2BZ6

Orally available Factor7a inhibitor

Summary for 2BZ6

• Entry DOI: 10.2210/pdb2bz6/pdb
• Related: 1BF9 1CVW 1DAN 1DVA 1F7E 1F7M 1FAK 1FF7 1FFM 1J9C 1JBU 1KLI 1KLJ 1NL8 1O5D 1QFK 1W0Y 1W2K 1W7X 1W8B 1YGC 1Z6J
• Descriptor: BLOOD COAGULATION FACTOR VIIA, (R)-(4-CARBAMIMIDOYL-PHENYLAMINO)-[5-ETHOXY-2-FLUORO-3-[(R)-TETRAHYDRO-FURAN-3-YLOXY]-PHENYL]-ACETIC ACID, SULFATE ION, ... (6 entities in total)
• Functional Keywords: serine protease, coagulation, enzyme complex, hydrolase
• Biological source: HOMO SAPIENS (HUMAN); More
• Cellular location: Secreted: P08709 P08709
• Total number of polymer chains: 2
• Total formula weight: 34401.28

Authors

Groebke-Zbinden, K.,Obst-Sander, U.,Hilpert, K.,Kuehne, H.,Banner, D.W.,Boehm, H.J.,Stahl, M.,Ackermann, J.,Alig, L.,Weber, L.,Wessel, H.P.,Riederer, M.A.,Tschopp, T.B.,Lave, T. (deposition date: 2005-08-11, release date: 2006-02-22, Last modification date: 2024-10-09)

Primary citation

Groebke-Zbinden, K.,Banner, D.W.,Hilpert, K.,Himber, J.,Lave, T.,Riederer, M.A.,Stahl, M.,Tschopp, T.B.,Obst-Sander, U.
Dose-Dependant Antithrombotic Activity of an Orally Active Tissue Factor/Factor Viia Inhibitor without Concomitant Enhancement of Bleeding Propensity.
Bioorg.Med.Chem., 14:5357-, 2006

PubMed Abstract: 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.

PubMed: 16621574
DOI: 10.1016/J.BMC.2006.03.042

Experimental method

X-RAY DIFFRACTION (1.6 Å)