Publications

Found 834 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
van Rosenburgh, I. K. van Alde, Lu, D. M., Grant, M. J., Stayrook, S. E., Phadke, M., Walther, Z., Goldberg, S. B., Politi, K., Lemmon, M. A., Ashtekar, K. D., and Tsutsui, Y. (2022) Biochemical and structural basis for differential inhibitor sensitivity of EGFR with distinct exon 19 mutations. Nat Commun. 13, 6791
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
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
Stille, J. K., Tjutrins, J., Wang, G., Venegas, F. A., Hennecker, C., Rueda, A. M., Sharon, I., Blaine, N., Miron, C. E., Pinus, S., Labarre, A., Plescia, J., Patrascu, M. Burai, Zhang, X., Wahba, A. S., Vlaho, D., Huot, M. J., T Schmeing, M., Mittermaier, A. K., and Moitessier, N. (2022) Design, synthesis and in vitro evaluation of novel SARS-CoV-2 3CL covalent inhibitors.. Eur J Med Chem. 229, 114046
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
Zhang, J., Huang, J., Xu, K., Xing, P., Huang, Y., Liu, Z., Tong, L., and Manley, J. L. (2022) DHX15 is involved in SUGP1-mediated RNA missplicing by mutant SF3B1 in cancer. Proc Natl Acad Sci U S A. 119, e2216712119
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
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
Xiong, X., Tian, S., Yang, P., Lebreton, F., Bao, H., Sheng, K., Yin, L., Chen, P., Zhang, J., Qi, W., Ruan, J., Wu, H., Chen, H., Breault, D. T., Wu, H., Earl, A. M., Gilmore, M. S., Abraham, J., and Dong, M. (2022) Emerging enterococcus pore-forming toxins with MHC/HLA-I as receptors. Cell. 185, 1157-1171.e22
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
Chen, W. - H., Kim, J. H., Bu, W., Board, N. L., Tsybovsky, Y., Wang, Y., Hostal, A., Andrews, S. F., Gillespie, R. A., Choe, M., Stephens, T., Yang, E. Sung, Pegu, A., Peterson, C. E., Fisher, B. E., Mascola, J. R., Pittaluga, S., McDermott, A. B., Kanekiyo, M., M Joyce, G., and Cohen, J. I. (2022) Epstein-Barr virus gH/gL has multiple sites of vulnerability for virus neutralization and fusion inhibition. Immunity. 55, 2135-2148.e6
Smith, C. R., Kulyk, S., Ahmad, M. Ud Din, Arkhipova, V., Christensen, J. G., Gunn, R. J., Ivetac, A., Ketcham, J. M., Kuehler, J., J Lawson, D., Thomas, N. C., Wang, X., and Marx, M. A. (2022) Fragment optimization and elaboration strategies - the discovery of two lead series of PRMT5/MTA inhibitors from five fragment hits. RSC Med Chem. 13, 1549-1564
Smith, C. R., Aranda, R., Bobinski, T. P., Briere, D. M., Burns, A. C., Christensen, J. G., Clarine, J., Engstrom, L. D., Gunn, R. J., Ivetac, A., Jean-Baptiste, R., Ketcham, J. M., Kobayashi, M., Kuehler, J., Kulyk, S., J Lawson, D., Moya, K., Olson, P., Rahbaek, L., Thomas, N. C., Wang, X., Waters, L. M., and Marx, M. A. (2022) Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of -Deleted Cancers.. J Med Chem. 10.1021/acs.jmedchem.1c01900
Wicky, B. I. M., Milles, L. F., Courbet, A., Ragotte, R. J., Dauparas, J., Kinfu, E., Tipps, S., Kibler, R. D., Baek, M., DiMaio, F., Li, X., Carter, L., Kang, A., Nguyen, H., Bera, A. K., and Baker, D. (2022) Hallucinating symmetric protein assemblies. Science. 378, 56-61
Sharma, S., Yang, J., Doamekpor, S. K., Grudizen-Nogalska, E., Tong, L., and Kiledjian, M. (2022) Identification of a novel deFADding activity in human, yeast and bacterial 5' to 3' exoribonucleases. Nucleic Acids Res. 50, 8807-8817
Bubenik, M., Mader, P., Mochirian, P., Vallée, F., Clark, J., Truchon, J. - F., Perryman, A. L., Pau, V., Kurinov, I., Zahn, K. E., Leclaire, M. - E., Papp, R., Mathieu, M. - C., Hamel, M., Duffy, N. M., Godbout, C., Casas-Selves, M., Falgueyret, J. - P., Baruah, P. S., Nicolas, O., Stocco, R., Poirier, H., Martino, G., Fortin, A. Bonneau, Roulston, A., Chefson, A., Dorich, S., St-Onge, M., Patel, P., Pellerin, C., Ciblat, S., Pinter, T., Barabé, F., Bakkouri, M. El, Parikh, P., Gervais, C., Sfeir, A., Mamane, Y., Morris, S. J., W Black, C., Sicheri, F., and Gallant, M. (2022) Identification of , an Orally Bioavailable Compound that Inhibits the DNA Polymerase Activity of Polθ.. J Med Chem. 10.1021/acs.jmedchem.2c00998
Lyons, N. S., Bogner, A. N., Tanner, J. J., and Sobrado, P. (2022) Kinetic and Structural Characterization of a Flavin-Dependent Putrescine -Hydroxylase from . Biochemistry. 61, 2607-2620
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
Shankar, S., Ramachandran, S., Tulsian, N., Radhakrishnan, S., Jobichen, C., and Sivaraman, J. (2022) A novel allosteric site employs a conserved inhibition mechanism in human kidney-type glutaminase. FEBS J. 10.1111/febs.16658

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