spacer
spacer

PDBsum entry 2p33

Go to PDB code: 
protein ligands links
Transferase PDB id
2p33
Jmol
Contents
Protein chain
332 a.a. *
Ligands
J07
Waters ×44
* Residue conservation analysis
PDB id:
2p33
Name: Transferase
Title: Synthesis and sar of aminopyrimidines as novel c-jun n- terminal kinase (jnk) inhibitors
Structure: C-jun n-terminal kinase 3. Chain: a. Fragment: protein kinase domain, residues 40-402. Synonym: mitogen-activated protein kinase 10, stress- activated protein kinase jnk3, map kinase p49 3f12. Engineered: yes
Source: Homo sapiens. Human. Organism_taxid: 9606. Gene: mapk10, jnk3, jnk3a, prkm10. Expressed in: escherichia coli. Expression_system_taxid: 562
Resolution:
2.40Å     R-factor:   0.253     R-free:   0.304
Authors: T.A.Ceska,A.Platt,M.Fortunato,K.M.Dickson,A.Sharpe
Key ref: M.Alam et al. (2007). Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors. Bioorg Med Chem Lett, 17, 3463-3467. PubMed id: 17459703 DOI: 10.1016/j.bmcl.2007.03.078
Date:
08-Mar-07     Release date:   19-Jun-07    
PROCHECK
Go to PROCHECK summary
 Headers
 References

Protein chain
Pfam   ArchSchema ?
P53779  (MK10_HUMAN) -  Mitogen-activated protein kinase 10
Seq:
Struc:
464 a.a.
332 a.a.
Key:    PfamA domain  Secondary structure  CATH domain

 Enzyme reactions 
   Enzyme class: E.C.2.7.11.24  - Mitogen-activated protein kinase.
[IntEnz]   [ExPASy]   [KEGG]   [BRENDA]
      Reaction: ATP + a protein = ADP + a phosphoprotein
ATP
+ protein
= ADP
+ phosphoprotein
Molecule diagrams generated from .mol files obtained from the KEGG ftp site
 Gene Ontology (GO) functional annotation 
  GO annot!
  Biological process     protein phosphorylation   1 term 
  Biochemical function     transferase activity, transferring phosphorus-containing groups     5 terms  

 

 
    reference    
 
 
DOI no: 10.1016/j.bmcl.2007.03.078 Bioorg Med Chem Lett 17:3463-3467 (2007)
PubMed id: 17459703  
 
 
Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.
M.Alam, R.E.Beevers, T.Ceska, R.J.Davenport, K.M.Dickson, M.Fortunato, L.Gowers, A.F.Haughan, L.A.James, M.W.Jones, N.Kinsella, C.Lowe, J.W.Meissner, A.L.Nicolas, B.G.Perry, D.J.Phillips, W.R.Pitt, A.Platt, A.J.Ratcliffe, A.Sharpe, L.J.Tait.
 
  ABSTRACT  
 
The development of a series of novel aminopyrimidines as inhibitors of c-Jun N-terminal kinases is described. The synthesis, in vitro inhibitory values for JNK1, JNK2 and CDK2, and the in vitro inhibitory value for a c-Jun cellular assay are discussed.
 

Literature references that cite this PDB file's key reference

  PubMed id Reference
21185177 R.Noël, Y.Shin, X.Song, Y.He, M.Koenig, W.Chen, Y.Y.Ling, L.Lin, C.H.Ruiz, P.LoGrasso, M.D.Cameron, D.R.Duckett, and T.M.Kamenecka (2011).
Synthesis and SAR of 4-(pyrazol-3-yl)-pyridines as novel c-jun N-terminal kinase inhibitors.
  Bioorg Med Chem Lett, 21, 2732-2735.  
19947601 T.Kamenecka, R.Jiang, X.Song, D.Duckett, W.Chen, Y.Y.Ling, J.Habel, J.D.Laughlin, J.Chambers, M.Figuera-Losada, M.D.Cameron, L.Lin, C.H.Ruiz, and P.V.LoGrasso (2010).
Synthesis, biological evaluation, X-ray structure, and pharmacokinetics of aminopyrimidine c-jun-N-terminal kinase (JNK) inhibitors.
  J Med Chem, 53, 419-431.
PDB code: 3kvx
20033049 W.Zhou, D.Ercan, L.Chen, C.H.Yun, D.Li, M.Capelletti, A.B.Cortot, L.Chirieac, R.E.Iacob, R.Padera, J.R.Engen, K.K.Wong, M.J.Eck, N.S.Gray, and P.A.Jänne (2009).
Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.
  Nature, 462, 1070-1074.
PDB code: 3ika
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.