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Mitogen-activated protein kinase 1/2 (MAPK1/MAPK3, ERK2/ERK1) are evolutionarily conserved serine/threonine protein kinases central to the MAP kinase signaling cascade. They integrate biochemical signals from growth factors, mitogens, and cellular stress to regulate cell proliferation, survival, differentiation, and gene expression. ERK1/2 are activated by dual phosphorylation via upstream kinases MEK1/2, translocate to the nucleus, and phosphorylate transcription factors and other nuclear targets, driving cellular responses crucial for development and homeostasis. Dysregulation of ERK1/2 signaling is implicated in multiple diseases, especially cancer and inflammation, making them key therapeutic targets for drug development
Inhibition of ERK1/2 catalytic activity (blocks phosphorylation of downstream targets); Modulation of ERK1/2 phosphorylation state (prevents nuclear translocation and gene expression regulation)
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