2uw0

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[[Image:2uw0.gif|left|200px]]<br /><applet load="2uw0" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:2uw0.gif|left|200px]]
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caption="2uw0, resolution 2.00&Aring;" />
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'''STRUCTURE OF PKA-PKB CHIMERA COMPLEXED WITH 6-(4-(4-(4-CHLORO-PHENYL)-PIPERIDIN-4-YL)-PHENYL)-9H-PURINE'''<br />
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{{Structure
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|PDB= 2uw0 |SIZE=350|CAPTION= <scene name='initialview01'>2uw0</scene>, resolution 2.00&Aring;
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|SITE= <scene name='pdbsite=AC1:Gvk+Binding+Site+For+Chain+A'>AC1</scene>
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|LIGAND= <scene name='pdbligand=GVK:6-{4-[4-(4-CHLOROPHENYL)PIPERIDIN-4-YL]PHENYL}-9H-PURINE'>GVK</scene>
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|ACTIVITY=
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|GENE=
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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'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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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].
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2UW0 is a [[Protein complex]] structure of sequences from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2UW0 OCA].
==Reference==
==Reference==
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17451235 17451235]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/17451235 17451235]
[[Category: Bos taurus]]
[[Category: Bos taurus]]
[[Category: Protein complex]]
[[Category: Protein complex]]
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[[Category: transferase/inhibitor complex]]
[[Category: transferase/inhibitor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:50:51 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 18:40:24 2008''

Revision as of 16:40, 20 March 2008

Image:2uw0.gif


PDB ID 2uw0

Drag the structure with the mouse to rotate
, resolution 2.00Å
Sites:
Ligands:
Coordinates: save as pdb, mmCIF, xml



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 Thu Mar 20 18:40:24 2008

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