Target intelligence / Profile preview

Mitogen-activated protein kinase 1 mRNA (MAPK1 mRNA)

Target
MAPK1 mRNA
Molecular classification
Nucleic acid, Messenger RNA
01

Overview

Mitogen-activated protein kinase 1 (MAPK1) mRNA, also known as ERK2 mRNA, is the transcript that encodes the ERK2 protein, a critical component of the Ras-Raf-MEK-ERK signaling cascade. This pathway is a central regulator of fundamental cellular processes including growth, proliferation, survival, and differentiation in response to extracellular stimuli (UniProt: P28482). In many human cancers, the MAPK pathway is constitutively active due to mutations in upstream regulators like RAS or BRAF, making the components of this pathway, including the mRNA of its terminal kinases, attractive therapeutic targets (PubMed: 30401435). While most clinical interventions currently focus on small molecule inhibitors of the ERK protein, targeting the mRNA via RNA interference (siRNA) or antisense oligonucleotides (ASOs) offers a method to deplete the protein reservoir entirely, potentially overcoming certain resistance mechanisms associated with kinase inhibitors (PubMed: 28813486). Therapeutic strategies targeting MAPK1 mRNA aim to downregulate the expression of the ERK2 protein to arrest tumor growth and induce apoptosis in MAPK-dependent malignancies.

Other names
ERK2 mRNAExtracellular signal-regulated kinase 2 mRNAPRKM1 mRNAP42MAPK mRNAMitogen-activated protein kinase 2 mRNA
02

Mechanism of action

RNA interference (siRNA) or RNase H-mediated degradation (ASO) to prevent the translation of the MAPK1 protein, thereby inhibiting the MAPK/ERK signaling pathway.

03

Biological functions

Protein codingSignal transductionCell proliferationCell differentiationCell cycle regulationTranscription regulation
04

Disease associations

CancerMelanomaColorectal cancerNon-small cell lung cancerInflammatory diseasesNoonan syndrome
05

Safety considerations

Off-target effects of RNA therapeuticsSystemic toxicity of delivery vehicles (e.g., lipid nanoparticles)Potential for compensatory activation of MAPK3 (ERK1)Inhibition of essential physiological signaling in healthy tissues
06

Interacting drugs

ERK2-siRNA (Experimental)

1 more in the full profile.

07

Biomarkers

MAPK1 mRNA expression levelsERK2 protein levelsPhospho-ERK1/2 levelsDUSP6 expression

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