Erythropoietin-producing hepatocellular receptor tyrosine kinase (Eph receptor) (Eph)

Eph receptor tyrosine kinases (Eph receptors) represent the largest subfamily of receptor tyrosine kinases, consisting of 14 members categorized into EphA and EphB groups based on their binding affinity for ephrin-A or ephrin-B ligands (Pasquale, 2008; UniProt). These receptors are distinguished by their ability to mediate bidirectional signaling, where both the receptor-bearing cell and the ligand-bearing cell initiate intracellular cascades upon contact (Kullander & Klein, 2002). They play fundamental roles in embryonic development, specifically in regulating axon guidance, vascular formation, and the establishment of tissue boundaries (Arvanitis & Davy, 2008). In human pathology, Eph receptors are frequently dysregulated in various cancers, where they influence tumor growth, metastasis, and neoangiogenesis, often acting in a context-dependent manner as either promoters or suppressors of malignancy (Janes et al., 2014). Pharmacological targeting of Eph receptors involves the use of small-molecule inhibitors like dasatinib, which exhibits off-target Eph activity, as well as highly specific monoclonal antibodies and peptides designed to disrupt ligand binding or induce receptor degradation (Lodola et al., 2017; PubMed). Current clinical efforts focus on leveraging these receptors as therapeutic targets in oncology and as biomarkers for disease progression (StatPearls).

Other names

Ephrin receptorEPHEph family receptor tyrosine kinase

Inhibition of tyrosine kinase activity, blockade of ephrin ligand binding, induction of receptor internalization and degradation, and antibody-dependent cellular cytotoxicity (ADCC).