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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Potent inhibition of DOT1L as treatment of MLL-fusion leukemia von 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.

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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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Selective Killing of SMARCA2- and SMARCA4-deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models von Chan-Penebre, Elayne, Armstrong, Kelli, Drew, Allison, Grassian, Alexandra R, Feldman, Igor, Knutson, Sarah K, Kuplast-Barr, Kristy, Roche, Maria, Campbell, John, Ho, Peter, Copeland, Robert A, Chesworth, Richard, Smith, Jesse J, Keilhack, Heike, Ribich, Scott A

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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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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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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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Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666 von 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

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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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Regiospecific and Stereoselective Syntheses of (±) Morphine, Codeine, and Thebaine via a Highly Stereocontrolled Intramolecular 4 + 2 Cycloaddition Leading to a Phenanthrofuran Sys... von Stork, Gilbert, Yamashita, Ayako, Adams, Julian, Schulte, Gary R., Chesworth, Richard, Miyazaki, Yoji, Farmer, Jay J.

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Modulation of γ-secretase by EVP-0015962 reduces amyloid deposition and behavioral deficits in Tg2576 mice von Rogers, Kathryn, Felsenstein, Kevin M, Hrdlicka, Lori, Tu, Zhiming, Albayya, Faris, Lee, Winnie, Hopp, Sarah, Miller, Mary-Jo, Spaulding, Darcie, Yang, Zhiyong, Hodgdon, Hilliary, Nolan, Scott, Wen, Melody, Costa, Don, Blain, Jean-Francois, Freeman, Emily, De Strooper, Bart, Vulsteke, Veerle, Scrocchi, Louise, Zetterberg, Henrik, Portelius, Erik, Hutter-Paier, Birgit, Havas, Daniel, Ahlijanian, Michael, Flood, Dorothy, Leventhal, Liza, Shapiro, Gideon, Patzke, Holger, Chesworth, Richard, Koenig, Gerhard

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Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss von 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.

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A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models von 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

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EVP-6124, a novel and selective α7 nicotinic acetylcholine receptor partial agonist, improves memory performance by potentiating the acetylcholine response of α7 nicotinic acetylch... von Prickaerts, Jos, van Goethem, Nick P., Chesworth, Richard, Shapiro, Gideon, Boess, Frank G., Methfessel, Christoph, Reneerkens, Olga A.H., Flood, Dorothy G., Hilt, Dana, Gawryl, Maria, Bertrand, Sonia, Bertrand, Daniel, König, Gerhard

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Identification of a CARM1 Inhibitor with Potent In Vitro and In Vivo Activity in Preclinical Models of Multiple Myeloma von 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.

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IRAK4 degradation abrogates cytokine release and improves disease endpoints in murine models of IL-33/36- as well as Th17-driven inflammation von Hubeau, Cedric J, Campbell, Veronica, Lee, Albert, Lurier, Emily, Skouras, Stephanie, Mayo, Michele, Fitzgerald, Michael, Wang, Amy, Chen, Dapeng, Rong, Haojing, Zheng, Xiaozhang, Chesworth, Richard, Gollob, Jared, Mainolfi, Nello, Slavin, Anthony

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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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Conformational-Design-Driven Discovery of EZM0414: A Selective, Potent SETD2 Inhibitor for Clinical Studies von Alford, Joshua S., Lampe, John W., Brach, Dorothy, Chesworth, Richard, Cosmopoulos, Kat, Duncan, Kenneth W., Eckley, Sean T., Kutok, Jeffrey L., Raimondi, Alejandra, Riera, Thomas V., Shook, Brian, Tang, Cuyue, Totman, Jennifer, Farrow, Neil A.

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Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound von 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.

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Identification of a First-in-Class SETD2 Inhibitor That Shows Potent and Selective Anti-Proliferative Activity in t(4;14) Multiple Myeloma: T(4;14) Multiple Myeloma Cells Are Depen... von Thomenius, Michael J, Totman, Jennifer, Cosmopoulos, Kat, Brach, Dorothy, Ci, Lei, Farrow, Neil, Smith, Jesse J, Chesworth, Richard, Duncan, Kenneth W., Tang, Cuyue, Riera, Thomas, Lampe, John

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