2uw0: Difference between revisions
No edit summary |
No edit summary |
||
| Line 4: | Line 4: | ||
==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== | ||
| Line 13: | Line 13: | ||
[[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]] | ||
| Line 36: | Line 36: | ||
[[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
|
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 GVK as ligand. Known structural/functional Site: AC1. 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
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
