A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment von Hyer, Marc L, Milhollen, Michael A, Ciavarri, Jeff, Fleming, Paul, Traore, Tary, Sappal, Darshan, Huck, Jessica, Shi, Judy, Gavin, James, Brownell, Jim, Yang, Yu, Stringer, Bradley, Griffin, Robert, Bruzzese, Frank, Soucy, Teresa, Duffy, Jennifer, Rabino, Claudia, Riceberg, Jessica, Hoar, Kara, Lublinsky, Anya, Menon, Saurabh, Sintchak, Michael, Bump, Nancy, Pulukuri, Sai M, Langston, Steve, Tirrell, Stephen, Kuranda, Mike, Veiby, Petter, Newcomb, John, Li, Ping, Wu, Jing Tao, Powe, Josh, Dick, Lawrence R, Greenspan, Paul, Galvin, Katherine, Manfredi, Mark, Claiborne, Chris, Amidon, Benjamin S, Bence, Neil F

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MAT2A Inhibition Blocks the Growth of MTAP-Deleted Cancer Cells by Reducing PRMT5-Dependent mRNA Splicing and Inducing DNA Damage von Kalev, Peter, Hyer, Marc L., Gross, Stefan, Konteatis, Zenon, Chen, Chi-Chao, Fletcher, Mark, Lein, Max, Aguado-Fraile, Elia, Frank, Victoria, Barnett, Amelia, Mandley, Everton, Goldford, Joshua, Chen, Yue, Sellers, Katie, Hayes, Sebastian, Lizotte, Kate, Quang, Phong, Tuncay, Yesim, Clasquin, Michelle, Peters, Rachel, Weier, Jaclyn, Simone, Eric, Murtie, Joshua, Liu, Wei, Nagaraja, Raj, Dang, Lenny, Sui, Zhihua, Biller, Scott A., Travins, Jeremy, Marks, Kevin M., Marjon, Katya

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Characterization of Alisertib (MLN8237), an Investigational Small-Molecule Inhibitor of Aurora A Kinase Using Novel In Vivo Pharmacodynamic Assays von MANFREDI, Mark G, ECSEDY, Jeffrey A, WYSONG, Deborah R, JANOWICK, David A, HYER, Marc L, LEROY, Patrick J, GERSHMAN, Rachel E, SILVA, Matthew D, GERMANOS, Melissa S, BOLEN, Joseph B, CLAIBORNE, Christopher F, SELLS, Todd B, CHAKRAVARTY, Arijit, SILVERMAN, Lee, MENGKUN ZHANG, HOAR, Kara M, STROUD, Stephen G, WEI CHEN, SHINDE, Vaishali, HUCK, Jessica J

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Preclinical evaluation of the selective small-molecule UBA1 inhibitor, TAK-243, in acute myeloid leukemia von Barghout, Samir H., Patel, Parasvi S., Wang, Xiaoming, Xu, G. Wei, Kavanagh, Simon, Halgas, Ondrej, Zarabi, Sara F., Gronda, Marcela, Hurren, Rose, Jeyaraju, Danny V., MacLean, Neil, Brennan, Shawn, Hyer, Marc L., Berger, Allison, Traore, Tary, Milhollen, Michael, Smith, Adam C., Minden, Mark D., Pai, Emil F., Hakem, Razq, Schimmer, Aaron D.

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Plk1 inhibition causes post-mitotic DNA damage and senescence in a range of human tumor cell lines von Driscoll, Denise L, Chakravarty, Arijit, Bowman, Doug, Shinde, Vaishali, Lasky, Kerri, Shi, Judy, Vos, Tricia, Stringer, Bradley, Amidon, Ben, D'Amore, Natalie, Hyer, Marc L

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Image Analysis Algorithms for Immunohistochemical Assessment of Cell Death Events and Fibrosis in Tissue Sections von Krajewska, Maryla, Smith, Layton H, Rong, Juan, Huang, Xianshu, Hyer, Marc L, Zeps, Nikolajs, Iacopetta, Barry, Linke, Steven P, Olson, Allen H, Reed, John C, Krajewski, Stan

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Discovery of a Potent and Orally Bioavailable Benzolactam-Derived Inhibitor of Polo-Like Kinase 1 (MLN0905) von Duffey, Matthew O, Vos, Tricia J, Adams, Ruth, Alley, Jennifer, Anthony, Justin, Barrett, Cynthia, Bharathan, Indu, Bowman, Douglas, Bump, Nancy J, Chau, Ryan, Cullis, Courtney, Driscoll, Denise L, Elder, Amy, Forsyth, Nancy, Frazer, Jonathan, Guo, Jianping, Guo, Luyi, Hyer, Marc L, Janowick, David, Kulkarni, Bheemashankar, Lai, Su-Jen, Lasky, Kerri, Li, Gang, Li, Jing, Liao, Debra, Little, Jeremy, Peng, Bo, Qian, Mark G, Reynolds, Dominic J, Rezaei, Mansoureh, Scott, Margaret Porter, Sells, Todd B, Shinde, Vaishali, Shi, Qiuju Judy, Sintchak, Michael D, Soucy, Francois, Sprott, Kevin T, Stroud, Stephen G, Nestor, Michelle, Visiers, Irache, Weatherhead, Gabriel, Ye, Yingchun, D’Amore, Natalie

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Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion von Konteatis, Zenon, Travins, Jeremy, Gross, Stefan, Marjon, Katya, Barnett, Amelia, Mandley, Everton, Nicolay, Brandon, Nagaraja, Raj, Chen, Yue, Sun, Yabo, Liu, Zhixiao, Yu, Jie, Ye, Zhixiong, Jiang, Fan, Wei, Wentao, Fang, Cheng, Gao, Yi, Kalev, Peter, Hyer, Marc L, DeLaBarre, Byron, Jin, Lei, Padyana, Anil K, Dang, Lenny, Murtie, Joshua, Biller, Scott A, Sui, Zhihua, Marks, Kevin M

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Leveraging Structure-Based Drug Design to Identify Next-Generation MAT2A Inhibitors, Including Brain-Penetrant and Peripherally Efficacious Leads von Li, Mingzong, Konteatis, Zenon, Nagaraja, Nelamangala, Chen, Yue, Zhou, Shubao, Ma, Guangning, Gross, Stefan, Marjon, Katya, Hyer, Marc L, Mandley, Everton, Lein, Max, Padyana, Anil K, Jin, Lei, Tong, Shuilong, Peters, Rachel, Murtie, Joshua, Travins, Jeremy, Medeiros, Matthew, Liu, Peng, Frank, Victoria, Judd, Evan T, Biller, Scott A, Marks, Kevin M, Sui, Zhihua, Reznik, Samuel K

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Triterpenoids display single agent anti-tumor activity in a transgenic mouse model of chronic lymphocytic leukemia and small B cell lymphoma von Kress, Christina L, Konopleva, Marina, Martínez-García, Vanesa, Krajewska, Maryla, Lefebvre, Sophie, Hyer, Marc L, McQueen, Teresa, Andreeff, Michael, Reed, John C, Zapata, Juan M

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Inhibition of mutant IDH1 promotes cycling of acute myeloid leukemia stem cells von Gruber, Emily, So, Joan, Lewis, Alexander C., Franich, Rheana, Cole, Rachel, Martelotto, Luciano G., Rogers, Amy J., Vidacs, Eva, Fraser, Peter, Stanley, Kym, Jones, Lisa, Trigos, Anna, Thio, Niko, Li, Jason, Nicolay, Brandon, Daigle, Scott, Tron, Adriana E., Hyer, Marc L., Shortt, Jake, Johnstone, Ricky W., Kats, Lev M.

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MLN8054, an inhibitor of Aurora A kinase, induces senescence in human tumor cells both in vitro and in vivo von Huck, Jessica J, Zhang, Mengkun, McDonald, Alice, Bowman, Doug, Hoar, Kara M, Stringer, Bradley, Ecsedy, Jeffery, Manfredi, Mark G, Hyer, Marc L

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Inhibition of D-2HG leads to upregulation of a proinflammatory gene signature in a novel HLA-A2/HLA-DR1 transgenic mouse model of IDH1R132H-expressing glioma von Chuntova, Pavlina, Yamamichi, Akane, Chen, Tiffany, Narayanaswamy, Rohini, Ronseaux, Sebastien, Hudson, Christine, Tron, Adriana E, Hyer, Marc L, Montoya, Megan, Mende, Abigail L, Nejo, Takahide, Downey, Kira M, Diebold, David, Lu, Min, Nicolay, Brandon, Okada, Hideho

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Translational exposure-efficacy modeling to optimize the dose and schedule of taxanes combined with the investigational Aurora A kinase inhibitor MLN8237 (alisertib) von Huck, Jessica J, Zhang, Mengkun, Mettetal, Jerome, Chakravarty, Arijit, Venkatakrishnan, Karthik, Zhou, Xiaofei, Kleinfield, Rob, Hyer, Marc L, Kannan, Karuppiah, Shinde, Vaishali, Dorner, Andy, Manfredi, Mark G, Shyu, Wen Chyi, Ecsedy, Jeffrey A

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Synthetic triterpenoids cooperate with tumor necrosis factor-related apoptosis-inducing ligand to induce apoptosis of breast cancer cells von Hyer, Marc L, Croxton, Rhonda, Krajewska, Maryla, Krajewski, Stanislaw, Kress, Christina L, Lu, Meiling, Suh, Nanjoo, Sporn, Michael B, Cryns, Vincent L, Zapata, Juan M, Reed, John C

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Apoptotic activity and mechanism of 2-cyano-3,12-dioxoolean-1,9-dien-28-oic-acid and related synthetic triterpenoids in prostate cancer von Hyer, Marc L, Shi, Ranxin, Krajewska, Maryla, Meyer, Colin, Lebedeva, Irina V, Fisher, Paul B, Reed, John C

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Downregulation of c-FLIP Sensitizes DU145 Prostate Cancer Cells to Fas-Mediated Apoptosis von Hyer, Marc L., Sudarshan, Sunil, Kim, Youngsoo, Reed, John C., Dong, Jian-yun, Schwartz, David A., Norris, James S.

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Abstract 3719: TAK-243, a small molecule inhibitor of the ubiquitin activating enzyme (UAE), disrupts DNA damage repair and sensitizes tumor cells and xenografts to ionizing radiat... von Milhollen, Michael A., Shi, Judy Qiuju, Traore, Tary, Huck, Jessica, Sappal, Darshan, Iwai, Kenichi, Ohashi, Akihiro, Rabino, Claudia, Duffy, Jennifer A., Lightcap, Eric, Ishii, Yuko, Ciavarri, Jeffrey, Bence, Neil, Berger, Allison J., Hyer, Marc L.

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The FLIP-side of fas signaling von HYER, Marc L, SAMUEL, Temesgen, REED, John C

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MLN0905, a small-molecule plk1 inhibitor, induces antitumor responses in human models of diffuse large B-cell lymphoma von Shi, Judy Quiju, Lasky, Kerri, Shinde, Vaishali, Stringer, Bradley, Qian, Mark G, Liao, Debra, Liu, Ray, Driscoll, Denise, Nestor, Michelle Tighe, Amidon, Benjamin S, Rao, Youlan, Duffey, Matt O, Manfredi, Mark G, Vos, Tricia J, D' Amore, Natalie, Hyer, Marc L

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