Rapid Evolution of 6-Phenylpurine Inhibitors of Protein Kinase B through Structure-Based Design
Journal of Medicinal Chemistry2007Vol. 50(10), pp. 2289–2292
Citations Over TimeTop 10% of 2007 papers
Alastair Donald, Tatiana McHardy, Martin Rowlands, Lisa-Jane K. Hunter, Thomas G. Davies, Valério Berdini, Robert G. Boyle, G. Wynne Aherne, Michelle D. Garrett, Ian Collins
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.
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