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...

Descrición completa

Gardado en:
Detalles Bibliográficos
Publicado en: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: American Chemical Society 2014
Acceso en liña: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
Tags: Engadir etiqueta
Sen Etiquetas, Sexa o primeiro en etiquetar este rexistro!

Títulos similares