Deregulation of translation initiation factor 4E (eIF4E) activity occurs in various types of cancer. Mitogen-activated protein kinase (MAPK)-interacting kinases 1 and 2 (MNK1 and MNK2) play important roles in the activation of eIF4E. Fragment hit expansion driven by structure-activity relationships led to the discovery of dual MNK1 and MNK2 inhibitors based on novel pyridine-benzamide scaffolds. These compounds showed promising in vitro and in vivo pharmacokinetic profiles and showed potent targeted inhibition of eIF4E phosphorylation in cells.
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