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2bz6

From Proteopedia

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[[Category: serine protease]]
[[Category: serine protease]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 12:30:37 2007''
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 16:52:59 2007''

Revision as of 14:48, 30 October 2007

Image:2bz6.gif

2bz6, resolution 1.60Å

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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.

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]. Structure known Active 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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