Target intelligence / Profile preview

Ephrin type-B receptor 3 (EPHB3)

Target
EPHB3
Molecular classification
Receptor tyrosine kinase (RTK), Receptor, Transmembrane protein
01

Overview

Ephrin type-B receptor 3 (EPHB3) is a transmembrane receptor tyrosine kinase, part of the Eph family, which is the largest subfamily within the RTK superfamily[1][3]. EPHB3 binds ephrin-B family ligands, mediating cell-cell contact-dependent bidirectional signaling pathways. These pathways regulate crucial processes such as axon guidance, cell migration, cell adhesion, vascular morphogenesis, and differentiation, especially during early development, neural formation, and vascular remodeling[3][5]. EPHB3 participates in signaling by interacting with ligands and intracellular proteins (e.g., RasGAP) to modulate cytoskeleton dynamics and cellular architecture[5]. Dysregulation of EPHB3 expression is linked to cancer progression and developmental disorders[3][4][5]. Its functional redundancy with other EphB receptors complicates therapeutic targeting[3][5]. No approved drugs directly target EPHB3; ongoing research explores its potential as a cancer and vascular disease target[3][4][5]. Safety challenges center on selectivity within the Eph/ephrin network and developmental toxicity. EPHB3 can be considered a candidate biomarker for cancers such as NSCLC due to its role in cell growth, migration, and survival[4].

Other names
EPHB3ETK2HEK2TYRO6EPH-like kinase 2EK2hEK2Hek2Tyro6EPH-like tyrosine kinase 2Embryonic kinase 2Tyrosine-protein kinase TYRO6ephrin type-B receptor 3human embryo kinase 2
02

Mechanism of action

For potential inhibitors: kinase inhibition disrupting signal transduction - For agonists (in theory): receptor activation promoting cell migration, axon guidance, or vascular morphogenesis - Bidirectional signaling (forward via EPHB3, reverse via ephrin-B ligand), modifying cell behavior locally[1][3][5]

03

Biological functions

Signal transductionAxon guidanceCell migration and adhesionVascular development and angiogenesisEmbryonic patterningCell positioning and differentiation (especially intestinal epithelium)
04

Disease associations

Cancer (notably non-small cell lung cancer and various developmental cancers)Neurological developmental disordersVascular diseases and congenital vascular defectsCraniofrontonasal syndrome
05

Safety considerations

Potential safety concerns include off-target effects (due to redundancy and promiscuity in Eph/ephrin signaling)Possible impacts on vascular and neural development if targeted therapeuticallyFunctional redundancy with other EphB receptors may reduce selectivity and amplify toxicity
06

Biomarkers

EPHB3 expression may be used as a biomarker for cancer progression (e.g., NSCLC)Developmental vascular disorders (rare research context)

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