1uv5
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GLYCOGEN SYNTHASE KINASE 3 BETA COMPLEXED WITH 6-BROMOINDIRUBIN-3'-OXIME
OverviewOverview
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 ... [(full description)]
About this StructureAbout 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]. Structure known Active Site: AC1. Full crystallographic information is available from [OCA].
ReferenceReference
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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