H3B-8800, an orally available small-molecule splicing modulator, induces lethality in spliceosome-mutant cancers von Seiler, Michael, Yoshimi, Akihide, Darman, Rachel, Chan, Betty, Keaney, Gregg, Thomas, Michael, Agrawal, Anant A, Caleb, Benjamin, Csibi, Alfredo, Sean, Eckley, Fekkes, Peter, Karr, Craig, Klimek, Virginia, Lai, George, Lee, Linda, Kumar, Pavan, Lee, Stanley Chun-Wei, Liu, Xiang, Mackenzie, Crystal, Meeske, Carol, Mizui, Yoshiharu, Padron, Eric, Park, Eunice, Pazolli, Ermira, Peng, Shouyong, Prajapati, Sudeep, Taylor, Justin, Teng, Teng, Wang, John, Warmuth, Markus, Yao, Huilan, Yu, Lihua, Zhu, Ping, Abdel-Wahab, Omar, Smith, Peter G, Buonamici, Silvia

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Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1 von Schoepfer, Joseph, Jahnke, Wolfgang, Berellini, Giuliano, Buonamici, Silvia, Cotesta, Simona, Cowan-Jacob, Sandra W, Dodd, Stephanie, Drueckes, Peter, Fabbro, Doriano, Gabriel, Tobias, Groell, Jean-Marc, Grotzfeld, Robert M, Hassan, A. Quamrul, Henry, Chrystèle, Iyer, Varsha, Jones, Darryl, Lombardo, Franco, Loo, Alice, Manley, Paul W, Pellé, Xavier, Rummel, Gabriele, Salem, Bahaa, Warmuth, Markus, Wylie, Andrew A, Zoller, Thomas, Marzinzik, Andreas L, Furet, Pascal

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The allosteric inhibitor ABL001 enables dual targeting of BCR–ABL1 von Wylie, Andrew A., Schoepfer, Joseph, Jahnke, Wolfgang, Cowan-Jacob, Sandra W., Loo, Alice, Furet, Pascal, Marzinzik, Andreas L., Pelle, Xavier, Donovan, Jerry, Zhu, Wenjing, Buonamici, Silvia, Hassan, A. Quamrul, Lombardo, Franco, Iyer, Varsha, Palmer, Michael, Berellini, Giuliano, Dodd, Stephanie, Thohan, Sanjeev, Bitter, Hans, Branford, Susan, Ross, David M., Hughes, Timothy P., Petruzzelli, Lilli, Vanasse, K. Gary, Warmuth, Markus, Hofmann, Francesco, Keen, Nicholas J., Sellers, William R.

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Loss of function JAK1 mutations occur at high frequency in cancers with microsatellite instability and are suggestive of immune evasion von Albacker, Lee A, Wu, Jeremy, Smith, Peter, Warmuth, Markus, Stephens, Philip J, Zhu, Ping, Yu, Lihua, Chmielecki, Juliann

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Expansion of Bcr-Abl-Positive Leukemic Stem Cells Is Dependent on Hedgehog Pathway Activation von Dierks, Christine, Beigi, Ronak, Guo, Gui-Rong, Zirlik, Katja, Stegert, Mario R., Manley, Paul, Trussell, Christopher, Schmitt-Graeff, Annette, Landwerlin, Klemens, Veelken, Hendrik, Warmuth, Markus

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H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma von Joshi, Jaya Julie, Coffey, Heather, Corcoran, Erik, Tsai, Jennifer, Huang, Chia-Ling, Ichikawa, Kana, Prajapati, Sudeep, Hao, Ming-Hong, Bailey, Suzanna, Wu, Jeremy, Rimkunas, Victoria, Karr, Craig, Subramanian, Vanitha, Kumar, Pavan, MacKenzie, Crystal, Hurley, Raelene, Satoh, Takashi, Yu, Kun, Park, Eunice, Rioux, Nathalie, Kim, Amy, Lai, Weidong G, Yu, Lihua, Zhu, Ping, Buonamici, Silvia, Larsen, Nicholas, Fekkes, Peter, Wang, John, Warmuth, Markus, Reynolds, Dominic J, Smith, Peter G, Selvaraj, Anand

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Cancer-Associated SF3B1 Hotspot Mutations Induce Cryptic 3′ Splice Site Selection through Use of a Different Branch Point von Darman, Rachel B., Seiler, Michael, Agrawal, Anant A., Lim, Kian H., Peng, Shouyong, Aird, Daniel, Bailey, Suzanna L., Bhavsar, Erica B., Chan, Betty, Colla, Simona, Corson, Laura, Feala, Jacob, Fekkes, Peter, Ichikawa, Kana, Keaney, Gregg F., Lee, Linda, Kumar, Pavan, Kunii, Kaiko, MacKenzie, Crystal, Matijevic, Mark, Mizui, Yoshiharu, Myint, Khin, Park, Eun Sun, Puyang, Xiaoling, Selvaraj, Anand, Thomas, Michael P., Tsai, Jennifer, Wang, John Y., Warmuth, Markus, Yang, Hui, Zhu, Ping, Garcia-Manero, Guillermo, Furman, Richard R., Yu, Lihua, Smith, Peter G., Buonamici, Silvia

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Synthesis, Structure–Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5‑Chloro‑N2‑(2-isopropoxy-5-methyl-4-... von Marsilje, Thomas H, Pei, Wei, Chen, Bei, Lu, Wenshuo, Uno, Tetsuo, Jin, Yunho, Jiang, Tao, Kim, Sungjoon, Li, Nanxin, Warmuth, Markus, Sarkisova, Yelena, Sun, Frank, Steffy, Auzon, Pferdekamper, AnneMarie C, Li, Allen G, Joseph, Sean B, Kim, Young, Liu, Bo, Tuntland, Tove, Cui, Xiaoming, Gray, Nathanael S, Steensma, Ruo, Wan, Yongqin, Jiang, Jiqing, Chopiuk, Greg, Li, Jie, Gordon, W. Perry, Richmond, Wendy, Johnson, Kevin, Chang, Jonathan, Groessl, Todd, He, You-Qun, Phimister, Andrew, Aycinena, Alex, Lee, Christian C, Bursulaya, Badry, Karanewsky, Donald S, Seidel, H. Martin, Harris, Jennifer L, Michellys, Pierre-Yves

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Splicing modulators act at the branch point adenosine binding pocket defined by the PHF5A–SF3b complex von Teng, Teng, Tsai, Jennifer HC, Puyang, Xiaoling, Seiler, Michael, Peng, Shouyong, Prajapati, Sudeep, Aird, Daniel, Buonamici, Silvia, Caleb, Benjamin, Chan, Betty, Corson, Laura, Feala, Jacob, Fekkes, Peter, Gerard, Baudouin, Karr, Craig, Korpal, Manav, Liu, Xiang, T. Lowe, Jason, Mizui, Yoshiharu, Palacino, James, Park, Eunice, Smith, Peter G., Subramanian, Vanitha, Wu, Zhenhua Jeremy, Zou, Jian, Yu, Lihua, Chicas, Agustin, Warmuth, Markus, Larsen, Nicholas, Zhu, Ping

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Sensitivity to splicing modulation of BCL2 family genes defines cancer therapeutic strategies for splicing modulators von Aird, Daniel, Teng, Teng, Huang, Chia-Ling, Pazolli, Ermira, Banka, Deepti, Cheung-Ong, Kahlin, Eifert, Cheryl, Furman, Craig, Wu, Zhenhua Jeremy, Seiler, Michael, Buonamici, Silvia, Fekkes, Peter, Karr, Craig, Palacino, James, Park, Eunice, Smith, Peter G., Yu, Lihua, Mizui, Yoshiharu, Warmuth, Markus, Chicas, Agustin, Corson, Laura, Zhu, Ping

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Evasion of immunosurveillance by genomic alterations of PPARγ/RXRα in bladder cancer von Korpal, Manav, Puyang, Xiaoling, Jeremy Wu, Zhenhua, Seiler, Roland, Furman, Craig, Oo, Htoo Zarni, Seiler, Michael, Irwin, Sean, Subramanian, Vanitha, Julie Joshi, Jaya, Wang, Chris K., Rimkunas, Victoria, Tortora, Davide, Yang, Hua, Kumar, Namita, Kuznetsov, Galina, Matijevic, Mark, Chow, Jesse, Kumar, Pavan, Zou, Jian, Feala, Jacob, Corson, Laura, Henry, Ryan, Selvaraj, Anand, Davis, Allison, Bloudoff, Kristjan, Douglas, James, Kiss, Bernhard, Roberts, Morgan, Fazli, Ladan, Black, Peter C., Fekkes, Peter, Smith, Peter G., Warmuth, Markus, Yu, Lihua, Hao, Ming-Hong, Larsen, Nicholas, Daugaard, Mads, Zhu, Ping

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Essential role of stromally induced hedgehog signaling in B-cell malignancies von Dierks, Christine, Grbic, Jovana, Zirlik, Katja, Beigi, Ronak, Englund, Nathan P, Guo, Gui-Rong, Veelken, Hendrik, Engelhardt, Monika, Mertelsmann, Roland, Kelleher, Joseph F, Schultz, Peter, Warmuth, Markus

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Loss of the tumor suppressor Snf5 leads to aberrant activation of the Hedgehog-Gli pathway von Jagani, Zainab, Mora-Blanco, E Lorena, Sansam, Courtney G, McKenna, Elizabeth S, Wilson, Boris, Chen, Dongshu, Klekota, Justin, Tamayo, Pablo, Nguyen, Phuong T L, Tolstorukov, Michael, Park, Peter J, Cho, Yoon-Jae, Hsiao, Kathy, Buonamici, Silvia, Pomeroy, Scott L, Mesirov, Jill P, Ruffner, Heinz, Bouwmeester, Tewis, Luchansky, Sarah J, Murtie, Joshua, Kelleher, Joseph F, Warmuth, Markus, Sellers, William R, Roberts, Charles W M, Dorsch, Marion

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Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK von Galkin, Anna V, Melnick, Jonathan S, Kim, Sungjoon, Hood, Tami L, Li, Nanxin, Li, Lintong, Xia, Gang, Steensma, Ruo, Chopiuk, Greg, Jiang, Jiqing, Wan, Yongqin, Ding, Peter, Liu, Yi, Sun, Fangxian, Schultz, Peter G, Gray, Nathanael S, Warmuth, Markus

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Hedgehog pathway activation in chronic myeloid leukemia: A promise for a novel combination therapeutic approach? von Jagani, Zainab, Dorsch, Marion, Warmuth, Markus

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Protein Kinase C Inhibitor Sotrastaurin Selectively Inhibits the Growth of CD79 Mutant Diffuse Large B-Cell Lymphomas von NAYLOR, Tara L, HUAPING TANG, YAO, Yung-Mae, WARMUTH, Markus, LENZ, Georg, STEGMEIER, Frank, RATSCH, Boris A, ENNS, Andreas, LOO, Alice, LIQING CHEN, LENZ, Peter, WATERS, Nigel J, SCHULER, Walter, DÖRKEN, Bernd

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Maintenance of adenomatous polyposis coli (APC)-mutant colorectal cancer is dependent on Wnt/β-catenin signaling von Scholer-Dahirel, Alix, Schlabach, Michael R, Loo, Alice, Bagdasarian, Linda, Meyer, Ronald, Guo, Ribo, Woolfenden, Steve, Yu, Kristine K, Markovits, Judit, Killary, Karen, Sonkin, Dmitry, Yao, Yung-Mae, Warmuth, Markus, Sellers, William R, Schlegel, Robert, Stegmeier, Frank, Mosher, Rebecca E, McLaughlin, Margaret E

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Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist von Pan, Shifeng, Wu, Xu, Jiang, Jiqing, Gao, Wenqi, Wan, Yongqin, Cheng, Dai, Han, Dong, Liu, Jun, Englund, Nathan P, Wang, Yan, Peukert, Stefan, Miller-Moslin, Karen, Yuan, Jing, Guo, Ribo, Matsumoto, Melissa, Vattay, Anthony, Jiang, Yun, Tsao, Jeffrey, Sun, Fangxian, Pferdekamper, AnneMarie C, Dodd, Stephanie, Tuntland, Tove, Maniara, Wieslawa, Kelleher, Joseph F, Yao, Yung-mae, Warmuth, Markus, Williams, Juliet, Dorsch, Marion

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NAMPT Is the Cellular Target of STF-31-Like Small-Molecule Probes von Adams, Drew J, Ito, Daisuke, Rees, Matthew G, Seashore-Ludlow, Brinton, Puyang, Xiaoling, Ramos, Alex H, Cheah, Jaime H, Clemons, Paul A, Warmuth, Markus, Zhu, Ping, Shamji, Alykhan F, Schreiber, Stuart L

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Trisomy 12 and elevated GLI1 and PTCH1 transcript levels are biomarkers for Hedgehog-inhibitor responsiveness in CLL von Decker, Sarah, Zirlik, Katja, Djebatchie, Lauritte, Hartmann, David, Ihorst, Gabriele, Schmitt-Graeff, Annette, Herchenbach, Dieter, Jumaa, Hassan, Warmuth, Markus, Veelken, Hendrik, Dierks, Christine

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