Target intelligence / Profile preview

Epsin-1 mRNA (EPN1 mRNA)

Target
EPN1 mRNA
Molecular classification
Messenger RNA, Endocytic adaptor protein (encoded protein), Clathrin-binding protein (encoded protein)
01

Overview

Epsin-1 (EPN1) mRNA encodes a critical endocytic adaptor protein that facilitates clathrin-mediated endocytosis and membrane curvature through its N-terminal homology (ENTH) domain (UniProt P57676). This protein is essential for the Notch signaling pathway, as it regulates the internalization of Notch ligands like Delta-like 4 (Dll4), which is a prerequisite for receptor activation and subsequent downstream signaling (PubMed: 22492590). In oncology, Epsin-1 is often overexpressed, and its role in promoting pathological angiogenesis makes its mRNA a high-priority therapeutic target for RNA-based interventions (PubMed: 33408344). By targeting the EPSIN1 mRNA with RNA interference (RNAi) or antisense oligonucleotides (ASOs), researchers aim to downregulate protein levels, thereby inhibiting the aberrant blood vessel formation that supports tumor growth. Preclinical studies have demonstrated that silencing EPN1 mRNA in vascular endothelial cells leads to defective Notch signaling and unproductive angiogenesis, significantly reducing tumor progression (PubMed: 25203565). However, therapeutic challenges include ensuring the specific delivery of RNA-based drugs to target tissues and avoiding potential off-target effects that could disrupt normal endocytic processes in healthy cells.

Other names
EPN1 mRNAEH domain-binding mitotic phosphoprotein mRNAEpsin 1 transcriptEPSIN1
02

Mechanism of action

RNA interference (RNAi) or antisense-mediated degradation of mRNA to prevent the translation of Epsin-1 protein, thereby inhibiting Notch-mediated pathological angiogenesis.

03

Biological functions

Clathrin-mediated endocytosisNotch signaling pathway regulationMembrane remodelingAngiogenesisVesicular transport
04

Disease associations

CancerTumor angiogenesisInflammationAtherosclerosis
05

Safety considerations

Off-target effects of RNA-based therapeuticsPotential disruption of normal endocytosis in healthy tissuesSystemic delivery challengesPotential for immune response to synthetic oligonucleotides
06

Interacting drugs

Experimental siRNA targeting EPN1

1 more in the full profile.

07

Biomarkers

EPN1 mRNA expression levelsEndothelial Epsin-1 protein levelsDll4-Notch signaling activity

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