Ephrin-A1

Ephrin-A1, the founding member of the ephrin family encoded by EFNA1, is a glycosylphosphatidylinositol (GPI)-anchored membrane ligand that activates EphA-class receptor tyrosine kinases such as EphA1, EphA2 and EphA4. Lacking a transmembrane domain and cytoplasmic tail, it signals mainly through its receptors, although GPI-dependent reverse signaling into the ligand-bearing cell has also been described. Ephrin-A1 is prominently expressed in activated and tumor-associated endothelium, where it contributes to angiogenesis and vascular remodeling, and it guides axon pathfinding during neural development. Because of its selective up-regulation in tumor vasculature, ephrin-A1 and its receptors are being explored as targets for vascular-disrupting and anticancer strategies.