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Allosteric inhibitors of the Eya2 phosphatase are selective and inhibit Eya2-mediated cell migration.

Krueger AB, Drasin DJ, Lea WA, Patrick AN, Patnaik S, Backos DS, Matheson CJ, Hu X, Barnaeva E, Holliday MJ, Blevins MA, Robin TP, Eisenmesser EZ, Ferrer M, Simeonov A, Southall N, Reigan P, Marugan J, Ford HL, Zhao R.

J Biol Chem. 2014 Jun 6;289(23):16349-61. doi: 10.1074/jbc.M114.566729. Epub 2014 Apr 22.


Identification of a selective small-molecule inhibitor series targeting the eyes absent 2 (Eya2) phosphatase activity.

Krueger AB, Dehdashti SJ, Southall N, Marugan JJ, Ferrer M, Li X, Ford HL, Zheng W, Zhao R.

J Biomol Screen. 2013 Jan;18(1):85-96. doi: 10.1177/1087057112453936. Epub 2012 Jul 20.


Crystal structure of ED-Eya2: insight into dual roles as a protein tyrosine phosphatase and a transcription factor.

Jung SK, Jeong DG, Chung SJ, Kim JH, Park BC, Tonks NK, Ryu SE, Kim SJ.

FASEB J. 2010 Feb;24(2):560-9. doi: 10.1096/fj.09-143891. Epub 2009 Oct 26.


The EYA tyrosine phosphatase activity is pro-angiogenic and is inhibited by benzbromarone.

Tadjuidje E, Wang TS, Pandey RN, Sumanas S, Lang RA, Hegde RS.

PLoS One. 2012;7(4):e34806. doi: 10.1371/journal.pone.0034806. Epub 2012 Apr 24.


Eya2 is required to mediate the pro-metastatic functions of Six1 via the induction of TGF-β signaling, epithelial-mesenchymal transition, and cancer stem cell properties.

Farabaugh SM, Micalizzi DS, Jedlicka P, Zhao R, Ford HL.

Oncogene. 2012 Feb 2;31(5):552-62. doi: 10.1038/onc.2011.259. Epub 2011 Jun 27.


Structure-based de novo design of Eya2 phosphatase inhibitors.

Park H, Ryu SE, Kim SJ.

J Mol Graph Model. 2012 Sep;38:382-8. doi: 10.1016/j.jmgm.2012.05.003. Epub 2012 Jun 5.


Structure-function analyses of the human SIX1-EYA2 complex reveal insights into metastasis and BOR syndrome.

Patrick AN, Cabrera JH, Smith AL, Chen XS, Ford HL, Zhao R.

Nat Struct Mol Biol. 2013 Apr;20(4):447-53. doi: 10.1038/nsmb.2505. Epub 2013 Feb 24.


Eya1 and Eya2 proteins are required for hypaxial somitic myogenesis in the mouse embryo.

Grifone R, Demignon J, Giordani J, Niro C, Souil E, Bertin F, Laclef C, Xu PX, Maire P.

Dev Biol. 2007 Feb 15;302(2):602-16. Epub 2006 Sep 1.


Epigenetic silencing of EYA2 in pancreatic adenocarcinomas promotes tumor growth.

Vincent A, Hong SM, Hu C, Omura N, Young A, Kim H, Yu J, Knight S, Ayars M, Griffith M, Van Seuningen I, Maitra A, Goggins M.

Oncotarget. 2014 May 15;5(9):2575-87.


Structure-based virtual screening approach to the discovery of novel inhibitors of eyes absent 2 phosphatase with various metal chelating moieties.

Park H, Jung SK, Yu KR, Kim JH, Kim YS, Ko JH, Park BC, Kim SJ.

Chem Biol Drug Des. 2011 Oct;78(4):642-50. doi: 10.1111/j.1747-0285.2011.01192.x. Epub 2011 Aug 29.


Dephosphorylation of the C-terminal tyrosyl residue of the DNA damage-related histone H2A.X is mediated by the protein phosphatase eyes absent.

Krishnan N, Jeong DG, Jung SK, Ryu SE, Xiao A, Allis CD, Kim SJ, Tonks NK.

J Biol Chem. 2009 Jun 12;284(24):16066-70. doi: 10.1074/jbc.C900032200. Epub 2009 Apr 7.


Synergistic regulation of vertebrate muscle development by Dach2, Eya2, and Six1, homologs of genes required for Drosophila eye formation.

Heanue TA, Reshef R, Davis RJ, Mardon G, Oliver G, Tomarev S, Lassar AB, Tabin CJ.

Genes Dev. 1999 Dec 15;13(24):3231-43.


The SIX1-EYA transcriptional complex as a therapeutic target in cancer.

Blevins MA, Towers CG, Patrick AN, Zhao R, Ford HL.

Expert Opin Ther Targets. 2015 Feb;19(2):213-25. doi: 10.1517/14728222.2014.978860. Epub 2015 Jan 2. Review.


miR-30a suppresses breast cancer cell proliferation and migration by targeting Eya2.

Fu J, Xu X, Kang L, Zhou L, Wang S, Lu J, Cheng L, Fan Z, Yuan B, Tian P, Zheng X, Yu C, Ye Q, Lv Z.

Biochem Biophys Res Commun. 2014 Mar 7;445(2):314-9. doi: 10.1016/j.bbrc.2014.01.174. Epub 2014 Feb 4.


Transcription coactivator Eya2 is a critical regulator of physiological hypertrophy.

Lee SH, Kim J, Ryu JY, Lee S, Yang DK, Jeong D, Kim J, Lee SH, Kim JM, Hajjar RJ, Park WJ.

J Mol Cell Cardiol. 2012 Mar;52(3):718-26. doi: 10.1016/j.yjmcc.2011.12.002. Epub 2011 Dec 14.


Crystal structures and inhibitor identification for PTPN5, PTPRR and PTPN7: a family of human MAPK-specific protein tyrosine phosphatases.

Eswaran J, von Kries JP, Marsden B, Longman E, Debreczeni JE, Ugochukwu E, Turnbull A, Lee WH, Knapp S, Barr AJ.

Biochem J. 2006 May 1;395(3):483-91.


Aberrant hypomethylation and overexpression of the eyes absent homologue 2 suppresses tumor cell growth of human lung adenocarcinoma cells.

Gao T, Zheng S, Li Q, Ran P, Sun L, Yuan Y, Xiao C.

Oncol Rep. 2015 Nov;34(5):2333-42. doi: 10.3892/or.2015.4245. Epub 2015 Sep 2.


Reciprocal signaling between the transcriptional co-factor Eya2 and specific members of the Galphai family.

Embry AC, Glick JL, Linder ME, Casey PJ.

Mol Pharmacol. 2004 Nov;66(5):1325-31. Epub 2004 Aug 12.


Cooperation of six and eya in activation of their target genes through nuclear translocation of Eya.

Ohto H, Kamada S, Tago K, Tominaga SI, Ozaki H, Sato S, Kawakami K.

Mol Cell Biol. 1999 Oct;19(10):6815-24.

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