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Mitogen-activated protein kinase 1 (MAPK1/ERK2) and Mitogen-activated protein kinase 3 (MAPK3/ERK1) are closely related serine/threonine kinases that serve as core components of the ERK/MAPK signaling cascade. They integrate extracellular signals to regulate diverse cellular processes, most notably cell proliferation, survival, and differentiation. ERK1/2 are activated by phosphorylation through upstream MEK1/2 in response to growth factors and other stimuli, subsequently translocating to the nucleus where they phosphorylate a wide range of transcription factors and other substrates. Dysregulation of ERK1/2 signaling contributes to the development and progression of many cancers and other diseases, which has made ERK1/2 compelling therapeutic targets.
Inhibition of kinase activity (blocking phosphorylation of downstream targets) Disruption of ERK activation, leading to decreased cell proliferation and/or increased apoptosis
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