2ow3

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[[Image:2ow3.jpg|left|200px]]
[[Image:2ow3.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2ow3 |SIZE=350|CAPTION= <scene name='initialview01'>2ow3</scene>, resolution 2.80&Aring;
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The line below this paragraph, containing "STRUCTURE_2ow3", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Bim+Binding+Site+For+Residue+A+387'>AC1</scene> and <scene name='pdbsite=AC2:Bim+Binding+Site+For+Residue+B+387'>AC2</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=BIM:BIS-(INDOLE)MALEIMIDE+PYRIDINOPHANE'>BIM</scene>, <scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/[Tau_protein]_kinase [Tau protein] kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.26 2.7.11.26] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= GSK3B ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2ow3| PDB=2ow3 | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2ow3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ow3 OCA], [http://www.ebi.ac.uk/pdbsum/2ow3 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2ow3 RCSB]</span>
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}}
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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]]
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[[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.]]
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[[Category: kinase-inhibitor complex]]
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[[Category: Kinase-inhibitor complex]]
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[[Category: transferase]]
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[[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 Mon Mar 31 04:24:00 2008''
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Revision as of 08:46, 4 May 2008

Template:STRUCTURE 2ow3

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

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