2uw0

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[[Image:2uw0.gif|left|200px]]
[[Image:2uw0.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2uw0 |SIZE=350|CAPTION= <scene name='initialview01'>2uw0</scene>, resolution 2.00&Aring;
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The line below this paragraph, containing "STRUCTURE_2uw0", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Gvk+Binding+Site+For+Chain+A'>AC1</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=GVK:6-{4-[4-(4-CHLOROPHENYL)PIPERIDIN-4-YL]PHENYL}-9H-PURINE'>GVK</scene>, <scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_2uw0| PDB=2uw0 | SCENE= }}
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|RELATEDENTRY=[[1cmk|1CMK]], [[1xh4|1XH4]], [[1xh5|1XH5]], [[1xh6|1XH6]], [[1xh7|1XH7]], [[1xh8|1XH8]], [[1xh9|1XH9]], [[1xha|1XHA]], [[1ydr|1YDR]], [[2c1a|2C1A]], [[2c1b|2C1B]], [[2f7e|2F7E]], [[2gni|2GNI]], [[2jds|2JDS]], [[2jdt|2JDT]], [[2jdv|2JDV]], [[1kmu|1KMU]], [[1kmw|1KMW]], [[1q24|1Q24]], [[1q61|1Q61]], [[1q62|1Q62]], [[1q8t|1Q8T]], [[1q8u|1Q8U]], [[1q8w|1Q8W]], [[1smh|1SMH]], [[1stc|1STC]], [[1sve|1SVE]], [[1svg|1SVG]], [[1svh|1SVH]], [[1szm|1SZM]], [[1veb|1VEB]], [[1yds|1YDS]], [[1ydt|1YDT]], [[2gfc|2GFC]], [[2gnf|2GNF]], [[2gng|2GNG]], [[2gnh|2GNH]], [[2gnj|2GNJ]], [[2gnl|2GNL]], [[2uvx|2UVX]], [[2uvy|2UVY]], [[2uvz|2UVZ]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2uw0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2uw0 OCA], [http://www.ebi.ac.uk/pdbsum/2uw0 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2uw0 RCSB]</span>
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}}
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'''STRUCTURE OF PKA-PKB CHIMERA COMPLEXED WITH 6-(4-(4-(4-CHLORO-PHENYL)-PIPERIDIN-4-YL)-PHENYL)-9H-PURINE'''
'''STRUCTURE OF PKA-PKB CHIMERA COMPLEXED WITH 6-(4-(4-(4-CHLORO-PHENYL)-PIPERIDIN-4-YL)-PHENYL)-9H-PURINE'''
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[[Category: Mchardy, T.]]
[[Category: Mchardy, T.]]
[[Category: Rowlands, M G.]]
[[Category: Rowlands, M G.]]
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[[Category: atp-binding]]
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[[Category: Atp-binding]]
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[[Category: camp]]
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[[Category: Camp]]
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[[Category: kinase]]
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[[Category: Kinase]]
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[[Category: lipoprotein]]
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[[Category: Lipoprotein]]
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[[Category: myristate]]
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[[Category: Myristate]]
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[[Category: nuclear protein]]
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[[Category: Nuclear protein]]
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[[Category: nucleotide-binding]]
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[[Category: Nucleotide-binding]]
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[[Category: phosphorylation]]
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[[Category: Phosphorylation]]
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[[Category: protein kinase inhibitor]]
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[[Category: Protein kinase inhibitor]]
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[[Category: serine/threonine-protein kinase]]
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[[Category: Serine/threonine-protein kinase]]
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[[Category: transferase]]
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[[Category: Transferase]]
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[[Category: transferase/inhibitor complex]]
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[[Category: Transferase/inhibitor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 17:37:18 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 05:05:14 2008''
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Revision as of 14:37, 4 May 2008

Image:2uw0.gif

Template:STRUCTURE 2uw0

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. 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 Sun May 4 17:37:18 2008

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OCA

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