EPH receptor A2

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EPH receptor A2
Protein EPHA2 PDB 1mqb.png
PDB rendering based on 1mqb.
Available structures
PDB Ortholog search: PDBe, RCSB
External IDs OMIM176946 MGI95278 HomoloGene20929 ChEMBL: 2068 GeneCards: EPHA2 Gene
EC number
RNA expression pattern
PBB GE EPHA2 203499 at tn.png
More reference expression data
Species Human Mouse
Entrez 1969 13836
Ensembl ENSG00000142627 ENSMUSG00000006445
UniProt P29317 Q03145
RefSeq (mRNA) NM_004431 NM_010139
RefSeq (protein) NP_004422 NP_034269
Location (UCSC) Chr 1:
16.12 – 16.16 Mb
Chr 4:
141.3 – 141.33 Mb
PubMed search [1] [2]

EPH receptor A2 (ephrin type-A receptor 2) is a protein that in humans is encoded by the EPHA2 gene.[1][2]


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 2 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.[2]

Clinical significance[edit]

It may be implicated in BRAF mutated melanomas becoming resistant to BRAF-inhibitors and MEK inhibitors.[3] It also the receptor by which Kaposi sarcoma-associated herpesvirus (KSHV) enters host cells and small molecule inhibitors of EphA2 have shown some ability to block KSHV entry into human cells.[4]


EPH receptor A2 has been shown to interact with:


  1. ^ Sulman EP, Tang XX, Allen C, Biegel JA, Pleasure DE, Brodeur GM, Ikegaki N (April 1997). "ECK, a human EPH-related gene, maps to 1p36.1, a common region of alteration in human cancers". Genomics 40 (2): 371–4. doi:10.1006/geno.1996.4569. PMID 9119409. 
  2. ^ a b "Entrez Gene: EPHA2 EPH receptor A2". 
  3. ^ "Counteracting Drug Resistance in Melanoma". 2015. 
  4. ^ Hahn AS, Kaufmann JK, Wies E, Naschberger E, Panteleev-Ivlev J, Schmidt K, Holzer A, Schmidt M, Chen J, König S, Ensser A, Myoung J, Brockmeyer NH, Stürzl M, Fleckenstein B, Neipel F (2012). "The ephrin receptor tyrosine kinase A2 is a cellular receptor for Kaposi's sarcoma–associated herpesvirus". Nat. Med. 18 (6): 961–6. doi:10.1038/nm.2805. PMC 3645317. PMID 22635007. 
  5. ^ Kikawa KD, Vidale DR, Van Etten RL, Kinch MS (October 2002). "Regulation of the EphA2 kinase by the low molecular weight tyrosine phosphatase induces transformation". J. Biol. Chem. 277 (42): 39274–9. doi:10.1074/jbc.M207127200. PMID 12167657. 
  6. ^ a b Pratt RL, Kinch MS (October 2002). "Activation of the EphA2 tyrosine kinase stimulates the MAP/ERK kinase signaling cascade". Oncogene 21 (50): 7690–9. doi:10.1038/sj.onc.1205758. PMID 12400011. 
  7. ^ Pandey A, Lazar DF, Saltiel AR, Dixit VM (December 1994). "Activation of the Eck receptor protein tyrosine kinase stimulates phosphatidylinositol 3-kinase activity". J. Biol. Chem. 269 (48): 30154–7. PMID 7982920. 

Further reading[edit]