In silico Discovery of Novel FXa Inhibitors by Pharmacophore Modeling and Molecular Docking
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DOI: 10.1007/s13659-017-0126-x
Abstract: Coagulation Factor Xa (FXa) is the crucial enzyme at the convergent point of the intrinsic and extrinsic coagulation pathways. The inhibition of FXa is an effective approach against thrombotic diseases. In the present study, a… read more here.
Keywords: fxa inhibitors; fxa; discovery novel; silico discovery ... See more keywords
Design, synthesis and biological evaluation of novel 2,3-dihydroquinazolin- 4(1H)-one derivatives as potential fXa inhibitors.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2016.09.055
Abstract: Coagulation factor Xa (fXa) is a particularly attractive target for the development of effective and safe anticoagulants. In this study, novel 2,3-dihydroquinazolin-4(1H)-one derivatives were designed as potential fXa inhibitors based on anthranilamide structure which has… read more here.
Keywords: fxa inhibitors; fxa; one derivatives; dihydroquinazolin one ... See more keywords
Engineering and evaluation of FXa bypassing agents that restore hemostasis following Apixaban associated bleeding
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DOI: 10.1038/s41467-024-48278-1
Abstract: Direct oral anticoagulants (DOACs) targeting activated factor Xa (FXa) are used to prevent or treat thromboembolic disorders. DOACs reversibly bind to FXa and inhibit its enzymatic activity. However, DOAC treatment carries the risk of anticoagulant-associated… read more here.
Keywords: engineering evaluation; associated bleeding; fxa; evaluation fxa ... See more keywords
Rivaroxaban, a specific FXa inhibitor, improved endothelium-dependent relaxation of aortic segments in diabetic mice
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DOI: 10.1038/s41598-019-47474-0
Abstract: Activated factor X (FXa) plays a central role in the coagulation cascade, while it also mediates vascular function through activation of protease-activated receptors (PARs). Here, we examined whether inhibition of FXa by rivaroxaban, a direct… read more here.
Keywords: fxa; rivaroxaban; fxa inhibitor; mice ... See more keywords
BFPI: A Minimal Prothrombinase Inhibitor from the Saliva of Simulium Vittatum
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DOI: 10.1182/blood-2018-99-118666
Abstract: Background: The black fly, Simulium Vittatum, has an anticoagulant protein in its saliva that allows it to feed on mammalian blood (black fly protease inhibitor; BFPI). Remarkably, BFPI is similar to the human anticoagulant tissue… read more here.
Keywords: bfpi; fxa; inhibitor; inhibition ... See more keywords
Comparison of reversal activity and mechanism of action of UHRA, andexanet, and PER977 on heparin and oral FXa inhibitors.
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DOI: 10.1182/bloodadvances.2016003616
Abstract: Anticoagulants such as unfractionated heparin (UFH), low-molecular-weight heparins (LMWHs), fondaparinux, and direct oral anticoagulants (DOACs) targeting thrombin (IIa) or factor Xa (FXa) are widely used in prevention and treatment of thromboembolic disorders. However, anticoagulant-associated bleeding… read more here.
Keywords: fxa inhibitors; fxa; uhra andexanet; per977 ... See more keywords
Andexanet alfa: a recombinant mimetic of human factor Xa for the reversal of anticoagulant therapies.
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DOI: 10.1358/dot.2017.53.5.2630780
Abstract: Activated coagulation factor X (FXa) is a common target for classic and newer anticoagulants. Parenteral anticoagulants with an indirect inhibitory action on FXa (low-molecular-weight heparins) have a well-established clinical efficacy in the prophylaxis and therapy… read more here.
Keywords: fxa; anticoagulant therapies; reversal anticoagulant; alfa ... See more keywords
Andexanet alfa effectively reverses edoxaban anticoagulation effects and associated bleeding in a rabbit acute hemorrhage model
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DOI: 10.1371/journal.pone.0195122
Abstract: Introduction Increasing use of factor Xa (FXa) inhibitors necessitates effective reversal agents to manage bleeding. Andexanet alfa, a novel modified recombinant human FXa, rapidly reverses the anticoagulation effects of direct and indirect FXa inhibitors. Objective… read more here.
Keywords: anticoagulation; fxa; andexanet; anti fxa ... See more keywords