2bz6: Difference between revisions
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'''ORALLY AVAILABLE FACTOR7A INHIBITOR''' | '''ORALLY AVAILABLE FACTOR7A INHIBITOR''' | ||
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[[Category: Weber, L.]] | [[Category: Weber, L.]] | ||
[[Category: Wessel, H P.]] | [[Category: Wessel, H P.]] | ||
[[Category: | [[Category: Serine protease,coagulation,enzyme complex,hydrolase]] | ||
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Revision as of 18:00, 3 May 2008
ORALLY AVAILABLE FACTOR7A INHIBITOR
Overview
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.
About this Structure
2BZ6 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Dose-dependent antithrombotic activity of an orally active tissue factor/factor VIIa inhibitor without concomitant enhancement of bleeding propensity., Groebke Zbinden K, Banner DW, Hilpert K, Himber J, Lave T, Riederer MA, Stahl M, Tschopp TB, Obst-Sander U, Bioorg Med Chem. 2006 Aug 1;14(15):5357-69. Epub 2006 Apr 18. PMID:16621574 Page seeded by OCA on Sat May 3 21:00:09 2008