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Journal Article
To, C., Beyett, T. S., Jang, J., Feng, W. W., Bahcall, M., Haikala, H. M., Shin, B. H., Heppner, D. E., Rana, J. K., Leeper, B. A., Soroko, K. M., Poitras, M. J., Gokhale, P. C., Kobayashi, Y., Wahid, K., Kurppa, K. J., Gero, T. W., Cameron, M. D., Ogino, A., Mushajiang, M., Xu, C., Zhang, Y., Scott, D. A., Eck, M. J., Gray, N. S., and Jänne, P. A. (2022) An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer. Nat Cancer. 3, 402-417
Del Pino, G. L. Gonzalez, Li, K., Park, E., Schmoker, A. M., Ha, B. Hak, and Eck, M. J. (2021) Allosteric MEK inhibitors act on BRAF/MEK complexes to block MEK activation. Proc Natl Acad Sci U S A. 10.1073/pnas.2107207118
Park, E., Rawson, S., Li, K., Kim, B. - W., Ficarro, S. B., Del Pino, G. Gonzalez-, Sharif, H., Marto, J. A., Jeon, H., and Eck, M. J. (2019) Architecture of autoinhibited and active BRAF-MEK1-14-3-3 complexes. Nature. 575, 545-550
Tu, D., Li, Y., Song, H. Kyu, Toms, A. V., Gould, C. J., Ficarro, S. B., Marto, J. A., Goode, B. L., and Eck, M. J. (2011) Crystal structure of a coiled-coil domain from human ROCK I. PLoS One. 6, e18080
McNally, R., Toms, A. V., and Eck, M. J. (2016) Crystal Structure of the FERM-SH2 Module of Human Jak2. PLoS One. 11, e0156218
Xu, Y., Moseley, J. B., Sagot, I., Poy, F., Pellman, D., Goode, B. L., and Eck, M. J. (2004) Crystal structures of a Formin Homology-2 domain reveal a tethered dimer architecture. Cell. 116, 711-23
Meyer, P. A., Socias, S., Key, J., Ransey, E., Tjon, E. C., Buschiazzo, A., Lei, M., Botka, C., Withrow, J., Neau, D., Rajashankar, K., Anderson, K. S., Baxter, R. H., Blacklow, S. C., Boggon, T. J., Bonvin, A. M. J. J., Borek, D., Brett, T. J., Caflisch, A., Chang, C. - I., Chazin, W. J., Corbett, K. D., Cosgrove, M. S., Crosson, S., Dhe-Paganon, S., Di Cera, E., Drennan, C. L., Eck, M. J., Eichman, B. F., Fan, Q. R., Ferré-D'Amaré, A. R., J Fromme, C., K Garcia, C., Gaudet, R., Gong, P., Harrison, S. C., Heldwein, E. E., Jia, Z., Keenan, R. J., Kruse, A. C., Kvansakul, M., McLellan, J. S., Modis, Y., Nam, Y., Otwinowski, Z., Pai, E. F., Pereira, P. José Barb, Petosa, C., Raman, C. S., Rapoport, T. A., Roll-Mecak, A., Rosen, M. K., Rudenko, G., Schlessinger, J., Schwartz, T. U., Shamoo, Y., Sondermann, H., Tao, Y. J., Tolia, N. H., Tsodikov, O. V., Westover, K. D., Wu, H., Foster, I., Fraser, J. S., Maia, F. R. N. C., Gonen, T., Kirchhausen, T., Diederichs, K., Crosas, M., and Sliz, P. (2016) Data publication with the structural biology data grid supports live analysis. Nat Commun. 7, 10882
Wittlinger, F., Heppner, D. E., To, C., Günther, M., Shin, B. Hee, Rana, J. K., Schmoker, A. M., Beyett, T. S., Berger, L. M., Berger, B. - T., Bauer, N., Vasta, J. D., Corona, C. R., Robers, M. B., Knapp, S., Jänne, P. A., Eck, M. J., and Laufer, S. A. (2021) Design of a "Two-in-One" Mutant-Selective Epidermal Growth Factor Receptor Inhibitor That Spans the Orthosteric and Allosteric Sites. J Med Chem. 10.1021/acs.jmedchem.1c00848
Tan, L., Akahane, K., McNally, R., Reyskens, K. M. S. E., Ficarro, S. B., Liu, S., Herter-Sprie, G. S., Koyama, S., Pattison, M. J., Labella, K., Johannessen, iv, L., Akbay, E. A., Wong, K. - K., Frank, D. A., Marto, J. A., Look, T. A., J Arthur, S. C., Eck, M. J., and Gray, N. S. (2015) Development of Selective Covalent Janus Kinase 3 Inhibitors. J Med Chem. 58, 6589-606
De Clercq, D. J. H., Heppner, D. E., To, C., Jang, J., Park, E., Yun, C. -hong, Mushajiang, M., Shin, B. Hee, Gero, T. W., Scott, D. A., Jänne, P. A., Eck, M. J., and Gray, N. S. (2019) Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors. ACS Med Chem Lett. 10, 1549-1553
McNally, R., Li, Q., Li, K., Dekker, C., Vangrevelinghe, E., Jones, M., Chene, P., Machauer, R., Radimerski, T., and Eck, M. J. (2019) Discovery and structural characterization of ATP-site ligands for the wild-type and V617F-mutant JAK2 pseudokinase domain. ACS Chem Biol. 10.1021/acschembio.8b00722
Jang, J., Son, J., Park, E., Kosaka, T., Saxon, J. A., De Clercq, D. J. H., Choi, H. Geun, Tanizaki, J., Eck, M. J., Jänne, P. A., and Gray, N. S. (2018) Discovery of a Highly Potent and Broadly Effective Epidermal Growth Factor Receptor and HER2 Exon 20 Insertion Mutant Inhibitor. Angew Chem Int Ed Engl. 57, 11629-11633
Begley, M. J., Yun, C. -hong, Gewinner, C. A., Asara, J. M., Johnson, J. L., Coyle, A. J., Eck, M. J., Apostolou, I., and Cantley, L. C. (2015) EGF-receptor specificity for phosphotyrosine-primed substrates provides signal integration with Src. Nat Struct Mol Biol. 22, 983-90
Wittlinger, F., Ogboo, B. C., Shevchenko, E., Damghani, T., Pham, C. D., Schaeffner, I. K., Oligny, B. T., Chitnis, S. P., Beyett, T. S., Rasch, A., Buckley, B., Urul, D. A., Shaurova, T., May, E. W., Schaefer, E. M., Eck, M. J., Hershberger, P. A., Poso, A., Laufer, S. A., and Heppner, D. E. (2024) Linking ATP and allosteric sites to achieve superadditive binding with bivalent EGFR kinase inhibitors. Commun Chem. 7, 38
Amrhein, J. A., Beyett, T. S., Feng, W. W., Krämer, A., Weckesser, J., Schaeffner, I. K., Rana, J. K., Jänne, P. A., Eck, M. J., Knapp, S., and Hanke, T. (2022) Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19. J Med Chem. 65, 15679-15697
Brewer, M. Red, Yun, C. -hong, Lai, D., Lemmon, M. A., Eck, M. J., and Pao, W. (2013) Mechanism for activation of mutated epidermal growth factor receptors in lung cancer. Proc Natl Acad Sci U S A. 110, E3595-604
Huang, H. - T., Seo, H. - S., Zhang, T., Wang, Y., Jiang, B., Li, Q., Buckley, D. L., Nabet, B., Roberts, J. M., Paulk, J., Dastjerdi, S., Winter, G. E., McLauchlan, H., Moran, J., Bradner, J. E., Eck, M. J., Dhe-Paganon, S., Zhao, J. J., and Gray, N. S. (2017) MELK is not necessary for the proliferation of basal-like breast cancer cells. Elife. 10.7554/eLife.26693
Beyett, T. S., To, C., Heppner, D. E., Rana, J. K., Schmoker, A. M., Jang, J., De Clercq, D. J. H., Gomez, G., Scott, D. A., Gray, N. S., Jänne, P. A., and Eck, M. J. (2022) Molecular basis for cooperative binding and synergy of ATP-site and allosteric EGFR inhibitors. Nat Commun. 13, 2530
Son, J., Jang, J., Beyett, T. S., Eum, Y., Haikala, H. M., Verano, A., Lin, M., Hatcher, J. M., Kwiatkowski, N. P., Eser, P. Özden, Poitras, M. J., Wang, S., Xu, M., Gokhale, P. C., Cameron, M. D., Eck, M. J., Gray, N. S., and Jänne, P. A. (2022) A novel HER2-selective kinase inhibitor is effective in HER2 mutant and amplified non-small cell lung cancer. Cancer Res. 10.1158/0008-5472.CAN-21-2693
Zhou, W., Ercan, D., Chen, L., Yun, C. -hong, Li, D., Capelletti, M., Cortot, A. B., Chirieac, L., Iacob, R. E., Padera, R., Engen, J. R., Wong, K. - K., Eck, M. J., Gray, N. S., and Jänne, P. A. (2009) Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 462, 1070-4
Bae, H., Viennet, T., Park, E., Chu, N., Salguero, A., Eck, M. J., Arthanari, H., and Cole, P. A. (2022) PH domain-mediated autoinhibition and oncogenic activation of Akt. Elife. 10.7554/eLife.80148
Gero, T. W., Heppner, D. E., Beyett, T. S., To, C., Azevedo, S. C., Jang, J., Bunnell, T., Feru, F., Li, Z., Shin, B. Hee, Soroko, K. M., Gokhale, P. C., Gray, N. S., Jänne, P. A., Eck, M. J., and Scott, D. A. (2022) Quinazolinones as allosteric fourth-generation EGFR inhibitors for the treatment of NSCLC. Bioorg Med Chem Lett. 10.1016/j.bmcl.2022.128718
To, C., Jang, J., Chen, T., Park, E., Mushajiang, M., De Clercq, D. J. H., Xu, M., Wang, S., Cameron, M. D., Heppner, D. E., Shin, B. Hee, Gero, T. W., Yang, A., Dahlberg, S. E., Wong, K. - K., Eck, M. J., Gray, N. S., and Jänne, P. A. (2019) Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor. Cancer Discov. 9, 926-943
Heppner, D. E., Günther, M., Wittlinger, F., Laufer, S. A., and Eck, M. J. (2020) Structural Basis for EGFR Mutant Inhibition by Trisubstituted Imidazole Inhibitors. J Med Chem. 10.1021/acs.jmedchem.0c00200
Heppner, D. E., Wittlinger, F., Beyett, T. S., Shaurova, T., Urul, D. A., Buckley, B., Pham, C. D., Schaeffner, I. K., Yang, B., Ogboo, B. C., May, E. W., Schaefer, E. M., Eck, M. J., Laufer, S. A., and Hershberger, P. A. (2022) Structural Basis for Inhibition of Mutant EGFR with Lazertinib (YH25448). ACS Med Chem Lett. 13, 1856-1863