Target intelligence / Profile preview

Ephrin type-A receptor 8 (EPHA8)

Target
EPHA8
Molecular classification
Receptor, Receptor tyrosine kinase, Protein kinase, Transmembrane protein
01

Overview

Ephrin type-A receptor 8 (EPHA8) is a member of the Eph family of receptor tyrosine kinases, and is encoded by the EPHA8 gene in humans[1][3]. It functions as a cell-surface receptor for glycosylphosphatidylinositol-anchored ephrin-A ligands (including ephrin-A2, -A3, -A5), transducing contact-dependent bi-directional signaling that plays a fundamental role in axonal guidance and other developmental processes in the nervous system[1][3][5]. EPHA8 regulates cell adhesion, migration, and neurite outgrowth via intracellular signaling cascades such as the PI3K/AKT and MAPK pathways[1][3][5]. In cancer biology, particularly breast cancer, elevated EPHA8 expression is associated with increased tumor growth, migration, invasion, and poor prognosis. Knockdown of EPHA8 in cancer cells inhibits proliferation and promotes apoptosis, and also sensitizes cells to chemotherapy such as paclitaxel by modulating signaling through PI3K/AKT and p53 pathways[5]. EPHA8 is being studied as a potential therapeutic target and biomarker in oncology due to its roles in tumorigenesis and chemotherapy response[5].

Other names
Ephrin type-A receptor 8EPHA8EEKHEK3KIAA1459EK3hEK3Hek3EPH- and ELK-related kinaseEPH-like kinase 3Tyrosine-protein kinase receptor EEKhydroxyaryl-protein kinaseprotein-tyrosine kinasetyrosylprotein kinase
02

Mechanism of action

Inhibition or knockdown of EPHA8 increases apoptosis and sensitivity to chemotherapy (paclitaxel) by downregulating PI3K/AKT signaling and upregulating p53 and pro-apoptotic proteins

03

Biological functions

Signal transductionAxonal guidanceCell migrationCell adhesionCell proliferationApoptosis
04

Disease associations

CancerNeurodevelopmental processesBreast cancer (specifically cited)
05

Safety considerations

Broad role in nervous system development may raise concern about potential effects on neurodevelopment or normal tissue repair if targetedFunctional redundancy and compensation among Eph receptor family members complicate therapeutic targeting
06

Interacting drugs

Paclitaxel
07

Biomarkers

EPHA8 expression level as a prognostic and predictive biomarker for breast cancer progression and response to chemotherapy

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