1h8f
From Proteopedia
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==Overview== | ==Overview== | ||
| - | Glycogen synthase kinase 3 beta (GSK3 beta) plays a key role in insulin, and Wnt signaling, phosphorylating downstream targets by default, and, becoming inhibited following the extracellular signaling event. The, crystal structure of human GSK3 beta shows a catalytically active, conformation in the absence of activation-segment phosphorylation, with, the sulphonate of a buffer molecule bridging the activation-segment and, N-terminal domain in the same way as the phosphate group of the, activation-segment phospho-Ser/Thr in other kinases. The location of this, oxyanion binding site in the substrate binding cleft indicates direct, coupling of P+4 phosphate-primed substrate binding and catalytic, activation, explains the ability of GSK3 beta to processively, hyperphosphorylate substrates | + | Glycogen synthase kinase 3 beta (GSK3 beta) plays a key role in insulin, and Wnt signaling, phosphorylating downstream targets by default, and, becoming inhibited following the extracellular signaling event. The, crystal structure of human GSK3 beta shows a catalytically active, conformation in the absence of activation-segment phosphorylation, with, the sulphonate of a buffer molecule bridging the activation-segment and, N-terminal domain in the same way as the phosphate group of the, activation-segment phospho-Ser/Thr in other kinases. The location of this, oxyanion binding site in the substrate binding cleft indicates direct, coupling of P+4 phosphate-primed substrate binding and catalytic, activation, explains the ability of GSK3 beta to processively, hyperphosphorylate substrates with Ser/Thr pentad-repeats, and suggests a, mechanism for autoinhibition in which the phosphorylated N terminus binds, as a competitive pseudosubstrate with phospho-Ser 9 occupying the P+4, site. |
==About this Structure== | ==About this Structure== | ||
| - | 1H8F is a | + | 1H8F 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 EPE as [http://en.wikipedia.org/wiki/ligand ligand]. 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] Structure known Active Site: AC1. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1H8F OCA]. |
==Reference== | ==Reference== | ||
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[[Category: kinase]] | [[Category: kinase]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 5 13:56:30 2007'' |
Revision as of 11:51, 5 November 2007
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GLYCOGEN SYNTHASE KINASE 3 BETA.
Overview
Glycogen synthase kinase 3 beta (GSK3 beta) plays a key role in insulin, and Wnt signaling, phosphorylating downstream targets by default, and, becoming inhibited following the extracellular signaling event. The, crystal structure of human GSK3 beta shows a catalytically active, conformation in the absence of activation-segment phosphorylation, with, the sulphonate of a buffer molecule bridging the activation-segment and, N-terminal domain in the same way as the phosphate group of the, activation-segment phospho-Ser/Thr in other kinases. The location of this, oxyanion binding site in the substrate binding cleft indicates direct, coupling of P+4 phosphate-primed substrate binding and catalytic, activation, explains the ability of GSK3 beta to processively, hyperphosphorylate substrates with Ser/Thr pentad-repeats, and suggests a, mechanism for autoinhibition in which the phosphorylated N terminus binds, as a competitive pseudosubstrate with phospho-Ser 9 occupying the P+4, site.
About this Structure
1H8F is a Single protein structure of sequence from Homo sapiens with EPE as ligand. 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.
Reference
Crystal structure of glycogen synthase kinase 3 beta: structural basis for phosphate-primed substrate specificity and autoinhibition., Dajani R, Fraser E, Roe SM, Young N, Good V, Dale TC, Pearl LH, Cell. 2001 Jun 15;105(6):721-32. PMID:11440715
Page seeded by OCA on Mon Nov 5 13:56:30 2007
