PDBsum entry 2vwv

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Transferase PDB id
Protein chain
255 a.a. *
Waters ×138
* Residue conservation analysis
PDB id:
Name: Transferase
Title: Ephb4 kinase domain inhibitor complex
Structure: Ephrin type-b receptor 4. Chain: a. Fragment: protein kinase domain, residues 598-899. Synonym: tyrosine-protein kinase receptor htk, tyrosine-protein kinase tyro11. Engineered: yes. Mutation: yes
Source: Homo sapiens. Human. Organism_taxid: 9606. Expressed in: spodoptera frugiperda. Expression_system_taxid: 7108. Expression_system_cell_line: sf21.
1.90Å     R-factor:   0.241     R-free:   0.287
Authors: J.Read,C.A.Brassington,I.Green,E.J.Mccall,A.L.Valentine, J.G.Kettle,A.G.Leach
Key ref: C.Bardelle et al. (2008). Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines. Bioorg Med Chem Lett, 18, 2776-2780. PubMed id: 18434142 DOI: 10.1016/j.bmcl.2008.04.015
27-Jun-08     Release date:   08-Jul-08    
Go to PROCHECK summary

Protein chain
Pfam   ArchSchema ?
P54760  (EPHB4_HUMAN) -  Ephrin type-B receptor 4
987 a.a.
255 a.a.
Key:    PfamA domain  Secondary structure  CATH domain

 Enzyme reactions 
   Enzyme class: E.C.  - Receptor protein-tyrosine kinase.
[IntEnz]   [ExPASy]   [KEGG]   [BRENDA]
      Reaction: ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
+ [protein]-L-tyrosine
+ [protein]-L-tyrosine phosphate
Molecule diagrams generated from .mol files obtained from the KEGG ftp site
 Gene Ontology (GO) functional annotation 
  GO annot!
  Biological process     regulation of signal transduction   2 terms 
  Biochemical function     transferase activity, transferring phosphorus-containing groups     5 terms  


DOI no: 10.1016/j.bmcl.2008.04.015 Bioorg Med Chem Lett 18:2776-2780 (2008)
PubMed id: 18434142  
Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines.
C.Bardelle, D.Cross, S.Davenport, J.G.Kettle, E.J.Ko, A.G.Leach, A.Mortlock, J.Read, N.J.Roberts, P.Robins, E.J.Williams.
A series of bis-anilinopyrimidines have been identified as potent inhibitors of the tyrosine kinase EphB4. Structural information from two alternative series identified from screening efforts was combined to identify the initial leads.

Literature references that cite this PDB file's key reference

  PubMed id Reference
21441027 B.Barlaam, R.Ducray, C.Lambert-van der Brempt, P.Plé, C.Bardelle, N.Brooks, T.Coleman, D.Cross, J.G.Kettle, and J.Read (2011).
Inhibitors of the tyrosine kinase EphB4. Part 4: Discovery and optimization of a benzylic alcohol series.
  Bioorg Med Chem Lett, 21, 2207-2211.
PDB code: 2xvd
20224755 B.Mosch, B.Reissenweber, C.Neuber, and J.Pietzsch (2010).
Eph receptors and ephrin ligands: important players in angiogenesis and tumor angiogenesis.
  J Oncol, 2010, 135285.  
19942586 D.Huang, T.Zhou, K.Lafleur, C.Nevado, and A.Caflisch (2010).
Kinase selectivity potential for inhibitors targeting the ATP binding site: a network analysis.
  Bioinformatics, 26, 198-204.  
20179713 E.B.Pasquale (2010).
Eph receptors and ephrins in cancer: bidirectional signalling and beyond.
  Nat Rev Cancer, 10, 165-180.  
20803239 G.Martiny-Baron, P.Holzer, E.Billy, C.Schnell, J.Brueggen, M.Ferretti, N.Schmiedeberg, J.M.Wood, P.Furet, and P.Imbach (2010).
The small molecule specific EphB4 kinase inhibitor NVP-BHG712 inhibits VEGF driven angiogenesis.
  Angiogenesis, 13, 259-267.  
19553108 Y.Choi, F.Syeda, J.R.Walker, P.J.Finerty, D.Cuerrier, A.Wojciechowski, Q.Liu, S.Dhe-Paganon, and N.S.Gray (2009).
Discovery and structural analysis of Eph receptor tyrosine kinase inhibitors.
  Bioorg Med Chem Lett, 19, 4467-4470.  
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