2bz6

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==About this Structure==
==About this Structure==
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2BZ6 is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with SO4, CA and 346 as [[http://en.wikipedia.org/wiki/ligands ligands]]. Active as [[http://en.wikipedia.org/wiki/Coagulation_factor_VIIa Coagulation factor VIIa]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.21 3.4.21.21]]. Structure known Active Site: AC1. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2BZ6 OCA]].
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2BZ6 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with SO4, CA and 346 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Coagulation_factor_VIIa Coagulation factor VIIa], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.21 3.4.21.21] Structure known Active Site: AC1. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2BZ6 OCA].
==Reference==
==Reference==
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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 16:52:59 2007''
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 5 14:01:50 2007''

Revision as of 11:56, 5 November 2007


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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