Results 211 to 220 of about 35,624 (244)
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Perspectives on Factor Xa Inhibition
Current Medicinal Chemistry, 2001Blood coagulation involves a complex cascade of enzymatic reactions, ultimately generating fibrin, the basis of all blood clots. This cascade is comprised of two arms, the intrinsic and extrinsic pathways which converge at factor Xa to form the common pathway.
R, Rai +3 more
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Perspectives in Drug Discovery and Design, 1994
Factor Xa is the serine protease that activates prothrombin to yield thrombin. Inhibitors of factor Xa play a crucial role in curtailing thrombin generation. Two key factor Xa inhibitors that are found in blood are antithrombin III and tissue factor pathway inhibitor.
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Factor Xa is the serine protease that activates prothrombin to yield thrombin. Inhibitors of factor Xa play a crucial role in curtailing thrombin generation. Two key factor Xa inhibitors that are found in blood are antithrombin III and tissue factor pathway inhibitor.
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Anti-factor Xa (Anti-Xa) Assay
2013The anti-factor Xa (anti-Xa) assay is a functional assay that facilitates the measurement of antithrombin (AT)-catalyzed inhibition of factor Xa by unfractionated heparin (UFH) and direct inhibition of factor Xa by low-molecular-weight heparin (LMWH) (Kitchen, Br J Haematol 111:397-406, 2000; Walenga et al., Semin Thromb Hemost 11:17-25, 1985; Levine ...
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Anthranilamide inhibitors of factor Xa
Bioorganic & Medicinal Chemistry Letters, 2007SAR about the B-ring of a series of N(2)-aroyl anthranilamide factor Xa (fXa) inhibitors is described. B-ring o-aminoalkylether and B-ring p-amine probes of the S1' and S4 sites, respectively, afforded picomolar fXa inhibitors that performed well in in vitro anticoagulation assays.
David, Mendel +20 more
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2023
Abstract Oral factor Xa (FXa) inhibitors exert their antithrombotic effects and increase the risk of bleeding by their effects on the coagulation system. The oral direct FXa inhibitors are highly potent, reversible active-site inhibitors of FXa with good bioavailability, rapid onset, and used in a daily standard dose without laboratory ...
Agneta Siegbahn +3 more
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Abstract Oral factor Xa (FXa) inhibitors exert their antithrombotic effects and increase the risk of bleeding by their effects on the coagulation system. The oral direct FXa inhibitors are highly potent, reversible active-site inhibitors of FXa with good bioavailability, rapid onset, and used in a daily standard dose without laboratory ...
Agneta Siegbahn +3 more
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2006
The importance of factor Xa in the initiation and propagation of coagulation, as well as its pluripotential cellular properties, has been discussed previously. Considered collectively, the effects exhibited by this particular protease make it an attractive target for pharmacologic inhibition. Factor Xa inhibition can be classified and subcategorized as
Richard C. Becker, Frederick A. Spencer
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The importance of factor Xa in the initiation and propagation of coagulation, as well as its pluripotential cellular properties, has been discussed previously. Considered collectively, the effects exhibited by this particular protease make it an attractive target for pharmacologic inhibition. Factor Xa inhibition can be classified and subcategorized as
Richard C. Becker, Frederick A. Spencer
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Protamine sulfate stimulates degradation of factor Xa and the factor Xa–antithrombin complex
Blood Coagulation & Fibrinolysis, 2011The effect of protamine sulfate on factor Xa (FXa) and the factor Xa-antithrombin complex was studied via SDS-PAGE and Western blot analysis. Human factor Xa [(FXaα) ∼52 kDa, FXaβ ∼47 kDa] and human antithrombin (AT ∼55 kDa) form a primary (1°) complex at 109 and 104 kDa, a secondary (2°) complex at 99 and 95 kDa, and a tertiary (3°) complex at 66 and ...
Martin H, Coggin +4 more
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Factor Xa-A Pleuripotential Protease
Journal of Thrombosis and Thrombolysis, 2003A current view of vascular thrombosis emphasizes the importance of cellular surface biochemistry and the integrated contribution of platelets, monocytes and endothelial cells that contribute to atherothrombosis. Initiation of coagulation occurs on tissue-factor bearing cells, while amplification (or priming) requires activation of platelets and ...
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Rivaroxaban: An Oral Factor Xa Inhibitor
Clinical Therapeutics, 2013Currently available anticoagulants utilized for venous thromboembolism (VTE) treatment and prevention and stroke prevention in patients with atrial fibrillation (AF) have proven effectiveness but are not optimally utilized because of barriers such as the need for subcutaneous administration and requisite routine laboratory monitoring.
Tyan F, Thomas +2 more
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Antidote for Factor Xa Anticoagulants
New England Journal of Medicine, 2015Oral anticoagulant options have exploded. Dabigatran, a direct thrombin inhibitor, was approved for use in the United States in 2010 for the prevention of stroke in patients with atrial fibrillation; this was rapidly followed by approval of the direct factor Xa inhibitors rivaroxaban, apixaban, and edoxaban within 5 years. The drive for the development
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