2bz6: Difference between revisions
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==Overview== | ==Overview== | ||
The discovery of a highly potent and selective tissue factor/factor VIIa | 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. | ||
==Disease== | ==Disease== | ||
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[[Category: Ackermann, J.]] | [[Category: Ackermann, J.]] | ||
[[Category: Alig, L.]] | [[Category: Alig, L.]] | ||
[[Category: Banner, D | [[Category: Banner, D W.]] | ||
[[Category: Boehm, H | [[Category: Boehm, H J.]] | ||
[[Category: Groebke-Zbinden, K.]] | [[Category: Groebke-Zbinden, K.]] | ||
[[Category: Hilpert, K.]] | [[Category: Hilpert, K.]] | ||
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[[Category: Riederer, M.]] | [[Category: Riederer, M.]] | ||
[[Category: Stahl, M.]] | [[Category: Stahl, M.]] | ||
[[Category: Tschopp, T | [[Category: Tschopp, T B.]] | ||
[[Category: Weber, L.]] | [[Category: Weber, L.]] | ||
[[Category: Wessel, H | [[Category: Wessel, H P.]] | ||
[[Category: 346]] | [[Category: 346]] | ||
[[Category: CA]] | [[Category: CA]] | ||
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[[Category: serine protease]] | [[Category: serine protease]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:43:12 2008'' | ||
Revision as of 14:43, 21 February 2008
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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.
Disease
Known diseases associated with this structure: Factor VII deficiency OMIM:[227500], Myocardial infarction, decreased susceptibility to OMIM:[227500]
About this Structure
2BZ6 is a Single protein structure of sequence from Homo sapiens with SO4, CA and 346 as ligands. Active as Coagulation factor VIIa, with EC number 3.4.21.21 Known structural/functional Site: AC1. 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
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