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Literature summary extracted from
- Functional analysis of mutant variants of thrombin-activatable fibrinolysis inhibitor resistant to activation by thrombin or plasmin (2009), J. Thromb. Haemost., 7, 665-672.
Activating Compound
| EC Number | Activating Compound | Comment | Organism | Structure |
|---|---|---|---|---|
| 3.4.17.20 | plasmin | overall catalytic efficiency for activation by plasmin is 1/5 of that for activation by thrombin in the presence of thrombomodulin | Homo sapiens | |
| 3.4.17.20 | thrombin | poor activator of TAFI | Homo sapiens | |
| 3.4.17.20 | thrombin-thrombomodulin | activation in the presence of thrombomodulin is considerably enhanced | Homo sapiens |
Cloned(Commentary)
| EC Number | Cloned (Comment) | Organism |
|---|---|---|
| 3.4.17.20 | - |
Homo sapiens |
| 3.4.17.20 | recombinant TAFI is expressed in BHK cells | Homo sapiens |
Protein Variants
| EC Number | Protein Variants | Comment | Organism |
|---|---|---|---|
| 3.4.17.20 | A93V | mutant is comparably to wild-type activated by thrombin, mutant is slightly less activated by thrombin in the presence of thrombomodulin, kcat (1/sec) (p-anisylazoformyl-L-arginine, activated by thrombin in the presence of thrombomodulin): 0.205, Km (mM) (p-anisylazoformyl-L-arginine, activated by thrombin in the presence of thrombomodulin): 0.000169, mutation shows no effect on the activation by plasmin, kcat (1/sec) (hippuryl-arginine, activated by plasmin): 0.00043, Km (mM) (hippuryl-arginine, activated by plasmin): 0.00001, intrinsic stability of activated TAFI (half-life): 6.3 min | Homo sapiens |
| 3.4.17.20 | additional information | variant mutants are constructed and expressed mutant variants that have key substitutions in the amino acids surrounding the scissile Arg92-Ala93 bond. Variants are identified that show patterns of resistance to specific activators. The variants that are tested also showed antifibrinolytic potentials that can be rationalized in terms of which enzymes are capable of activating them | Homo sapiens |
| 3.4.17.20 | P91S | mutant exhibits specific impairment of activation by thrombin or thrombin-TM, thrombin alone, and thrombin alone or plasmin, respectively | Homo sapiens |
| 3.4.17.20 | P91S | mutant is not activated by thrombin or by thrombin in the presence of thrombomodulin, mutant is weakly activated by plasmin, kcat (1/sec) (hippuryl-arginine, activated by plasmin): 0.00020, Km (mM) (hippuryl-arginine, activated by plasmin): 0.000007, intrinsic stability of activated TAFI (half-life): 6.3 min | Homo sapiens |
| 3.4.17.20 | R92K | mutant exhibits specific impairment of activation by thrombin or thrombin-TM, thrombin alone, and thrombin alone or plasmin, respectively | Homo sapiens |
| 3.4.17.20 | R92K | mutant is not activated by thrombin, mutant is very efficiently activated by thrombin in the presence of thrombomodulin, kcat (1/sec) (p-anisylazoformyl-L-arginine, activated by thrombin in the presence of thrombomodulin): 0.215, Km (mM) (p-anisylazoformyl-L-arginine, activated by thrombin in the presence of thrombomodulin): 0.000229, mutant is activated by plasmin with similar kinetics as wild-type, kcat (1/sec) (hippuryl-arginine, activated by plasmin): 0.00039, Km (mM) (hippuryl-arginine, activated by plasmin): 0.000006, intrinsic stability of activated TAFI (half-life): 7.1 min | Homo sapiens |
| 3.4.17.20 | S90D/S94V/S90D | mutant is not activated by thrombin or by thrombin in the presence of thrombomodulin, mutant is weakly activated by plasmin, kcat (1/sec) (hippuryl-arginine, activated by plasmin): 0.00004, Km (mM) (hippuryl-arginine, activated by plasmin): 0.000005, intrinsic stability of activated TAFI (half-life): 5.9 min | Homo sapiens |
| 3.4.17.20 | S90P | mutant exhibits specific impairment of activation by thrombin or thrombin-TM, thrombin alone, and thrombin alone or plasmin, respectively | Homo sapiens |
| 3.4.17.20 | S90P | mutant is not activated by thrombin, mutant is very efficiently activated by thrombin in the presence of thrombomodulin, kcat (1/sec) (p-anisylazoformyl-L-arginine, activated by thrombin in the presence of thrombomodulin): 0.377, Km (mM) (p-anisylazoformyl-L-arginine, activated by thrombin in the presence of thrombomodulin): 0.000162, mutant is weakly activated by plasmin, kcat (1/sec) (hippuryl-arginine, activated by plasmin): 0.00008, Km (mM) (hippuryl-arginine, activated by plasmin): 0.000009, intrinsic stability of activated TAFI (half-life): 5.5 min | Homo sapiens |
| 3.4.17.20 | S94V | mutant is considerably more effectively activated by thrombin, mutant is also activated by thrombin in the presence of thrombomodulin, kcat (1/sec) (p-anisylazoformyl-L-arginine, activated by thrombin in the presence of thrombomodulin): 0.328, Km (mM) (p-anisylazoformyl-L-arginine, activated by thrombin in the presence of thrombomodulin): 0.000232, mutation shows no effect on the activation by plasmin, kcat (1/sec) (hippuryl-arginine, activated by plasmin): 0.0003, Km (mM) (hippuryl-arginine, activated by plasmin): 0.000006, intrinsic stability of activated TAFI (half-life): 6.1 min | Homo sapiens |
General Stability
| EC Number | General Stability | Organism |
|---|---|---|
| 3.4.17.20 | intrinsic stability of activated TAFI (half-life): 6.8 min (wild-type) | Homo sapiens |
KM Value [mM]
| EC Number | KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 3.4.17.20 | 0.000005 | - |
hippuryl-arginine | mutant S90D/S94V/S90D, activation of TAFI by plasmin | Homo sapiens |  |
| 3.4.17.20 | 0.000005 | - |
hippuryl-arginine | wild-type, activation of TAFI by plasmin | Homo sapiens | |
| 3.4.17.20 | 0.000006 | - |
hippuryl-arginine | mutant R92K, activation of TAFI by plasmin | Homo sapiens | |
| 3.4.17.20 | 0.000006 | - |
hippuryl-arginine | mutant S94V, activation of TAFI by plasmin | Homo sapiens | |
| 3.4.17.20 | 0.000007 | - |
hippuryl-arginine | mutant P91S, activation of TAFI by plasmin | Homo sapiens | |
| 3.4.17.20 | 0.000009 | - |
hippuryl-arginine | mutant S90P, activation of TAFI by plasmin | Homo sapiens | |
| 3.4.17.20 | 0.00001 | - |
hippuryl-arginine | mutant A93V, activation of TAFI by plasmin | Homo sapiens | |
| 3.4.17.20 | 0.000162 | - |
p-anisylazoformyl-L-arginine | mutant S90P, activation of TAFI by thrombin in the presence of thrombomodulin | Homo sapiens | |
| 3.4.17.20 | 0.000169 | - |
p-anisylazoformyl-L-arginine | mutant A93V, activation of TAFI by thrombin in the presence of thrombomodulin | Homo sapiens | |
| 3.4.17.20 | 0.000178 | - |
p-anisylazoformyl-L-arginine | wild-type, activation of TAFI by thrombin in the presence of thrombomodulin | Homo sapiens | |
| 3.4.17.20 | 0.000229 | - |
p-anisylazoformyl-L-arginine | mutant R92K, activation of TAFI by thrombin in the presence of thrombomodulin | Homo sapiens | |
| 3.4.17.20 | 0.000232 | - |
p-anisylazoformyl-L-arginine | mutant S94V, activation of TAFI by thrombin in the presence of thrombomodulin | Homo sapiens | |
| 3.4.21.5 | 0.000178 | - |
thrombin-activatable fibrinolysis inhibitor | presence of thrombomodulin, Km(app) value | Homo sapiens | |
| 3.4.21.7 | 0.005 | - |
thrombin-activatable fibrinolysis inhibitor | - |
Homo sapiens |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 3.4.17.20 | Homo sapiens | - |
- |
- |
| 3.4.21.5 | Homo sapiens | - |
- |
- |
| 3.4.21.7 | Homo sapiens | - |
- |
- |
Purification (Commentary)
| EC Number | Purification (Comment) | Organism |
|---|---|---|
| 3.4.17.20 | using immunoaffinity chromatography in which monoclonal antibody MA-T4E3 is coupled to CNBr-activated Sepharose 4B | Homo sapiens |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.4.17.20 | hippuryl-arginine + H2O | substrate is used to measure the TAFI activation by plasmin | Homo sapiens | hippuric acid + L-arginine | - |
? | |
| 3.4.17.20 | p-anisylazoformyl-L-arginine + H2O | substrate is used to measure the TAFI activation by thrombin and thrombin-thrombomodulin | Homo sapiens | p-anisylazoformic acid + L-arginine | - |
? | |
| 3.4.21.5 | additional information | protein context, as well as the identity of amino acids at protease cleavage sites, dictate protease specificity | Homo sapiens | ? | - |
? | |
| 3.4.21.5 | thrombin-activatable fibrinolysis inhibitor + H2O | mutant variants with variants in the amino acids surrounding the scissile R92-A93 bond such as P91S, R92K, and S90P exhibit specific impairment of activation by thrombin or thrombin/thrombomodulin | Homo sapiens | ? | - |
? | |
| 3.4.21.7 | additional information | protein context, as well as the identity of amino acids at protease cleavage sites, dictate protease specificity | Homo sapiens | ? | - |
? | |
| 3.4.21.7 | thrombin-activatable fibrinolysis inhibitor + H2O | mutant variants with variants in the amino acids surrounding the scissile R92-A93 bond such as P91S, R92K, and S90P exhibit specific impairment of activation by plasmin | Homo sapiens | ? | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 3.4.17.20 | TAFI | - |
Homo sapiens |
| 3.4.17.20 | thrombin-activatable fibrinolysis inhibitor | - |
Homo sapiens |
Turnover Number [1/s]
| EC Number | Turnover Number Minimum [1/s] | Turnover Number Maximum [1/s] | Substrate | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 3.4.17.20 | 0.00004 | - |
hippuryl-arginine | mutant S90D/S94V/S90D, activation of TAFI by plasmin | Homo sapiens | |
| 3.4.17.20 | 0.00008 | - |
hippuryl-arginine | mutant S90P, activation of TAFI by plasmin | Homo sapiens | |
| 3.4.17.20 | 0.0002 | - |
hippuryl-arginine | mutant P91S, activation of TAFI by plasmin | Homo sapiens | |
| 3.4.17.20 | 0.0003 | - |
hippuryl-arginine | mutant S94V, activation of TAFI by plasmin | Homo sapiens | |
| 3.4.17.20 | 0.00039 | - |
hippuryl-arginine | mutant R92K, activation of TAFI by plasmin | Homo sapiens | |
| 3.4.17.20 | 0.00042 | - |
hippuryl-arginine | wild-type, activation of TAFI by plasmin | Homo sapiens | |
| 3.4.17.20 | 0.00043 | - |
hippuryl-arginine | mutant A93V, activation of TAFI by plasmin | Homo sapiens | |
| 3.4.17.20 | 0.205 | - |
p-anisylazoformyl-L-arginine | mutant A93V, activation of TAFI by thrombin in the presence of thrombomodulin | Homo sapiens | |
| 3.4.17.20 | 0.215 | - |
p-anisylazoformyl-L-arginine | mutant R92K, activation of TAFI by thrombin in the presence of thrombomodulin | Homo sapiens | |
| 3.4.17.20 | 0.315 | - |
p-anisylazoformyl-L-arginine | wild-type, activation of TAFI by thrombin in the presence of thrombomodulin | Homo sapiens | |
| 3.4.17.20 | 0.328 | - |
p-anisylazoformyl-L-arginine | mutant S94V, activation of TAFI by thrombin in the presence of thrombomodulin | Homo sapiens | |
| 3.4.17.20 | 0.377 | - |
p-anisylazoformyl-L-arginine | mutant S90P, activation of TAFI by thrombin in the presence of thrombomodulin | Homo sapiens | |
| 3.4.21.5 | 0.315 | - |
thrombin-activatable fibrinolysis inhibitor | presence of thrombomodulin, kcat(app) value | Homo sapiens | |
| 3.4.21.7 | 0.00042 | - |
thrombin-activatable fibrinolysis inhibitor | - |
Homo sapiens |
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