Selected Publications

View a complete list of publications on PubMed.

• Park E, Rawson S, Schmoker AM, Kim BW, Oh S, Song K, Jeon H, Eck MJ. Cryo-EM structure of a RAS/RAF recruitment complex. Nat Commun. 14, 5517 (2023). https://doi.org/10.1038/s41467-023-41365-9
• Hauseman ZJ, Fodor M, Dhembi A, Viscomi J, Egli D, Bleu M, Katz S, Park E, Jang DM, Porter KA, Meili F, Guo H, Kerr G, Mollé S, Velez-Vega C, Beyer KS, Galli GG, Maira SM, Stams T, Clark K, Eck MJ, Tordella L, Thoma CR, King DA. Structure of the MRAS-SHOC2-PP1C phosphatase complex. Nature. 2022 Sep;609(7926):416-423. doi: 10.1038/s41586-022-05086-1. Epub 2022 Jul 13. PMID: 35830882
• Gonzalez-Del Pino GL, Li K, Park E, Schmoker AM, Ha BH, Eck MJ. Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation. Proc Natl Acad Sci U S A. 2021 Sep 7;118(36):e2107207118.
• Park E, Rawson S, Li K, Kim BW, Ficarro SB, Gonzalez-Del Pino G, Sharif H, Marto JA, Jeon H, Eck MJ. Architecture of autoinhibited and active BRAF-MEK-14-3-3 complexes. Nature. 2019 Nov;575(7783):545-550.
  • Caught in the Act: First snapshots of cancer protein B-Raf illuminate basic biology, drug design

• Beyett TS, To C, Heppner DE, Rana JK, Schmoker AM, Jang J, De Clercq DJH, Gomez G, Scott DA, Gray NS, Jänne PA, Eck MJ. Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors. Nat Commun. 2022 May 9;13(1):2530. doi: 10.1038/s41467-022-30258-y. PMID: 35534503.
• To C, Beyett TS, Jang J, Feng WF, Bahcall M, Haikala HM, Shin BH, Heppner DE, Rana JK,  Leeper BA, Soroko KM, Poitras MJ, Gokhale PC, Kobayashi Y, Wahid K, Kurppa KJ, Gero TW, Cameron CD, Ogino A, Mushajiang M, Xu C, Zhang Y, Scott DA, Michael J. Eck MJ, Gray NS, Jänne PA. An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer. Nature Cancer. 2022.
  • Commentary: Resistance is futile with fourth-generation EGFR inhibitors
• Jang J, Son J, Park E, Kosaka T, Saxon JA, De Clercq DJH, Choi HG, Tanizaki J, Eck MJ, Jänne PA, Gray NS. Discovery of a Highly Potent and Broadly Effective Epidermal Growth Factor Receptor and HER2 Exon 20 Insertion Mutant Inhibitor. Angew Chem Int Ed Engl. 2018 Sep 3; 57(36): 11629–11633.
• Jia Y, Yun CH, Park E, Ercan D, Manuia M, Juarez, J, Xu C, Rhee K, Chen T, Zhang H, Palakurthi S, Jang J, Lelias G, DiDinato M, Bursulaya B, Michellys PY, Epple R, Marsilje TH, McNeil M, Lu W, Harris J, Bender S, Wong KK, Janne PA, Eck MJ. Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant selective allosteric inhibitors. Nature. 2016 June Jun 2;534(7605):129-32. 
• Begley MJ, Yun CH, Gewinner CA, Asara JM, Johnson JL, Coyle AJ, Eck MJ, Apostolou I, Cantley LC. EGF-receptor specificity for phosphotyrosine-primed substrates provides signal integration with Src. Nat Strcut Mol Biol. 2015 Dec;22(12):983-90. 
• Park E, Kim N, Ficarro SB, Zhang Y, Lee BI, Cho A, Kim K, Park AK, Park WY, Murray B, Meyerson M, Beroukhim R, Maro JA, Cho J, Eck MJ. Structure and mechanism of activity-based inhibition of the EGF receptor by Mig6. Nat Struct Mol Biol. 2015 Sep;22(9):703-711.
• Ercan D, Choi HG, Yun CH, Capelleti M, Xie T, Eck mJ, Gray NS, Janne PA. EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors. Clin Cancer Res. 2015 Sep 1;21(17):3913-23.
• Yasuda H, Park E, Yun CH, Sng NJ, Lucena-Araujo AR, Yeo WL, Huberman MS, Cohen DW, Nakayama, S, Ishioka K, Yamaguchi N, Hanna M, Oxnard GR, Lathan CS, Moran T, Sequist LV, Chaft JE, Rely GJ, Arcila ME, Soo RA, Meyerson M, Eck MJ, Kobayashi SS, Costa DB. Structural, biochemical, and clinical characterization of epidermal growth factor receptor (EGFR) exon 20 insertion mutations in lung cancer. Sci Transl Med. 2013 Dec 18;5(216):216ra177.
• Zhou W, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R, Engen JR, Wong KK, Eck MJ, Gray NS, Janne PA. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24;462(7276):1070-4.
• Yun CH, Mengwasser KE, Toms AV, Woo MS, Greukich H, Wong KK, Meyerson M, Eck MJ. The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. Proc Natl Acad Sci U S A. 2008 Feb 12;105(6):2070-5.
• Yun CH, Boggon TJ, Li Y, Woo MS, Greulich H, Meyerson M, Eck MJ. Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity. Cancer Cell. 2007 Mar;11(3):217-27.

• McNally R, Li Q, Li K, Dekker C, Vangrevelinghe E, Jones M, Chène P, Machauer R, Radimerski T, Eck MJ. Discovery and Structural Characterization of ATP-Site Ligands for the Wild-Type and V617F Mutant JAK2 Pseudokinase Domain. ACS Chem Biol. 2019 Apr 19;14(4):587-593.
• McNally R, Toms AV, Eck MJ. Crystal Structure of the FERM-SH2 Module of Human Jak2. PLos One. 2016 May 26;11(5):e0156218.
• Tan L, Akahane K, McNally R, Reyskens KM, Ficaroo SB, Liu S, Herter-Sprie GS, Koyama S, Pattison MJ, Labella K, Johannessen L, Akbay EA, Wong KK, Frank DA, Marto JA, Look TA, Arthur JS, Eck MJ, Gray NS. Development of Selective Covalent Janus Kinase 3 Inhibitors. J. Med Chem. 2015 Aug 27;58(16):6589-606.
• Toms Av, Deshpande A, McNally R, Jeong Y, Rogers JM, Kim CU, Gruner SM, Ficarro SB, Marto JA, Sattler M,Griffin JD, Eck MJ. Structure of a psuedokinase-domain switch that controls oncogenic activation of Jak kinases. Nat Struct Mol Biol. 2013 Oct;20(10):1221-3.
• Boggon TJ, Li Y, Manley PW, Eck MJ. Crystal structure of the Jak3 kinase domain in complex with a staurosporine analog. Blood. 2005 Aug 1;106(3):996-1002. 

• Boczkowska M, Yurtsever Z, Rebowski G, Eck MJ, Dominguez R. Crystal Structure of Leiomodin 2 in Complex with Actin: A Structural and Functional Reexamination. Biophys J. 2017 Aug 22;113(4):889-899.
• Park E, Graziano BR, Zheng W, Garabedian M, Goode BL, Eck MJ. Structure of a Bud6/Actin Complex Reveals a Novel WH2-like Actin Monomer Recruitment Motif. Structure. 2015 Aug 4;23(8):1492-9.
• Tu D, Graziano BR, Park E, Zheng W, Li Y, Goode BL, Eck MJ. Structure of the formin-interaction domain of the actin nucleation-promoting factor Bud6. Proc Natl Acad Sci U S A. 2012 Dec 11;109(50):E3424-33.
• Vizcarra CL. Kreutz B, Rodal AA, Toms AV, Lu J, Zheng W, Quinlan ME, Eck MJ. Structure and function of the interacting domains of Spire and Fmn-family formins. Proc Natl Acad Sci U S A. 2011 Jul 19;108(29):11884-9.
• Nezami A, Poy F, Toms A , Zheng W, Eck MJ. Crystal structure of a complex between amino and carboxy terminal fragments of mDia1: insights into autoinhibition of diaphanous-related formins. PLos One. 2010 Sep 30;5(9). pii: e12992.
• Nezami AG, Poy F, Eck MJ. Structure of the autoinhibitory switch in formin mDia1. Structure. 2006 Feb;14(2):257-63.
• Xu Y, Moseley JB, Sagot I, Poy F, Pellman D, Goode BL, Eck MJ. Crystal structures of a Formin Homology-2 domain reveal a tethered dimer architecture. Cell. 2004 Mar 5;116(5):711-23.

• Cai X, Lietha D, Ceccarelli DF, Karginov AV, Rajfur Z, Jacobson K, Hahn KM, Eck MJ, Schaller MD. Spatial and temporal regulation of focal adhesion kinase activity in living cells. Mol Cell Biol. 2008 Jan;28(1):201-14.
• Lietha D, Eck MJ. Crystal structures of the FAK kinase in complex with TAE226 and related bis-anilino pyrimidine inhibitors reveal a helical DFG conformation. PloS One. 2008;3(11):e3800.
• Lietha D, Cai X, Ceccarelli DF, Li Y, Schaller MD, Eck MJ. Structural basis for the autoinhibition of focal adhesion kinase. Cell. 2007 Jun 15;129(6):1177-87.
• Ceccarelli DF, Song HK, Poy F, Schaller MD, Eck MJ. Crystal structure of the FERM domain of focal adhesion kinase. J Biol Chem. 2006 Jan 6;281(1):252-9.

• Huang HT, Seo HS, Zhang T, Wang Y, Jiang B, Li Q, Buckley DL, Nabet B, Roberts JM, Paulk J, Dastjerdi S, Winter GE, McLauchlan H, Moran J, Bradner JE, Eck MJ, Dhe-Paganon S, Zhao JJ, Gray NS. MELK is not necessary for the proliferation of basal-like breast cancer cells. Elife. 2017 Sep 19;6. pii: e26693. doi: 10.7554/eLife.26693.
• Cai W, Sakaguchi M, Kleinridders A, Gonzalez-Del Pino G, Dreyfuss JM, O'Neill BT, Ramirez AK, Pan H, Winnay JN, Boucher J, Eck MJ, Kahn CR. Domain-dependent effects of insulin and IGF-1 receptors on signalling and gene expression. Nat Commun. 2017 Mar 27;8:14892. doi: 10.1038/ncomms14892.
• Tu D, Zhu Z, Zhou AY, Yun CH, Lee KE, Toms AV, Li Y, Dunn GP, Chan E, Thai T, Yang S, Ficarro SB, Marto JA, Jeon H, Hahn WC, Barbie DA, Eck MJ. ​Structure and ubiquitination-dependent activation of TANK-binding kinase 1. Cell Rep. 2013 Mar 28;3(3):747-58. doi: 10.1016/j.celrep.2013.01.033.​

• EAI-432, a mutant-selective allosteric EGFR inhibitor for L858R-mutant lung cancer.