Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2 von Knutson, Sarah K., Warholic, Natalie M., Wigle, Tim J., Klaus, Christine R., Allain, Christina J., Raimondi, Alejandra, Scott, Margaret Porter, Chesworth, Richard, Moyer, Mikel P., Copeland, Robert A., Richon, Victoria M., Pollock, Roy M., Kuntz, Kevin W., Keilhack, Heike

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Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas von Sneeringer, Christopher J., Scott, Margaret Porter, Kuntz, Kevin W., Knutson, Sarah K., Pollock, Roy M., Richon, Victoria M., Copeland, Robert A., Wells, James A.

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Preclinical Evidence of Anti-Tumor Activity Induced by EZH2 Inhibition in Human Models of Synovial Sarcoma von Kawano, Satoshi, Grassian, Alexandra R, Tsuda, Masumi, Knutson, Sarah K, Warholic, Natalie M, Kuznetsov, Galina, Xu, Shanqin, Xiao, Yonghong, Pollock, Roy M, Smith, Jesse S, Kuntz, Kevin K, Ribich, Scott, Minoshima, Yukinori, Matsui, Junji, Copeland, Robert A, Tanaka, Shinya, Keilhack, Heike

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Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma von Knutson, Sarah K, Kawano, Satoshi, Minoshima, Yukinori, Warholic, Natalie M, Huang, Kuan-Chun, Xiao, Yonghong, Kadowaki, Tadashi, Uesugi, Mai, Kuznetsov, Galina, Kumar, Namita, Wigle, Tim J, Klaus, Christine R, Allain, Christina J, Raimondi, Alejandra, Waters, Nigel J, Smith, Jesse J, Porter-Scott, Margaret, Chesworth, Richard, Moyer, Mikel P, Copeland, Robert A, Richon, Victoria M, Uenaka, Toshimitsu, Pollock, Roy M, Kuntz, Kevin W, Yokoi, Akira, Keilhack, Heike

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A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells von Knutson, Sarah K, Wigle, Tim J, Warholic, Natalie M, Sneeringer, Christopher J, Allain, Christina J, Klaus, Christine R, Sacks, Joelle D, Raimondi, Alejandra, Majer, Christina R, Song, Jeffrey, Scott, Margaret Porter, Jin, Lei, Smith, Jesse J, Olhava, Edward J, Chesworth, Richard, Moyer, Mikel P, Richon, Victoria M, Copeland, Robert A, Keilhack, Heike, Pollock, Roy M, Kuntz, Kevin W

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PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity von Gozgit, Joseph M., Vasbinder, Melissa M., Abo, Ryan P., Kunii, Kaiko, Kuplast-Barr, Kristy G., Gui, Bin, Lu, Alvin Z., Molina, Jennifer R., Minissale, Elena, Swinger, Kerren K., Wigle, Tim J., Blackwell, Danielle J., Majer, Christina R., Ren, Yue, Niepel, Mario, Varsamis, Zacharenia A., Nayak, Sunaina P., Bamberg, Ellen, Mo, Jan-Rung, Church, W. David, Mady, Ahmed S.A., Song, Jeff, Utley, Luke, Rao, Patricia E., Mitchison, Timothy J., Kuntz, Kevin W., Richon, Victoria M., Keilhack, Heike

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Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor von Daigle, Scott R., Olhava, Edward J., Therkelsen, Carly A., Majer, Christina R., Sneeringer, Christopher J., Song, Jeffrey, Johnston, L. Danielle, Scott, Margaret Porter, Smith, Jesse J., Xiao, Yonghong, Jin, Lei, Kuntz, Kevin W., Chesworth, Richard, Moyer, Mikel P., Bernt, Kathrin M., Tseng, Jen-Chieh, Kung, Andrew L., Armstrong, Scott A., Copeland, Robert A., Richon, Victoria M., Pollock, Roy M.

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The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat von Kuntz, Kevin W, Campbell, John E, Keilhack, Heike, Pollock, Roy M, Knutson, Sarah K, Porter-Scott, Margaret, Richon, Victoria M, Sneeringer, Chris J, Wigle, Tim J, Allain, Christina J, Majer, Christina R, Moyer, Mikel P, Copeland, Robert A, Chesworth, Richard

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Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas von Knutson, Sarah K, Warholic, Natalie M, Johnston, L Danielle, Klaus, Christine R, Wigle, Tim J, Iwanowicz, Dorothy, Littlefield, Bruce A, Porter-Scott, Margaret, Smith, Jesse J, Moyer, Mikel P, Copeland, Robert A, Pollock, Roy M, Kuntz, Kevin W, Raimondi, Alejandra, Keilhack, Heike

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Identification of a peptide inhibitor for the histone methyltransferase WHSC1 von Morrison, Michael J, Boriack-Sjodin, P Ann, Swinger, Kerren K, Wigle, Tim J, Sadalge, Dipti, Kuntz, Kevin W, Scott, Margaret Porter, Janzen, William P, Chesworth, Richard, Duncan, Kenneth W, Harvey, Darren M, Lampe, John W, Mitchell, Lorna H, Copeland, Robert A

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A687V EZH2 is a gain-of-function mutation found in lymphoma patients von Majer, Christina R., Jin, Lei, Scott, Margaret Porter, Knutson, Sarah K., Kuntz, Kevin W., Keilhack, Heike, Smith, Jesse J., Moyer, Mikel P., Richon, Victoria M., Copeland, Robert A., Wigle, Tim J.

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Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation von Thomenius, Michael J, Totman, Jennifer, Harvey, Darren, Mitchell, Lorna H, Riera, Thomas V, Cosmopoulos, Kat, Grassian, Alexandra R, Klaus, Christine, Foley, Megan, Admirand, Elizabeth A, Jahic, Haris, Majer, Christina, Wigle, Tim, Jacques, Suzanne L, Gureasko, Jodi, Brach, Dorothy, Lingaraj, Trupti, West, Kip, Smith, Sherri, Rioux, Nathalie, Waters, Nigel J, Tang, Cuyue, Raimondi, Alejandra, Munchhof, Michael, Mills, James E, Ribich, Scott, Porter Scott, Margaret, Kuntz, Kevin W, Janzen, William P, Moyer, Mikel, Smith, Jesse J, Chesworth, Richard, Copeland, Robert A, Boriack-Sjodin, P Ann

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A potent and selective PARP14 inhibitor decreases protumor macrophage gene expression and elicits inflammatory responses in tumor explants von Schenkel, Laurie B., Molina, Jennifer R., Swinger, Kerren K., Abo, Ryan, Blackwell, Danielle J., Lu, Alvin Z., Cheung, Anne E., Church, W. David, Kunii, Kaiko, Kuplast-Barr, Kristy G., Majer, Christina R., Minissale, Elena, Mo, Jan-Rung, Niepel, Mario, Reik, Christopher, Ren, Yue, Vasbinder, Melissa M., Wigle, Tim J., Richon, Victoria M., Keilhack, Heike, Kuntz, Kevin W.

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The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states von Wigle, Tim J., Knutson, Sarah K., Jin, Lei, Kuntz, Kevin W., Pollock, Roy M., Richon, Victoria M., Copeland, Robert A., Scott, Margaret Porter

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Correction: Preclinical Evidence of Anti-Tumor Activity Induced by EZH2 Inhibition in Human Models of Synovial Sarcoma von Kawano, Satoshi, Grassian, Alexandra R, Tsuda, Masumi, Knutson, Sarah K, Warholic, Natalie M, Kuznetsov, Galina, Xu, Shanqin, Xiao, Yonghong, Pollock, Roy M, Smith, Jesse J, Kuntz, Kevin W, Ribich, Scott, Minoshima, Yukinori, Matsui, Junji, Copeland, Robert A, Tanaka, Shinya, Keilhack, Heike

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In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement von Wigle, Tim J., Blackwell, Danielle J., Schenkel, Laurie B., Ren, Yue, Church, W. David, Desai, Hetvi J., Swinger, Kerren K., Santospago, Andrew G., Majer, Christina R., Lu, Alvin Z., Niepel, Mario, Perl, Nicholas R., Vasbinder, Melissa M., Keilhack, Heike, Kuntz, Kevin W.

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Targeted Degradation of PARP14 Using a Heterobifunctional Small Molecule von Wigle, Tim J., Ren, Yue, Molina, Jennifer R., Blackwell, Danielle J., Schenkel, Laurie B., Swinger, Kerren K., Kuplast‐Barr, Kristy, Majer, Christina R., Church, W. David, Lu, Alvin Z., Mo, Jason, Abo, Ryan, Cheung, Anne, Dorsey, Bryan W., Niepel, Mario, Perl, Nicholas R., Vasbinder, Melissa M., Keilhack, Heike, Kuntz, Kevin W.

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Conformational Adaptation Drives Potent, Selective and Durable Inhibition of the Human Protein Methyltransferase DOT1L von Basavapathruni, Aravind, Jin, Lei, Daigle, Scott R., Majer, Christina R. A., Therkelsen, Carly A., Wigle, Tim J., Kuntz, Kevin W., Chesworth, Richard, Pollock, Roy M., Scott, Margaret P., Moyer, Mikel P., Richon, Victoria M., Copeland, Robert A., Olhava, Edward J.

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EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity von Campbell, John E, Kuntz, Kevin W, Knutson, Sarah K, Warholic, Natalie M, Keilhack, Heike, Wigle, Tim J, Raimondi, Alejandra, Klaus, Christine R, Rioux, Nathalie, Yokoi, Akira, Kawano, Satoshi, Minoshima, Yukinori, Choi, Hyeong-Wook, Porter Scott, Margaret, Waters, Nigel J, Smith, Jesse J, Chesworth, Richard, Moyer, Mikel P, Copeland, Robert A

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Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor von Mitchell, Lorna H, Boriack-Sjodin, P. Ann, Smith, Sherri, Thomenius, Michael, Rioux, Nathalie, Munchhof, Michael, Mills, James E, Klaus, Christine, Totman, Jennifer, Riera, Thomas V, Raimondi, Alejandra, Jacques, Suzanne L, West, Kip, Foley, Megan, Waters, Nigel J, Kuntz, Kevin W, Wigle, Tim J, Scott, Margaret Porter, Copeland, Robert A, Smith, Jesse J, Chesworth, Richard

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