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Target intelligence / Profile preview
Extracellular signal-regulated kinase 1 and 2 (ERK1/2)
- Target
- ERK1/2
- Molecular classification
- Enzyme, Serine/threonine kinase, Protein kinase, Mitogen-activated protein kinase family
01
Overview
Extracellular signal-regulated kinases (ERK1 and ERK2) are serine/threonine protein kinases in the mitogen-activated protein kinase (MAPK) family that play central roles in the regulation of cell growth, proliferation, differentiation, and survival. They are activated by phosphorylation through a signaling cascade (Ras-Raf-MEK-ERK pathway) following extracellular signals such as growth factors, cytokines, and other stimuli. Activated (phosphorylated) ERK translocates to the nucleus where it phosphorylates a range of transcription factors, regulating gene expression. Abnormal ERK signaling is implicated in many diseases, particularly cancer, making ERK proteins and their activation states important therapeutic targets.
- Other names
- ERK1 (also MAPK3)ERK2 (also MAPK1)MAP kinaseClassical MAP kinase
02
Mechanism of action
Inhibition of ERK kinase activity Inhibition of upstream kinases (RAF/MEK), preventing ERK phosphorylation/activation
03
Biological functions
Signal transductionCell proliferationCell differentiationCell cycle regulationApoptosisDevelopmentStress response
04
Disease associations
Cancer (oncogenesis, tumor progression)InflammationNeurodegenerative diseaseCardiovascular disease
05
Safety considerations
On-target toxicity in normal cells (affecting cell division, survival)Resistance mechanisms (reactivation of pathway upstream or parallel signaling pathways)Effects on normal tissue homeostasis, especially skin and heart
06
Interacting drugs
Trametinib (MEK inhibitor; indirectly affects ERK activation)
3 more in the full profile.
07
Biomarkers
Phosphorylated ERK (pERK) is used as a biomarker for pathway activation, potential efficacy marker in cancers with MAPK pathway activation
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