Fragment-Based Discovery of Type I Inhibitors of Maternal Embryonic Leucine Zipper Kinase

[Image: see text] Fragment-based drug design was successfully applied to maternal embryonic leucine zipper kinase (MELK). A low affinity (160 μM) fragment hit was identified, which bound to the hinge region with an atypical binding mode, and this was optimized using structure-based design into a low...

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Veröffentlicht in:ACS Med Chem Lett
Hauptverfasser: Johnson, Christopher N., Berdini, Valerio, Beke, Lijs, Bonnet, Pascal, Brehmer, Dirk, Coyle, Joseph E., Day, Phillip J., Frederickson, Martyn, Freyne, Eddy J. E., Gilissen, Ron A. H. J., Hamlett, Christopher C. F., Howard, Steven, Meerpoel, Lieven, McMenamin, Rachel, Patel, Sahil, Rees, David C., Sharff, Andrew, Sommen, François, Wu, Tongfei, Linders, Joannes T. M.
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2014
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4291735/
https://ncbi.nlm.nih.gov/pubmed/25589925
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml5001245
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