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PDBsum entry 3ugc
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protein ligands links
Transferase/transferase inhibitor PDB id
3ugc

 

 

 

 

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Contents
Protein chain
274 a.a.
Ligands
046
MLI
Waters ×275
PDB id:
3ugc
Name: Transferase/transferase inhibitor
Title: Structural basis of jak2 inhibition by the type ii inhibtor nvp-bbt594
Structure: Tyrosine-protein kinase jak2. Chain: a. Fragment: unp residues 840-1132. Synonym: janus kinase 2, jak-2. Engineered: yes. Mutation: yes
Source: Homo sapiens. Human. Organism_taxid: 9606. Expressed in: spodoptera frugiperda. Expression_system_taxid: 7108. Expression_system_cell_line: sf9de.
Resolution:
1.34Å     R-factor:   0.177     R-free:   0.189
Authors: C.Scheufler,G.A.Tavares,P.W.Manley,C.Pissot-Soldermann,M.Kroemer
Key ref: R.Andraos et al. (2012). Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent. Cancer Discov, 2, 512-523. PubMed id: 22684457 DOI: 10.1158/2159-8290.CD-11-0324
Date:
02-Nov-11     Release date:   16-May-12    
PROCHECK
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 Headers
 References

Protein chain
Pfam   ArchSchema ?
O60674  (JAK2_HUMAN) -  Tyrosine-protein kinase JAK2 from Homo sapiens
Seq:
Struc: 		 
Seq:
Struc: 		 
Seq:
Struc: 		1132 a.a.
274 a.a.
Key:    PfamA domain  Secondary structure  CATH domain

 Enzyme reactions 
   Enzyme class: E.C.2.7.10.2  - non-specific protein-tyrosine kinase.
[IntEnz]   [ExPASy]   [KEGG]   [BRENDA]
      Reaction: L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H+
L-tyrosyl-[protein]
 + ATP
 = O-phospho-L-tyrosyl-[protein]
 + ADP
 + H(+)
Molecule diagrams generated from .mol files obtained from the KEGG ftp site

 

 
    Added reference    
 
 
DOI no: 10.1158/2159-8290.CD-11-0324 Cancer Discov 2:512-523 (2012)
PubMed id: 22684457  
 
 
Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent.
R.Andraos, Z.Qian, D.Bonenfant, J.Rubert, E.Vangrevelinghe, C.Scheufler, F.Marque, C.H.Régnier, A.De Pover, H.Ryckelynck, N.Bhagwat, P.Koppikar, A.Goel, L.Wyder, G.Tavares, F.Baffert, C.Pissot-Soldermann, P.W.Manley, C.Gaul, H.Voshol, R.L.Levine, W.R.Sellers, F.Hofmann, T.Radimerski.
 
  ABSTRACT  
 
No abstract given.

 

Literature references that cite this PDB file's key reference

  PubMed id Reference
22820254 P.Koppikar, N.Bhagwat, O.Kilpivaara, T.Manshouri, M.Adli, T.Hricik, F.Liu, L.M.Saunders, A.Mullally, O.Abdel-Wahab, L.Leung, A.Weinstein, S.Marubayashi, A.Goel, M.Gönen, Z.Estrov, B.L.Ebert, G.Chiosis, S.D.Nimer, B.E.Bernstein, S.Verstovsek, and R.L.Levine (2012).
Heterodimeric JAK-STAT activation as a mechanism of persistence to JAK2 inhibitor therapy.
  Nature, 489, 155-159.  
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.

 

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