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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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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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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Journal Article
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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Potent inhibition of DOT1L as treatment of MLL-fusion leukemia
Daigle, Scott R., Olhava, Edward J., Therkelsen, Carly A., Basavapathruni, Aravind, Jin, Lei, Boriack-Sjodin, P. Ann, Allain, Christina J., Klaus, Christine R., Raimondi, Alejandra, Scott, Margaret Porter, Waters, Nigel J., Chesworth, Richard, Moyer, Mikel P., Copeland, Robert A., Richon, Victoria M., Pollock, Roy M.
Published in Blood (08.08.2013)
Published in Blood (08.08.2013)
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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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Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss
Fedoriw, Andrew, Rajapurkar, Satyajit R., O'Brien, Shane, Gerhart, Sarah V., Mitchell, Lorna H., Adams, Nicholas D., Rioux, Nathalie, Lingaraj, Trupti, Ribich, Scott A., Pappalardi, Melissa B., Shah, Niyant, Laraio, Jenny, Liu, Yan, Butticello, Michael, Carpenter, Chris L., Creasy, Caretha, Korenchuk, Susan, McCabe, Michael T., McHugh, Charles F., Nagarajan, Raman, Wagner, Craig, Zappacosta, Francesca, Annan, Roland, Concha, Nestor O., Thomas, Roberta A., Hart, Timothy K., Smith, Jesse J., Copeland, Robert A., Moyer, Mikel P., Campbell, John, Stickland, Kim, Mills, James, Jacques-O’Hagan, Suzanne, Allain, Christina, Johnston, Danielle, Raimondi, Alejandra, Porter Scott, Margaret, Waters, Nigel, Swinger, Kerren, Boriack-Sjodin, Ann, Riera, Tom, Shapiro, Gideon, Chesworth, Richard, Prinjha, Rabinder K., Kruger, Ryan G., Barbash, Olena, Mohammad, Helai P.
Published in Cancer cell (08.07.2019)
Published in Cancer cell (08.07.2019)
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A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models
Chan-Penebre, Elayne, Kuplast, Kristy G, Majer, Christina R, Boriack-Sjodin, P Ann, Wigle, Tim J, Johnston, L Danielle, Rioux, Nathalie, Munchhof, Michael J, Jin, Lei, Jacques, Suzanne L, West, Kip A, Lingaraj, Trupti, Stickland, Kimberly, Ribich, Scott A, Raimondi, Alejandra, Scott, Margaret Porter, Waters, Nigel J, Pollock, Roy M, Smith, Jesse J, Barbash, Olena, Pappalardi, Melissa, Ho, Thau F, Nurse, Kelvin, Oza, Khyati P, Gallagher, Kathleen T, Kruger, Ryan, Moyer, Mikel P, Copeland, Robert A, Chesworth, Richard, Duncan, Kenneth W
Published in Nature chemical biology (01.06.2015)
Published in Nature chemical biology (01.06.2015)
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Journal Article
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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Journal Article
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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Journal Article
DOT1L inhibitor EPZ-5676 displays synergistic antiproliferative activity in combination with standard of care drugs and hypomethylating agents in MLL-rearranged leukemia cells
Klaus, Christine R, Iwanowicz, Dorothy, Johnston, Danielle, Campbell, Carly A, Smith, Jesse J, Moyer, Mikel P, Copeland, Robert A, Olhava, Edward J, Scott, Margaret Porter, Pollock, Roy M, Daigle, Scott R, Raimondi, Alejandra
Published in The Journal of pharmacology and experimental therapeutics (01.09.2014)
Published in The Journal of pharmacology and experimental therapeutics (01.09.2014)
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Journal Article
Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma
Drew, Allison E., Moradei, Oscar, Jacques, Suzanne L., Rioux, Nathalie, Boriack-Sjodin, Ann P., Allain, Christina, Scott, Margaret Porter, Jin, Lei, Raimondi, Alejandra, Handler, Jessica L., Ott, Heidi M., Kruger, Ryan G., McCabe, Michael T., Sneeringer, Christopher, Riera, Thomas, Shapiro, Gideon, Waters, Nigel J., Mitchell, Lorna H., Duncan, Kenneth W., Moyer, Mikel P., Copeland, Robert A., Smith, Jesse, Chesworth, Richard, Ribich, Scott A.
Published in Scientific reports (21.12.2017)
Published in Scientific reports (21.12.2017)
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Journal Article
Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666
Duncan, Kenneth W, Rioux, Nathalie, Boriack-Sjodin, P. Ann, Munchhof, Michael J, Reiter, Lawrence A, Majer, Christina R, Jin, Lei, Johnston, L. Danielle, Chan-Penebre, Elayne, Kuplast, Kristy G, Porter Scott, Margaret, Pollock, Roy M, Waters, Nigel J, Smith, Jesse J, Moyer, Mikel P, Copeland, Robert A, Chesworth, Richard
Published in ACS medicinal chemistry letters (11.02.2016)
Published in ACS medicinal chemistry letters (11.02.2016)
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Journal Article
Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound
Mitchell, Lorna H., Drew, Allison E., Ribich, Scott A., Rioux, Nathalie, Swinger, Kerren K., Jacques, Suzanne L., Lingaraj, Trupti, Boriack-Sjodin, P. Ann, Waters, Nigel J., Wigle, Tim J., Moradei, Oscar, Jin, Lei, Riera, Tom, Porter-Scott, Margaret, Moyer, Mikel P., Smith, Jesse J., Chesworth, Richard, Copeland, Robert A.
Published in ACS medicinal chemistry letters (11.06.2015)
Published in ACS medicinal chemistry letters (11.06.2015)
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Journal Article
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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Journal Article
Structural Insights into Ternary Complex Formation of Human CARM1 with Various Substrates
Boriack-Sjodin, P. Ann, Jin, Lei, Jacques, Suzanne L, Drew, Allison, Sneeringer, Chris, Scott, Margaret Porter, Moyer, Mikel P, Ribich, Scott, Moradei, Oscar, Copeland, Robert A
Published in ACS chemical biology (18.03.2016)
Published in ACS chemical biology (18.03.2016)
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Abstract 232: Pharmacological and genetic dissection of one carbon pathway provides novel insights into generation, transformation and utilization of one carbon units
Suri, Vipin, Mainolfi, Nello, Friedman, Adam, Moyer, Mikel P., Ducker, Greg, Rabinowitz, Joshua D., Manfredi, Mark
Published in Cancer research (Chicago, Ill.) (15.07.2016)
Published in Cancer research (Chicago, Ill.) (15.07.2016)
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A High-Throughput Mass Spectrometry Assay Coupled with Redox Activity Testing Reduces Artifacts and False Positives in Lysine Demethylase Screening
Wigle, Tim J, Swinger, Kerren K, Campbell, John E, Scholle, Michael D, Sherrill, John, Admirand, Elizabeth A, Boriack-Sjodin, P Ann, Kuntz, Kevin W, Chesworth, Richard, Moyer, Mikel P, Scott, Margaret Porter, Copeland, Robert A
Published in Journal of biomolecular screening (01.07.2015)
Published in Journal of biomolecular screening (01.07.2015)
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Metabolism and disposition of the DOT1L inhibitor, pinometostat (EPZ-5676), in rat, dog and human
Waters, Nigel J., Smith, Sherri A., Olhava, Edward J., Duncan, Kenneth W., Burton, Richard D., O’Neill, James, Rodrigue, Marie-Eve, Pollock, Roy M., Moyer, Mikel P., Chesworth, Richard
Published in Cancer chemotherapy and pharmacology (2016)
Published in Cancer chemotherapy and pharmacology (2016)
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