2uw0: Difference between revisions
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[[Image:2uw0.gif|left|200px]] | [[Image:2uw0.gif|left|200px]] | ||
'''STRUCTURE OF PKA-PKB CHIMERA COMPLEXED WITH 6-(4-(4-(4-CHLORO-PHENYL)-PIPERIDIN-4-YL)-PHENYL)-9H-PURINE''' | {{Structure | ||
|PDB= 2uw0 |SIZE=350|CAPTION= <scene name='initialview01'>2uw0</scene>, resolution 2.00Å | |||
|SITE= <scene name='pdbsite=AC1:Gvk+Binding+Site+For+Chain+A'>AC1</scene> | |||
|LIGAND= <scene name='pdbligand=GVK:6-{4-[4-(4-CHLOROPHENYL)PIPERIDIN-4-YL]PHENYL}-9H-PURINE'>GVK</scene> | |||
|ACTIVITY= | |||
|GENE= | |||
}} | |||
'''STRUCTURE OF PKA-PKB CHIMERA COMPLEXED WITH 6-(4-(4-(4-CHLORO-PHENYL)-PIPERIDIN-4-YL)-PHENYL)-9H-PURINE''' | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
2UW0 is a [ | 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== | ||
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:// | 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]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | ''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
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| 2uw0, resolution 2.00Å | |||||||||||||
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| Sites: | AC1 | ||||||||||||
| Ligands: | GVK | ||||||||||||
| 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
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
