Target intelligence / Profile preview

Mitogen-activated protein kinase kinase 1 (MEK1), Mitogen-activated protein kinase kinase 2 (MEK2) (MEK1, MEK2)

Target
MEK1, MEK2
Molecular classification
Enzyme, Protein kinase, Serine/threonine kinase
01

Overview

Mitogen-activated protein kinase kinase 1 (MEK1) and Mitogen-activated protein kinase kinase 2 (MEK2) are dual-specificity protein kinases that play a central role in the RAS-RAF-MEK-ERK signaling cascade. This pathway transmits signals from cell surface receptors to the nucleus to regulate cell proliferation, differentiation, and survival. Abnormal activation of MEK1/2, often due to upstream mutations in RAS or BRAF, drives oncogenesis in various cancers. Selective inhibition of MEK1/2 with small-molecule drugs like selumetinib interrupts this signaling, providing a therapeutic strategy for cancers with dysregulated MAPK pathway activity.

Other names
MEK1MAP2K1MEK2MAP2K2
02

Mechanism of action

Inhibition of MEK1/2 blocks phosphorylation and activation of ERK1/2, suppressing MAPK signaling

03

Biological functions

Signal transductionCell proliferationCell differentiationCell survival
04

Disease associations

CancerNeurofibromatosisOther proliferative diseases
05

Safety considerations

Rashdiarrheafatigueocular toxicitycardiomyopathyinterstitial lung disease
06

Interacting drugs

Selumetinib

3 more in the full profile.

07

Biomarkers

BRAF mutationRAS mutationNF1 gene mutation

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