3cqw: Difference between revisions

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{{STRUCTURE_3cqw|  PDB=3cqw  |  SCENE=  }}  
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'''Crystal Structure of Akt-1 complexed with substrate peptide and inhibitor'''
===Crystal Structure of Akt-1 complexed with substrate peptide and inhibitor===




==Overview==
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Based on a high throughput screening hit, pyrrolopyrimidine inhibitors of the Akt kinase are explored. X-ray co-crystal structures of two lead series results in the understanding of key binding interactions, the design of new lead series, and enhanced potency. The syntheses of these series and their biological activities are described. Spiroindoline 13j is found to have an Akt1 kinase IC(50) of 2.4+/-0.6nM, Akt cell potency of 50+/-19nM, and provides 68% inhibition of tumor growth in a mouse xenograft model (50mg/kg, qd, po).
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{{ABSTRACT_PUBMED_18456494}}


==About this Structure==
==About this Structure==
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[[Category: Transport]]
[[Category: Transport]]
[[Category: Wnt signaling pathway]]
[[Category: Wnt signaling pathway]]
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Revision as of 19:04, 27 July 2008

File:3cqw.png

Template:STRUCTURE 3cqw

Crystal Structure of Akt-1 complexed with substrate peptide and inhibitorCrystal Structure of Akt-1 complexed with substrate peptide and inhibitor

Template:ABSTRACT PUBMED 18456494

About this StructureAbout this Structure

3CQW is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

ReferenceReference

Synthesis and structure based optimization of novel Akt inhibitors., Lippa B, Pan G, Corbett M, Li C, Kauffman GS, Pandit J, Robinson S, Wei L, Kozina E, Marr ES, Borzillo G, Knauth E, Barbacci-Tobin EG, Vincent P, Troutman M, Baker D, Rajamohan F, Kakar S, Clark T, Morris J, Bioorg Med Chem Lett. 2008 Apr 15;. PMID:18456494

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