2ow3

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{{STRUCTURE_2ow3| PDB=2ow3 | SCENE= }}
{{STRUCTURE_2ow3| PDB=2ow3 | SCENE= }}
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'''Glycogen synthase kinase-3 beta in complex with bis-(indole)maleimide pyridinophane inhibitor'''
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===Glycogen synthase kinase-3 beta in complex with bis-(indole)maleimide pyridinophane inhibitor===
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==Overview==
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Novel bis(indolyl)maleimide pyridinophanes 3, 9a, 9b, 10a, 10b, and 11 were prepared by cobalt-mediated [2+2+2] cycloaddition of an appropriate alpha,omega-diyne with an N,N-dialkylcyanamide. These macrocyclic heterophanes were found to be potent, selective inhibitors of glycogen synthase kinase-3beta. An X-ray structure of a co-crystal of GSK-3beta and 3 (IC(50)=3nM) depicts the hydrogen bonding and hydrophobic interactions in the ATP-binding pocket of this serine/threonine protein kinase.
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{{ABSTRACT_PUBMED_17350261}}
==About this Structure==
==About this Structure==
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[[Category: Kinase-inhibitor complex]]
[[Category: Kinase-inhibitor complex]]
[[Category: Transferase]]
[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 11:46:58 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 15:15:22 2008''

Revision as of 12:15, 27 July 2008

Image:2ow3.png

Template:STRUCTURE 2ow3

Glycogen synthase kinase-3 beta in complex with bis-(indole)maleimide pyridinophane inhibitor

Template:ABSTRACT PUBMED 17350261

About this Structure

2OW3 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Novel bis(indolyl)maleimide pyridinophanes that are potent, selective inhibitors of glycogen synthase kinase-3., Zhang HC, Bonaga LV, Ye H, Derian CK, Damiano BP, Maryanoff BE, Bioorg Med Chem Lett. 2007 May 15;17(10):2863-8. Epub 2007 Feb 25. PMID:17350261

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