4d2s
From Proteopedia
(Difference between revisions)
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| - | ''' | + | ==Human TTK in complex with a Dyrk1B inhibitor== |
| + | <StructureSection load='4d2s' size='340' side='right' caption='[[4d2s]], [[Resolution|resolution]] 2.50Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[4d2s]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4D2S OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4D2S FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=DYK:N-{2-METHOXY-4-[(1-METHYLPIPERIDIN-4-YL)OXY]PHENYL}-4-(1H-PYRROLO[2,3-C]PYRIDIN-3-YL)PYRIMIDIN-2-AMINE'>DYK</scene></td></tr> | ||
| + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4d2r|4d2r]]</td></tr> | ||
| + | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Dual-specificity_kinase Dual-specificity kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.12.1 2.7.12.1] </span></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=4d2s FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4d2s OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4d2s RCSB], [http://www.ebi.ac.uk/pdbsum/4d2s PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [[http://www.uniprot.org/uniprot/TTK_HUMAN TTK_HUMAN]] Phosphorylates proteins on serine, threonine, and tyrosine. Probably associated with cell proliferation. Essential for chromosome alignment by enhancing AURKB activity (via direct CDCA8 phosphorylation) at the centromere, and for the mitotic checkpoint.<ref>PMID:18243099</ref> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Potent and selective inhibitors of Dyrk1B kinase were developed to explore the hypothesis, based on siRNA studies, that Dyrk1B may be a resistance mechanism in cells undergoing a stress response. | ||
| - | + | Discovery and Optimization of a Novel Series of Dyrk1B Kinase Inhibitors To Explore a MEK Resistance Hypothesis.,Kettle JG, Ballard P, Bardelle C, Cockerill M, Colclough N, Critchlow SE, Debreczeni J, Fairley G, Fillery S, Graham MA, Goodwin L, Guichard S, Hudson K, Ward RA, Whittaker D J Med Chem. 2015 Mar 26;58(6):2834-44. doi: 10.1021/acs.jmedchem.5b00098. Epub, 2015 Mar 12. PMID:25738750<ref>PMID:25738750</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
| - | + | == References == | |
| - | [[Category: | + | <references/> |
| - | [[Category: | + | __TOC__ |
| + | </StructureSection> | ||
| + | [[Category: Dual-specificity kinase]] | ||
| + | [[Category: Ballard, P]] | ||
| + | [[Category: Bardelle, C]] | ||
[[Category: Butterworth, S]] | [[Category: Butterworth, S]] | ||
| + | [[Category: Colclough, N]] | ||
| + | [[Category: Crichlow, S]] | ||
| + | [[Category: Debreczeni, J E]] | ||
[[Category: Fairley, G]] | [[Category: Fairley, G]] | ||
[[Category: Fillery, S]] | [[Category: Fillery, S]] | ||
| - | [[Category: Ward, R.A]] | ||
| - | [[Category: Vincent, J]] | ||
| - | [[Category: Mahmood, A]] | ||
| - | [[Category: Whittaker, J]] | ||
| - | [[Category: Colclough, N]] | ||
[[Category: Goodwin, L]] | [[Category: Goodwin, L]] | ||
| - | [[Category: | + | [[Category: Graham, M A]] |
| - | + | ||
| - | + | ||
[[Category: Guichard, S]] | [[Category: Guichard, S]] | ||
| - | [[Category: | + | [[Category: Hudson, K]] |
| - | [[Category: | + | [[Category: Kettle, J G]] |
| - | [[Category: | + | [[Category: Mahmood, A]] |
| + | [[Category: Vincent, J]] | ||
| + | [[Category: Ward, R A]] | ||
| + | [[Category: Whittaker, D]] | ||
| + | [[Category: Oncology]] | ||
| + | [[Category: Transferase]] | ||
Revision as of 12:39, 22 April 2015
Human TTK in complex with a Dyrk1B inhibitor
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