Results 211 to 220 of about 40,684 (247)
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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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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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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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1992
The assembly and function of the prothrombinase complex on the bovine and human platelet membrane is mediated through binding interactions in which factor Va bound to the platelet surface forms at least part of the "receptor" for factor Xa in a 1:1 stoichiometric complex. A model depicting these binding interactions is shown in Fig. 12.
P B, Tracy, M E, Nesheim, K G, Mann
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The assembly and function of the prothrombinase complex on the bovine and human platelet membrane is mediated through binding interactions in which factor Va bound to the platelet surface forms at least part of the "receptor" for factor Xa in a 1:1 stoichiometric complex. A model depicting these binding interactions is shown in Fig. 12.
P B, Tracy, M E, Nesheim, K G, Mann
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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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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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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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Current Pharmaceutical Design, 1996
Thrombin occupies a central position in thrombus formation and eventually has been a target to develop anticoagulant agents. Although both heparin and warfarin have been used as anticoagulants, a more useful, ideal anticoagulant is desired at bedside.
Satoshi Kunitada, Takayasu Nagahara
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Thrombin occupies a central position in thrombus formation and eventually has been a target to develop anticoagulant agents. Although both heparin and warfarin have been used as anticoagulants, a more useful, ideal anticoagulant is desired at bedside.
Satoshi Kunitada, Takayasu Nagahara
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2023
This chapter describes factor Xa as a key enzyme involved in thrombosis and clot formation. It considers factor Xa inhibitors as potential anticoagulants for the treatment of deep-vein thrombosis and pulmonary embolism. It also highlights the first factor Xa inhibitors to reach the market and covers the design process that led to the discovery of ...
openaire +1 more source
This chapter describes factor Xa as a key enzyme involved in thrombosis and clot formation. It considers factor Xa inhibitors as potential anticoagulants for the treatment of deep-vein thrombosis and pulmonary embolism. It also highlights the first factor Xa inhibitors to reach the market and covers the design process that led to the discovery of ...
openaire +1 more source