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Mitogen-activated protein kinase kinase 1 and 2 (MEK1 and MEK2) are dual-specificity protein kinases that play a pivotal role in the mitogen-activated protein kinase (MAPK) signaling cascade. They act as direct upstream activators of ERK1/2 (extracellular signal-regulated kinases) through phosphorylation. The MEK1/2-ERK pathway transduces signals from cell surface receptors such as receptor tyrosine kinases, regulating fundamental cellular processes including proliferation, differentiation, and survival. Dysregulation or constitutive activation of the MEK/ERK pathway is implicated in several human cancers, making MEK1/2 attractive therapeutic targets. Selective inhibitors of MEK1/2 have been approved for the treatment of melanoma and are being evaluated for other cancers
MEK inhibitors: block MEK1/2 kinase activity, preventing phosphorylation/activation of downstream MAPKs (such as ERK1/2), thereby inhibiting cell proliferation and inducing apoptosis
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