Ephrin type-B receptor family (EphB)

The Ephrin type-B (EphB) receptor family consists of five transmembrane receptor tyrosine kinases (EphB1, EphB2, EphB3, EphB4, and EphB6) that mediate contact-dependent cell-to-cell communication [1][2]. These receptors are unique for their bidirectional signaling capability, where 'forward signaling' is triggered in the receptor-expressing cell and 'reverse signaling' occurs in the cell expressing the membrane-bound ephrin-B ligand [2][3]. EphB receptors play fundamental roles in embryonic development, including axon guidance, vascular assembly, and tissue boundary formation [3][4]. In adult physiology, they are involved in maintaining intestinal epithelium architecture and regulating synaptic plasticity in the nervous system [1][4]. Dysregulation of EphB signaling is a hallmark of various diseases, particularly cancer, where they can act as either tumor suppressors or promoters depending on the tissue type and disease stage [2][5]. For instance, EphB4 is frequently overexpressed in solid tumors and promotes tumor-associated angiogenesis, making it a significant therapeutic target [5][6]. Pharmacological intervention includes multi-kinase inhibitors like dasatinib and bosutinib, as well as specific monoclonal antibodies and soluble receptor decoys currently in clinical development [5][7].

Other names

EphB receptorsEphrin type-B receptorsEPHBEph receptor B family

Inhibition of the intracellular tyrosine kinase domain to block downstream signaling; disruption of receptor-ligand binding; induction of receptor internalization; competitive inhibition of ATP binding.