Mitogen-activated protein kinase 1 and 3 (ERK1/ERK2)

Mitogen-activated protein kinase 1 (ERK2) and mitogen-activated protein kinase 3 (ERK1) are closely related serine/threonine protein kinases that function as critical effectors in the MAPK/ERK pathway. Activated by upstream kinases (MEK1/2) in response to growth factors and other signals, ERK1/2 regulate a host of cellular processes, including proliferation, differentiation, survival, and transcription. Dysregulation of ERK1 and ERK2 is strongly linked to human diseases, particularly cancer, where the pathway is frequently constitutively active; this has made both kinases important therapeutic targets for kinase inhibitor development. Drugs directly targeting ERK1/2 remain investigational but are in clinical development, especially for cancers that have developed resistance to BRAF or MEK inhibitors[3][4][6].

Other names

Extracellular signal-regulated kinase 1MAP kinase 1p44-ERK1MAPK 3PRKM3ERT2Insulin-stimulated MAP2 kinaseMicrotubule-associated protein 2 kinasep44 MAP kinaseMNK1Mtap2kExtracellular signal-regulated kinase 2MAP kinase 2p42-ERK2MAPK 1PRKM1ERT1ERK-2p41p40MAPK2

Inhibition of kinase activity to block phosphorylation of downstream targets in the MAPK pathway, thereby reducing cell proliferation and inducing apoptosis in tumors with MAPK pathway activation.