MNK1 inhibitor

MNK1 inhibitors are a class of therapeutic agents designed to target Mitogen-activated protein kinase-interacting kinase 1 (MNK1). MNK1, along with its isoform MNK2, is the only known kinase responsible for the phosphorylation of eukaryotic translation initiation factor 4E (eIF4E) at the Ser209 residue. This phosphorylation event is a critical step in the translation of specific mRNAs that promote tumor progression, metastasis, and resistance to therapy. Because MNK1/2 are largely dispensable for normal cellular function, their inhibition is considered a promising strategy for cancer treatment with a potentially favorable safety profile. The class includes various modalities, such as ATP-competitive small molecules (e.g., BAY 1143269, CGP57380), inhibitors that stabilize the inactive DFD-out conformation (e.g., EB1), and novel proteolysis-targeting chimera (PROTAC) degraders (e.g., P11-2). These agents are being investigated for a range of malignancies, including glioblastoma, T-cell acute lymphoblastic leukemia (T-ALL), and non-small cell lung cancer (NSCLC), often in combination with other treatments to overcome resistance.

Other names

MAPK-interacting kinase 1 inhibitorMnk1 inhibitorMnk-1 inhibitorMnk 1 inhibitorMAPK-interacting serine/threonine-protein kinase 1 inhibitor