2uvx
From Proteopedia
| Line 11: | Line 11: | ||
'''STRUCTURE OF PKA-PKB CHIMERA COMPLEXED WITH 7-AZAINDOLE''' | '''STRUCTURE OF PKA-PKB CHIMERA COMPLEXED WITH 7-AZAINDOLE''' | ||
| + | |||
| + | ==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== | ==About this Structure== | ||
2UVX 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=2UVX OCA]. | 2UVX 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=2UVX 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:[http://www.ncbi.nlm.nih.gov/pubmed/17451235 17451235] | ||
[[Category: Bos taurus]] | [[Category: Bos taurus]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
| Line 25: | Line 31: | ||
[[Category: Mchardy, T.]] | [[Category: Mchardy, T.]] | ||
[[Category: Rowlands, M G.]] | [[Category: Rowlands, M G.]] | ||
| - | [[Category: Atp-binding]] | + | [[Category: Atp- binding]] |
[[Category: Camp]] | [[Category: Camp]] | ||
[[Category: Kinase]] | [[Category: Kinase]] | ||
| Line 37: | Line 43: | ||
[[Category: Transferase]] | [[Category: Transferase]] | ||
[[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 May 22 22:30:05 2008'' |
Revision as of 19:30, 22 May 2008
STRUCTURE OF PKA-PKB CHIMERA COMPLEXED WITH 7-AZAINDOLE
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
2UVX 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 May 22 22:30:05 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. | Atp- binding | Camp | Kinase | Lipoprotein | Myristate | Nuclear protein | Nucleotide-binding | Phosphorylation | Protein kinase inhibitor | Serine/threonine-protein kinase | Transferase | Transferase/inhibitor complex
