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Synthetic inhibitors of coagulation factor Xa
Expert Opinion on Investigational Drugs, 1999The antithrombotic efficacy of low molecular weight heparins suggest that specific inhibition of blood coagulation factor Xa (fXa) is an appropriate target for drug discovery. Clinical evidence also supports the effectiveness of warfarin, an orally bioavailable non-specific anticoagulant.
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European Journal of Clinical Investigation, 2005
P, Bramlage, D, Pittrow, W, Kirch
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P, Bramlage, D, Pittrow, W, Kirch
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Heparin-Binding Exosite of Factor Xa
Trends in Cardiovascular Medicine, 2000Recent studies have indicated that the basic residues Arg(93), Lys(96), Arg(125), Arg(165), Lys(169), Lys(236), and Arg(240) (chymotrypsin numbering) constitute an exosite in the catalytic domain of factor Xa that can effectively bind heparin only if the acidic N-terminal Gla domain of the proteinase was neutralized by physiological levels of calcium ...
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Preservation of factor Xa activity
Thrombosis Research, 1978V Y, Wu, W H, Seegers
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Factor Xa inhibitors (Berlex).
IDrugs : the investigational drugs journal, 2005Berlex Biosciences is investigating several series of Factor Xa inhibitors aimed at the prevention and treatment of thrombotic disorders [297584]. Some compounds are based on the structure of ZK-805412, a Z,Z-2,7-bis(dibenzylidene)cycloheptanone, which showed nanomolar Factor Xa inhibitor potency [301618].
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