EPH receptor A2

This gene belongs to the ephrin receptor subfamily of the protein-tyrosine kinase family. EPH and EPH-related receptors have been implicated in mediating developmental events, particularly in the nervous system. Receptors in the EPH subfamily typically have a single kinase domain and an extracellular region containing a Cys-rich domain and 2 fibronectin type III repeats. The ephrin receptors are divided into two groups based on the similarity of their extracellular domain sequences and their affinities for binding ephrin-A and ephrin-B ligands. This gene encodes a protein that binds ephrin-A ligands.^[6]

It may be implicated in BRAF mutated melanomas becoming resistant to BRAF-inhibitors and MEK inhibitors.^[7] It is also the receptor by which Kaposi's sarcoma-associated herpesvirus (KSHV) enters host cells; small molecule inhibitors of EphA2 have shown some ability to block KSHV entry into human cells.^[8]

EPH receptor A2 has been shown to interact with:

• Ephrin A1^[9]
• ACP1^[10]
• Grb2,^[11]
• PIK3R1,^[12] and
• SHC1.^[11]

It was also shown that doxazosin is a small molecule agonist of EPH receptor A2.^[13]

• Vasculogenic mimicry