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Target intelligence / Profile preview
Extracellular signal-regulated kinases (ERK)
- Target
- ERK
- Molecular classification
- Serine/threonine protein kinase, Enzyme
01
Overview
Extracellular signal-regulated kinases (ERKs) are a family of serine/threonine protein kinases that play a central role in the regulation of diverse cellular processes, including proliferation, differentiation, survival, migration, and gene expression. ERKs are key components of the mitogen-activated protein kinase (MAPK) signaling pathway and are widely expressed in mammalian cells. Disruption or hyperactivation of the Ras-Raf-MEK-ERK pathway is common in many cancers. Targeted inhibition has become an important anti-cancer strategy; however, only certain inhibitors like those against mutant B-Raf have shown significant clinical efficacy so far. Other diseases associated with aberrant regulation include chronic inflammation disorders such as arthritis or osteoporosis.
- Other names
- p44 MAPKp42 MAPKMAPK1MAPK3MAPK4MAPK6MAPK7
02
Mechanism of action
Inhibition of ERK phosphorylation and activation
03
Biological functions
Signal transductionCell cycle controlCell proliferationCell differentiationCell survivalApoptosisCell migrationGene expressionMetabolism
04
Disease associations
CancerInflammationArthritisOsteoporosis
05
Safety considerations
Resistance to inhibitorsOff-target effects of inhibitors
06
Interacting drugs
B-Raf inhibitors (e.g., for mutant B-Raf)
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