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Literature summary for 3.4.21.6 extracted from
- Coagulation factor Xa inhibition: biological background and rationale (2001), Curr. Top. Med. Chem., 1, 151-159.
Application
| Application | Comment | Organism |
|---|---|---|
| pharmacology | factor Xa is a therapeutic target for development of potent and selective direct enzyme inhibitors as antithrombotic compounds for the improved therapy of ischemic heart disease and cerebrovascular disease, no bleeding effect, only modest change in markers of systemic anticoagulation, use of animal models, overview | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| antistasin | naturally occurring inhibitor, anticoagulant isolated from Mexican leech Haementeria officinalis, slow, tight-binding, selective inhibitor protein | Homo sapiens | |
| CI-1031 | i.e. ZK-807834, small molecule direct inhibitor of facor Xa, prevention of thrombosis when administered in vivo | Canis lupus familiaris |  |
| CI-1031 | i.e. ZK-807834, small molecule direct inhibitor of facor Xa | Homo sapiens | |
| DX9065a | small, potent and selective direct inhibitor of fXa, prevents thrombosis in vivo | Homo sapiens | |
| FXV673 | small molecule direct inhibitor of facor Xa, prevention of thrombosis when administered in vivo | Canis lupus familiaris | |
| FXV673 | small molecule direct inhibitor of facor Xa | Homo sapiens | |
| heparin | alos induces thrombocytopenia | Homo sapiens | |
| heparin pentasaccharide | - |
Homo sapiens | |
| RPR120844 | potent direct inhibitor, overview over effects in vivo | Homo sapiens | |
| RPR208566 | potent direct inhibitor, overview over effects in vivo | Homo sapiens | |
| SK549 | potent direct inhibitor, overview over effects in vivo | Homo sapiens | |
| SR90107A/ORG31540 | synthetic pentasaccharide, selective, antithrombin-III dependent factor Xa inhibitor, inhibition of platelet and fibrin deposition onshunts in vivo, prevention of thrombosis | Homo sapiens | |
| tick anticoagulant peptide | i.e. TAP, 60 amino acid peptide, isolated from the tick Ornithodoros moubata, reversible, slow, tight-binding inhibitor, short-term inhibition of clot-associated procoagulant activity in vitro and in vivo | Homo sapiens | |
| warfarin | - |
Homo sapiens | |
| YM-60828 | potent direct inhibitor, overview over effects in vivo | Homo sapiens | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| extracellular | - |
Homo sapiens | - |
- |
| extracellular | - |
Canis lupus familiaris | - |
- |
Natural Substrates/ Products (Substrates)
| Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | Homo sapiens | properties of and indications for different enzyme inhibitors, overview, the enzyme is responsible for clot-associated procoagulant activity, enzyme inhibition lead to reduced platelet deposition and aggregation at thrombic sites | ? | - |
? | |
| additional information | Canis lupus familiaris | the enzyme is responsible for clot-associated procoagulant activity | ? | - |
? | |
| prothrombin + H2O | Homo sapiens | procoagulant activity | thrombin + ? | - |
? | |
| prothrombin + H2O | Canis lupus familiaris | procoagulant activity | thrombin + ? | - |
? | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Canis lupus familiaris | - |
dog | - |
| Homo sapiens | - |
- |
- |
Reaction
| Reaction | Comment | Organism | Reaction ID |
|---|---|---|---|
| selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin | scutelarin has similar specificity | Homo sapiens | |
| selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin | scutelarin has similar specificity | Canis lupus familiaris |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| thrombus | enzyme associated with thrombi is enzymatically active | Homo sapiens | - |
| thrombus | enzyme associated with thrombi is enzymatically active | Canis lupus familiaris | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| additional information | properties of and indications for different enzyme inhibitors, overview, the enzyme is responsible for clot-associated procoagulant activity, enzyme inhibition lead to reduced platelet deposition and aggregation at thrombic sites | Homo sapiens | ? | - |
? | |
| additional information | the enzyme is responsible for clot-associated procoagulant activity | Canis lupus familiaris | ? | - |
? | |
| prothrombin + H2O | - |
Homo sapiens | thrombin + ? | - |
? | |
| prothrombin + H2O | - |
Canis lupus familiaris | thrombin + ? | - |
? | |
| prothrombin + H2O | procoagulant activity | Homo sapiens | thrombin + ? | - |
? | |
| prothrombin + H2O | procoagulant activity | Canis lupus familiaris | thrombin + ? | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| coagulation factor Xa | - |
Homo sapiens |
| coagulation factor Xa | - |
Canis lupus familiaris |
| factor Xa | - |
Homo sapiens |
| factor Xa | - |
Canis lupus familiaris |
| FXa | - |
Homo sapiens |
| FXa | - |
Canis lupus familiaris |
| More | the enzyme belongs to the peptidase family S1, i.e. trypsin family | Homo sapiens |
| More | the enzyme belongs to the peptidase family S1, i.e. trypsin family | Canis lupus familiaris |
Ki Value [mM]
| Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|
| 0.0000003 | 0.0000006 | antistasin | - |
Homo sapiens | |
| 0.0000005 | - |
tick anticoagulant peptide | - |
Homo sapiens |
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