2uvz
STRUCTURE OF PKA-PKB CHIMERA COMPLEXED WITH C-PHENYL-C-(4-(9H-PURIN-6-YL)-PHENYL)-METHYLAMINE
OverviewOverview
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.
About this StructureAbout this Structure
2UVZ is a Protein complex structure of sequences from Bos taurus. Full crystallographic information is available from OCA.
ReferenceReference
Rapid evolution of 6-phenylpurine inhibitors of protein kinase B through structure-based design., Donald A, McHardy T, Rowlands MG, Hunter LJ, Davies TG, Berdini V, Boyle RG, Aherne GW, Garrett MD, Collins I, J Med Chem. 2007 May 17;50(10):2289-92. Epub 2007 Apr 24. PMID:17451235 Page seeded by OCA on Thu May 22 22:30:14 2008