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2uw0
From Proteopedia
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| - | [[Image:2uw0.gif|left|200px]]<br /><applet load="2uw0" size=" | + | [[Image:2uw0.gif|left|200px]]<br /><applet load="2uw0" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="2uw0, resolution 2.00Å" /> | caption="2uw0, resolution 2.00Å" /> | ||
'''STRUCTURE OF PKA-PKB CHIMERA COMPLEXED WITH 6-(4-(4-(4-CHLORO-PHENYL)-PIPERIDIN-4-YL)-PHENYL)-9H-PURINE'''<br /> | '''STRUCTURE OF PKA-PKB CHIMERA COMPLEXED WITH 6-(4-(4-(4-CHLORO-PHENYL)-PIPERIDIN-4-YL)-PHENYL)-9H-PURINE'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2UW0 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] with GVK as [http://en.wikipedia.org/wiki/ligand ligand]. Known structural/functional Site: <scene name='pdbsite=AC1:Gvk Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http:// | + | 2UW0 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus] with <scene name='pdbligand=GVK:'>GVK</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Known structural/functional Site: <scene name='pdbsite=AC1:Gvk Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2UW0 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: transferase/inhibitor complex]] | [[Category: transferase/inhibitor complex]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 13:24:50 2008'' |
Revision as of 11:24, 23 January 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 Wed Jan 23 13:24:50 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
