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Mitogen-activated protein kinase 1 (MAPK1) and Mitogen-activated protein kinase 2 (MAPK2) (MAPK1 (ERK2), MAPK2 (ERK1))
- Target
- MAPK1 (ERK2), MAPK2 (ERK1)
- Molecular classification
- Protein kinase, Enzyme, Serine/threonine kinase, Mitogen-activated protein kinase family, Signal transduction protein
01
Overview
Mitogen-activated protein kinase 1 (MAPK1, also known as ERK2) and Mitogen-activated protein kinase 3 (MAPK3, also known as ERK1) are serine/threonine kinases that function as central components of the MAP kinase signaling cascade, relaying signals from cell surface receptors to nuclear targets in response to a variety of extracellular stimuli. They are activated by dual phosphorylation via upstream MAP2K (MEK1/2) kinases, and mediate diverse cellular processes including proliferation, differentiation, survival, and gene expression[1][5]. Dysregulation of MAPK1/2 signaling is implicated in various malignancies and developmental syndromes due to their critical roles in cell cycle control, apoptosis, and cellular differentiation[1][4][5].
- Other names
- MAPK1ERK2p42MAPKPRKM1MAPK3ERK1p44MAPKPRKM3
02
Mechanism of action
Inhibition of MAPK/ERK pathway to suppress cell proliferation and induce apoptosis (primarily via MEK inhibition upstream)
03
Biological functions
Signal transductionCell proliferationDiferentiationTranscription regulationDevelopmentApoptosisSurvival
04
Disease associations
CancerCardiovascular diseaseDevelopmental disordersInflammation
05
Safety considerations
On-target toxicity in normal proliferative tissues (skin, gut, hematopoietic system)Compensatory activation of parallel pathways, leading to resistanceCardiotoxicitySkin rashGastrointestinal effects
06
Interacting drugs
Trametinib
3 more in the full profile.
07
Biomarkers
Phospho-ERK (active phosphorylated ERK1/2)Mutations in MAPK pathway genes (e.g., BRAF, KRAS, NRAS)Total ERK1/2 protein expression in tumor tissue
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