2ow3
From Proteopedia
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[[Image:2ow3.jpg|left|200px]] | [[Image:2ow3.jpg|left|200px]] | ||
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'''Glycogen synthase kinase-3 beta in complex with bis-(indole)maleimide pyridinophane inhibitor''' | '''Glycogen synthase kinase-3 beta in complex with bis-(indole)maleimide pyridinophane inhibitor''' | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
- | [[Category: [Tau protein] kinase]] | ||
[[Category: Bonaga, L V.]] | [[Category: Bonaga, L V.]] | ||
[[Category: Damiano, B P.]] | [[Category: Damiano, B P.]] | ||
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[[Category: Ye, H.]] | [[Category: Ye, H.]] | ||
[[Category: Zhang, H C.]] | [[Category: Zhang, H C.]] | ||
- | [[Category: | + | [[Category: Kinase-inhibitor complex]] |
- | [[Category: | + | [[Category: Transferase]] |
- | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 11:46:58 2008'' | |
- | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + |
Revision as of 08:46, 4 May 2008
Glycogen synthase kinase-3 beta in complex with bis-(indole)maleimide pyridinophane inhibitor
Overview
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.
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 Page seeded by OCA on Sun May 4 11:46:58 2008