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Eph receptors and ephrins engage in cellular cannibalism.

Pasquale EB.

J Cell Biol. 2019 Oct 7;218(10):3168-3170. doi: 10.1083/jcb.201908074. Epub 2019 Sep 19.


Engineering nanomolar peptide ligands that differentially modulate EphA2 receptor signaling.

Gomez-Soler M, Petersen Gehring M, Lechtenberg BC, Zapata-Mercado E, Hristova K, Pasquale EB.

J Biol Chem. 2019 May 31;294(22):8791-8805. doi: 10.1074/jbc.RA119.008213. Epub 2019 Apr 23.


Inhibition of EphB4-Ephrin-B2 Signaling Reprograms the Tumor Immune Microenvironment in Head and Neck Cancers.

Bhatia S, Oweida A, Lennon S, Darragh LB, Milner D, Phan AV, Mueller AC, Van Court B, Raben D, Serkova NJ, Wang XJ, Jimeno A, Clambey ET, Pasquale EB, Karam SD.

Cancer Res. 2019 May 15;79(10):2722-2735. doi: 10.1158/0008-5472.CAN-18-3257. Epub 2019 Mar 20.


Genetically Encoded FRET Biosensor for Visualizing EphA4 Activity in Different Compartments of the Plasma Membrane.

Pan Y, Lu S, Lei L, Lamberto I, Wang Y, Pasquale EB, Wang Y.

ACS Sens. 2019 Feb 22;4(2):294-300. doi: 10.1021/acssensors.8b00465. Epub 2019 Jan 16.


Erratum: Author Correction: The EphA2 receptor is activated through induction of distinct, ligand-dependent oligomeric structures.

Singh DR, Kanvinde P, King C, Pasquale EB, Hristova K.

Commun Biol. 2018 Apr 19;1:40. doi: 10.1038/s42003-018-0044-4. eCollection 2018.


The EphA2 receptor is activated through induction of distinct, ligand-dependent oligomeric structures.

Singh DR, Kanvinde P, King C, Pasquale EB, Hristova K.

Commun Biol. 2018 Feb 22;1:15. doi: 10.1038/s42003-018-0017-7. eCollection 2018. Erratum in: Commun Biol. 2018 Apr 19;1:40.


SORLA attenuates EphA4 signaling and amyloid β-induced neurodegeneration.

Huang TY, Zhao Y, Jiang LL, Li X, Liu Y, Sun Y, Piña-Crespo JC, Zhu B, Masliah E, Willnow TE, Pasquale EB, Xu H.

J Exp Med. 2017 Dec 4;214(12):3669-3685. doi: 10.1084/jem.20171413. Epub 2017 Nov 7.


Structure-Guided Strategy for the Development of Potent Bivalent ERK Inhibitors.

Lechtenberg BC, Mace PD, Sessions EH, Williamson R, Stalder R, Wallez Y, Roth GP, Riedl SJ, Pasquale EB.

ACS Med Chem Lett. 2017 Jun 12;8(7):726-731. doi: 10.1021/acsmedchemlett.7b00127. eCollection 2017 Jul 13.


Evaluation of EphA2 and EphB4 as Targets for Image-Guided Colorectal Cancer Surgery.

Stammes MA, Prevoo HA, Ter Horst MC, Groot SA, Van de Velde CJ, Chan AB, de Geus-Oei LF, Kuppen PJ, Vahrmeijer AL, Pasquale EB, Sier CF.

Int J Mol Sci. 2017 Feb 3;18(2). pii: E307. doi: 10.3390/ijms18020307.


Enhancing radiosensitization in EphB4 receptor-expressing Head and Neck Squamous Cell Carcinomas.

Bhatia S, Hirsch K, Sharma J, Oweida A, Griego A, Keysar S, Jimeno A, Raben D, Krasnoperov V, Gill PS, Pasquale EB, Wang XJ, Karam SD.

Sci Rep. 2016 Dec 12;6:38792. doi: 10.1038/srep38792.


The SAM domain inhibits EphA2 interactions in the plasma membrane.

Singh DR, Ahmed F, Paul MD, Gedam M, Pasquale EB, Hristova K.

Biochim Biophys Acta Mol Cell Res. 2017 Jan;1864(1):31-38. doi: 10.1016/j.bbamcr.2016.10.011. Epub 2016 Oct 21.


Modifications of a Nanomolar Cyclic Peptide Antagonist for the EphA4 Receptor To Achieve High Plasma Stability.

Olson EJ, Lechtenberg BC, Zhao C, Rubio de la Torre E, Lamberto I, Riedl SJ, Dawson PE, Pasquale EB.

ACS Med Chem Lett. 2016 Jun 25;7(9):841-6. doi: 10.1021/acsmedchemlett.6b00132. eCollection 2016 Sep 8.


Protein kinase A can block EphA2 receptor-mediated cell repulsion by increasing EphA2 S897 phosphorylation.

Barquilla A, Lamberto I, Noberini R, Heynen-Genel S, Brill LM, Pasquale EB.

Mol Biol Cell. 2016 Sep 1;27(17):2757-70. doi: 10.1091/mbc.E16-01-0048. Epub 2016 Jul 6.


Exosomes expand the sphere of influence of Eph receptors and ephrins.

Pasquale EB.

J Cell Biol. 2016 Jul 4;214(1):5-7. doi: 10.1083/jcb.201606074. Epub 2016 Jun 27.


A small peptide promotes EphA2 kinase-dependent signaling by stabilizing EphA2 dimers.

Singh DR, Pasquale EB, Hristova K.

Biochim Biophys Acta. 2016 Sep;1860(9):1922-8. doi: 10.1016/j.bbagen.2016.06.004. Epub 2016 Jun 6.


Regional expression and ultrastructural localization of EphA7 in the hippocampus and cerebellum of adult rat.

Amegandjin CA, Jammow W, Laforest S, Riad M, Baharnoori M, Badeaux F, DesGroseillers L, Murai KK, Pasquale EB, Drolet G, Doucet G.

J Comp Neurol. 2016 Aug 15;524(12):2462-78. doi: 10.1002/cne.23962. Epub 2016 Feb 26.


EphA2 Receptor Unliganded Dimers Suppress EphA2 Pro-tumorigenic Signaling.

Singh DR, Ahmed F, King C, Gupta N, Salotto M, Pasquale EB, Hristova K.

J Biol Chem. 2015 Nov 6;290(45):27271-9. doi: 10.1074/jbc.M115.676866. Epub 2015 Sep 11.


Unliganded EphA3 dimerization promoted by the SAM domain.

Singh DR, Cao Q, King C, Salotto M, Ahmed F, Zhou XY, Pasquale EB, Hristova K.

Biochem J. 2015 Oct 1;471(1):101-9. doi: 10.1042/BJ20150433. Epub 2015 Jul 31.


Targeting the Eph System with Peptides and Peptide Conjugates.

Riedl SJ, Pasquale EB.

Curr Drug Targets. 2015;16(10):1031-47. Review.


Distinctive Structure of the EphA3/Ephrin-A5 Complex Reveals a Dual Mode of Eph Receptor Interaction for Ephrin-A5.

Forse GJ, Uson ML, Nasertorabi F, Kolatkar A, Lamberto I, Pasquale EB, Kuhn P.

PLoS One. 2015 May 20;10(5):e0127081. doi: 10.1371/journal.pone.0127081. eCollection 2015.


Knockdown of EphB1 receptor decreases medulloblastoma cell growth and migration and increases cellular radiosensitization.

Bhatia S, Baig NA, Timofeeva O, Pasquale EB, Hirsch K, MacDonald TJ, Dritschilo A, Lee YC, Henkemeyer M, Rood B, Jung M, Wang XJ, Kool M, Rodriguez O, Albanese C, Karam SD.

Oncotarget. 2015 Apr 20;6(11):8929-46.


Ligand-independent EPHA2 signaling drives the adoption of a targeted therapy-mediated metastatic melanoma phenotype.

Paraiso KH, Das Thakur M, Fang B, Koomen JM, Fedorenko IV, John JK, Tsao H, Flaherty KT, Sondak VK, Messina JL, Pasquale EB, Villagra A, Rao UN, Kirkwood JM, Meier F, Sloot S, Gibney GT, Stuart D, Tawbi H, Smalley KS.

Cancer Discov. 2015 Mar;5(3):264-73. doi: 10.1158/2159-8290.CD-14-0293. Epub 2014 Dec 26.


Eph receptors and ephrins: therapeutic opportunities.

Barquilla A, Pasquale EB.

Annu Rev Pharmacol Toxicol. 2015;55:465-87. doi: 10.1146/annurev-pharmtox-011112-140226. Epub 2014 Oct 3. Review.


Development and structural analysis of a nanomolar cyclic peptide antagonist for the EphA4 receptor.

Lamberto I, Lechtenberg BC, Olson EJ, Mace PD, Dawson PE, Riedl SJ, Pasquale EB.

ACS Chem Biol. 2014 Dec 19;9(12):2787-95. doi: 10.1021/cb500677x. Epub 2014 Oct 14.


Design, synthesis and bioevaluation of an EphA2 receptor-based targeted delivery system.

Barile E, Wang S, Das SK, Noberini R, Dahl R, Stebbins JL, Pasquale EB, Fisher PB, Pellecchia M.

ChemMedChem. 2014 Jul;9(7):1403-12. doi: 10.1002/cmdc.201400067. Epub 2014 Mar 26.


EphA4 activation of c-Abl mediates synaptic loss and LTP blockade caused by amyloid-β oligomers.

Vargas LM, Leal N, Estrada LD, González A, Serrano F, Araya K, Gysling K, Inestrosa NC, Pasquale EB, Alvarez AR.

PLoS One. 2014 Mar 21;9(3):e92309. doi: 10.1371/journal.pone.0092309. eCollection 2014.


UniPR129 is a competitive small molecule Eph-ephrin antagonist blocking in vitro angiogenesis at low micromolar concentrations.

Hassan-Mohamed I, Giorgio C, Incerti M, Russo S, Pala D, Pasquale EB, Zanotti I, Vicini P, Barocelli E, Rivara S, Mor M, Lodola A, Tognolini M.

Br J Pharmacol. 2014 Dec;171(23):5195-208. doi: 10.1111/bph.12669. Epub 2014 Aug 28.


Association of the breast cancer antiestrogen resistance protein 1 (BCAR1) and BCAR3 scaffolding proteins in cell signaling and antiestrogen resistance.

Wallez Y, Riedl SJ, Pasquale EB.

J Biol Chem. 2014 Apr 11;289(15):10431-44. doi: 10.1074/jbc.M113.541839. Epub 2014 Feb 28.


Attenuation of eph receptor kinase activation in cancer cells by coexpressed ephrin ligands.

Falivelli G, Lisabeth EM, Rubio de la Torre E, Perez-Tenorio G, Tosato G, Salvucci O, Pasquale EB.

PLoS One. 2013 Nov 29;8(11):e81445. doi: 10.1371/journal.pone.0081445. eCollection 2013.


Design and Synthesis of Potent Bivalent Peptide Agonists Targeting the EphA2 Receptor.

Duggineni S, Mitra S, Lamberto I, Han X, Xu Y, An J, Pasquale EB, Huang Z.

ACS Med Chem Lett. 2013 Feb 5;4(3). doi: 10.1021/ml3004523.


Unique structure and dynamics of the EphA5 ligand binding domain mediate its binding specificity as revealed by X-ray crystallography, NMR and MD simulations.

Huan X, Shi J, Lim L, Mitra S, Zhu W, Qin H, Pasquale EB, Song J.

PLoS One. 2013 Sep 24;8(9):e74040. doi: 10.1371/journal.pone.0074040. eCollection 2013.


Eph receptor signaling and ephrins.

Lisabeth EM, Falivelli G, Pasquale EB.

Cold Spring Harb Perspect Biol. 2013 Sep 1;5(9). pii: a009159. doi: 10.1101/cshperspect.a009159. Review.


Ephrin-A1/EphA4-mediated adhesion of monocytes to endothelial cells.

Jellinghaus S, Poitz DM, Ende G, Augstein A, Weinert S, Stütz B, Braun-Dullaeus RC, Pasquale EB, Strasser RH.

Biochim Biophys Acta. 2013 Oct;1833(10):2201-11. doi: 10.1016/j.bbamcr.2013.05.017. Epub 2013 May 23.


Structure of ERK2 bound to PEA-15 reveals a mechanism for rapid release of activated MAPK.

Mace PD, Wallez Y, Egger MF, Dobaczewska MK, Robinson H, Pasquale EB, Riedl SJ.

Nat Commun. 2013;4:1681. doi: 10.1038/ncomms2687.


Amino acid conjugates of lithocholic acid as antagonists of the EphA2 receptor.

Incerti M, Tognolini M, Russo S, Pala D, Giorgio C, Hassan-Mohamed I, Noberini R, Pasquale EB, Vicini P, Piersanti S, Rivara S, Barocelli E, Mor M, Lodola A.

J Med Chem. 2013 Apr 11;56(7):2936-47. doi: 10.1021/jm301890k. Epub 2013 Mar 22.


HTS by NMR of combinatorial libraries: a fragment-based approach to ligand discovery.

Wu B, Zhang Z, Noberini R, Barile E, Giulianotti M, Pinilla C, Houghten RA, Pasquale EB, Pellecchia M.

Chem Biol. 2013 Jan 24;20(1):19-33. doi: 10.1016/j.chembiol.2012.10.015.


Design, synthesis and characterization of novel small molecular inhibitors of ephrin-B2 binding to EphB4.

Duggineni S, Mitra S, Noberini R, Han X, Lin N, Xu Y, Tian W, An J, Pasquale EB, Huang Z.

Biochem Pharmacol. 2013 Feb 15;85(4):507-13. doi: 10.1016/j.bcp.2012.12.005. Epub 2012 Dec 17.


The EphA2 receptor drives self-renewal and tumorigenicity in stem-like tumor-propagating cells from human glioblastomas.

Binda E, Visioli A, Giani F, Lamorte G, Copetti M, Pitter KL, Huse JT, Cajola L, Zanetti N, DiMeco F, De Filippis L, Mangiola A, Maira G, Anile C, De Bonis P, Reynolds BA, Pasquale EB, Vescovi AL.

Cancer Cell. 2012 Dec 11;22(6):765-80. doi: 10.1016/j.ccr.2012.11.005.


NSP-CAS Protein Complexes: Emerging Signaling Modules in Cancer.

Wallez Y, Mace PD, Pasquale EB, Riedl SJ.

Genes Cancer. 2012 May;3(5-6):382-93. doi: 10.1177/1947601912460050.


Targeted delivery of paclitaxel to EphA2-expressing cancer cells.

Wang S, Noberini R, Stebbins JL, Das S, Zhang Z, Wu B, Mitra S, Billet S, Fernandez A, Bhowmick NA, Kitada S, Pasquale EB, Fisher PB, Pellecchia M.

Clin Cancer Res. 2013 Jan 1;19(1):128-37. doi: 10.1158/1078-0432.CCR-12-2654. Epub 2012 Nov 15.


Inhibition of Eph receptor-ephrin ligand interaction by tea polyphenols.

Noberini R, Koolpe M, Lamberto I, Pasquale EB.

Pharmacol Res. 2012 Oct;66(4):363-73. doi: 10.1016/j.phrs.2012.05.010. Epub 2012 Jun 28.


Profiling Eph receptor expression in cells and tissues: a targeted mass spectrometry approach.

Noberini R, Rubio de la Torre E, Pasquale EB.

Cell Adh Migr. 2012 Mar-Apr;6(2):102-12. doi: 10.4161/cam.19620. Epub 2012 Mar 1.


Structure-activity relationships and mechanism of action of Eph-ephrin antagonists: interaction of cholanic acid with the EphA2 receptor.

Tognolini M, Incerti M, Hassan-Mohamed I, Giorgio C, Russo S, Bruni R, Lelli B, Bracci L, Noberini R, Pasquale EB, Barocelli E, Vicini P, Mor M, Lodola A.

ChemMedChem. 2012 Jun;7(6):1071-83. doi: 10.1002/cmdc.201200102. Epub 2012 Apr 23.


Distinctive binding of three antagonistic peptides to the ephrin-binding pocket of the EphA4 receptor.

Lamberto I, Qin H, Noberini R, Premkumar L, Bourgin C, Riedl SJ, Song J, Pasquale EB.

Biochem J. 2012 Jul 1;445(1):47-56. doi: 10.1042/BJ20120408.


Novel targeted system to deliver chemotherapeutic drugs to EphA2-expressing cancer cells.

Wang S, Placzek WJ, Stebbins JL, Mitra S, Noberini R, Koolpe M, Zhang Z, Dahl R, Pasquale EB, Pellecchia M.

J Med Chem. 2012 Mar 8;55(5):2427-36. doi: 10.1021/jm201743s. Epub 2012 Feb 27.


Cancer somatic mutations disrupt functions of the EphA3 receptor tyrosine kinase through multiple mechanisms.

Lisabeth EM, Fernandez C, Pasquale EB.

Biochemistry. 2012 Feb 21;51(7):1464-75. doi: 10.1021/bi2014079. Epub 2012 Feb 8.


PEGylation potentiates the effectiveness of an antagonistic peptide that targets the EphB4 receptor with nanomolar affinity.

Noberini R, Mitra S, Salvucci O, Valencia F, Duggineni S, Prigozhina N, Wei K, Tosato G, Huang Z, Pasquale EB.

PLoS One. 2011;6(12):e28611. doi: 10.1371/journal.pone.0028611. Epub 2011 Dec 14.


NSP-Cas protein structures reveal a promiscuous interaction module in cell signaling.

Mace PD, Wallez Y, Dobaczewska MK, Lee JJ, Robinson H, Pasquale EB, Riedl SJ.

Nat Struct Mol Biol. 2011 Nov 13;18(12):1381-7. doi: 10.1038/nsmb.2152.


Targeting Eph receptors with peptides and small molecules: progress and challenges.

Noberini R, Lamberto I, Pasquale EB.

Semin Cell Dev Biol. 2012 Feb;23(1):51-7. doi: 10.1016/j.semcdb.2011.10.023. Epub 2011 Oct 25. Review.


Complementary expression and repulsive signaling suggest that EphB receptors and ephrin-B ligands control cell positioning in the gastric epithelium.

Ogawa K, Takemoto N, Ishii M, Pasquale EB, Nakajima T.

Histochem Cell Biol. 2011 Dec;136(6):617-36. doi: 10.1007/s00418-011-0867-2. Epub 2011 Sep 30.


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