2bz6: Difference between revisions
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[[Image:2bz6.gif|left|200px]]<br /><applet load="2bz6" size=" | [[Image:2bz6.gif|left|200px]]<br /><applet load="2bz6" size="350" color="white" frame="true" align="right" spinBox="true" | ||
caption="2bz6, resolution 1.60Å" /> | caption="2bz6, resolution 1.60Å" /> | ||
'''ORALLY AVAILABLE FACTOR7A INHIBITOR'''<br /> | '''ORALLY AVAILABLE FACTOR7A INHIBITOR'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
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] Known structural/functional Site: <scene name='pdbsite=AC1:So4 Binding Site For Chain H'>AC1</scene>. Full crystallographic information is available from [http:// | 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]. | ||
==Reference== | ==Reference== | ||
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[[Category: serine protease]] | [[Category: serine protease]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb 3 10:29:37 2008'' | ||
Revision as of 08:29, 3 February 2008
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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.
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: 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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