Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary extracted from

  • Leadley, R.J., Jr.
    Coagulation factor Xa inhibition: biological background and rationale (2001), Curr. Top. Med. Chem., 1, 151-159.
    View publication on PubMed

Application

EC Number Application Comment Organism
3.4.21.6 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

EC Number Inhibitors Comment Organism Structure
3.4.21.6 antistasin naturally occurring inhibitor, anticoagulant isolated from Mexican leech Haementeria officinalis, slow, tight-binding, selective inhibitor protein Homo sapiens
3.4.21.6 CI-1031 i.e. ZK-807834, small molecule direct inhibitor of facor Xa, prevention of thrombosis when administered in vivo Canis lupus familiaris
3.4.21.6 CI-1031 i.e. ZK-807834, small molecule direct inhibitor of facor Xa Homo sapiens
3.4.21.6 DX9065a small, potent and selective direct inhibitor of fXa, prevents thrombosis in vivo Homo sapiens
3.4.21.6 FXV673 small molecule direct inhibitor of facor Xa, prevention of thrombosis when administered in vivo Canis lupus familiaris
3.4.21.6 FXV673 small molecule direct inhibitor of facor Xa Homo sapiens
3.4.21.6 heparin alos induces thrombocytopenia Homo sapiens
3.4.21.6 heparin pentasaccharide
-
Homo sapiens
3.4.21.6 RPR120844 potent direct inhibitor, overview over effects in vivo Homo sapiens
3.4.21.6 RPR208566 potent direct inhibitor, overview over effects in vivo Homo sapiens
3.4.21.6 SK549 potent direct inhibitor, overview over effects in vivo Homo sapiens
3.4.21.6 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
3.4.21.6 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
3.4.21.6 warfarin
-
Homo sapiens
3.4.21.6 YM-60828 potent direct inhibitor, overview over effects in vivo Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.4.21.6 extracellular
-
Homo sapiens
-
-
3.4.21.6 extracellular
-
Canis lupus familiaris
-
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.4.21.6 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 ?
-
?
3.4.21.6 additional information Canis lupus familiaris the enzyme is responsible for clot-associated procoagulant activity ?
-
?
3.4.21.6 prothrombin + H2O Homo sapiens procoagulant activity thrombin + ?
-
?
3.4.21.6 prothrombin + H2O Canis lupus familiaris procoagulant activity thrombin + ?
-
?

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.6 Canis lupus familiaris
-
dog
-
3.4.21.6 Homo sapiens
-
-
-

Reaction

EC Number Reaction Comment Organism Reaction ID
3.4.21.6 selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin scutelarin has similar specificity Homo sapiens
3.4.21.6 selective cleavage of Arg-/-Thr and then Arg-/-Ile bonds in prothrombin to form thrombin scutelarin has similar specificity Canis lupus familiaris

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.6 thrombus enzyme associated with thrombi is enzymatically active Homo sapiens
-
3.4.21.6 thrombus enzyme associated with thrombi is enzymatically active Canis lupus familiaris
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.6 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 ?
-
?
3.4.21.6 additional information the enzyme is responsible for clot-associated procoagulant activity Canis lupus familiaris ?
-
?
3.4.21.6 prothrombin + H2O
-
Homo sapiens thrombin + ?
-
?
3.4.21.6 prothrombin + H2O
-
Canis lupus familiaris thrombin + ?
-
?
3.4.21.6 prothrombin + H2O procoagulant activity Homo sapiens thrombin + ?
-
?
3.4.21.6 prothrombin + H2O procoagulant activity Canis lupus familiaris thrombin + ?
-
?

Synonyms

EC Number Synonyms Comment Organism
3.4.21.6 coagulation factor Xa
-
Homo sapiens
3.4.21.6 coagulation factor Xa
-
Canis lupus familiaris
3.4.21.6 factor Xa
-
Homo sapiens
3.4.21.6 factor Xa
-
Canis lupus familiaris
3.4.21.6 FXa
-
Homo sapiens
3.4.21.6 FXa
-
Canis lupus familiaris
3.4.21.6 More the enzyme belongs to the peptidase family S1, i.e. trypsin family Homo sapiens
3.4.21.6 More the enzyme belongs to the peptidase family S1, i.e. trypsin family Canis lupus familiaris

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.6 0.0000003 0.0000006 antistasin
-
Homo sapiens
3.4.21.6 0.0000005
-
tick anticoagulant peptide
-
Homo sapiens