2uw0 | pdb_00002uw0
|
STRUCTURE OF PKA-PKB CHIMERA COMPLEXED WITH 6-(4-(4-(4-CHLORO-PHENYL)-PIPERIDIN-4-YL)-PHENYL)-9H-PURINE
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
2UW0 is a [Protein complex] structure of sequences from [Bos taurus] with GVK as [ligand]. 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 Mon Oct 29 17:04:26 2007
Proteopedia Page Contributors and Editors (what is this?)
- Pages with broken file links
- Bos taurus
- Protein complex
- Aherne, G.W.
- Boyle, R.G.
- Collins, I.
- Davies, T.G.
- Donald, A.
- Garrett, M.D.
- Hunter, L.J.
- Mchardy, T.
- Rowlands, M.G.
- GVK
- Atp-binding
- Camp
- Kinase
- Lipoprotein
- Myristate
- Nuclear protein
- Nucleotide-binding
- Phosphorylation
- Protein kinase inhibitor
- Serine/threonine-protein kinase
- Transferase
- Transferase/inhibitor complex
