USP28 deletion and small-molecule inhibition destabilizes c-MYC and elicits regression of squamous cell lung carcinoma von Ruiz, E Josue, Pinto-Fernandez, Adan, Turnbull, Andrew P, Lan, Linxiang, Charlton, Thomas M, Scott, Hannah C, Damianou, Andreas, Vere, George, Riising, Eva M, Da Costa, Clive, Krajewski, Wojciech W, Guerin, David, Kearns, Jeffrey D, Ioannidis, Stephanos, Katz, Marie, McKinnon, Crystal, O'Connell, Jonathan, Moncaut, Natalia, Rosewell, Ian, Nye, Emma, Jones, Neil, Heride, Claire, Gersch, Malte, Wu, Min, Dinsmore, Christopher J, Hammonds, Tim R, Kim, Sunkyu, Komander, David, Urbe, Sylvie, Clague, Michael J, Kessler, Benedikt M, Behrens, Axel

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The JAK2 Inhibitor AZD1480 Potently Blocks Stat3 Signaling and Oncogenesis in Solid Tumors von Hedvat, Michael, Huszar, Dennis, Herrmann, Andreas, Gozgit, Joseph M., Schroeder, Anne, Sheehy, Adam, Buettner, Ralf, Proia, David, Kowolik, Claudia M., Xin, Hong, Armstrong, Brian, Bebernitz, Geraldine, Weng, Shaobu, Wang, Lin, Ye, Minwei, McEachern, Kristen, Chen, Huawei, Morosini, Deborah, Bell, Kirsten, Alimzhanov, Marat, Ioannidis, Stephanos, McCoon, Patricia, Cao, Zhu A., Yu, Hua, Jove, Richard, Zinda, Michael

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AZD4320, A Dual Inhibitor of Bcl-2 and Bcl-xL, Induces Tumor Regression in Hematologic Cancer Models without Dose-limiting Thrombocytopenia von Balachander, Srividya B., Criscione, Steven W., Byth, Kate F., Cidado, Justin, Adam, Ammar, Lewis, Paula, Macintyre, Terry, Wen, Shenghua, Lawson, Deborah, Burke, Kathleen, Lubinski, Tristan, Tyner, Jeffrey W., Kurtz, Stephen E., McWeeney, Shannon K., Varnes, Jeffrey, Diebold, R. Bruce, Gero, Thomas, Ioannidis, Stephanos, Hennessy, Edward J., McCoull, William, Saeh, Jamal C., Tabatabai, Areya, Tavana, Omid, Su, Nancy, Schuller, Alwin, Garnett, Mathew J., Jaaks, Patricia, Coker, Elizabeth A., Gregory, Gareth P., Newbold, Andrea, Johnstone, Ricky W., Gangl, Eric, Wild, Martin, Zinda, Michael, Secrist, J. Paul, Davies, Barry R., Fawell, Stephen E., Gibbons, Francis D.

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The deubiquitylase USP9X controls ribosomal stalling von Clancy, Anne, Heride, Claire, Pinto-Fernández, Adán, Elcocks, Hannah, Kallinos, Andreas, Kayser-Bricker, Katherine J, Wang, Weiping, Smith, Victoria, Davis, Simon, Fessler, Shawn, McKinnon, Crystal, Katz, Marie, Hammonds, Tim, Jones, Neil P, O'Connell, Jonathan, Follows, Bruce, Mischke, Steven, Caravella, Justin A, Ioannidis, Stephanos, Dinsmore, Christopher, Kim, Sunkyu, Behrens, Axel, Komander, David, Kessler, Benedikt M, Urbé, Sylvie, Clague, Michael J

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USP30 sets a trigger threshold for PINK1-PARKIN amplification of mitochondrial ubiquitylation von Rusilowicz-Jones, Emma V, Jardine, Jane, Kallinos, Andreas, Pinto-Fernandez, Adan, Guenther, Franziska, Giurrandino, Mariacarmela, Barone, Francesco G, McCarron, Katy, Burke, Christopher J, Murad, Alejandro, Martinez, Aitor, Marcassa, Elena, Gersch, Malte, Buckmelter, Alexandre J, Kayser-Bricker, Katherine J, Lamoliatte, Frederic, Gajbhiye, Akshada, Davis, Simon, Scott, Hannah C, Murphy, Emma, England, Katherine, Mortiboys, Heather, Komander, David, Trost, Matthias, Kessler, Benedikt M, Ioannidis, Stephanos, Ahlijanian, Michael K, Urbé, Sylvie, Clague, Michael J

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Discovery of Checkpoint Kinase Inhibitor (S)-5-(3-Fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by Structure-Based Design and Optimization of Thiophene... von Oza, Vibha, Ashwell, Susan, Almeida, Lynsie, Brassil, Patrick, Breed, Jason, Deng, Chun, Gero, Thomas, Grondine, Michael, Horn, Candice, Ioannidis, Stephanos, Liu, Dongfang, Lyne, Paul, Newcombe, Nicholas, Pass, Martin, Read, Jon, Ready, Shannon, Rowsell, Siân, Su, Mei, Toader, Dorin, Vasbinder, Melissa, Yu, Dingwei, Yu, Yan, Xue, Yafeng, Zabludoff, Sonya, Janetka, James

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Effects of the JAK2 Inhibitor, AZ960, on Pim/BAD/BCL-xL Survival Signaling in the Human JAK2 V617F Cell Line SET-2 von Gozgit, Joseph M., Bebernitz, Geraldine, Patil, Pankaj, Ye, Minwei, Parmentier, Julie, Wu, Jiaquan, Su, Nancy, Wang, Tao, Ioannidis, Stephanos, Davies, Audrey, Huszar, Dennis, Zinda, Michael

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Pyrimidinone Nicotinamide Mimetics as Selective Tankyrase and Wnt Pathway Inhibitors Suitable for in Vivo Pharmacology von Johannes, Jeffrey W, Almeida, Lynsie, Barlaam, Bernard, Boriack-Sjodin, P. Ann, Casella, Robert, Croft, Rosemary A, Dishington, Allan P, Gingipalli, Lakshmaiah, Gu, Chungang, Hawkins, Janet L, Holmes, Jane L, Howard, Tina, Huang, Jian, Ioannidis, Stephanos, Kazmirski, Steven, Lamb, Michelle L, McGuire, Thomas M, Moore, Jane E, Ogg, Derek, Patel, Anil, Pike, Kurt G, Pontz, Timothy, Robb, Graeme R, Su, Nancy, Wang, Haiyun, Wu, Xiaoyun, Zhang, Hai-Jun, Zhang, Yue, Zheng, Xiaolan, Wang, Tao

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Towards the next generation of dual Bcl-2/Bcl-xL inhibitors von Varnes, Jeffrey G., Gero, Thomas, Huang, Shan, Diebold, R. Bruce, Ogoe, Claude, Grover, Paul T., Su, Mei, Mukherjee, Prasenjit, Saeh, Jamal Carlos, MacIntyre, Terry, Repik, Galina, Dillman, Keith, Byth, Kate, Russell, Daniel John, Ioannidis, Stephanos

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Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors von Janetka, James W., Almeida, Lynsie, Ashwell, Susan, Brassil, Patrick J., Daly, Kevin, Deng, Chun, Gero, Thomas, Glynn, Roberta E., Horn, Candice L., Ioannidis, Stephanos, Lyne, Paul, Newcombe, Nicholas J., Oza, Vibha B., Pass, Martin, Springer, Stephanie K., Su, Mei, Toader, Dorin, Vasbinder, Melissa M., Yu, Dingwei, Yu, Yan, Zabludoff, Sonya D.

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Molecular basis of USP7 inhibition by selective small-molecule inhibitors von Turnbull, Andrew P., Ioannidis, Stephanos, Krajewski, Wojciech W., Pinto-Fernandez, Adan, Heride, Claire, Martin, Agnes C. L., Tonkin, Louise M., Townsend, Elizabeth C., Buker, Shane M., Lancia, David R., Caravella, Justin A., Toms, Angela V., Charlton, Thomas M., Lahdenranta, Johanna, Wilker, Erik, Follows, Bruce C., Evans, Nicola J., Stead, Lucy, Alli, Cristina, Zarayskiy, Vladislav V., Talbot, Adam C., Buckmelter, Alexandre J., Wang, Minghua, McKinnon, Crystal L., Saab, Fabienne, McGouran, Joanna F., Century, Hannah, Gersch, Malte, Pittman, Marc S., Marshall, C. Gary, Raynham, Tony M., Simcox, Mary, Stewart, Lorna M. D., McLoughlin, Sheila B., Escobedo, Jaime A., Bair, Kenneth W., Dinsmore, Christopher J., Hammonds, Tim R., Kim, Sunkyu, Urbé, Sylvie, Clague, Michael J., Kessler, Benedikt M., Komander, David

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Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway von Ioannidis, Stephanos, Lamb, Michelle L, Wang, Tao, Almeida, Lynsie, Block, Michael H, Davies, Audrey M, Peng, Bo, Su, Mei, Zhang, Hai-Jun, Hoffmann, Ethan, Rivard, Caroline, Green, Isabelle, Howard, Tina, Pollard, Hannah, Read, Jon, Alimzhanov, Marat, Bebernitz, Geraldine, Bell, Kirsten, Ye, Minwei, Huszar, Dennis, Zinda, Michael

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Abstract 311: AZD4320 is a potent, dual Bcl-2/xLinhibitor that rapidly induces apoptosis in preclinical hematologic tumor models von Cidado, Justin, Secrist, J Paul, Gibbons, Francis D., Hennessy, Edward J., Ioannidis, Stephanos, Clark, Edwin A.

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Small Molecule Inhibition of CPS1 Activity through an Allosteric Pocket von Yao, Shihua, Nguyen, Tuong-Vi, Rolfe, Alan, Agrawal, Anant A., Ke, Jiyuan, Peng, Shouyong, Colombo, Federico, Yu, Sean, Bouchard, Patricia, Wu, Jiayi, Huang, Kuan-Chun, Bao, Xingfeng, Omoto, Kiyoyuki, Selvaraj, Anand, Yu, Lihua, Ioannidis, Stephanos, Vaillancourt, Frédéric H., Zhu, Ping, Larsen, Nicholas A., Bolduc, David M.

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Discovery of 1-Methyl-1 H -imidazole Derivatives as Potent Jak2 Inhibitors von Su, Qibin, Ioannidis, Stephanos, Chuaqui, Claudio, Almeida, Lynsie, Alimzhanov, Marat, Bebernitz, Geraldine, Bell, Kirsten, Block, Michael, Howard, Tina, Huang, Shan, Huszar, Dennis, Read, Jon A., Rivard Costa, Caroline, Shi, Jie, Su, Mei, Ye, Minwei, Zinda, Michael

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Abstract 2334: Discovery of selective inhibitors of carbamoyl phosphate synthetase I (CPS1) to modulate cancer relevant metabolic pathways von Yao, Shihua, Nguyen, Tuong-Vi, Rolfe, Alan, Agrawal, Anant A., Ke, Jiyuan, Peng, Shouyong, Colombo, Federico, Yu, Sean, Bouchard, Patricia, Wu, Jiayi, Huang, Kuan-Chun, Bao, Xingfeng, Omoto, Kiyoyuki, Selvaraj, Anand, Yu, Lihua, Ioannidis, Stephanos, Vaillancourt, Frédéric H., Zhu, Ping, Larsen, Nicholas A., Bolduc, David M.

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Discovery of 5-Chloro-N 2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N 4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a Novel Inhibitor of the Jak/Stat Pathway von Ioannidis, Stephanos, Lamb, Michelle L, Wang, Tao, Almeida, Lynsie, Block, Michael H, Davies, Audrey M, Peng, Bo, Su, Mei, Zhang, Hai-Jun, Hoffmann, Ethan, Rivard, Caroline, Green, Isabelle, Howard, Tina, Pollard, Hannah, Read, Jon, Alimzhanov, Marat, Bebernitz, Geraldine, Bell, Kirsten, Ye, Minwei, Huszar, Dennis, Zinda, Michael

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Adventures in Scaffold Morphing: Discovery of Fused Ring Heterocyclic Checkpoint Kinase 1 (CHK1) Inhibitors von Yang, Bin, Vasbinder, Melissa M, Hird, Alexander W, Su, Qibin, Wang, Haixia, Yu, Yan, Toader, Dorin, Lyne, Paul D, Read, Jon A, Breed, Jason, Ioannidis, Stephanos, Deng, Chun, Grondine, Michael, DeGrace, Nancy, Whitston, David, Brassil, Patrick, Janetka, James W

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Discovery of 1‑Methyl‑1H‑imidazole Derivatives as Potent Jak2 Inhibitors von Su, Qibin, Ioannidis, Stephanos, Chuaqui, Claudio, Almeida, Lynsie, Alimzhanov, Marat, Bebernitz, Geraldine, Bell, Kirsten, Block, Michael, Howard, Tina, Huang, Shan, Huszar, Dennis, Read, Jon A, Rivard Costa, Caroline, Shi, Jie, Su, Mei, Ye, Minwei, Zinda, Michael

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Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering von Johannes, Jeffrey W., Almeida, Lynsie, Daly, Kevin, Ferguson, Andrew D., Grosskurth, Shaun E., Guan, Huiping, Howard, Tina, Ioannidis, Stephanos, Kazmirski, Steven, Lamb, Michelle L., Larsen, Nicholas A., Lyne, Paul D., Mikule, Keith, Ogoe, Claude, Peng, Bo, Petteruti, Philip, Read, Jon A., Su, Nancy, Sylvester, Mark, Throner, Scott, Wang, Wenxian, Wang, Xin, Wu, Jiaquan, Ye, Qing, Yu, Yan, Zheng, Xiaolan, Scott, David A.

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