2bz6
From Proteopedia
| |||||||
| , 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
Categories: Coagulation factor VIIa | Homo sapiens | Single protein | Ackermann, J. | Alig, L. | Banner, D W. | Boehm, H J. | Groebke-Zbinden, K. | Hilpert, K. | Kuehne, H. | Lave, T. | Obst-Sander, U. | Riederer, M. | Stahl, M. | Tschopp, T B. | Weber, L. | Wessel, H P. | 346 | CA | SO4 | Coagulation | Enzyme complex | Hydrolase | Serine protease
