Target intelligence / Profile preview

Ephrin type-A receptor 2 (EphA2)

Target
EphA2
Molecular classification
Receptor Tyrosine Kinase
01

Overview

Ephrin type-A receptor 2 (EphA2) is a receptor tyrosine kinase involved in cell signaling, development, and disease. It regulates cell adhesion, migration, tissue boundary formation, and axon guidance. In cancer, EphA2 is often overexpressed and promotes tumorigenesis through ligand-dependent and ligand-independent mechanisms. It is a potential therapeutic target and a biomarker for cancer progression and drug resistance. It also serves as an entry receptor for certain viruses. Loss-of-function mutations can lead to congenital defects or age-related diseases.

02

Mechanism of action

EphA2 is a receptor tyrosine kinase that binds to ephrin-A ligands, leading to autophosphorylation and activation of downstream signaling pathways such as MAPK/ERK and Rho GTPases. In cancer, EphA2 can signal independently of ligand binding by interacting with other RTKs. Small molecule inhibitors can block viral entry by targeting EphA2. Doxazosin acts as an agonist. AHCC® downregulates EPHA2 mRNA/protein levels via modulation of natural antisense transcripts.

03

Biological functions

Cell adhesionCell migrationTissue patterningNeural developmentCell-cell communicationSignal transduction
04

Disease associations

Cancer progressionMetastasisDrug resistanceViral entryCongenital defectsAge-related diseases
05

Safety considerations

Potential for off-target effects due to promiscuous ligand bindingComplex and context-dependent signaling, leading to unpredictable effectsDevelopment of resistance mechanisms in cancer therapyLoss-of-function mutations may affect tissue integrity
06

Interacting drugs

BRAF/MEK inhibitors

3 more in the full profile.

07

Biomarkers

EphA2 overexpression in tumor tissuesEPHA2 mRNA levelsEPHA2 protein levels

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