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Target intelligence / Profile preview
Dual Specificity Mitogen-Activated Protein Kinase Kinase 1 (MEK1)
- Target
- MEK1
- Molecular classification
- Enzyme, Protein Kinase, Dual-specificity protein kinase, MAP kinase kinase
01
Overview
MEK1 is a dual-specificity protein kinase that functions as a central component of the RAS–RAF–MEK–ERK signal transduction cascade. It phosphorylates and activates ERK1/2, regulating key cellular processes such as cell proliferation, differentiation, apoptosis, and cell cycle progression. MEK1 is activated by RAF kinases and inhibited by ERK-mediated feedback phosphorylation. Aberrant activation of MEK1, often due to upstream mutations in RAS or BRAF, is implicated in various cancers, making it an important therapeutic target.
- Other names
- MAP2K1PRKMK1MKK1MAPKK 1MAPK/ERK kinase 1
02
Mechanism of action
Inhibition of MEK1/2 kinase activity, thereby blocking downstream ERK1/2 signaling.
03
Biological functions
Signal transductionCell proliferationDifferentiationApoptosisCell cycle progressionMigrationMetabolismTranscription regulationDevelopmentRegulation of ERK1/2 activity
04
Disease associations
CancerMelanoma
05
Safety considerations
Resistance to MEK inhibitorsToxicities associated with MEK inhibition
06
Interacting drugs
MEKi (MEK inhibitors)
07
Biomarkers
BRAF mutationsRAS mutations
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