1uv5
From Proteopedia
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| - | [[Image:1uv5.gif|left|200px]]<br /> | + | [[Image:1uv5.gif|left|200px]]<br /><applet load="1uv5" size="450" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1uv5" size="450" color="white" frame="true" align="right" spinBox="true" | + | |
caption="1uv5, resolution 2.80Å" /> | caption="1uv5, resolution 2.80Å" /> | ||
'''GLYCOGEN SYNTHASE KINASE 3 BETA COMPLEXED WITH 6-BROMOINDIRUBIN-3'-OXIME'''<br /> | '''GLYCOGEN SYNTHASE KINASE 3 BETA COMPLEXED WITH 6-BROMOINDIRUBIN-3'-OXIME'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1UV5 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with PO4, CL, CO and BRW as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37] | + | 1UV5 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with PO4, CL, CO and BRW as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37] Known structural/functional Site: <scene name='pdbsite=AC1:Po4 Binding Site For Chain A'>AC1</scene>. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1UV5 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: wnt signaling pathway]] | [[Category: wnt signaling pathway]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Dec 18 18:13:03 2007'' |
Revision as of 16:03, 18 December 2007
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GLYCOGEN SYNTHASE KINASE 3 BETA COMPLEXED WITH 6-BROMOINDIRUBIN-3'-OXIME
Overview
Gastropod mollusks have been used for over 2500 years to produce the, "Tyrian purple" dye made famous by the Phoenicians. This dye is, constituted of mixed bromine-substituted indigo and indirubin isomers., Among these, the new natural product 6-bromoindirubin and its synthetic, cell-permeable derivative, 6-bromoindirubin-3'-oxime (BIO), display, remarkable selective inhibition of glycogen synthase kinase-3 (GSK-3)., Cocrystal structure of GSK-3beta/BIO and CDK5/p25/indirubin-3'-oxime were, resolved, providing a detailed view of indirubins' interactions within the, ATP binding pocket of these kinases. BIO but not 1-methyl-BIO, its kinase, inactive analog, also inhibited the phosphorylation on Tyr276/216, a, GSK-3alpha/beta activation site. BIO but not 1-methyl-BIO reduced, beta-catenin phosphorylation on a GSK-3-specific site in cellular models., BIO but not 1-methyl-BIO closely mimicked Wnt signaling in Xenopus, embryos. 6-bromoindirubins thus provide a new scaffold for the development, of selective and potent pharmacological inhibitors of GSK-3.
About this Structure
1UV5 is a Single protein structure of sequence from Homo sapiens with PO4, CL, CO and BRW as ligands. Active as Transferred entry: 2.7.11.1, with EC number 2.7.1.37 Known structural/functional Site: . Full crystallographic information is available from OCA.
Reference
GSK-3-selective inhibitors derived from Tyrian purple indirubins., Meijer L, Skaltsounis AL, Magiatis P, Polychronopoulos P, Knockaert M, Leost M, Ryan XP, Vonica CA, Brivanlou A, Dajani R, Crovace C, Tarricone C, Musacchio A, Roe SM, Pearl L, Greengard P, Chem Biol. 2003 Dec;10(12):1255-66. PMID:14700633
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