroglobulin and pregnancy zone protein, which does not inhibit the enzyme | Homo sapiens | ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| Procarboxypeptidase B | - |
Mus musculus |
| Procarboxypeptidase B | - |
Homo sapiens |
| procarboxypeptidase R | - |
Mus musculus |
| procarboxypeptidase R | - |
Homo sapiens |
| procarboxypeptidase U | - |
Mus musculus |
| procarboxypeptidase U | - |
Homo sapiens |
| TAFI | - |
Mus musculus |
| TAFI | - |
Homo sapiens |
| thrombin-activatable fibrinolysis inhibitor | - |
Mus musculus |
| thrombin-activatable fibrinolysis inhibitor | - |
Homo sapiens |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.000004 | - |
potato carboxypeptidase inhibitor | - |
Homo sapiens | |
| 0.8 | - |
epsilon-amino caproic acid | - |
Homo sapiens | |
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