2bz6: Difference between revisions
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[[Image:2bz6.gif|left|200px]] | [[Image:2bz6.gif|left|200px]] | ||
'''ORALLY AVAILABLE FACTOR7A INHIBITOR''' | {{Structure | ||
|PDB= 2bz6 |SIZE=350|CAPTION= <scene name='initialview01'>2bz6</scene>, resolution 1.60Å | |||
|SITE= <scene name='pdbsite=AC1:So4+Binding+Site+For+Chain+H'>AC1</scene> | |||
|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> | |||
|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] | |||
|GENE= | |||
}} | |||
'''ORALLY AVAILABLE FACTOR7A INHIBITOR''' | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
2BZ6 is a [ | 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== | ||
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:// | 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]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | ''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
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| 2bz6, resolution 1.60Å | |||||||||||||
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| Sites: | AC1 | ||||||||||||
| Ligands: | SO4, CA and 346 | ||||||||||||
| Activity: | Coagulation factor VIIa, with EC number 3.4.21.21 | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
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. 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
