Target intelligence / Profile preview

Mitogen-activated ERK kinase cascade (MAPK/ERK Pathway)

Target
MAPK/ERK Pathway
Molecular classification
Signal Transduction Pathway, Kinase Cascade
01

Overview

The mitogen-activated ERK kinase cascade, also known as the RAF–MEK–ERK or MAPK/ERK pathway, is a highly conserved signal transduction pathway that relays extracellular signals from cell surface receptors to the nucleus. This cascade plays a central role in regulating key cellular processes such as proliferation, differentiation, survival, gene expression, and apoptosis. Aberrant activation of this pathway is implicated in cancer development (tumorigenesis), developmental disorders ("RASopathies"), schizophrenia spectrum disorders, bipolar disorder, migraines, among others. Due to its central role in cell fate decisions—and frequent dysregulation in cancers—the MAPK/ERK pathway has been extensively targeted pharmacologically.

Other names
RAF-MEK-ERK pathwayERK kinase cascade
02

Mechanism of action

Inhibition of RAF, MEK, or ERK kinases to block downstream signaling.

03

Biological functions

Cell proliferationCell differentiationCell survivalGene expressionApoptosisSignal transductionCell cycle progression
04

Disease associations

CancerTumorigenesisDevelopmental disordersRASopathiesSchizophrenia spectrum disordersBipolar disorderMigraines
05

Safety considerations

Resistance mechanismsAdaptive responsesOff-target effects of inhibitorsToxicity
06

Interacting drugs

RAF inhibitors

2 more in the full profile.

07

Biomarkers

Expression levels of pathway componentsPhosphorylation status of pathway componentsMutations in pathway genes (e.g., RAS, RAF)

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