Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2
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
Published in Proceedings of the National Academy of Sciences - PNAS (07.05.2013)
Published in Proceedings of the National Academy of Sciences - PNAS (07.05.2013)
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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
Sneeringer, Christopher J., Scott, Margaret Porter, Kuntz, Kevin W., Knutson, Sarah K., Pollock, Roy M., Richon, Victoria M., Copeland, Robert A., Wells, James A.
Published in Proceedings of the National Academy of Sciences - PNAS (07.12.2010)
Published in Proceedings of the National Academy of Sciences - PNAS (07.12.2010)
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Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma
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
Published in Molecular cancer therapeutics (01.04.2014)
Published in Molecular cancer therapeutics (01.04.2014)
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A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells
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
Published in Nature chemical biology (01.11.2012)
Published in Nature chemical biology (01.11.2012)
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Selective Killing of Mixed Lineage Leukemia Cells by a Potent Small-Molecule DOT1L Inhibitor
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.
Published in Cancer cell (12.07.2011)
Published in Cancer cell (12.07.2011)
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Preclinical Evidence of Anti-Tumor Activity Induced by EZH2 Inhibition in Human Models of Synovial Sarcoma
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
Published in PloS one (08.07.2016)
Published in PloS one (08.07.2016)
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PARP7 negatively regulates the type I interferon response in cancer cells and its inhibition triggers antitumor immunity
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
Published in Cancer cell (13.09.2021)
Published in Cancer cell (13.09.2021)
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The Importance of Being Me: Magic Methyls, Methyltransferase Inhibitors, and the Discovery of Tazemetostat
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
Published in Journal of medicinal chemistry (25.02.2016)
Published in Journal of medicinal chemistry (25.02.2016)
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Synergistic Anti-Tumor Activity of EZH2 Inhibitors and Glucocorticoid Receptor Agonists in Models of Germinal Center Non-Hodgkin Lymphomas
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
Published in PloS one (10.12.2014)
Published in PloS one (10.12.2014)
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Identification of a peptide inhibitor for the histone methyltransferase WHSC1
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
Published in PloS one (09.05.2018)
Published in PloS one (09.05.2018)
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A potent and selective PARP14 inhibitor decreases protumor macrophage gene expression and elicits inflammatory responses in tumor explants
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.
Published in Cell chemical biology (19.08.2021)
Published in Cell chemical biology (19.08.2021)
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A687V EZH2 is a gain-of-function mutation found in lymphoma patients
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.
Published in FEBS letters (21.09.2012)
Published in FEBS letters (21.09.2012)
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Small molecule inhibitors and CRISPR/Cas9 mutagenesis demonstrate that SMYD2 and SMYD3 activity are dispensable for autonomous cancer cell proliferation
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
Published in PloS one (01.06.2018)
Published in PloS one (01.06.2018)
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The Y641C mutation of EZH2 alters substrate specificity for histone H3 lysine 27 methylation states
Wigle, Tim J., Knutson, Sarah K., Jin, Lei, Kuntz, Kevin W., Pollock, Roy M., Richon, Victoria M., Copeland, Robert A., Scott, Margaret Porter
Published in FEBS letters (03.10.2011)
Published in FEBS letters (03.10.2011)
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In Vitro and Cellular Probes to Study PARP Enzyme Target Engagement
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
Published in Cell chemical biology (16.07.2020)
Published in Cell chemical biology (16.07.2020)
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Targeted Degradation of PARP14 Using a Heterobifunctional Small Molecule
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.
Published in Chembiochem : a European journal of chemical biology (15.06.2021)
Published in Chembiochem : a European journal of chemical biology (15.06.2021)
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Correction: Preclinical Evidence of Anti-Tumor Activity Induced by EZH2 Inhibition in Human Models of Synovial Sarcoma
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
Published in PloS one (13.01.2017)
Published in PloS one (13.01.2017)
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Conformational Adaptation Drives Potent, Selective and Durable Inhibition of the Human Protein Methyltransferase DOT1L
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.
Published in Chemical biology & drug design (01.12.2012)
Published in Chemical biology & drug design (01.12.2012)
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Journal Article
EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity
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
Published in ACS medicinal chemistry letters (14.05.2015)
Published in ACS medicinal chemistry letters (14.05.2015)
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Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor
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
Published in ACS medicinal chemistry letters (11.02.2016)
Published in ACS medicinal chemistry letters (11.02.2016)
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