Target intelligence / Profile preview

Mitogen-activated protein kinase (MAP kinase) (MAPK)

Target
MAPK
Molecular classification
Enzyme, Serine/threonine-specific protein kinase, Kinase (protein kinase superfamily), Signal transduction molecule
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Overview

Mitogen-activated protein kinases (MAPKs) are a family of serine/threonine-specific protein kinases that play crucial roles in transmitting extracellular signals into intracellular responses, regulating key cellular processes such as proliferation, differentiation, apoptosis, and response to stress. The canonical mammalian MAPK family consists of three main groups: extracellular signal-regulated kinases (ERKs), c-Jun N-terminal kinases (JNKs), and p38 MAP kinases. Each MAPK cascade generally involves a three-tiered structure: a MAPK kinase kinase (MAPKKK), a MAPK kinase (MAPKK, also known as MEK), and a MAPK, with each kinase activating the next by phosphorylation. Dysregulation of MAPK activity is implicated in many diseases, notably cancer, and many therapies are designed to target upstream components of this pathway. However, "Mitogen-activated protein kinase pathway proteins" is not a single protein but a term encompassing multiple proteins within a signaling cascade.

Other names
MAP kinaseMAPKMitogen-activated protein kinase family
02

Mechanism of action

Inhibition of signal transduction cascade by blocking kinase activity (often MEK, upstream activator of MAPK/ERK)\nPrevents activation (phosphorylation) of MAPKs, reducing downstream signaling for cell proliferation/survival

03

Biological functions

Signal transductionCell proliferationCell differentiationApoptosis (cell death)Gene expression regulationCell survivalCellular stress response
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Disease associations

CancerInflammationNeurodegenerative diseasesCardiovascular diseaseInfectionOther (as MAPK pathways regulate numerous cellular processes implicated in many diseases)
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Safety considerations

Acquired resistance (due to pathway reactivation)Skin toxicityCardiotoxicitySecondary malignancies (with pathway inhibition)
06

Interacting drugs

Trametinib (MEK inhibitor; indirectly blocks MAPK signaling)

4 more in the full profile.

07

Biomarkers

Phosphorylated ERK (p-ERK) as a biomarker of MAPK pathway activityPhosphorylated MEKBRAF V600E mutation (indirect indicator of MAPK pathway activation)

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