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2uvy

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Revision as of 19:30, 22 May 2008 by OCA (Talk | contribs)
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Image:2uvy.jpg

Template:STRUCTURE 2uvy

STRUCTURE OF PKA-PKB CHIMERA COMPLEXED WITH METHYL-(4-(9H-PURIN-6-YL)-BENZYL)-AMINE


Overview

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 Structure

2UVY is a Protein complex structure of sequences from Bos taurus. Full crystallographic information is available from OCA.

Reference

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 22:30:13 2008

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