AUM003
BBB penetrating mRNA
translation inhibitor
AUM003 inhibits activity of the serine/threonine kinases MNK1/MNK2 and down-regulates eukaryotic translation initiation factor 4E (eIF4E) by down regulating S209 phosphorylation on eIF4E by MNK1 and MNK2. Thus, by preventing the phosphorylation of eIF4E, MNK inhibition could provide a viable therapeutic approach in high-eIF4E dependent cancers, neurodevelopmental disorders, and psychiatric disorders. AUM003 is a blood brain barrier penetrant with strong monotherapy activity in various cancers.
MECHANISM OF ACTION
Modulation of MNK activity affects translation of mRNAs involved in cancer development, progression, and their resistance to therapies. Serine/threonine kinases MNK1/MNK2 inhibition Down-regulates eIF4E by S209 phosphorylation on eIF4E. Downregulation of eIF4E does not impact normal cellular function but appears to make the cell less likely to exhibit tumor phenotype.
