Ephrin type-B receptor 4 (EPHB4) (EPHB4)

Ephrin type-B receptor 4 (EPHB4) is a receptor tyrosine kinase that, together with its ligand Ephrin-B2, mediates critical cell-to-cell communication during vascular development and tissue morphogenesis. This interaction initiates bidirectional signaling, where forward signaling occurs in the EPHB4-expressing cell and reverse signaling occurs in the Ephrin-B2-expressing cell, regulating processes like cell migration and repulsion. In various cancers, EPHB4 is frequently overexpressed and functions as a survival factor that promotes tumor growth, angiogenesis, and metastasis. The extracellular domain (ECD) of EPHB4 is the primary site for ligand binding and has become a focal point for therapeutic intervention. Soluble versions of the ECD, such as sEphB4-HSA, act as decoy receptors to sequester Ephrin-B2, thereby inhibiting both forward and reverse signaling pathways. Clinical investigations have explored these EPHB4-targeted therapies in malignancies like urothelial and prostate cancer, though challenges such as treatment-induced hypertension have been noted.

Other names

HTKMYK1TYRO11CMAVM2HFASDLMPHM7Hepatoma transmembrane kinaseEph receptor B4

Decoy receptor activity by sequestering the ligand Ephrin-B2, inhibition of receptor tyrosine kinase autophosphorylation, and blockade of bidirectional forward and reverse signaling pathways.