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

Mitogen-activated protein kinase kinase 1/2 are crucial dual-specificity kinases in the MAPK signaling cascade, transmitting signals from upstream activators (such as Ras and Raf) to ERK1/2 MAP kinases[1][4][5]. Activation of MEK1/2 promotes cell proliferation, survival, and differentiation, while dysregulation is implicated in various cancers, especially those with activating mutations in upstream molecules like BRAF[1][4]. Therapeutic blockade of MEK inhibits downstream signaling, leading to antiproliferative and pro-apoptotic effects, which is the basis for their use in oncology[1][4][5]. They remain central targets for cancer drug development, though therapeutic challenges persist due to resistance and toxicity[1][4].

Other names

MAP2K1 (MEK1, MAPKK1)MAP2K2 (MEK2, MAPKK2)MAPKKMEK

Kinase inhibition: Drugs block phosphorylation and activation of ERK1/2 by MEK1/2; Suppression of cell proliferation and induction of apoptosis