6lvk
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Crystal structure of FGFR2 in complex with 1,3,5-triazine derivative== | |
| + | <StructureSection load='6lvk' size='340' side='right'caption='[[6lvk]], [[Resolution|resolution]] 2.29Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[6lvk]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6LVK OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6LVK FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.29Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=EVC:~{N}-ethyl-2-[[4-[[4-(4-methylpiperazin-1-yl)-3-(2-morpholin-4-ylethoxy)phenyl]amino]-1,3,5-triazin-2-yl]amino]benzenesulfonamide'>EVC</scene>, <scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr> | ||
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=6lvk FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6lvk OCA], [https://pdbe.org/6lvk PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6lvk RCSB], [https://www.ebi.ac.uk/pdbsum/6lvk PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6lvk ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Fibroblast growth factor receptor 3 (FGFR3) is an attractive therapeutic target for the treatment of bladder cancer. We identified 1,3,5-triazine derivative 18b and pyrimidine derivative 40a as novel structures with potent and highly selective FGFR3 inhibitory activity over vascular endothelial growth factor receptor 2 (VEGFR2) using a structure-based drug design (SBDD) approach. X-ray crystal structure analysis suggests that interactions between 18b and amino acid residues located in the solvent region (Lys476 and Met488), and between 40a and Met529 located in the back pocket of FGFR3 may underlie the potent FGFR3 inhibitory activity and high kinase selectivity over VEGFR2. | ||
| - | + | Structure-based drug design of 1,3,5-triazine and pyrimidine derivatives as novel FGFR3 inhibitors with high selectivity over VEGFR2.,Kuriwaki I, Kameda M, Hisamichi H, Kikuchi S, Iikubo K, Kawamoto Y, Moritomo H, Kondoh Y, Amano Y, Tateishi Y, Echizen Y, Iwai Y, Noda A, Tomiyama H, Suzuki T, Hirano M Bioorg Med Chem. 2020 May 15;28(10):115453. doi: 10.1016/j.bmc.2020.115453. Epub , 2020 Mar 28. PMID:32278710<ref>PMID:32278710</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| - | [[Category: Amano | + | <div class="pdbe-citations 6lvk" style="background-color:#fffaf0;"></div> |
| - | [[Category: Echizen | + | |
| - | [[Category: Tateishi | + | ==See Also== |
| + | *[[Fibroblast growth factor receptor 3D receptor|Fibroblast growth factor receptor 3D receptor]] | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Amano Y]] | ||
| + | [[Category: Echizen Y]] | ||
| + | [[Category: Tateishi Y]] | ||
Current revision
Crystal structure of FGFR2 in complex with 1,3,5-triazine derivative
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