2bz6

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[[Image:2bz6.gif|left|200px]]<br /><applet load="2bz6" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:2bz6.gif|left|200px]]
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caption="2bz6, resolution 1.60&Aring;" />
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'''ORALLY AVAILABLE FACTOR7A INHIBITOR'''<br />
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{{Structure
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|PDB= 2bz6 |SIZE=350|CAPTION= <scene name='initialview01'>2bz6</scene>, resolution 1.60&Aring;
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|SITE= <scene name='pdbsite=AC1:So4+Binding+Site+For+Chain+H'>AC1</scene>
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|LIGAND= <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene> and <scene name='pdbligand=346:(R)-(4-CARBAMIMIDOYL-PHENYLAMINO)-[5-ETHOXY-2-FLUORO-3-[(R)-TETRAHYDRO-FURAN-3-YLOXY]-PHENYL]-ACETIC ACID'>346</scene>
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|ACTIVITY= [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]
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|GENE=
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}}
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'''ORALLY AVAILABLE FACTOR7A INHIBITOR'''
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==Overview==
==Overview==
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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 <scene name='pdbligand=SO4:'>SO4</scene>, <scene name='pdbligand=CA:'>CA</scene> and <scene name='pdbligand=346:'>346</scene> 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] Known structural/functional Site: <scene name='pdbsite=AC1:So4+Binding+Site+For+Chain+H'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2BZ6 OCA].
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2BZ6 is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2BZ6 OCA].
==Reference==
==Reference==
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16621574 16621574]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/16621574 16621574]
[[Category: Coagulation factor VIIa]]
[[Category: Coagulation factor VIIa]]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: serine protease]]
[[Category: serine protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:43:12 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 16:08:39 2008''

Revision as of 14:08, 20 March 2008

Image:2bz6.gif


PDB ID 2bz6

Drag the structure with the mouse to rotate
, resolution 1.60Å
Sites:
Ligands: , and
Activity: Coagulation factor VIIa, with EC number 3.4.21.21
Coordinates: save as pdb, mmCIF, xml



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. 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 Thu Mar 20 16:08:39 2008

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