Publications

Found 40 results
Filters: Author is Sicheri, Frank  [Clear All Filters]
2022
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
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
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
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
Veggiani, G., Yates, B. P., Martyn, G. D., Manczyk, N., Singer, A. U., Kurinov, I., Sicheri, F., and Sidhu, S. S. (2022) Panel of Engineered Ubiquitin Variants Targeting the Family of Human Ubiquitin Interacting Motifs. ACS Chem Biol. 17, 941-956
2021
Kelso, S., Orlicky, S., Beenstock, J., Ceccarelli, D. F., Kurinov, I., Gish, G., and Sicheri, F. (2021) Bipartite binding of the N terminus of Skp2 to cyclin A. Structure. 10.1016/j.str.2021.04.011
St-Cyr, D., Ceccarelli, D. F., Orlicky, S., van der Sloot, A. M., Tang, X., Kelso, S., Moore, S., James, C., Posternak, G., Coulombe-Huntington, J., Bertomeu, T., Marinier, A., Sicheri, F., and Tyers, M. (2021) Identification and optimization of molecular glue compounds that inhibit a noncovalent E2 enzyme-ubiquitin complex. Sci Adv. 7, eabi5797
2020
Wiechmann, S., Maisonneuve, P., Grebbin, B. Moyo, Hoffmeister, M., Kaulich, M., Clevers, H., Rajalingam, K., Kurinov, I., Farin, H. F., Sicheri, F., and Ernst, A. (2020) Conformation-specific inhibitors of activated Ras GTPases reveal limited Ras dependency of patient-derived cancer organoids. J Biol Chem. 10.1074/jbc.RA119.011025
Posternak, G., Tang, X., Maisonneuve, P., Jin, T., Lavoie, H., Daou, S., Orlicky, S., de Rugy, T. Goullet, Caldwell, L., Chan, K., Aman, A., Prakesch, M., Poda, G., Mader, P., Wong, C., Maier, S., Kitaygorodsky, J., Larsen, B., Colwill, K., Yin, Z., Ceccarelli, D. F., Batey, R. A., Taipale, M., Kurinov, I., Uehling, D., Wrana, J., Durocher, D., Gingras, A. - C., Al-awar, R., Therrien, M., and Sicheri, F. (2020) Functional characterization of a PROTAC directed against BRAF mutant V600E. Nat Chem Biol. 10.1038/s41589-020-0609-7
2019
Ceccarelli, D. F., Ivantsiv, S., Mullin, A. Anne, Coyaud, E., Manczyk, N., Maisonneuve, P., Kurinov, I., Zhao, L., Go, C., Gingras, A. - C., Raught, B., Cordes, S., and Sicheri, F. (2019) FAM105A/OTULINL Is a Pseudodebuiquitinase of the OTU-Class that Localizes to the ER Membrane. Structure. 10.1016/j.str.2019.03.022
Assadieskandar, A., Yu, C., Maisonneuve, P., Kurinov, I., Sicheri, F., and Zhang, C. (2019) Rigidification Dramatically Improves Inhibitor Selectivity for RAF Kinases. ACS Med Chem Lett. 10, 1074-1080
Garg, P., Ceccarelli, D. F., Keszei, A. Fa, Kourinov, I., Sicheri, F., and Sidhu, S. S. (2019) Structural and Functional Analysis of Ubiquitin-based inhibitors that Target the Backsides of E2 Enzymes. J Mol Biol. 10.1016/j.jmb.2019.09.024
Teyra, J., Singer, A. U., Schmitges, F. W., Jaynes, P., Lui, S. Kit Leng, Polyak, M. J., Fodil, N., Krieger, J. R., Tong, J., Schwerdtfeger, C., Brasher, B. B., Ceccarelli, D. F. J., Moffat, J., Sicheri, F., Moran, M. F., Gros, P., Eichhorn, P. J. A., Lenter, M., Boehmelt, G., and Sidhu, S. S. (2019) Structural and Functional Characterization of Ubiquitin Variant Inhibitors of USP15. Structure. 27, 590-605.e5
2018
Assadieskandar, A., Yu, C., Maisonneuve, P., Liu, X., Chen, Y. - C., Prakash, G. K. Surya, Kurinov, I., Sicheri, F., and Zhang, C. (2018) Effects of rigidity on the selectivity of protein kinase inhibitors. Eur J Med Chem. 146, 519-528
Lavoie, H., Sahmi, M., Maisonneuve, P., Marullo, S. A., Thevakumaran, N., Jin, T., Kurinov, I., Sicheri, F., and Therrien, M. (2018) MEK drives BRAF activation through allosteric control of KSR proteins. Nature. 10.1038/nature25478
Xiong, S., Lorenzen, K., Couzens, A. L., Templeton, C. M., Rajendran, D., Mao, D. Y. L., Juang, Y. - C., Chiovitti, D., Kurinov, I., Guettler, S., Gingras, A. - C., and Sicheri, F. (2018) Structural Basis for Auto-Inhibition of the NDR1 Kinase Domain by an Atypically Long Activation Segment. Structure. 26, 1101-1115.e6
Gorelik, M., Manczyk, N., Pavlenco, A., Kurinov, I., Sidhu, S. S., and Sicheri, F. (2018) A Structure-Based Strategy for Engineering Selective Ubiquitin Variant Inhibitors of Skp1-Cul1-F-Box Ubiquitin Ligases. Structure. 10.1016/j.str.2018.06.004
2017
Couzens, A. L., Xiong, S., Knight, J. D. R., Mao, D. Y., Guettler, S., Picaud, S., Kurinov, I., Filippakopoulos, P., Sicheri, F., and Gingras, A. - C. (2017) MOB1 Mediated Phospho-recognition in the Core Mammalian Hippo Pathway. Mol Cell Proteomics. 16, 1098-1110
Xiong, S., Couzens, A. L., Kean, M. J., Mao, D. Y., Guettler, S., Kurinov, I., Gingras, A. - C., and Sicheri, F. (2017) Regulation of Protein Interactions by Mps One Binder (MOB1) Phosphorylation. Mol Cell Proteomics. 16, 1111-1125
2016
Gorelik, M., Orlicky, S., Sartori, M. A., Tang, X., Marcon, E., Kurinov, I., Greenblatt, J. F., Tyers, M., Moffat, J., Sicheri, F., and Sidhu, S. S. (2016) Inhibition of SCF ubiquitin ligases by engineered ubiquitin variants that target the Cul1 binding site on the Skp1-F-box interface. Proc Natl Acad Sci U S A. 113, 3527-32
2015
Zeqiraj, E., Tian, L., Piggott, C. A., Pillon, M. C., Duffy, N. M., Ceccarelli, D. F., Keszei, A. F. A., Lorenzen, K., Kurinov, I., Orlicky, S., Gish, G. D., Heck, A. J. R., Guarné, A., Greenberg, R. A., and Sicheri, F. (2015) Higher-Order Assembly of BRCC36-KIAA0157 Is Required for DUB Activity and Biological Function. Mol Cell. 59, 970-83
2014
Huang, H., Zeqiraj, E., Dong, B., Jha, B. Kant, Duffy, N. M., Orlicky, S., Thevakumaran, N., Talukdar, M., Pillon, M. C., Ceccarelli, D. F., Wan, L. C. K., Juang, Y. - C., Mao, D. Y. L., Gaughan, C., Brinton, M. A., Perelygin, A. A., Kourinov, I., Guarné, A., Silverman, R. H., and Sicheri, F. (2014) Dimeric structure of pseudokinase RNase L bound to 2-5A reveals a basis for interferon-induced antiviral activity. Mol Cell. 53, 221-34
Huang, H., Ceccarelli, D. F., Orlicky, S., St-Cyr, D. J., Ziemba, A., Garg, P., Plamondon, S., Auer, M., Sidhu, S., Marinier, A., Kleiger, G., Tyers, M., and Sicheri, F. (2014) E2 enzyme inhibition by stabilization of a low-affinity interface with ubiquitin. Nat Chem Biol. 10, 156-163
Zeqiraj, E., Tang, X., Hunter, R. W., García-Rocha, M., Judd, A., Deak, M., von Wilamowitz-Moellendorff, A., Kurinov, I., Guinovart, J. J., Tyers, M., Sakamoto, K., and Sicheri, F. (2014) Structural basis for the recruitment of glycogen synthase by glycogenin. Proc Natl Acad Sci U S A. 111, E2831-40

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