2bz6: Difference between revisions
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|PDB= 2bz6 |SIZE=350|CAPTION= <scene name='initialview01'>2bz6</scene>, resolution 1.60Å | |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> | |SITE= <scene name='pdbsite=AC1:So4+Binding+Site+For+Chain+H'>AC1</scene> | ||
|LIGAND= | |LIGAND= <scene name='pdbligand=346:(R)-(4-CARBAMIMIDOYL-PHENYLAMINO)-[5-ETHOXY-2-FLUORO-3-[(R)-TETRAHYDRO-FURAN-3-YLOXY]-PHENYL]-ACETIC+ACID'>346</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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] | |ACTIVITY= <span class='plainlinks'>[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] </span> | ||
|GENE= | |GENE= | ||
|DOMAIN= | |||
|RELATEDENTRY= | |||
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2bz6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2bz6 OCA], [http://www.ebi.ac.uk/pdbsum/2bz6 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2bz6 RCSB]</span> | |||
}} | }} | ||
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==Overview== | ==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. | 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. | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Weber, L.]] | [[Category: Weber, L.]] | ||
[[Category: Wessel, H P.]] | [[Category: Wessel, H P.]] | ||
[[Category: | [[Category: serine protease,coagulation,enzyme complex,hydrolase]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:13:57 2008'' | ||
Revision as of 23:13, 30 March 2008
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| 2bz6, resolution 1.60Å | |||||||||||||
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| Sites: | AC1 | ||||||||||||
| Ligands: | 346, CA, SO4 | ||||||||||||
| Activity: | Coagulation factor VIIa, with EC number 3.4.21.21 | ||||||||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||||||
| 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.
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 Mon Mar 31 02:13:57 2008
