Document Report Card

ID: ALA1139878

Journal: J Med Chem

Title: Rapid evolution of 6-phenylpurine inhibitors of protein kinase B through structure-based design.

Authors: Donald A, McHardy T, Rowlands MG, Hunter LJ, Davies TG, Berdini V, Boyle RG, Aherne GW, Garrett MD, Collins I.

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.

CiteXplore: 17451235

DOI: 10.1021/jm0700924