1uv5: Difference between revisions

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[[Image:1uv5.~~gif~~|left|200px]]

[[Image:1uv5.png|left|200px]]

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~~'''~~GLYCOGEN SYNTHASE KINASE 3 BETA COMPLEXED WITH 6-BROMOINDIRUBIN-3'-OXIME~~'''~~

===GLYCOGEN SYNTHASE KINASE 3 BETA COMPLEXED WITH 6-BROMOINDIRUBIN-3'-OXIME===

~~==Overview==~~

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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.

The line below this paragraph, {{ABSTRACT_PUBMED_14700633}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 14700633 is the PubMed ID number.

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==About this Structure==

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[[Category: Transferase serine/threonine-protein kinase]]

[[Category: Wnt signaling pathway]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Sat May 3 11~~:43:57 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 14:00:52 2008''

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-[[Image:1uv5.gif|left|200px]]
+{{Seed}}
+[[Image:1uv5.png|left|200px]]
 <!--
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 {{STRUCTURE_1uv5|  PDB=1uv5  |  SCENE=  }}
-'''GLYCOGEN SYNTHASE KINASE 3 BETA COMPLEXED WITH 6-BROMOINDIRUBIN-3'-OXIME'''
+===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.
+The line below this paragraph, {{ABSTRACT_PUBMED_14700633}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 14700633 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_14700633}}
 ==About this Structure==
@@ Line 30: / Line 34: @@
 [[Category: Transferase serine/threonine-protein kinase]]
 [[Category: Wnt signaling pathway]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 11:43:57 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 14:00:52 2008''