NCIt definition : An orally bioavailable inhibitor of mitogen-activated protein kinase interacting serine/threonine-protein
kinase 1 (MKNK1), with potential antineoplastic activity. Upon oral administration,
MKNK1 inhibitor BAY 1143269 binds to MKNK1, thereby preventing its activation and
the downstream MKNK1-mediated phosphorylation and activation of eukaryotic translation
initiation factor 4E (eIF4E). As eIF4E enhances the synthesis of oncogenic proteins,
preventing eIF4E activity inhibits the synthesis of tumor angiogenic factors and leads
to both the inhibition of cellular proliferation and apoptosis in susceptible tumor
cells. eIF4E, overexpressed in a variety of cancer cells, plays a key role in tumor
cell proliferation and survival.;
Semantic type(s)