 |
PDBsum entry 2uw0
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
Transferase/inhibitor
|
PDB id
|
|
|
|
2uw0
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
References listed in PDB file
|
|
|
Key reference
|
|
|
Title
|
|
Rapid evolution of 6-Phenylpurine inhibitors of protein kinase b through structure-Based design.
|
|
|
Authors
|
|
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.
|
|
|
Ref.
|
|
J Med Chem, 2007,
50,
2289-2292.
|
|
|
PubMed id
|
|
|
|
|
|
Abstract
|
|
|
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.
|
|
|
|
|
|
|
