Publications

Found 18 results
Filters: Author is Gray, Nathanael S  [Clear All Filters]
2021
Wang, E. S., Verano, A. L., Nowak, R. P., J Yuan, C., Donovan, K. A., Eleuteri, N. A., Yue, H., Ngo, K. H., Lizotte, P. H., Gokhale, P. C., Gray, N. S., and Fischer, E. S. (2021) Acute pharmacological degradation of Helios destabilizes regulatory T cells. Nat Chem Biol. 17, 711-717
Dubiella, C., Pinch, B. J., Koikawa, K., Zaidman, D., Poon, E., Manz, T. D., Nabet, B., He, S., Resnick, E., Rogel, A., Langer, E. M., Daniel, C. J., Seo, H. - S., Chen, Y., Adelmant, G., Sharifzadeh, S., Ficarro, S. B., Jamin, Y., da Costa, B. Martins, Zimmerman, M. W., Lian, X., Kibe, S., Kozono, S., Doctor, Z. M., Browne, C. M., Yang, A., Stoler-Barak, L., Shah, R. B., Vangos, N. E., Geffken, E. A., Oren, R., Koide, E., Sidi, S., Shulman, Z., Wang, C., Marto, J. A., Dhe-Paganon, S., Look, T., Zhou, X. Zhen, Lu, K. Ping, Sears, R. C., Chesler, L., Gray, N. S., and London, N. (2021) Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo. Nat Chem Biol. 10.1038/s41589-021-00786-7
2020
Manz, T. D., Sivakumaren, S. Carmen, Ferguson, F. M., Zhang, T., Yasgar, A., Seo, H. - S., Ficarro, S. B., Card, J. D., Shim, H., Miduturu, C. V., Simeonov, A., Shen, M., Marto, J. A., Dhe-Paganon, S., Hall, M. D., Cantley, L. C., and Gray, N. S. (2020) Discovery and Structure-Activity Relationship Study of ()-5-Methylenethiazolidin-4-one Derivatives as Potent and Selective Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors. J Med Chem. 10.1021/acs.jmedchem.0c00227
Pinch, B. J., Doctor, Z. M., Nabet, B., Browne, C. M., Seo, H. - S., Mohardt, M. L., Kozono, S., Lian, X., Manz, T. D., Chun, Y., Kibe, S., Zaidman, D., Daitchman, D., Yeoh, Z. C., Vangos, N. E., Geffken, E. A., Tan, L., Ficarro, S. B., London, N., Marto, J. A., Buratowski, S., Dhe-Paganon, S., Zhou, X. Zhen, Lu, K. Ping, and Gray, N. S. (2020) Identification of a potent and selective covalent Pin1 inhibitor. Nat Chem Biol. 16, 979-987
Faust, T. B., Yoon, H., Nowak, R. P., Donovan, K. A., Li, Z., Cai, Q., Eleuteri, N. A., Zhang, T., Gray, N. S., and Fischer, E. S. (2020) Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15. Nat Chem Biol. 16, 7-14
Sivakumaren, S. Carmen, Shim, H., Zhang, T., Ferguson, F. M., Lundquist, M. R., Browne, C. M., Seo, H. - S., Paddock, M. N., Manz, T. D., Jiang, B., Hao, M. - F., Krishnan, P., Wang, D. G., T Yang, J., Kwiatkowski, N. P., Ficarro, S. B., Cunningham, J. M., Marto, J. A., Dhe-Paganon, S., Cantley, L. C., and Gray, N. S. (2020) Targeting the PI5P4K Lipid Kinase Family in Cancer Using Covalent Inhibitors. Cell Chem Biol. 10.1016/j.chembiol.2020.02.003
2019
Wang, L., Ferrao, R., Li, Q., Hatcher, J. M., Choi, H. Geun, Buhrlage, S. J., Gray, N. S., and Wu, H. (2019) Conformational flexibility and inhibitor binding to unphosphorylated interleukin-1 receptor-associated kinase 4 (IRAK4). J Biol Chem. 10.1074/jbc.RA118.005428
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
Remillard, D., Buckley, D. L., Seo, H. - S., Ferguson, F. M., Dhe-Paganon, S., Bradner, J. E., and Gray, N. S. (2019) Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold. ACS Med Chem Lett. 10, 1443-1449
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
2018
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
Nowak, R. P., DeAngelo, S. L., Buckley, D., He, Z., Donovan, K. A., An, J., Safaee, N., Jedrychowski, M. P., Ponthier, C. M., Ishoey, M., Zhang, T., Mancias, J. D., Gray, N. S., Bradner, J. E., and Fischer, E. S. (2018) Plasticity in binding confers selectivity in ligand-induced protein degradation. Nat Chem Biol. 10.1038/s41589-018-0055-y
Wang, J., Erazo, T., Ferguson, F. M., Buckley, D. L., Gomez, N., Muñoz-Guardiola, P., Diéguez-Martínez, N., Deng, X., Hao, M., Massefski, W., Fedorov, O., Offei-Addo, N. Kwaku, Park, P. M., Dai, L., DiBona, A., Becht, K., Kim, N. Doo, McKeown, M. R., Roberts, J. M., Zhang, J., Sim, T., Alessi, D. R., Bradner, J. E., Lizcano, J. M., Blacklow, S. C., Qi, J., Xu, X., and Gray, N. S. (2018) Structural and Atropisomeric Factors Governing the Selectivity of Pyrimido-benzodiazipinones as Inhibitors of Kinases and Bromodomains. ACS Chem Biol. 10.1021/acschembio.7b00638
Zhou, W., Whiteley, A. T., Mann, C. C. de Olive, Morehouse, B. R., Nowak, R. P., Fischer, E. S., Gray, N. S., Mekalanos, J. J., and Kranzusch, P. J. (2018) Structure of the Human cGAS-DNA Complex Reveals Enhanced Control of Immune Surveillance. Cell. 174, 300-311.e11
2017
Wang, L., Qiao, Q., Ferrao, R., Shen, C., Hatcher, J. M., Buhrlage, S. J., Gray, N. S., and Wu, H. (2017) Crystal structure of human IRAK1. Proc Natl Acad Sci U S A. 10.1073/pnas.1714386114
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
2015
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
2009
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