2bz6
From Proteopedia
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==Overview== | ==Overview== | ||
| - | The discovery of a highly potent and selective tissue factor/factor VIIa | + | 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== | ==Disease== | ||
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[[Category: Ackermann, J.]] | [[Category: Ackermann, J.]] | ||
[[Category: Alig, L.]] | [[Category: Alig, L.]] | ||
| - | [[Category: Banner, D | + | [[Category: Banner, D W.]] |
| - | [[Category: Boehm, H | + | [[Category: Boehm, H J.]] |
[[Category: Groebke-Zbinden, K.]] | [[Category: Groebke-Zbinden, K.]] | ||
[[Category: Hilpert, K.]] | [[Category: Hilpert, K.]] | ||
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[[Category: Riederer, M.]] | [[Category: Riederer, M.]] | ||
[[Category: Stahl, M.]] | [[Category: Stahl, M.]] | ||
| - | [[Category: Tschopp, T | + | [[Category: Tschopp, T B.]] |
[[Category: Weber, L.]] | [[Category: Weber, L.]] | ||
| - | [[Category: Wessel, H | + | [[Category: Wessel, H P.]] |
[[Category: 346]] | [[Category: 346]] | ||
[[Category: CA]] | [[Category: CA]] | ||
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[[Category: serine protease]] | [[Category: serine protease]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:43:12 2008'' |
Revision as of 14:43, 21 February 2008
|
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 with , and as ligands. Active as Coagulation factor VIIa, with EC number 3.4.21.21 Known structural/functional Site: . 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 Feb 21 16:43:12 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
