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PDBsum entry 2uvz
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Transferase/inhibitor
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PDB id
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2uvz
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References listed in PDB file
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Key reference
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Title
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Rapid evolution of 6-Phenylpurine inhibitors of protein kinase b through structure-Based design.
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Authors
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A.Donald,
T.Mchardy,
M.G.Rowlands,
L.J.Hunter,
T.G.Davies,
V.Berdini,
R.G.Boyle,
G.W.Aherne,
M.D.Garrett,
I.Collins.
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Ref.
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J Med Chem, 2007,
50,
2289-2292.
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PubMed id
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Note In the PDB file this reference is
annotated as "TO BE PUBLISHED".
The citation details given above were identified by an automated
search of PubMed on title and author
names, giving a
perfect match.
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Abstract
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6-phenylpurines were identified as novel, ATP-competitive inhibitors of protein
kinase B (PKB/Akt) from a fragment-based screen and were rapidly progressed to
potent compounds using iterative protein-ligand crystallography with a PKA-PKB
chimeric protein. An elaborated lead compound showed cell growth inhibition and
effects on cellular signaling pathways characteristic of PKB inhibition.
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