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EPH receptor A2

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EPHA2
Available structures
PDBOrtholog search: PDBe RCSB
Identifiers
AliasesEPHA2, Epha2, AW545284, Eck, Myk2, Sek-2, Sek2, ARCC2, CTPA, CTPP1, CTRCT6, EPH receptor A2, ECK
External IDsOMIM: 176946; MGI: 95278; HomoloGene: 20929; GeneCards: EPHA2; OMA:EPHA2 - orthologs
Orthologs
SpeciesHumanMouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

NM_004431
NM_001329090

NM_010139

RefSeq (protein)

NP_001316019
NP_004422

NP_034269

Location (UCSC)Chr 1: 16.12 – 16.16 MbChr 4: 141.03 – 141.06 Mb
PubMed search[3][4]
Wikidata
View/Edit HumanView/Edit Mouse

EPH receptor A2 (ephrin type-A receptor 2) is a protein that in humans is encoded by the EPHA2 gene.[5][6]

Function

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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]

Clinical significance

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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]

Interactions

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EPH receptor A2 has been shown to interact with:

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

See also

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References

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  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000142627Ensembl, May 2017
  2. ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000006445Ensembl, May 2017
  3. ^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  4. ^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
  5. ^ 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.
  6. ^ a b "Entrez Gene: EPHA2 EPH receptor A2".
  7. ^ "Counteracting Drug Resistance in Melanoma". 2015. Archived from the original on 2015-02-04. Retrieved 2015-02-04.
  8. ^ 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.
  9. ^ Himanen JP, Goldgur Y, Miao H, Myshkin E, Guo H, Buck M, Nguyen M, Rajashankar KR, Wang BC, Nikolov DB (July 2009). "Ligand recognition by A-class Eph receptors: crystal structures of the EphA2 ligand-binding domain and the EphA2/ephrin-A1 complex". EMBO Rep. 10 (7): 722–8. doi:10.1038/embor.2009.91. PMC 2727437. PMID 19525919.
  10. ^ 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.
  11. ^ 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. S2CID 7083192.
  12. ^ 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. doi:10.1016/S0021-9258(18)43790-8. PMID 7982920.
  13. ^ Petty A, Myshkin E, Qin H, Guo H, Miao H, Tochtrop GP, Hsieh JT, Page P, Liu L, Lindner DJ, Acharya C, MacKerell AD, Ficker E, Song J, Wang BC (August 2012). "A small molecule agonist of EphA2 receptor tyrosine kinase inhibits tumor cell migration in vitro and prostate cancer metastasis in vivo". PLOS ONE. 7 (8): e42120. Bibcode:2012PLoSO...742120P. doi:10.1371/journal.pone.0042120. PMC 3419725. PMID 22916121.

Further reading

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  • Overview of all the structural information available in the PDB for UniProt: P29317 (Human Ephrin type-A receptor 2) at the PDBe-KB.
  • Overview of all the structural information available in the PDB for UniProt: Q03145 (Mouse Ephrin type-A receptor 2) at the PDBe-KB.