2uvy: Difference between revisions

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'''STRUCTURE OF PKA-PKB CHIMERA COMPLEXED WITH METHYL-(4-(9H-PURIN-6-YL)-BENZYL)-AMINE'''

==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==

2UVY 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=2UVY 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: Protein complex]]

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[[Category: Transferase]]

[[Category: Transferase/inhibitor complex]]

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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu May 22 22:30:13 2008''

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@@ Line 11: / Line 11: @@
 '''STRUCTURE OF PKA-PKB CHIMERA COMPLEXED WITH METHYL-(4-(9H-PURIN-6-YL)-BENZYL)-AMINE'''
+==Overview==
+-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==
 UVY 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=2UVY 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: Protein complex]]
@@ Line 37: / Line 43: @@
 [[Category: Transferase]]
 [[Category: Transferase/inhibitor complex]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May  4 17:37:06 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu May 22 22:30:13 2008''