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Target intelligence / Profile preview
Mitogen-Activated Protein Kinase Kinase 1 (MEK1)
- Target
- MEK1
- Molecular classification
- Enzyme, Dual-specificity protein kinase
01
Overview
MEK1 is a dual-specificity kinase that phosphorylates and activates ERKs (extracellular signal-regulated kinases), specifically ERK1 and ERK2. It acts as a central node in the RAS–RAF–MEK–ERK signaling cascade, regulating cell proliferation, differentiation, transcription regulation, development, apoptosis control, and cell cycle progression. Altered or mutated MAP2K1/MEK1 is implicated in various cancers. It is activated by phosphorylation at Ser218 and Ser222 by RAF kinases, and is subject to feedback inhibition via T292 phosphorylation by active ERKs.
- Other names
- MAP2K1Dual specificity mitogen-activated protein kinase kinase 1MAPKKERK kinase
02
Mechanism of action
Small-molecule inhibitors that bind to and inhibit the kinase activity of MEK1/2, preventing the phosphorylation and activation of ERK1/2.
03
Biological functions
Signal transductionCell proliferationCell differentiationTranscription regulationDevelopmentApoptosis controlCell cycle progression
04
Disease associations
Cancer
05
Interacting drugs
U0126
4 more in the full profile.
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