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Target intelligence / Profile preview
Mitogen-activated protein kinase ERK2 (ERK2)
- Target
- ERK2
- Molecular classification
- Enzyme, Serine/threonine kinase
01
Overview
Mitogen-activated protein kinase ERK2, also known as MAPK1, is a serine/threonine kinase that plays a central role in the Ras-Raf-MEK-ERK signal transduction cascade. This pathway regulates diverse cellular processes such as cell proliferation, differentiation, survival, migration, metabolism, and gene expression. ERK2 is activated by dual phosphorylation on Thr185 and Tyr187 by MEK1/2 kinases. Once activated, ERK2 phosphorylates numerous cytoplasmic and nuclear substrates, including transcription factors. The Ras-Raf-MEK-ERK pathway, including ERK2, is frequently hyperactivated in human cancers, making it an important target for anti-tumor therapies.
- Other names
- MAPK1
02
Mechanism of action
Kinase inhibitors targeting MEK or ERK.
03
Biological functions
Signal transductionCell proliferationCell differentiationCell survivalCell migrationMetabolismGene expression
04
Disease associations
CancerMetabolic syndrome
05
Safety considerations
Direct targeting of downstream kinases like MEKs or potentially even ERKs remains under investigation due to their central roles in normal physiology as well as disease states.
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