Target intelligence / Profile preview

Ephrin type-A receptor 2 mRNA (EphA2 mRNA)

Target
EphA2 mRNA
Molecular classification
Nucleic acid, Messenger RNA
01

Overview

Ephrin type-A receptor 2 (EphA2) mRNA is the messenger RNA transcript that encodes the EphA2 protein, a receptor tyrosine kinase involved in various cellular processes (UniProt P29317). While EphA2 protein expression is typically low in adult epithelial tissues, the mRNA is frequently overexpressed in a wide range of cancers, including breast, lung, and ovarian cancers, as well as glioblastoma (Landen et al., 2005). This overexpression correlates with increased tumor aggressiveness, poor prognosis, and metastatic potential. Targeting the EphA2 mRNA using RNA interference (RNAi) or antisense oligonucleotides (ASOs) provides a mechanism to silence the gene before the protein is synthesized. One notable therapeutic candidate, EPHARNA (siRNA-EphA2-DOPC), utilizes a neutral liposomal delivery system to transport siRNA into tumor cells, where it triggers the degradation of EphA2 mRNA (Wagner et al., 2017). This degradation leads to a significant reduction in EphA2 protein levels, thereby inhibiting oncogenic signaling pathways such as the PI3K/Akt and MAPK pathways. Therapeutic targeting of the mRNA transcript is particularly advantageous for proteins like EphA2 that are difficult to inhibit effectively with small molecules or antibodies alone. Clinical trials have demonstrated the feasibility of this approach, although challenges remain regarding systemic delivery and potential off-target effects (Duxbury et al., 2004).

Other names
EPH receptor A2 mRNAEpithelial cell kinase mRNAECK mRNAARCC2 mRNACTPA mRNACTPP1 mRNACTRCT6 mRNA
02

Mechanism of action

RNA interference (RNAi) mediated by siRNA or antisense-mediated degradation by RNase H, leading to the reduction of EphA2 protein synthesis (Wagner et al., 2017).

03

Biological functions

Protein synthesisRegulation of cell signalingCell migrationAngiogenesisCell-cell adhesion
04

Disease associations

CancerSolid tumorsBreast cancerLung cancerGlioblastomaProstate cancerOvarian cancer
05

Safety considerations

Off-target gene silencingActivation of the innate immune system (e.g., via TLR7/8)Delivery efficiency to non-hepatic tissuesPotential liver toxicity from lipid-based delivery vehicles
06

Interacting drugs

EPHARNA (siRNA-EphA2-DOPC)

2 more in the full profile.

07

Biomarkers

EphA2 mRNA expression levelsEphA2 protein expressionTumor volume reduction

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