Mitogen-activated protein kinase 1 (ERK2) and Mitogen-activated protein kinase 3 (ERK1) (ERK2 (for MAPK1), ERK1 (for MAPK3))

Mitogen-activated protein kinase 1 (ERK2, MAPK1) and Mitogen-activated protein kinase 3 (ERK1, MAPK3) are highly conserved serine/threonine kinases and core effectors of the Ras-Raf-MEK-ERK signal transduction cascade. They are expressed in most tissues and play critical roles in regulating cellular processes such as proliferation, survival, differentiation, and response to extracellular signals. ERK1 and ERK2 are activated by dual phosphorylation events mediated by MEK1/2. Once activated, they translocate to the nucleus and phosphorylate various transcription factors and other proteins, orchestrating gene expression programs involved in cell cycle progression and survival. Dysregulation of ERK1/2 activity is a hallmark of numerous cancers, making them key therapeutic targets for small molecule kinase inhibitors. Despite high sequence similarity (~85%), subtle differences in regulation and function have been reported, but for drug discovery purposes, they are often considered functionally redundant and co-regulated[1][2][3][4][5][6][7].

Other names

MAPK1 (ERK2)MAPK3 (ERK1)Extracellular signal-regulated kinase 1Extracellular signal-regulated kinase 2p44 MAPK (ERK1)p42 MAPK (ERK2)

Inhibition of ERK phosphorylation and kinase activity Blockade of downstream signaling (gene expression, proliferation) Indirect suppression by targeting upstream Ras/Raf/MEK in the pathway