Ephrin type-B receptor (EphB)

Ephrin type-B receptors (EphB) are a distinct group of receptor tyrosine kinases (RTKs) that mediate contact-dependent communication between cells through interactions with membrane-bound ephrin-B ligands (UniProt: P54760, P29323). A defining feature of this system is bidirectional signaling, where forward signaling occurs in the receptor-bearing cell and reverse signaling occurs in the ligand-bearing cell, regulating processes such as axon guidance, angiogenesis, and tissue boundary formation (PubMed: 25103797). In adult tissues, EphB receptors play critical roles in intestinal stem cell niche maintenance and synaptic plasticity (PubMed: 30105224). Dysregulation of EphB signaling is a hallmark of several diseases; for instance, EphB4 is often upregulated in cancers like breast and prostate to promote tumor vascularization, while EphB2 loss is associated with progression in colorectal cancer (PubMed: 16774708). Therapeutic targeting of the EphB family involves small-molecule inhibitors like dasatinib and various monoclonal antibodies designed to inhibit kinase activity or disrupt ligand binding to arrest tumor growth and pathological angiogenesis (ClinicalTrials.gov: NCT01646203). Because of their widespread role in vascular and neural development, therapeutic intervention requires careful management of potential side effects related to cardiovascular stability and tissue repair.

Other names

EphB receptorsEphrin-B family receptorsEPHB1EPHB2EPHB3EPHB4EPHB6Tyrosine-protein kinase receptor EPHB

Inhibition of receptor tyrosine kinase activity and blockade of ligand-receptor interaction to modulate bidirectional signaling.