2uw0
From Proteopedia
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==Overview== | ==Overview== | ||
| - | 6-phenylpurines were identified as novel, ATP-competitive inhibitors of | + | 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== | ==About this Structure== | ||
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[[Category: Bos taurus]] | [[Category: Bos taurus]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
| - | [[Category: Aherne, G | + | [[Category: Aherne, G W.]] |
| - | [[Category: Boyle, R | + | [[Category: Boyle, R G.]] |
[[Category: Collins, I.]] | [[Category: Collins, I.]] | ||
| - | [[Category: Davies, T | + | [[Category: Davies, T G.]] |
[[Category: Donald, A.]] | [[Category: Donald, A.]] | ||
| - | [[Category: Garrett, M | + | [[Category: Garrett, M D.]] |
| - | [[Category: Hunter, L | + | [[Category: Hunter, L J.]] |
[[Category: Mchardy, T.]] | [[Category: Mchardy, T.]] | ||
| - | [[Category: Rowlands, M | + | [[Category: Rowlands, M G.]] |
[[Category: GVK]] | [[Category: GVK]] | ||
[[Category: atp-binding]] | [[Category: atp-binding]] | ||
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[[Category: transferase/inhibitor complex]] | [[Category: transferase/inhibitor complex]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:50:51 2008'' |
Revision as of 16:50, 21 February 2008
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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 as ligand. Known structural/functional Site: . 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 Feb 21 18:50:51 2008
Categories: 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
