2bz6 | pdb_00002bz6
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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
