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PDBsum entry 4flh

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protein ligands links
Transferase/inhibitor PDB id
4flh
Jmol
Contents
Protein chain
840 a.a.
Ligands
SO4 ×4
14K
Waters ×42
PDB id:
4flh
Name: Transferase/inhibitor
Title: Crystal structure of human pi3k-gamma in complex with amg511
Structure: Phosphatidylinositol 4,5-bisphosphate 3-kinase ca subunit gamma isoform. Chain: a. Fragment: catalytic domain, unp residues 144-1102. Synonym: pi3-kinase subunit gamma, pi3k-gamma, pi3kgamma, p kinase subunit gamma, phosphatidylinositol 4,5-bisphosphate 110 kda catalytic subunit gamma, ptdins-3-kinase subunit p1 p110gamma, phosphoinositide-3-kinase catalytic gamma polype serine/threonine protein kinase pik3cg, p120-pi3k.
Source: Homo sapiens. Human. Organism_taxid: 9606. Gene: pik3cg. Expressed in: spodoptera frugiperda. Expression_system_taxid: 7108. Expression_system_cell_line: sf9.
Resolution:
2.60Å     R-factor:   0.202     R-free:   0.244
Authors: D.A.Whittington,J.Tang,P.Yakowec
Key ref: M.H.Norman et al. (2012). Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511. J Med Chem, 55, 7796-7816. PubMed id: 22897589 DOI: 10.1021/jm300846z
Date:
14-Jun-12     Release date:   29-Aug-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.
840 a.a.
Key:    PfamA domain  Secondary structure  CATH domain

 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    
 
 
DOI no: 10.1021/jm300846z J Med Chem 55:7796-7816 (2012)
PubMed id: 22897589  
 
 
Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511.
M.H.Norman, K.L.Andrews, Y.Y.Bo, S.K.Booker, S.Caenepeel, V.J.Cee, N.D.D'Angelo, D.J.Freeman, B.J.Herberich, F.T.Hong, C.L.Jackson, J.Jiang, B.A.Lanman, L.Liu, J.D.McCarter, E.L.Mullady, N.Nishimura, L.H.Pettus, A.B.Reed, T.S.Miguel, A.L.Smith, M.M.Stec, S.Tadesse, A.Tasker, D.Aidasani, X.Zhu, R.Subramanian, N.A.Tamayo, L.Wang, D.A.Whittington, B.Wu, T.Wu, R.P.Wurz, K.Yang, L.Zalameda, N.Zhang, P.E.Hughes.
 
  ABSTRACT  
 
No abstract given.