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Ephrin-A1, also known as EFNA1, is encoded in humans by the EFNA1 gene, which encodes a member of the Eph family. Ephrins and Eph-related receptors constitute the largest subfamily of receptor tyrosine kinases involved in regulating the development of the nervous and hematopoietic systems. According to their structure and sequence relationship, ephrins can be divided into ephrin-A (EFNA) class and ephrin-B (EFNB) class. The Ephrin-A ligand binds the EphA receptor and is anchored to the plasma membrane via a glycosylphosphatidylinositol (GPI) linkage. The ephrin-B ligand, on the other hand, binds to the EphB receptor and is anchored to the plasma membrane through the transmembrane domain. Ephrin-A1 and one of its receptors, EphA2, are expressed in xenografted endothelial cells and tumor cells, and play a role in human cancer to some extent by affecting tumor neovascularization.