4acc
From Proteopedia
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| - | [[ | + | ==GSK3b in complex with inhibitor== |
| + | <StructureSection load='4acc' size='340' side='right' caption='[[4acc]], [[Resolution|resolution]] 2.21Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[4acc]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4ACC OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4ACC FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=7YG:3-AMINO-6-(4-{[2-(DIMETHYLAMINO)ETHYL]SULFAMOYL}PHENYL)-N-PYRIDIN-3-YLPYRAZINE-2-CARBOXAMIDE'>7YG</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene></td></tr> | ||
| + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1gng|1gng]], [[1h8f|1h8f]], [[1i09|1i09]], [[1j1b|1j1b]], [[1j1c|1j1c]], [[1o6k|1o6k]], [[1o6l|1o6l]], [[1o9u|1o9u]], [[1pyx|1pyx]], [[1q3d|1q3d]], [[1q3w|1q3w]], [[1q41|1q41]], [[1q4l|1q4l]], [[1q5k|1q5k]], [[1r0e|1r0e]], [[1uv5|1uv5]], [[2jdo|2jdo]], [[2jdr|2jdr]], [[2jld|2jld]], [[2uw9|2uw9]], [[2x37|2x37]], [[2x39|2x39]], [[2xh5|2xh5]], [[3zrk|3zrk]], [[3zrl|3zrl]], [[3zrm|3zrm]], [[4acd|4acd]], [[4acg|4acg]], [[4ach|4ach]]</td></tr> | ||
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4acc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4acc OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4acc RCSB], [http://www.ebi.ac.uk/pdbsum/4acc PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Glycogen synthase kinase-3beta, also called tau phosphorylating kinase, is a proline-directed serine/threonine kinase which was originally identified due to its role in glycogen metabolism. Active forms of GSK3beta localize to pretangle pathology including dystrophic neuritis and neurofibrillary tangles in Alzheimer's disease (AD) brain. By using a high throughput screening (HTS) approach to search for new chemical series and cocrystallization of key analogues to guide the optimization and synthesis of our pyrazine series, we have developed highly potent and selective inhibitors showing cellular efficacy and blood-brain barrier penetrance. The inhibitors are suitable for in vivo efficacy testing and may serve as a new treatment strategy for Alzheimer's disease. | ||
| - | + | Discovery of Novel Potent and Highly Selective Glycogen Synthase Kinase-3beta (GSK3beta) Inhibitors for Alzheimer's Disease: Design, Synthesis, and Characterization of Pyrazines.,Berg S, Bergh M, Hellberg S, Hogdin K, Lo-Alfredsson Y, Soderman P, von Berg S, Weigelt T, Ormo M, Xue Y, Tucker J, Neelissen J, Jerning E, Nilsson Y, Bhat R J Med Chem. 2012 Apr 27. PMID:22489897<ref>PMID:22489897</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| + | </div> | ||
| - | + | ==See Also== | |
| - | + | *[[Glycogen synthase kinase 3|Glycogen synthase kinase 3]] | |
| - | == | + | == References == |
| - | [[ | + | <references/> |
| - | + | __TOC__ | |
| - | == | + | </StructureSection> |
| - | < | + | |
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
| - | [[Category: Ormo, M | + | [[Category: Ormo, M]] |
| - | [[Category: Xue, Y | + | [[Category: Xue, Y]] |
[[Category: Transferase]] | [[Category: Transferase]] | ||
Revision as of 17:04, 9 December 2014
GSK3b in complex with inhibitor
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