2bz6

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==Overview==
==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.
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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==Disease==
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Known diseases associated with this structure: Factor VII deficiency OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=227500 227500]], Myocardial infarction, decreased susceptibility to OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=227500 227500]]
==About this Structure==
==About this Structure==
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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 Mon Nov 5 17:53:45 2007''
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 21:08:20 2007''

Revision as of 19:01, 12 November 2007


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 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

Page seeded by OCA on Mon Nov 12 21:08:20 2007

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