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PDBsum entry 1w8b
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protein ligands metals Protein-protein interface(s) links
Hydrolase PDB id
1w8b

 

 

 

 

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Contents
Protein chains
247 a.a. *
56 a.a. *
Ligands
413
Metals
_CA
Waters ×59
* Residue conservation analysis
PDB id:
1w8b
Name: Hydrolase
Title: Factor7 - 413 complex
Structure: 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 148-204.
Source: Homo sapiens. Human. Organism_taxid: 9606. Expressed in: escherichia coli. Expression_system_taxid: 562. Expression_system_taxid: 562
Biol. unit: Dimer (from PDB file)
Resolution:
3.00Å     R-factor:   0.197     R-free:   0.272
Authors: J.Ackermann,L.Alig,D.W.Banner,H.-J.Boehm,K.Groebke-Zbinden,K.Hilpert, T.Lave,H.Kuehne,U.Obst-Sander,M.A.Riederer,M.Stahl,T.B.Tschopp, L.Weber,H.P.Wessel
Key ref: K.G.Zbinden et al. (2005). Selective and orally bioavailable phenylglycine tissue factor/factor VIIa inhibitors. Bioorg Med Chem Lett, 15, 5344-5352. PubMed id: 16213138 DOI: 10.1016/j.bmcl.2005.04.079
Date:
17-Sep-04     Release date:   25-Oct-05    
PROCHECK
Go to PROCHECK summary
 Headers
 References

Protein chain
Pfam   ArchSchema ?
P08709  (FA7_HUMAN) -  Coagulation factor VII from Homo sapiens
Seq:
Struc: 		466 a.a.
247 a.a.
Protein chain
Pfam   ArchSchema ?
P08709  (FA7_HUMAN) -  Coagulation factor VII from Homo sapiens
Seq:
Struc: 		466 a.a.
56 a.a.
Key:    PfamA domain  Secondary structure  CATH domain

 Enzyme reactions 
   Enzyme class: Chains H, L: E.C.3.4.21.21  - coagulation factor VIIa.
[IntEnz]   [ExPASy]   [KEGG]   [BRENDA]
      Reaction: Hydrolyzes one Arg-|-Ile bond in factor X to form factor Xa.

 

 
DOI no: 10.1016/j.bmcl.2005.04.079 Bioorg Med Chem Lett 15:5344-5352 (2005)
PubMed id: 16213138  
 
 
Selective and orally bioavailable phenylglycine tissue factor/factor VIIa inhibitors.
K.G.Zbinden, U.Obst-Sander, K.Hilpert, H.Kühne, D.W.Banner, H.J.Böhm, M.Stahl, J.Ackermann, L.Alig, L.Weber, H.P.Wessel, M.A.Riederer, T.B.Tschopp, T.Lavé.
 
  ABSTRACT  
 
We describe the structure-based design and synthesis of highly potent, orally bioavailable tissue factor/factor VIIa inhibitors which interfere with the coagulation cascade by selective inhibition of the extrinsic pathway.
 

Literature references that cite this PDB file's key reference

  PubMed id Reference
20045964 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.
  Chem Pharm Bull (Tokyo), 58, 38-44.
PDB code: 2zzu
19490111 E.Persson, and O.H.Olsen (2009).
Activation loop 3 and the 170 loop interact in the active conformation of coagulation factor VIIa.
  FEBS J, 276, 3099-3109.  
18425569 M.H.Umer Usman, S.Raza, S.Raza, and M.Ezekowitz (2008).
Advancement in antithrombotics for stroke prevention in atrial fibrillation.
  J Interv Card Electrophysiol, 22, 129-137.  
17406624 S.Marcaccini, and T.Torroba (2007).
The use of the Ugi four-component condensation.
  Nat Protoc, 2, 632-639.  
16621574 K.Groebke Zbinden, D.W.Banner, K.Hilpert, J.Himber, T.Lavé, M.A.Riederer, M.Stahl, T.B.Tschopp, and U.Obst-Sander (2006).
Dose-dependent antithrombotic activity of an orally active tissue factor/factor VIIa inhibitor without concomitant enhancement of bleeding propensity.
  Bioorg Med Chem, 14, 5357-5369.
PDB code: 2bz6
16757484 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.
  J Biol Chem, 281, 24873-24888.
PDB codes: 2a2q 2aer 2fir
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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