Results 341 to 350 of about 12,986,553 (373)
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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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Anticoagulation via anti-Factor Xa inhibition
Lupus, 2006Hospital-acquired deep vein thrombosis (DVT) affects 10-25% of medical patients and up to 60% of surgical patients. While thromboprophylaxis is without a doubt under utilized in the hospital setting, there is also a need for more efficacious agents. Fondaparinux, the first of a new class of agents Factor Xa inhibitiors, has recently come into clinical
N, Wiles, B J, Hunt
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Heterogeneity of Synthetic Factor Xa Inhibitors
Current Pharmaceutical Design, 2005Heparins and vitamin K antagonists are the landmarks of antithrombotic treatment. Both of them were discovered by serendipity; they are multi-targeted drugs and share several limitations. New molecules have been designed in order to be both more selective concerning their biological target and more homogeneous in their biochemical structure aiming at ...
Grigoris T, Gerotziafas, Meyer M, Samama
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Hämostaseologie, 2009
SummaryOral factor Xa (FXa) inhibitors are a promising alternative to current anticoagulants. This paper reviews the latest developments of oral direct FXa inhibitors and focuses on those which have been approved for the prevention of venous thromboembolism (VTE) after total hip or knee replacement or are in advanced development and have passed phase ...
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SummaryOral factor Xa (FXa) inhibitors are a promising alternative to current anticoagulants. This paper reviews the latest developments of oral direct FXa inhibitors and focuses on those which have been approved for the prevention of venous thromboembolism (VTE) after total hip or knee replacement or are in advanced development and have passed phase ...
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Tetrahydro-isoquinoline-Based Factor Xa Inhibitors
Journal of Medicinal Chemistry, 1998Derivatives of (2-amidino-1,2,3, 4-tetrahydro-isoquinolin-7-yloxy)phenylacetic acid (TIPAC) were developed as inhibitors of factor Xa (fXa). The compounds are prepared using 15 synthetic steps on average. The most potent compounds (14, 17, 22-26) display inhibition constants of Ki = 21-55 nM but do not inhibit thrombin (Ki = 5->100 microM) and only ...
R, Kucznierz +5 more
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Phenyltriazolinones as potent factor Xa inhibitors
Bioorganic & Medicinal Chemistry Letters, 2010We have discovered that phenyltriazolinone is a novel and potent P1 moiety for coagulation factor Xa. X-ray structures of the inhibitors with a phenyltriazolinone in the P1 position revealed that the side chain of Asp189 has reoriented resulting in a novel S1 binding pocket which is larger in size to accommodate the phenyltriazolinone P1 substrate.
Mimi L, Quan +12 more
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1999
Thrombin occupies a central position in thrombus formation and recently has been a target for the development of anticoagulant agents. As is well known, blood coagulation operates as a cascade or multiple enzymatic amplification process. In the classical intrinsic pathway, factor (f) IXa in the presence of fVIIIa, Ca2+ and phospholipid converts fX to ...
S. Kunitada, T. Nagahara, T. Hara
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Thrombin occupies a central position in thrombus formation and recently has been a target for the development of anticoagulant agents. As is well known, blood coagulation operates as a cascade or multiple enzymatic amplification process. In the classical intrinsic pathway, factor (f) IXa in the presence of fVIIIa, Ca2+ and phospholipid converts fX to ...
S. Kunitada, T. Nagahara, T. Hara
openaire +1 more source