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Functional and Structural Characterization of Treatment-Emergent Nirmatrelvir Resistance Mutations at Low Frequencies in the Main Protease (Mpro) Reveals a Unique Evolutionary Route for SARS-CoV-2 to Gain Resistance Deschenes, Natalie M.; Perez-Vargas, Jimena; Zhong, Zoe; Thomas, Merrilee; Kenward, Calem; Mosimann, Wesley A.; Worrall, Liam J.; Waglechner, Nicholas; Li, Angel XinLiu; Maguire, Finlay; Aftanas, Patryk; Smith, Jason R.; Lim, Jared; Young, Robert N.; Cherkasov, Artem; Farooqi, Lubna; Moinuddin, Adnan; Siddiqi, Lina; Malik, Imaan; Lefebvre, Maxime; Paetzel, Mark; Strynadka, Natalie C. J.; Jean, Francois; McGeer, Allison; Kozak, Robert A. Share Save
Characterization of novel small molecule inhibitors of estrogen receptor-activation function 2 (ER-AF2) Foo, Jane; Gentile, Francesco; Massah, Shabnam; Morin, Helene; Singh, Kriti; Lee, Joseph; Smith, Jason; Ban, Fuqiang; Leblanc, Eric; Young, Robert; Strynadka, Natalie; Lallous, Nada; Cherkasov, Artem Share Save
A novel class of broad-spectrum active-site-directed 3C-like protease inhibitors with nanomolar antiviral activity against highly immune-evasive SARS-CoV-2 Omicron subvariants Perez-Vargas, Jimena; Worrall, Liam J.; Olmstead, Andrea D.; Ton, Anh-Tien; Lee, Jaeyong; Villanueva, Ivan; Thompson, Connor A. H.; Dudek, Svenja; Ennis, Siobhan; Smith, Jason R.; Shapira, Tirosh; De Guzman, Joshua; Gang, Shutong; Ban, Fuqiang; Vuckovic, Marija; Bielecki, Michael; Kovacic, Suzana; Kenward, Calem; Hong, Christopher Yee; Gordon, Danielle G.; Levett, Paul N.; Krajden, Mel; Leduc, Richard; Boudreault, Pierre-Luc; Niikura, Masahiro; Paetzel, Mark; Young, Robert N.; Cherkasov, Artem; Strynadka, Natalie C. J.; Jean, Francois Share Save
Large-Scale Virtual Screening for the Discovery of SARS-CoV-2 Papain-like Protease (PLpro) Non-covalent Inhibitors Garland, Olivia; Ton, Anh-Tien; Moradi, Shoeib; Smith, Jason R.; Kovacic, Suzana; Ng, Kurtis; Pandey, Mohit; Ban, Fuqiang; Lee, Jaeyong; Vuckovic, Marija; Worrall, Liam J.; Young, Robert N.; Pantophlet, Ralph; Strynadka, Natalie C. J.; Cherkasov, Artem Share Save
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Development of 2-(5,6,7-Trifluoro-1H-Indol-3-yl)-quinoline-5-carboxamide as a Potent, Selective, and Orally Available Inhibitor of Human Androgen Receptor Targeting Its Binding Function-3 for the Treatment of Castration-Resistant Prostate Cancer Leblanc, Eric; Ban, Fuqiang; Cavga, Ayse Derya; Lawn, Sam; Huang, Chia-Chi Flora; Mohan, Sankar; Chang, Matthew E. K.; Flory, Mark R.; Ghaidi, Fariba; Lingadahalli, Shreyas; Chen, Gang; Yu, Ivan Pak Lok; Morin, Helene; Lallous, Nada; Gleave, Martin E.; Mohammed, Hisham; Young, Robert N.; Rennie, Paul S.; Lack, Nathan A.; Cherkasov, Artem Share Save
E-type prostanoid receptor 4 drives resolution of intestinal inflammation by blocking epithelial necroptosis Patankar, Jay V.; Muller, Tanja M.; Kantham, Srinivas; Acera, Miguel Gonzalez; Mascia, Fabrizio; Scheibe, Kristina; Mahapatro, Mousumi; Heichler, Christina; Yu, Yuqiang; Li, Wei; Ruder, Barbara; Gunther, Claudia; Leppkes, Moritz; Mathew, Mano J.; Wirtz, Stefan; Neufert, Clemens; Kuhl, Anja A.; Paquette, Jay; Jacobson, Kevan; Atreya, Raja; Zundler, Sebastian; Neurath, Markus F.; Young, Robert N.; Becker, Christoph Share Save
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A new quinoline-based chemical probe inhibits the autophagy-related cysteine protease ATG4B Bosc, D.; Vezenkov, L.; Bortnik, S.; An, J.; Xu, J.; Choutka, C.; Hannigan, A. M.; Kovacic, S.; Loo, S.; Clark, P. G. K.; Chen, G.; Guay-Ross, R. N.; Yang, K.; Dragowska, W. H.; Zhang, F.; Go, N. E.; Leung, A.; Honson, N. S.; Pfeifer, T. A.; Gleave, M.; Bally, M.; Jones, S. J.; Gorski, S. M.; Young, R. N. Share Save
Lipophilicity of the Cystic Fibrosis Drug, Ivacaftor (VX-770), and Its Destabilizing Effect on the Major CF-causing Mutation: F508del Chin, Stephanie; Hung, Maurita; Won, Amy; Wu, Yu-Sheng; Ahmadi, Saumel; Yang, Donghe; Elmallah, Salma; Toutah, Krimo; Hamilton, C. Michael; Young, Robert N.; Viirre, Russell D.; Yip, Christopher M.; Bear, Christine E. Share Save
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Targeting Binding Function-3 of the Androgen Receptor Blocks Its Co-Chaperone Interactions, Nuclear Translocation, and Activation Lallous, Nada; Leblanc, Eric; Munuganti, Ravi S. N.; Hassona, Mohamed D. H.; Al Nakouzi, Nader; Awrey, Shannon; Morin, Helene; Roshan-Moniri, Mani; Singh, Kriti; Lawn, Sam; Yamazaki, Takeshi; Adomat, Hans H.; Andre, Christophe; Daugaard, Mads; Young, Robert N.; Guns, Emma S. Tomlinson; Rennie, Paul S.; Cherkasov, Artem Share Save
Precision autophagy: Will the next wave of selective autophagy markers and specific autophagy inhibitors feed clinical pipelines? Lebovitz, Chandra B.; DeVorkin, Lindsay; Bosc, Damien; Rothe, Katharina; Singh, Jagbir; Bally, Marcel; Jiang, Xiaoyan; Young, Robert N.; Lum, Julian J.; Gorski, Sharon M. Share Save
The promise and peril of chemical probes (vol 11, pg 536, 2015) Arrowsmith, Cheryl H.; Audia, James E.; Austin, Christopher; Baell, Jonathan; Bennett, Jonathan; Blagg, Julian; Bountra, Chas; Brennan, Paul E.; Brown, Peter J.; Bunnage, Mark E.; Buser-Doepner, Carolyn; Campbell, Robert M.; Carter, Adrian J.; Cohen, Philip; Copeland, Robert A.; Cravatt, Ben; Dahlin, Jayme L.; Dhanak, Dashyant; Edwards, Aled M.; Frederiksen, Mathias; Frye, Stephen V.; Gray, Nathanael; Grimshaw, Charles E.; Hepworth, David; Howe, Trevor; Huber, Kilian V. M.; Jin, Jian; Knapp, Stefan; Kotz, Joanne D.; Kruger, Ryan G.; Lowe, Derek; Mader, Mary M.; Marsden, Brian; Mueller-Fahrnow, Anke; Mueller, Susanne; O'Hagan, Ronan C.; Overington, John P.; Owen, Dafydd R.; Rosenberg, Saul H.; Ross, Ruth; Roth, Bryan; Schapira, Matthieu; Schreiber, Stuart L.; Shoichet, Brian; Sundstroem, Michael; Superti-Furga, Giulio; Taunton, Jack; Toledo-Sherman, Leticia; Walpole, Chris; Walters, Michael A.; Willson, Timothy M.; Workman, Paul; Young, Robert N.; Zuercher, William J. Share Save
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