Target intelligence / Profile preview

Erythropoietin-producing hepatocellular receptor family (Eph receptors) (Eph receptors)

Target
Eph receptors
Molecular classification
Receptor tyrosine kinase, Enzyme, Receptor
01

Overview

The Erythropoietin-producing hepatocellular (Eph) receptor family constitutes the largest subfamily of receptor tyrosine kinases (RTKs) in the human genome (UniProt, 2023). These receptors are divided into two classes, EphA and EphB, based on their sequence homology and binding affinity for their membrane-bound ligands, known as ephrins (NCBI, 2022). Eph receptors play a critical role in mediating cell-to-cell communication, influencing processes such as axon guidance, angiogenesis, and tissue patterning during development (PubMed, PMID: 25145844). In adult tissues, dysregulation of Eph signaling is frequently associated with various pathologies, most notably cancer, where they contribute to tumor growth, metastasis, and neoangiogenesis (Nature Reviews Cancer, 2014). Because of their cell-surface expression and involvement in disease progression, Eph receptors are significant targets for therapeutic intervention, including small-molecule kinase inhibitors like dasatinib, monoclonal antibodies like KB004, and antibody-drug conjugates (PubChem, 2024). Their unique bidirectional signaling mechanism, where both the receptor and the ligand can initiate intracellular signals, adds a layer of complexity to their role in physiology and disease (PubMed, PMID: 24457415).

Other names
Ephrin receptorsEPH receptorsEph family receptor tyrosine kinases
02

Mechanism of action

Inhibition of receptor tyrosine kinase activity, disruption of ephrin ligand-mediated bidirectional signaling, and antibody-mediated targeting of receptor-expressing cells (PubMed, PMID: 25145844).

03

Biological functions

Signal transductionCell migrationAxon guidanceAngiogenesisTissue boundary formationSynaptic plasticity
04

Disease associations

CancerNeurodegenerative diseaseCardiovascular diseaseFibrosis
05

Safety considerations

Cardiovascular toxicityImpaired wound healingPotential neurotoxicityOff-target kinase inhibitionBleeding risk
06

Interacting drugs

Dasatinib

6 more in the full profile.

07

Biomarkers

EphA2 expressionEphB4 expressionEphA3 expression

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