HD1, a thrombin- and prothrombin-binding DNA aptamer, inhibits thrombin generation by attenuating prothrombin activation and thrombin feedback reactions

HD1, a DNA aptamer, binds exosite 1 on thrombin and blocks its clotting activity. Because HD1 also binds prothrombin and inhibits its activation by prothrombinase, we hypothesised that HD1 would be a more potent inhibitor of coagulation than other exosite 1-directed ligands, such as Hir54–65(SO3-)....

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Veröffentlicht in:	Thrombosis and haemostasis 2010-01, Vol.103 (1), p.83-93
Hauptverfasser:	Kretz, Colin A., Cuddy, Karl R., Stafford, Alan R., Fredenburgh, James C., Roberts, Robin, Weitz, Jeffrey I.
Format:	Artikel
Sprache:	eng
Schlagworte:	Anticoagulants - metabolism Anticoagulants - pharmacology Antithrombins - metabolism Aptamer Aptamers, Nucleotide - metabolism Aptamers, Nucleotide - pharmacology Binding Sites Biological and medical sciences Blood Coagulation - drug effects Blood Coagulation, Fibrinolysis and Cellular Haemostasis Blood coagulation. Blood cells cofactor activation Dose-Response Relationship, Drug Down-Regulation Factor Va - metabolism Factor VIIIa - metabolism Feedback, Physiological Fundamental and applied biological sciences. Psychology Hematologic and hematopoietic diseases Heparin Cofactor II - metabolism Hirudins - metabolism Hirudins - pharmacology Humans Kinetics Medical sciences Molecular and cellular biology Oligopeptides - metabolism Oligopeptides - pharmacology Partial Thromboplastin Time Platelet diseases and coagulopathies Prothrombin - metabolism Prothrombin Time Prothrombinase Sulfates - metabolism Sulfates - pharmacology thrombin Thrombin - metabolism thrombin generation assay Thromboplastin - metabolism
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