Search Results - "Tschopp, Thomas B"
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Dose-dependent antithrombotic activity of an orally active tissue factor/factor VIIa inhibitor without concomitant enhancement of bleeding propensity
Published in Bioorganic & medicinal chemistry (01-08-2006)“…The discovery of a highly potent and selective tissue factor/factor VIIa inhibitor is described. Upon oral administration of its double prodrug in the guinea…”
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Selective and orally bioavailable phenylglycine tissue factor/factor VIIa inhibitors
Published in Bioorganic & medicinal chemistry letters (01-12-2005)“…We describe the structure-based design and synthesis of nanomolar, orally bioavailable tissue factor/factor VIIa inhibitors which interfere with the…”
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Can the calculation of ligand binding free energies be improved with continuum solvent electrostatics and an ideal‐gas entropy correction?
Published in Journal of computational chemistry (01-09-2002)“…The prediction of a ligand binding constant requires generating three‐dimensional structures of the complex concerned and reliably scoring these structures…”
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Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors
Published in Bioorganic & medicinal chemistry letters (01-02-2005)“…Proof of concept experiments have shown that tissue factor/factor VIIa inhibitors have antithrombotic activity without enhancing bleeding propensity. Starting…”
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Design and Synthesis of Potent and Highly Selective Thrombin Inhibitors
Published in Journal of medicinal chemistry (01-11-1994)“…Thrombin, a serine protease, plays a central role in the initiation and propagation of thrombotic events. An extensive search for new thrombin inhibitors was…”
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Dissociation of antithrombotic effect and bleeding time prolongation in rabbits by inhibiting tissue factor function
Published in Thrombosis and haemostasis (01-09-1997)“…Inhibition of the tissue factor/factor VIIa (TF/F.VIIa) complex attenuates thrombosis in different animal models of arterial thrombosis. However, it remains…”
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Active Site-Blocked Factors VIIa and IXa Differentially Inhibit Fibrin Formation in a Human Ex Vivo Thrombosis Model
Published in Arteriosclerosis, thrombosis, and vascular biology (01-08-1995)“…The role of tissue factor/factor VIIa (FVIIa) and factor VIIIa/factor IXa (FVIIIa/FIXa) complexes in thrombus formation was examined in a human ex vivo blood…”
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Activated clotting time as a appropriate test to compare heparin and direct thrombin inhibitors such as hirudin or Ro 46-6240 in experimental arterial thrombosis
Published in Circulation (New York, N.Y.) (01-03-1995)“…Specific thrombin inhibitors are considered to be more potent antithrombotics than heparin. However, the relation between the systemic anticoagulation…”
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Impaired interaction (adhesion-aggregation) of platelets with the subendothelium in storage-pool disease and after aspirin ingestion. A comparison with von Willebrand's disease
Published in The New England journal of medicine (25-09-1975)“…Possible defects in the interaction of platelets with the subendothelial surface were evaluated in six patients with storeage-pool disease, nine patients with…”
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Endothelial cells stimulated with tumor necrosis factor-alpha express varying amounts of tissue factor resulting in inhomogenous fibrin deposition in a native blood flow system. Effects of thrombin inhibitors
Published in The Journal of clinical investigation (01-05-1994)“…TNF-alpha induces changes in endothelial cell functions, such as upregulation of tissue factor, resulting in endothelial procoagulant activity which may play a…”
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Role of Collagen-Adherent Platelets in Mediating Fibrin Formation in Flowing Whole Blood
Published in Blood (15-11-1995)“…Activated platelets provide assembly sites for coagulation enzyme complexes and in this way can mediate coagulation during hemostasis and thrombosis. In this…”
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Relationship between tissue factor expression and deposition of fibrin, platelets, and leukocytes on cultured endothelial cells under venous blood flow conditions
Published in Blood (15-04-1993)“…Endothelial cell-mediated coagulation and leukocyte adhesion are processes that might be connected by the generation of thrombin. To examine the interaction of…”
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The heparin-like antiproliferative activity of sulfated tetrasaccharides is sensitive to structural variation
Published in Bioorganic & medicinal chemistry letters (02-03-1995)“…The sulfated tetrasaccharide β-maltosyl-(1→4)-α,α-trehalose 2 with high antiproliferative activity on smooth muscle cells was modified in the maltosyl moiety…”
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Heparin, carboxyl-reduced sulfated heparin, and Trestatin A sulfate. Antiproliferative and anticoagulant activities
Published in Carbohydrate research (05-09-1990)“…Human smooth muscle cells were used to investigate the antiproliferative activities of sulfated carbohydrates. The antiproliferative potencies of coarse…”
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The Development of Potent and Highly Selective Thrombin Inhibitors
Published in European journal of medicinal chemistry (1995)Get full text
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Platelet adhesion, release and aggregation in flowing blood: effects of surface properties and platelet function
Published in Thrombosis and haemostasis (01-01-1976)“…Platelet adhesion to natural and artificial surfaces and adhesion-induced aggregation were investigated in vitro using an annular perfusion chamber. The…”
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Hereditary Defect in Platelet Function in Rats
Published in Blood (01-08-1972)“…Hemostatic parameters of fawn- hooded (FH) rats with an inherited hemorrhagic diathesis were compared with those of normal rats. Prothrombin time, partial…”
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Platelet interaction with collagen fibrils in flowing blood. II. Impaired adhesion-aggregation in bleeding disorders. A comparison with subendothelium
Published in Thrombosis and haemostasis (28-02-1977)“…Anticoagulated whole blood from patients and control subjects was circulated through an annular perfusion chamber in which the fibrillar collagen of alpha…”
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