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PDBsum entry 2bz6
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* Residue conservation analysis
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PDB id:
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Hydrolase
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Title:
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Orally available factor7a inhibitor
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Structure:
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Blood coagulation factor viia. Chain: h. Fragment: factor vii heavy chain, residues 213-466. Synonym: serum prothrombin conversion accelerator, spca, proconvertin, eptacog alfa, novoseven. Engineered: yes. Blood coagulation factor viia. Chain: l. Fragment: factor vii light chain, residues 150-202.
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Source:
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Homo sapiens. Human. Organism_taxid: 9606. Expressed in: escherichia coli. Expression_system_taxid: 562. Expression_system_taxid: 562
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Biol. unit:
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Dimer (from
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Resolution:
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1.60Å
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R-factor:
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0.168
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R-free:
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0.193
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Authors:
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K.Groebke-Zbinden,U.Obst-Sander,K.Hilpert,H.Kuehne,D.W.Banner, H.J.Boehm,M.Stahl,J.Ackermann,L.Alig,L.Weber,H.P.Wessel, M.A.Riederer,T.B.Tschopp,T.Lave
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Key ref:
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K.Groebke Zbinden
et al.
(2006).
Dose-dependent antithrombotic activity of an orally active tissue factor/factor VIIa inhibitor without concomitant enhancement of bleeding propensity.
Bioorg Med Chem Lett,
14,
5357-5369.
PubMed id:
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Date:
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11-Aug-05
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Release date:
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22-Feb-06
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PROCHECK
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Headers
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References
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Enzyme class:
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Chains H, L:
E.C.3.4.21.21
- coagulation factor VIIa.
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Reaction:
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Hydrolyzes one Arg-|-Ile bond in factor X to form factor Xa.
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Bioorg Med Chem Lett
14:5357-5369
(2006)
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PubMed id:
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Dose-dependent antithrombotic activity of an orally active tissue factor/factor VIIa inhibitor without concomitant enhancement of bleeding propensity.
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K.Groebke Zbinden,
D.W.Banner,
K.Hilpert,
J.Himber,
T.Lavé,
M.A.Riederer,
M.Stahl,
T.B.Tschopp,
U.Obst-Sander.
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ABSTRACT
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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.
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Literature references that cite this PDB file's key reference
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PubMed id
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Reference
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T.Shiraishi,
S.Kadono,
M.Haramura,
H.Kodama,
Y.Ono,
H.Iikura,
T.Esaki,
T.Koga,
K.Hattori,
Y.Watanabe,
A.Sakamoto,
K.Yoshihashi,
T.Kitazawa,
K.Esaki,
M.Ohta,
H.Sato,
and
T.Kozono
(2010).
Design and synthesis of peptidomimetic factor VIIa inhibitors.
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Chem Pharm Bull (Tokyo),
58,
38-44.
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PDB code:
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V.Chandrasekaran,
C.J.Lee,
R.E.Duke,
L.Perera,
and
L.G.Pedersen
(2008).
Computational study of the putative active form of protein Z (PZa): sequence design and structural modeling.
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Protein Sci,
17,
1354-1361.
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The most recent references are shown first.
Citation data come partly from CiteXplore and partly
from an automated harvesting procedure. Note that this is likely to be
only a partial list as not all journals are covered by
either method. However, we are continually building up the citation data
so more and more references will be included with time.
Where a reference describes a PDB structure, the PDB
code is
shown on the right.
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Links
