Mitogen-activated protein kinase kinase 1 (MEK1) and Mitogen-activated protein kinase kinase 2 (MEK2) (MEK1 (MAP2K1) and MEK2 (MAP2K2))

Mitogen-activated protein kinase kinase 1 (MEK1) and mitogen-activated protein kinase kinase 2 (MEK2) are serine/threonine kinases integral to the MAPK/ERK signaling pathway, which transmits proliferation signals from the cell surface to the nucleus. They are directly downstream of BRAF and upstream of ERK in the pathway. In many cancers, especially melanoma, mutations in BRAF (most commonly V600E or V600K) lead to constitutive activation of MEK and subsequent uncontrolled cell growth. Trametinib is a highly selective, reversible allosteric inhibitor of MEK1/2 and is used to treat tumors harboring activating BRAF mutations, often in combination with BRAF inhibitors such as dabrafenib

Other names

MEK1MEK2MAP2K1MAP2K2dual specificity mitogen-activated protein kinase kinase 1/2

Allosteric inhibition of MEK1 and MEK2 kinase activity, blocking MAPK/ERK signaling downstream of mutated BRAF