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PDBsum entry 4anw

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protein ligands links
Transferase PDB id
4anw
Jmol
Contents
Protein chain
833 a.a.
Ligands
SO4
O92
Waters ×66
PDB id:
4anw
Name: Transferase
Title: Complexes of pi3kgamma with isoform selective inhibitors.
Structure: Phosphatidylinositol-4,5-bisphosphate 3-kinase ca subunit gamma isoform. Chain: a. Fragment: catalytic subunit gamma, residues 144-1102. Synonym: pi3-kinase subunit gamma, pi3k-gamma, pi3kgamma, ptdins-3-kinase subunit gamma, phosphatidylinositol-4\,5-bisphosphate 3-kinase 110 kda ca subunit gamma, ptdins-3-kinase subunit p110-gamma, p110gam phosphoinositide-3-kinase catalytic gamma polypeptide,
Source: Homo sapiens. Human. Organism_taxid: 9606. Expressed in: spodoptera frugiperda. Expression_system_taxid: 7108. Expression_system_cell_line: sf9.
Resolution:
2.31Å     R-factor:   0.238     R-free:   0.296
Authors: P.G.Foster,J.C.Lougheed
Key ref: J.W.Leahy et al. (2012). Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase γ inhibitors. J Med Chem, 55, 5467-5482. PubMed id: 22548342
Date:
22-Mar-12     Release date:   09-May-12    
PROCHECK
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 Headers
 References

Protein chain
Pfam   ArchSchema ?
P48736  (PK3CG_HUMAN) -  Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
Seq:
Struc:
 
Seq:
Struc:
 
Seq:
Struc:
1102 a.a.
833 a.a.*
Key:    PfamA domain  Secondary structure  CATH domain
* PDB and UniProt seqs differ at 1 residue position (black cross)

 Enzyme reactions 
   Enzyme class 2: E.C.2.7.1.153  - Phosphatidylinositol-4,5-bisphosphate 3-kinase.
[IntEnz]   [ExPASy]   [KEGG]   [BRENDA]

      Pathway:
1-Phosphatidyl-myo-inositol Metabolism
      Reaction: ATP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate = ADP + 1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate
ATP
+ 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate
= ADP
+ 1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate
   Enzyme class 3: E.C.2.7.11.1  - Non-specific serine/threonine protein kinase.
[IntEnz]   [ExPASy]   [KEGG]   [BRENDA]
      Reaction: ATP + a protein = ADP + a phosphoprotein
ATP
+ protein
= ADP
+ phosphoprotein
Note, where more than one E.C. class is given (as above), each may correspond to a different protein domain or, in the case of polyprotein precursors, to a different mature protein.
Molecule diagrams generated from .mol files obtained from the KEGG ftp site
 Gene Ontology (GO) functional annotation 
  GO annot!
  Biological process     phosphatidylinositol-mediated signaling   2 terms 
  Biochemical function     transferase activity, transferring phosphorus-containing groups     2 terms  

 

 
    reference    
 
 
J Med Chem 55:5467-5482 (2012)
PubMed id: 22548342  
 
 
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase γ inhibitors.
J.W.Leahy, C.A.Buhr, H.W.Johnson, B.G.Kim, T.Baik, J.Cannoy, T.P.Forsyth, J.W.Jeong, M.S.Lee, S.Ma, K.Noson, L.Wang, M.Williams, J.M.Nuss, E.Brooks, P.Foster, L.Goon, N.Heald, C.Holst, C.Jaeger, S.Lam, J.Lougheed, L.Nguyen, A.Plonowski, J.Song, T.Stout, X.Wu, M.F.Yakes, P.Yu, W.Zhang, P.Lamb, O.Raeber.
 
  ABSTRACT  
 
No abstract given.