4uzd
From Proteopedia
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| - | ''' | + | ==SAR156497 an exquisitely selective inhibitor of Aurora kinases== |
| + | <StructureSection load='4uzd' size='340' side='right' caption='[[4uzd]], [[Resolution|resolution]] 3.20Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[4uzd]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4UZD OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4UZD FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=QMN:ETHYL+(9S)-9-[3-(1H-BENZIMIDAZOL-2-YLOXY)PHENYL]-8-OXO-4,5,6,7,8,9-HEXAHYDRO-2H-PYRROLO[3,4-B]QUINOLINE-3-CARBOXYLATE'>QMN</scene></td></tr> | ||
| + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4uzh|4uzh]]</td></tr> | ||
| + | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </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=4uzd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4uzd OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4uzd RCSB], [http://www.ebi.ac.uk/pdbsum/4uzd PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | The Aurora family of serine/threonine kinases is essential for mitosis. Their crucial role in cell cycle regulation and aberrant expression in a broad range of malignancies have been demonstrated and have prompted intensive search for small molecule Aurora inhibitors. Indeed, several of them have reached the clinic as potential anticancer therapies. We report herein the discovery and optimization of a novel series of tricyclic molecules that has led to SAR156497, an exquisitely selective Aurora A-C inhibitor with in vitro and in vivo efficacy. We also provide insights into its mode of binding to its target proteins, which could explain its selectivity. | ||
| - | + | SAR156497 an exquisitely selective inhibitor of Aurora kinases.,Carry JC, Clerc FF, Minoux H, Schio L, Mauger J, Nair A, Parmantier E, Le Moigne R, Delorme C, Nicolas JP, Krick A, Abecassis PY, Crocq-Stuerga V, Pouzieux S, Delarbre L, Maignan S, Bertrand T, Bjergarde K, Ma N, Lachaud S, Guizani H, Lebel R, Doerflinger G, Monget S, Perron S, Gasse F, Angouillant-Boniface O, Filoche-Romme BJ, Murer M, Gontier S, Prevost C, Monteiro ML, Combeau C J Med Chem. 2014 Nov 4. PMID:25369539<ref>PMID:25369539</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
| - | + | == References == | |
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Non-specific serine/threonine protein kinase]] | ||
| + | [[Category: Crenne, J Y]] | ||
| + | [[Category: Delarbre, L]] | ||
| + | [[Category: Pouzieux, S]] | ||
| + | [[Category: Transferase]] | ||
Revision as of 12:38, 19 November 2014
SAR156497 an exquisitely selective inhibitor of Aurora kinases
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