Target intelligence / Profile preview

Mitogen-activated protein kinase (MAPK) (MAPK)

Target
MAPK
Molecular classification
Enzyme, Protein kinase, Signal transduction molecule
01

Overview

The mitogen-activated protein kinase (MAPK) pathway is a signal transduction system composed of a cascade of serine/threonine-specific protein kinases, including ERK, JNK, and p38 kinases. These components regulate cellular responses to a wide variety of stimuli including growth factors, cytokines, and environmental stresses. MAPKs transmit signals from the cell surface to the nucleus, influencing cell proliferation, differentiation, survival, apoptosis, and immune response. Dysregulation of MAPK pathway components is implicated in many diseases, including cancer, inflammation, and neurodegenerative disorders. Therapeutic targeting of MAPK components (such as MEK and RAF) is the basis for several approved and investigational drugs in oncology and beyond[1][3][4][5][6][10].

Other names
ERK (extracellular signal-regulated kinase)JNK (c-Jun N-terminal kinase)p38 kinaseMAP kinase
02

Mechanism of action

Inhibition of phosphorylation and signal transduction to prevent cell proliferation Induction of apoptosis in tumor cells Blocking downstream mitogenic and survival signaling cascades

03

Biological functions

Signal transductionCell proliferationDifferentiationApoptosisImmune responseCell survivalStress response
04

Disease associations

CancerInflammationNeurodegenerative diseaseCardiovascular diseaseDevelopmental disorders
05

Safety considerations

Drug resistance due to pathway re-activation or compensatory signalingToxicity due to inhibition of physiology-essential MAPK signaling in normal tissuesOff-target effects and paradoxical activation
06

Interacting drugs

MEK inhibitors (e.g., trametinib)

3 more in the full profile.

07

Biomarkers

Phosphorylated ERK (p-ERK)Mutations in BRAF (e.g., V600E)KRAS or NRAS mutationsActivation status of pathway components

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