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2f7z

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[[Image:2f7z.gif|left|200px]]
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{{STRUCTURE_2f7z| PDB=2f7z | SCENE= }}
{{STRUCTURE_2f7z| PDB=2f7z | SCENE= }}
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'''Protein Kinase A bound to (R)-1-(1H-Indol-3-ylmethyl)-2-(2-pyridin-4-yl-[1,7]naphtyridin-5-yloxy)-ehylamine'''
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===Protein Kinase A bound to (R)-1-(1H-Indol-3-ylmethyl)-2-(2-pyridin-4-yl-[1,7]naphtyridin-5-yloxy)-ehylamine===
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==Overview==
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Structure-based design and synthesis of the 3,4'-bispyridinylethylene series led to the discovery of 3-isoquinolinylpyridine 13a as a potent PKB/Akt inhibitor with an IC(50) of 1.3nM against Akt1. Compound 13a shows excellent selectivity against distinct families of kinases such as tyrosine kinases and CAMK, and displays poor to marginal selectivity against closely related kinases in the AGC and CMGC families. Moreover, 13a demonstrates potent cellular activity comparable to staurosporine, with IC(50) values of 0.42 and 0.59microM against MiaPaCa-2 and the Akt1 overexpressing FL5.12-Akt1, respectively. Inhibition of phosphorylation of the Akt downstream target GSK3 was also observed in FL5.12-Akt1 cells with an EC(50) of 1.5microM. The X-ray structures of 12 and 13a in complex with PKA in the ATP-binding site were determined.
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(as it appears on PubMed at http://www.pubmed.gov), where 16413780 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16413780}}
==About this Structure==
==About this Structure==
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[[Category: Akt inhibitor]]
[[Category: Akt inhibitor]]
[[Category: Protein kinase some]]
[[Category: Protein kinase some]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 03:34:13 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 12:45:57 2008''

Revision as of 09:46, 28 July 2008

Image:2f7z.png

Template:STRUCTURE 2f7z

Protein Kinase A bound to (R)-1-(1H-Indol-3-ylmethyl)-2-(2-pyridin-4-yl-[1,7]naphtyridin-5-yloxy)-ehylamine

Template:ABSTRACT PUBMED 16413780

About this Structure

2F7Z is a Single protein structure of sequence from Bos taurus. Full crystallographic information is available from OCA.

Reference

Synthesis and structure-activity relationship of 3,4'-bispyridinylethylenes: discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer., Li Q, Woods KW, Thomas S, Zhu GD, Packard G, Fisher J, Li T, Gong J, Dinges J, Song X, Abrams J, Luo Y, Johnson EF, Shi Y, Liu X, Klinghofer V, Des Jong R, Oltersdorf T, Stoll VS, Jakob CG, Rosenberg SH, Giranda VL, Bioorg Med Chem Lett. 2006 Apr 1;16(7):2000-7. Epub 2006 Jan 18. PMID:16413780

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