Publications

Found 28 results
Filters: Author is Gray, Nathanael S  [Clear All Filters]
2024
Li, Z., Jiang, J., Ficarro, S. B., Beyett, T. S., To, C., Tavares, I., Zhu, Y., Li, J., Eck, M. J., Jänne, P. A., Marto, J. A., Zhang, T., Che, J., and Gray, N. S. (2024) Molecular Bidents with Two Electrophilic Warheads as a New Pharmacological Modality. ACS Cent Sci. 10, 1156-1166
Li, Z., Lu, W., Beyett, T. S., Ficarro, S. B., Jiang, J., Tse, J., Kim, A. Yong- Ju, Marto, J. A., Che, J., Jänne, P. A., Eck, M. J., Zhang, T., and Gray, N. S. (2024) ZNL0325, a Pyrazolopyrimidine-Based Covalent Probe, Demonstrates an Alternative Binding Mode for Kinases. J Med Chem. 67, 2837-2848
2023
Darabedian, N., Ji, W., Fan, M., Lin, S., Seo, H. - S., Vinogradova, E. V., Yaron, T. M., Mills, E. L., Xiao, H., Senkane, K., Huntsman, E. M., Johnson, J. L., Che, J., Cantley, L. C., Cravatt, B. F., Dhe-Paganon, S., Stegmaier, K., Zhang, T., Gray, N. S., and Chouchani, E. T. (2023) Depletion of creatine phosphagen energetics with a covalent creatine kinase inhibitor. Nat Chem Biol. 10.1038/s41589-023-01273-x
2022
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
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
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
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
Teng, M., Jiang, J., Ficarro, S. B., Seo, H. - S., Bae, J. Hyun, Donovan, K. A., Fischer, E. S., Zhang, T., Dhe-Paganon, S., Marto, J. A., and Gray, N. S. (2021) Exploring Ligand-Directed -Acyl--alkylsulfonamide-Based Acylation Chemistry for Potential Targeted Degrader Development. ACS Med Chem Lett. 12, 1302-1307
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
Manz, T. D., Sivakumaren, S. C., Yasgar, A., Hall, M. D., Davis, M. I., Seo, H. - S., Card, J. D., Ficarro, S. B., Shim, H., Marto, J. A., Dhe-Paganon, S., Sasaki, A. T., Boxer, M. B., Simeonov, A., Cantley, L. C., Shen, M., Zhang, T., Ferguson, F. M., and Gray, N. S. (2020) Structure-Activity Relationship Study of Covalent Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors. ACS Med Chem Lett. 11, 346-352
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
Fontán, L., Qiao, Q., Hatcher, J. M., Casalena, G., Us, I., Teater, M., Durant, M., Du, G., Xia, M., Bilchuk, N., Chennamadhavuni, S., Palladino, G., Inghirami, G., Philippar, U., Wu, H., Scott, D. A., Gray, N. S., and Melnick, A. (2018) Specific covalent inhibition of MALT1 paracaspase suppresses B cell lymphoma growth. J Clin Invest. 128, 4397-4412
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

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