Targeting MEK

    • Mitogen-activated protein kinase kinases or MAPKK (also known as MEK or MAP2K) is a family of kinase enzymes in the RAS MAPK pathway.
    • MEK family consists of seven genes: MEK1 (MAP2K1), MEK2 (MAPK2K2), MKK3 (MAP2K3), MKK4 (MAP2K4), MKK5 (MAP2K5), MKK6 (MAP2K6), and MKK7 (MAP2K7).
    • MEK1 and MEK2 activate MAPK, MKK3 and MKK6 activate p38, and MKK4 and MKK7 activate JNK.
    • Inhibitors of MEK1/2 have shown efficacy in BRAF- and KRAS-mutated cancers.
    • Mutations in MEK1/2 and BRAF amplification have been identified as potential mechanisms of resistance to MEK inhibitors in cancer cells boring BRAF V600E mutation.
    Other topics in Molecular Targets and Pathways