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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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 SMARCA2- and SMARCA4-deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models
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
Published in Molecular cancer therapeutics (01.05.2017)
Published in Molecular cancer therapeutics (01.05.2017)
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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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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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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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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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Regiospecific and Stereoselective Syntheses of (±) Morphine, Codeine, and Thebaine via a Highly Stereocontrolled Intramolecular 4 + 2 Cycloaddition Leading to a Phenanthrofuran System
Stork, Gilbert, Yamashita, Ayako, Adams, Julian, Schulte, Gary R., Chesworth, Richard, Miyazaki, Yoji, Farmer, Jay J.
Published in Journal of the American Chemical Society (19.08.2009)
Published in Journal of the American Chemical Society (19.08.2009)
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Modulation of γ-secretase by EVP-0015962 reduces amyloid deposition and behavioral deficits in Tg2576 mice
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
Published in Molecular neurodegeneration (18.12.2012)
Published in Molecular neurodegeneration (18.12.2012)
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RETRACTED: Biomimetic approach to Galbulimina type I alkaloids
Tchabanenko, Kirill, Chesworth, Richard, Parker, Jeremy S., Anand, Neel K., Russell, Andrew T., Adlington, Robert M., Baldwin, Jack E.
Published in Tetrahedron (01.12.2005)
Published in Tetrahedron (01.12.2005)
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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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Neuronal Store-Operated Calcium Entry Pathway as a Novel Therapeutic Target for Huntington's Disease Treatment
Wu, Jun, Shih, Hsin-Pei, Vigont, Vladimir, Hrdlicka, Lori, Diggins, Len, Singh, Carol, Mahoney, Matt, Chesworth, Richard, Shapiro, Gideon, Zimina, Olga, Chen, Xuesong, Wu, Qingqing, Glushankova, Lyubov, Ahlijanian, Michael, Koenig, Gerhard, Mozhayeva, Galina N., Kaznacheyeva, Elena, Bezprozvanny, Ilya
Published in Chemistry & biology (24.06.2011)
Published in Chemistry & biology (24.06.2011)
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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 acetylcholine receptors
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
Published in Neuropharmacology (01.02.2012)
Published in Neuropharmacology (01.02.2012)
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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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IRAK4 degradation abrogates cytokine release and improves disease endpoints in murine models of IL-33/36- as well as Th17-driven inflammation
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
Published in The Journal of immunology (1950) (01.05.2021)
Published in The Journal of immunology (1950) (01.05.2021)
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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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