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EPH receptor A2

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Identifiers
SymbolsEPHA2 ; ARCC2; CTPA; CTPP1; CTRCT6; ECK
External IDsOMIM176946 MGI95278 HomoloGene20929 IUPHAR: 1822 ChEMBL: 2068 GeneCards: EPHA2 Gene
EC number2.7.10.1
RNA expression pattern
File:PBB GE EPHA2 203499 at tn.png
More reference expression data
Orthologs
SpeciesHumanMouse
Entrez196913836
EnsemblENSG00000142627ENSMUSG00000006445
UniProtP29317Q03145
RefSeq (mRNA)NM_004431NM_010139
RefSeq (protein)NP_004422NP_034269
Location (UCSC)Chr 1:
16.45 – 16.48 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]

Function

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

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]

Interactions

EPH receptor A2 has been shown to interact with:

References

  1. ^ Sulman EP, Tang XX, Allen C, Biegel JA, Pleasure DE, Brodeur GM et al. (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. PMID 9119409. doi:10.1006/geno.1996.4569. 
  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 et al. (2012). "The ephrin receptor tyrosine kinase A2 is a cellular receptor for Kaposi's sarcoma–associated herpesvirus". Nat. Med. 18 (6): 961–6. PMC 3645317. PMID 22635007. doi:10.1038/nm.2805. 
  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. PMID 12167657. doi:10.1074/jbc.M207127200. 
  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. PMID 12400011. doi:10.1038/sj.onc.1205758. 
  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

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