Discovery of novel Mnk inhibitors using mutation‐based induced‐fit virtual high‐throughput screening

Mnk kinases (Mnk1 and 2) are downstream effectors of Map kinase pathways and regulate phosphorylation of eukaryotic initiation factor 4E. Engagement of the Mnk pathway is critical in acute myeloid leukemia (AML) leukemogenesis and Mnk inhibitors have potent antileukemic properties in vitro and in vi...

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Veröffentlicht in:	Chemical biology & drug design 2019-10, Vol.94 (4), p.1813-1823
Hauptverfasser:	Mishra, Rama K., Clutter, Matthew R., Blyth, Gavin T., Kosciuczuk, Ewa M., Blackburn, Amy Z., Beauchamp, Elspeth M., Schiltz, Gary E., Platanias, Leonidas C.
Format:	Artikel
Sprache:	eng
Schlagworte:	AML Drug Discovery eIF4E Glide Humans IFD Intracellular Signaling Peptides and Proteins - antagonists & inhibitors Intracellular Signaling Peptides and Proteins - metabolism Leukemia, Myeloid, Acute - drug therapy Leukemia, Myeloid, Acute - enzymology Mnk1 Mnk2 Molecular Docking Simulation Neoplasm Proteins - antagonists & inhibitors Neoplasm Proteins - metabolism Protein Kinase Inhibitors - chemistry Protein-Serine-Threonine Kinases - antagonists & inhibitors Protein-Serine-Threonine Kinases - metabolism vHTS
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