3cqu

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{{STRUCTURE_3cqu| PDB=3cqu | SCENE= }}
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'''Crystal Structure of Akt-1 complexed with substrate peptide and inhibitor'''
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===Crystal Structure of Akt-1 complexed with substrate peptide and inhibitor===
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==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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(as it appears on PubMed at http://www.pubmed.gov), where 18456494 is the PubMed ID number.
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{{ABSTRACT_PUBMED_18456494}}
==About this Structure==
==About this Structure==
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[[Category: Transport]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed May 28 09:22:49 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 13:12:06 2008''

Revision as of 10:12, 29 July 2008

Image:3cqu.png

Template:STRUCTURE 3cqu

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

Template:ABSTRACT PUBMED 18456494

About this Structure

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

Reference

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

Page seeded by OCA on Tue Jul 29 13:12:06 2008

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