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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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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: 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.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2014
Acesso em linha: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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