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PDBsum entry 2bz6
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References listed in PDB file
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Key reference
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Title
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Dose-Dependent antithrombotic activity of an orally active tissue factor/factor viia inhibitor without concomitant enhancement of bleeding propensity.
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Authors
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K.Groebke zbinden,
D.W.Banner,
K.Hilpert,
J.Himber,
T.Lavé,
M.A.Riederer,
M.Stahl,
T.B.Tschopp,
U.Obst-Sander.
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Ref.
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Bioorg Med Chem Lett, 2006,
14,
5357-5369.
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PubMed id
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Abstract
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The discovery of a highly potent and selective tissue factor/factor VIIa
inhibitor is described. Upon oral administration of its double prodrug in the
guinea pig, a dose-dependent antithrombotic effect is observed in an established
model of arterial thrombosis without prolonging bleeding time. The
pharmacodynamic properties of this selective inhibitor are compared to the
behaviour of a mixed factor VIIa/factor Xa inhibitor.
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