2bz6

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Image:2bz6.gif

2bz6, resolution 1.60Å

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ORALLY AVAILABLE FACTOR7A INHIBITOR

Contents

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: . 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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