4o6e

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<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4o6e FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4o6e OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4o6e RCSB], [http://www.ebi.ac.uk/pdbsum/4o6e PDBsum]</span></td></tr>
<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4o6e FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4o6e OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4o6e RCSB], [http://www.ebi.ac.uk/pdbsum/4o6e PDBsum]</span></td></tr>
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== Publication Abstract from PubMed ==
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The discovery and optimization of a series of tetrahydropyridopyrimidine based extracellular signal-regulated kinase (Erks) inhibitors discovered via HTS and structure based drug design is reported. The compounds demonstrate potent and selective inhibition of Erk2 and knockdown of phospho-RSK levels in HepG2 cells and tumor xenografts.
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Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2.,Blake JF, Gaudino JJ, De Meese J, Mohr P, Chicarelli M, Tian H, Garrey R, Thomas A, Siedem CS, Welch MB, Kolakowski G, Kaus R, Burkard M, Martinson M, Chen H, Dean B, Dudley DA, Gould SE, Pacheco P, Shahidi-Latham S, Wang W, West K, Yin J, Moffat J, Schwarz JB Bioorg Med Chem Lett. 2014 Jun 15;24(12):2635-9. doi: 10.1016/j.bmcl.2014.04.068., Epub 2014 Apr 29. PMID:24813737<ref>PMID:24813737</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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== References ==
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<references/>
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Revision as of 05:10, 25 June 2014

Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine Inhibitors of Erk2

4o6e, resolution 1.95Å

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