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251 a.a.
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142 a.a.
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188 a.a.
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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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Tf7a_3771 complex
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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 heavy chain, residues 61-202.
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Source:
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Homo sapiens. Human. Organism_taxid: 9606. Expressed in: cricetulus griseus. Expression_system_taxid: 10029. Expression_system_cell_line: baby hamster kidney cells (bhk). Expressed in: escherichia coli. Expression_system_taxid: 562
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Biol. unit:
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Trimer (from PDB file)
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Resolution:
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2.50Å
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R-factor:
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0.199
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R-free:
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0.258
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Authors:
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D.W.Banner,A.D'Arcy,K.Groebke-Zbinden,J.Ackermann, D.Kirchhofer,Y.-H.Ji,T.B.Tschopp,S.Wallbaum,L.Weber
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Key ref:
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K.Groebke Zbinden
et al.
(2005).
Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors.
Bioorg Med Chem Lett,
15,
817-822.
PubMed id:
DOI:
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Date:
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15-Jun-04
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Release date:
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21-Jan-05
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PROCHECK
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Headers
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References
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P08709
(FA7_HUMAN) -
Coagulation factor VII
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Seq:
Struc:
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466 a.a.
251 a.a.
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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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Gene Ontology (GO) functional annotation
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Cellular component
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extracellular region
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2 terms
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Biological process
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blood coagulation
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2 terms
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Biochemical function
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catalytic activity
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4 terms
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DOI no:
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Bioorg Med Chem Lett
15:817-822
(2005)
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PubMed id:
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Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors.
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K.Groebke Zbinden,
D.W.Banner,
J.Ackermann,
A.D'Arcy,
D.Kirchhofer,
Y.H.Ji,
T.B.Tschopp,
S.Wallbaum,
L.Weber.
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ABSTRACT
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Proof of concept experiments have shown that tissue factor/factor VIIa
inhibitors have antithrombotic activity without enhancing bleeding propensity.
Starting from lead compounds generated by a biased combinatorial approach,
phenylglycine amide tissue factor/factor VIIa inhibitors with low nanomolar
affinity and good selectivity against other serine proteases of the coagulation
cascade were designed, using the guidance of X-ray structural analysis and
molecular modelling.
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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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A.Poleksic,
J.F.Danzer,
B.A.Palmer,
B.D.Olafson,
and
D.A.Debe
(2006).
SPINFAST: using structure alignment profiles to enhance the accuracy and assess the reliability of protein side-chain modeling.
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Proteins, 65,
953-958.
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S.P.Bajaj,
A.E.Schmidt,
S.Agah,
M.S.Bajaj,
and
K.Padmanabhan
(2006).
High resolution structures of p-aminobenzamidine- and benzamidine-VIIa/soluble tissue factor: unpredicted conformation of the 192-193 peptide bond and mapping of Ca2+, Mg2+, Na+, and Zn2+ sites in factor VIIa.
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J Biol Chem, 281,
24873-24888.
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PDB codes:
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A.G.Olivero,
C.Eigenbrot,
R.Goldsmith,
K.Robarge,
D.R.Artis,
J.Flygare,
T.Rawson,
D.P.Sutherlin,
S.Kadkhodayan,
M.Beresini,
L.O.Elliott,
G.G.DeGuzman,
D.W.Banner,
M.Ultsch,
U.Marzec,
S.R.Hanson,
C.Refino,
S.Bunting,
and
D.Kirchhofer
(2005).
A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo.
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J Biol Chem, 280,
9160-9169.
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PDB code:
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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
codes are
shown on the right.
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