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PDBsum entry 1yw2

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protein ligands links
Transferase PDB id
1yw2
Jmol
Contents
Protein chain
341 a.a. *
Ligands
PGJ
Waters ×195
* Residue conservation analysis
PDB id:
1yw2
Name: Transferase
Title: Mutated mus musculus p38 kinase (mp38)
Structure: Mitogen-activated protein kinase 14. Chain: a. Synonym: mitogen-activated protein kinase p38alpha, map kinase p38alpha, crk1. Engineered: yes. Mutation: yes
Source: Mus musculus. House mouse. Organism_taxid: 10090. Gene: mapk14, crk1, csbp1, csbp2. Expressed in: escherichia coli. Expression_system_taxid: 562
Resolution:
2.01Å     R-factor:   0.207     R-free:   0.290
Authors: S.K.Laughlin,M.P.Clark,J.F.Djung,A.Golebiowski,T.A.Brugel, M.Sabat,R.G.Bookland,M.J.Laufersweiler,J.C.Vanrens, J.A.Townes,B.De,L.C.Hsieh,S.C.Xu,R.L.Walter,M.J.Mekel, M.J.Janusz
Key ref: S.K.Laughlin et al. (2005). The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-alpha) production. Bioorg Med Chem Lett, 15, 2399-2403. PubMed id: 15837333 DOI: 10.1016/j.bmcl.2005.02.066
Date:
16-Feb-05     Release date:   10-May-05    
PROCHECK
Go to PROCHECK summary
 Headers
 References

Protein chain
Pfam   ArchSchema ?
P47811  (MK14_MOUSE) -  Mitogen-activated protein kinase 14
Seq:
Struc:
360 a.a.
341 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!
  Cellular component     cell   6 terms 
  Biological process     intracellular signal transduction   40 terms 
  Biochemical function     nucleotide binding     10 terms  

 

 
    reference    
 
 
DOI no: 10.1016/j.bmcl.2005.02.066 Bioorg Med Chem Lett 15:2399-2403 (2005)
PubMed id: 15837333  
 
 
The development of new isoxazolone based inhibitors of tumor necrosis factor-alpha (TNF-alpha) production.
S.K.Laughlin, M.P.Clark, J.F.Djung, A.Golebiowski, T.A.Brugel, M.Sabat, R.G.Bookland, M.J.Laufersweiler, J.C.VanRens, J.A.Townes, B.De, L.C.Hsieh, S.C.Xu, R.L.Walter, M.J.Mekel, M.J.Janusz.
 
  ABSTRACT  
 
4-Aryl-3-pyridyl and 4-aryl-3-pyrimidinyl based tumor necrosis factor-alpha (TNF-alpha) inhibitors, which contain a novel isoxazolone five-membered heterocyclic core are described. Many showed sub-micromolar activity against lipopolysaccharide-induced TNF-alpha production.
 

Literature references that cite this PDB file's key reference

  PubMed id Reference
21201524 S.Margutti, D.Schollmeyer, and S.Laufer (2008).
4-(4-Fluoro-phen-yl)-2-methyl-3-(1-oxy-4-pyridyl)isoxazol-5(2H)-one.
  Acta Crystallogr Sect E Struct Rep Online, 64, o504.  
21200862 S.Margutti, D.Schollmeyer, and S.Laufer (2007).
4-[4-(4-Fluoro-phen-yl)-2-methyl-5-oxo-2,5-dihydro-isoxazol-3-yl]-1-methyl-pyridinium iodide-4-[3-(4-fluoro-phen-yl)-2-methyl-5-oxo-2,5-dihydro-isoxazol-4-yl]-1-methyl-pyridinium iodide (0.6/0.4).
  Acta Crystallogr Sect E Struct Rep Online, 64, o298-o299.  
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.