Publications

Found 1282 results
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2022
Steimbach, R. R., Herbst-Gervasoni, C. J., Lechner, S., Stewart, T. Murray, Klinke, G., Ridinger, J., Géraldy, M. N. E., Tihanyi, G., Foley, J. R., Uhrig, U., Kuster, B., Poschet, G., Casero, R. A., Médard, G., Oehme, I., Christianson, D. W., Gunkel, N., and Miller, A. K. (2022) Aza-SAHA Derivatives Are Selective Histone Deacetylase 10 Chemical Probes That Inhibit Polyamine Deacetylation and Phenocopy HDAC10 Knockout. J Am Chem Soc. 144, 18861-18875
Johnson, A. G., Wein, T., Mayer, M. L., Duncan-Lowey, B., Yirmiya, E., Oppenheimer-Shaanan, Y., Amitai, G., Sorek, R., and Kranzusch, P. J. (2022) Bacterial gasdermins reveal an ancient mechanism of cell death. Science. 375, 221-225
Kelso, S., O'Brien, S., Kurinov, I., Angers, S., and Sicheri, F. (2022) Crystal structure of the CDK11 kinase domain bound to the small-molecule inhibitor OTS964. Structure. 10.1016/j.str.2022.10.003
Kelso, S., O'Brien, S., Kurinov, I., Angers, S., and Sicheri, F. (2022) Crystal structure of the CDK11 kinase domain bound to the small-molecule inhibitor OTS964. Structure. 10.1016/j.str.2022.10.003
Clark, N. E., Katolik, A., Welch, A., Schorl, C., Holloway, S. P., Schuermann, J. P., P Hart, J., Taylor, A. B., Damha, M. J., and Fairbrother, W. G. (2022) Crystal Structure of the RNA Lariat Debranching Enzyme Dbr1 with Hydrolyzed Phosphorothioate RNA Product. Biochemistry. 10.1021/acs.biochem.2c00590
Gannam, Z. T. K., Jamali, H., Kweon, O. Sang, Herrington, J., Shillingford, S. R., Papini, C., Gentzel, E., Lolis, E., Bennett, A. M., Ellman, J. A., and Anderson, K. S. (2022) Defining the structure-activity relationship for a novel class of allosteric MKP5 inhibitors. Eur J Med Chem. 243, 114712
Ketcham, J. M., Haling, J., Khare, S., Bowcut, V., Briere, D. M., Burns, A. C., Gunn, R. J., Ivetac, A., Kuehler, J., Kulyk, S., Laguer, J., J Lawson, D., Moya, K., Nguyen, N., Rahbaek, L., Saechao, B., Smith, C. R., Sudhakar, N., Thomas, N. C., Vegar, L., Vanderpool, D., Wang, X., Yan, L., Olson, P., Christensen, J. G., and Marx, M. A. (2022) Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction. J Med Chem. 65, 9678-9690
Ketcham, J. M., Haling, J., Khare, S., Bowcut, V., Briere, D. M., Burns, A. C., Gunn, R. J., Ivetac, A., Kuehler, J., Kulyk, S., Laguer, J., J Lawson, D., Moya, K., Nguyen, N., Rahbaek, L., Saechao, B., Smith, C. R., Sudhakar, N., Thomas, N. C., Vegar, L., Vanderpool, D., Wang, X., Yan, L., Olson, P., Christensen, J. G., and Marx, M. A. (2022) Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction. J Med Chem. 65, 9678-9690
Ketcham, J. M., Haling, J., Khare, S., Bowcut, V., Briere, D. M., Burns, A. C., Gunn, R. J., Ivetac, A., Kuehler, J., Kulyk, S., Laguer, J., J Lawson, D., Moya, K., Nguyen, N., Rahbaek, L., Saechao, B., Smith, C. R., Sudhakar, N., Thomas, N. C., Vegar, L., Vanderpool, D., Wang, X., Yan, L., Olson, P., Christensen, J. G., and Marx, M. A. (2022) Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction. J Med Chem. 65, 9678-9690
Ketcham, J. M., Haling, J., Khare, S., Bowcut, V., Briere, D. M., Burns, A. C., Gunn, R. J., Ivetac, A., Kuehler, J., Kulyk, S., Laguer, J., J Lawson, D., Moya, K., Nguyen, N., Rahbaek, L., Saechao, B., Smith, C. R., Sudhakar, N., Thomas, N. C., Vegar, L., Vanderpool, D., Wang, X., Yan, L., Olson, P., Christensen, J. G., and Marx, M. A. (2022) Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction. J Med Chem. 65, 9678-9690
Cao, L., Coventry, B., Goreshnik, I., Huang, B., Park, J. Sung, Jude, K. M., Marković, I., Kadam, R. U., Verschueren, K. H. G., Verstraete, K., Walsh, S. Thomas Rus, Bennett, N., Phal, A., Yang, A., Kozodoy, L., DeWitt, M., Picton, L., Miller, L., Strauch, E. - M., DeBouver, N. D., Pires, A., Bera, A. K., Halabiya, S., Hammerson, B., Yang, W., Bernard, S., Stewart, L., Wilson, I. A., Ruohola-Baker, H., Schlessinger, J., Lee, S., Savvides, S. N., K Garcia, C., and Baker, D. (2022) Design of protein binding proteins from target structure alone. Nature. 10.1038/s41586-022-04654-9
Cao, L., Coventry, B., Goreshnik, I., Huang, B., Park, J. Sung, Jude, K. M., Marković, I., Kadam, R. U., Verschueren, K. H. G., Verstraete, K., Walsh, S. Thomas Rus, Bennett, N., Phal, A., Yang, A., Kozodoy, L., DeWitt, M., Picton, L., Miller, L., Strauch, E. - M., DeBouver, N. D., Pires, A., Bera, A. K., Halabiya, S., Hammerson, B., Yang, W., Bernard, S., Stewart, L., Wilson, I. A., Ruohola-Baker, H., Schlessinger, J., Lee, S., Savvides, S. N., K Garcia, C., and Baker, D. (2022) Design of protein binding proteins from target structure alone. Nature. 10.1038/s41586-022-04654-9
Liu, H., Iketani, S., Zask, A., Khanizeman, N., Bednarova, E., Forouhar, F., Fowler, B., Hong, S. Jung, Mohri, H., Nair, M. S., Huang, Y., Tay, N. E. S., Lee, S., Karan, C., Resnick, S. J., Quinn, C., Li, W., Shion, H., Xia, X., Daniels, J. D., Bartolo-Cruz, M., Farina, M., Rajbhandari, P., Jurtschenko, C., Lauber, M. A., McDonald, T., Stokes, M. E., Hurst, B. L., Rovis, T., Chavez, A., Ho, D. D., and Stockwell, B. R. (2022) Development of optimized drug-like small molecule inhibitors of the SARS-CoV-2 3CL protease for treatment of COVID-19. Nat Commun. 13, 1891
Liu, H., Iketani, S., Zask, A., Khanizeman, N., Bednarova, E., Forouhar, F., Fowler, B., Hong, S. Jung, Mohri, H., Nair, M. S., Huang, Y., Tay, N. E. S., Lee, S., Karan, C., Resnick, S. J., Quinn, C., Li, W., Shion, H., Xia, X., Daniels, J. D., Bartolo-Cruz, M., Farina, M., Rajbhandari, P., Jurtschenko, C., Lauber, M. A., McDonald, T., Stokes, M. E., Hurst, B. L., Rovis, T., Chavez, A., Ho, D. D., and Stockwell, B. R. (2022) Development of optimized drug-like small molecule inhibitors of the SARS-CoV-2 3CL protease for treatment of COVID-19. Nat Commun. 13, 1891
Serafim, R. A. M., Santiago, Ada Silva, Schwalm, M. P., Hu, Z., Reis, C. V. Dos, Takarada, J. E., Mezzomo, P., Massirer, K. B., Kudolo, M., Gerstenecker, S., Chaikuad, A., Zender, L., Knapp, S., Laufer, S., Couñago, R. M., and Gehringer, M. (2022) Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor. J Med Chem. 65, 3173-3192
Serafim, R. A. M., Santiago, Ada Silva, Schwalm, M. P., Hu, Z., Reis, C. V. Dos, Takarada, J. E., Mezzomo, P., Massirer, K. B., Kudolo, M., Gerstenecker, S., Chaikuad, A., Zender, L., Knapp, S., Laufer, S., Couñago, R. M., and Gehringer, M. (2022) Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor. J Med Chem. 65, 3173-3192
Chana, C. K., Maisonneuve, P., Posternak, G., Grinberg, N. G. A., Poirson, J., Ona, S. M., Ceccarelli, D. F., Mader, P., St-Cyr, D. J., Pau, V., Kurinov, I., Tang, X., Deng, D., Cui, W., Su, W., Kuai, L., Soll, R., Tyers, M., Röst, H. L., Batey, R. A., Taipale, M., Gingras, A. - C., and Sicheri, F. (2022) Discovery and Structural Characterization of Small Molecule Binders of the Human CTLH E3 Ligase Subunit GID4. J Med Chem. 10.1021/acs.jmedchem.2c00509
Chana, C. K., Maisonneuve, P., Posternak, G., Grinberg, N. G. A., Poirson, J., Ona, S. M., Ceccarelli, D. F., Mader, P., St-Cyr, D. J., Pau, V., Kurinov, I., Tang, X., Deng, D., Cui, W., Su, W., Kuai, L., Soll, R., Tyers, M., Röst, H. L., Batey, R. A., Taipale, M., Gingras, A. - C., and Sicheri, F. (2022) Discovery and Structural Characterization of Small Molecule Binders of the Human CTLH E3 Ligase Subunit GID4. J Med Chem. 10.1021/acs.jmedchem.2c00509
Szychowski, J., Papp, R., Dietrich, E., Liu, B., Vallée, F., Leclaire, M. - E., Fourtounis, J., Martino, G., Perryman, A. L., Pau, V., Yin, S. Yun, Mader, P., Roulston, A., Truchon, J. - F., C Marshall, G., Diallo, M., Duffy, N. M., Stocco, R., Godbout, C., Bonneau-Fortin, A., Kryczka, R., Bhaskaran, V., Mao, D., Orlicky, S., Beaulieu, P., Turcotte, P., Kurinov, I., Sicheri, F., Mamane, Y., Gallant, M., and W Black, C. (2022) Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306. J Med Chem. 10.1021/acs.jmedchem.2c00552
Szychowski, J., Papp, R., Dietrich, E., Liu, B., Vallée, F., Leclaire, M. - E., Fourtounis, J., Martino, G., Perryman, A. L., Pau, V., Yin, S. Yun, Mader, P., Roulston, A., Truchon, J. - F., C Marshall, G., Diallo, M., Duffy, N. M., Stocco, R., Godbout, C., Bonneau-Fortin, A., Kryczka, R., Bhaskaran, V., Mao, D., Orlicky, S., Beaulieu, P., Turcotte, P., Kurinov, I., Sicheri, F., Mamane, Y., Gallant, M., and W Black, C. (2022) Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306. J Med Chem. 10.1021/acs.jmedchem.2c00552
Hanan, E. J., Braun, M. - G., Heald, R. A., MacLeod, C., Chan, C., Clausen, S., Edgar, K. A., Eigenbrot, C., Elliott, R., Endres, N., Friedman, L. S., Gogol, E., Gu, X. - H., Thibodeau, R. Hong, Jackson, P. S., Kiefer, J. R., Knight, J. D., Nannini, M., Narukulla, R., Pace, A., Pang, J., Purkey, H. E., Salphati, L., Sampath, D., Schmidt, S., Sideris, S., Song, K., Sujatha-Bhaskar, S., Ultsch, M., Wallweber, H., Xin, J., Yeap, S. K., Young, A., Zhong, Y., and Staben, S. T. (2022) Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.. J Med Chem. 10.1021/acs.jmedchem.2c01422
Hanan, E. J., Braun, M. - G., Heald, R. A., MacLeod, C., Chan, C., Clausen, S., Edgar, K. A., Eigenbrot, C., Elliott, R., Endres, N., Friedman, L. S., Gogol, E., Gu, X. - H., Thibodeau, R. Hong, Jackson, P. S., Kiefer, J. R., Knight, J. D., Nannini, M., Narukulla, R., Pace, A., Pang, J., Purkey, H. E., Salphati, L., Sampath, D., Schmidt, S., Sideris, S., Song, K., Sujatha-Bhaskar, S., Ultsch, M., Wallweber, H., Xin, J., Yeap, S. K., Young, A., Zhong, Y., and Staben, S. T. (2022) Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.. J Med Chem. 10.1021/acs.jmedchem.2c01422
Park, K. - S., Xiong, Y., Yim, H., Velez, J., Babault, N., Kumar, P., Liu, J., and Jin, J. (2022) Discovery of the First-in-Class G9a/GLP Covalent Inhibitors. J Med Chem. 10.1021/acs.jmedchem.2c00652
Rohaim, A., Vermeulen, B. J. A., Li, J., Kümmerer, F., Napoli, F., Blachowicz, L., Medeiros-Silva, J., Roux, B., and Weingarth, M. (2022) A distinct mechanism of C-type inactivation in the Kv-like KcsA mutant E71V. Nat Commun. 13, 1574
Martyn, G. D., Veggiani, G., Kusebauch, U., Morrone, S. R., Yates, B. P., Singer, A. U., Tong, J., Manczyk, N., Gish, G., Sun, Z., Kurinov, I., Sicheri, F., Moran, M. F., Moritz, R. L., and Sidhu, S. S. (2022) Engineered SH2 Domains for Targeted Phosphoproteomics. ACS Chem Biol. 17, 1472-1484

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