EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations von McCabe, Michael T., Ott, Heidi M., Ganji, Gopinath, Korenchuk, Susan, Thompson, Christine, Van Aller, Glenn S., Liu, Yan, Graves, Alan P., III, Anthony Della Pietra, Diaz, Elsie, LaFrance, Louis V., Mellinger, Mark, Duquenne, Celine, Tian, Xinrong, Kruger, Ryan G., McHugh, Charles F., Brandt, Martin, Miller, William H., Dhanak, Dashyant, Verma, Sharad K., Tummino, Peter J., Creasy, Caretha L.

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Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2 von Verma, Sharad K, Tian, Xinrong, LaFrance, Louis V, Duquenne, Céline, Suarez, Dominic P, Newlander, Kenneth A, Romeril, Stuart P, Burgess, Joelle L, Grant, Seth W, Brackley, James A, Graves, Alan P, Scherzer, Daryl A, Shu, Art, Thompson, Christine, Ott, Heidi M, Aller, Glenn S. Van, Machutta, Carl A, Diaz, Elsie, Jiang, Yong, Johnson, Neil W, Knight, Steven D, Kruger, Ryan G, McCabe, Michael T, Dhanak, Dashyant, Tummino, Peter J, Creasy, Caretha L, Miller, William H

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Identification of 4-(2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a Novel Inhibitor... von Heerding, Dirk A, Rhodes, Nelson, Leber, Jack D, Clark, Tammy J, Keenan, Richard M, Lafrance, Louis V, Li, Mei, Safonov, Igor G, Takata, Dennis T, Venslavsky, Joseph W, Yamashita, Dennis S, Choudhry, Anthony E, Copeland, Robert A, Lai, Zhihong, Schaber, Michael D, Tummino, Peter J, Strum, Susan L, Wood, Edgar R, Duckett, Derek R, Eberwein, Derek, Knick, Victoria B, Lansing, Timothy J, McConnell, Randy T, Zhang, ShuYun, Minthorn, Elisabeth A, Concha, Nestor O, Warren, Gregory L, Kumar, Rakesh

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Discovery and Cocrystal Structure of Benzodiazepinedione HDM2 Antagonists That Activate p53 in Cells von Grasberger, Bruce L, Lu, Tianbao, Schubert, Carsten, Parks, Daniel J, Carver, Theodore E, Koblish, Holly K, Cummings, Maxwell D, LaFrance, Louis V, Milkiewicz, Karen L, Calvo, Raul R, Maguire, Diane, Lattanze, Jennifer, Franks, Carol F, Zhao, Shuyuan, Ramachandren, Kannan, Bylebyl, Gwendolyn R, Zhang, Marie, Manthey, Carl L, Petrella, Eugene C, Pantoliano, Michael W, Deckman, Ingrid C, Spurlino, John C, Maroney, Anna C, Tomczuk, Bruce E, Molloy, Christopher J, Bone, Roger F

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Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation in vitro and sensitize tumors to doxorubicin in vivo von Koblish, Holly K, Zhao, Shuyuan, Franks, Carol F, Donatelli, Robert R, Tominovich, Rose M, LaFrance, Louis V, Leonard, Kristi A, Gushue, Joan M, Parks, Daniel J, Calvo, Raul R, Milkiewicz, Karen L, Marugán, Juan José, Raboisson, Pierre, Cummings, Maxwell D, Grasberger, Bruce L, Johnson, Dana L, Lu, Tianbao, Molloy, Christopher J, Maroney, Anna C

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1,4-Benzodiazepine-2,5-diones as small molecule antagonists of the HDM2–p53 interaction: discovery and SAR von Parks, Daniel J., LaFrance, Louis V., Calvo, Raul R., Milkiewicz, Karen L., Gupta, Varsha, Lattanze, Jennifer, Ramachandren, Kannan, Carver, Theodore E., Petrella, Eugene C., Cummings, Maxwell D., Maguire, Diane, Grasberger, Bruce L., Lu, Tianbao

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Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein–protein interaction through structure-based drug design von Parks, Daniel J., LaFrance, Louis V., Calvo, Raul R., Milkiewicz, Karen L., José Marugán, Juan, Raboisson, Pierre, Schubert, Carsten, Koblish, Holly K., Zhao, Shuyuan, Franks, Carol F., Lattanze, Jennifer, Carver, Theodore E., Cummings, Maxwell D., Maguire, Diane, Grasberger, Bruce L., Maroney, Anna C., Lu, Tianbao

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Substituted 1,4-Benzodiazepine-2,5-diones as α-Helix Mimetic Antagonists of the HDM2-p53 Protein-Protein Interaction von Cummings, Maxwell D., Schubert, Carsten, Parks, Daniel J., Calvo, Raul R., LaFrance, Louis V., Lattanze, Jennifer, Milkiewicz, Karen L., Lu, Tianbao

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A facile method for the synthesis of substituted pyrazolo[3,4- c]pyridines von Verma, Sharad K., LaFrance, Louis V.

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Discovery of Proline-Based p300/CBP Inhibitors Using DNA-Encoded Library Technology in Combination with High-Throughput Screening von Tian, Xinrong, Suarez, Dominic, Thomson, Douglas, Li, William, King, Elizabeth A., LaFrance, Louis, Boehm, Jeffrey, Barton, Linda, Di Marco, Christina, Martyr, Cuthbert, Thalji, Reema, Medina, Jesus, Knight, Steven, Heerding, Dirk, Gao, Enoch, Nartey, Eldridge, Cecconie, Ted, Nixon, Christopher, Zhang, Guofeng, Berrodin, Thomas J., Phelps, Christopher, Patel, Amish, Bai, Xiaopeng, Lind, Ken, Prabhu, Ninad, Messer, Jeffrey, Zhu, Zhengrong, Shewchuk, Lisa, Reid, Rob, Graves, Alan P., McHugh, Charles, Mangatt, Biju

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Cell-Based Drug Discovery: Identification and Optimization of Small Molecules that Reduce c‑MYC Protein Levels in Cells von Medina, Jesús R, Tian, Xinrong, Li, William H, Suarez, Dominic, Mack, James F, LaFrance, Louis, Martyr, Cuthbert, Brackley, James, Di Marco, Christina, Rivero, Ralph, Heerding, Dirk A, McHugh, Charles, Minthorn, Elisabeth, Bhaskar, Aishwarya, Rubin, Jacob, Butticello, Michael, Carpenter, Christopher, Nartey, Eldridge N, Berrodin, Thomas J, Kallal, Lorena A, Mangatt, Biju

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Development and Validation of Reagents and Assays for EZH2 Peptide and Nucleosome High-Throughput Screens von Diaz, Elsie, Machutta, Carl A., Chen, Stephanie, Jiang, Yong, Nixon, Christopher, Hofmann, Glenn, Key, Danielle, Sweitzer, Sharon, Patel, Mehul, Wu, Zining, Creasy, Caretha L., Kruger, Ryan G., LaFrance, Louis, Verma, Sharad K., Pappalardi, Melissa B., Le, Baochau, Van Aller, Glenn S., McCabe, Michael T., Tummino, Peter J., Pope, Andrew J., Thrall, Sara H., Schwartz, Benjamin, Brandt, Martin

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Abstract 5379: A potent EZH2 inhibitor exhibits long residence time and anti-tumor activity von Ott, Heidi, van Aller, Glenn, Ward, Jessica, Le, BaoChau, Rominger, Cynthia, Foley, James, Korenchuk, Susan, McHugh, Charles, Butticello, Michael, Blackledge, Charles, Brackley, James, Burgess, Joelle, Duquenne, Celine, Johnson, Neil, Kasparec, Jiri, LaFrance, Louis, Li, Mei, McNulty, Kenneth, Newlander, Kenneth, Romeril, Stuart, Schmidt, Stanley, Schulz, Mark, Su, Dai-Shi, Suarez, Dominic, Tian, Xinrong, Carpenter, Christopher, Luengo, Juan, Kruger, Ryan, Knight, Steven, McCabe, Michael T.

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Abstract 3260: Identification and synthesis of benzimidazole carboxamides as potent inhibitors of focal adhesion kinase (FAK) von Verma, Sharad K., Leber, Jack D., LaFrance, Louis V., Li, Mei, Duquenne, Celine, Cui, Guanglei, Miller, William H.

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Abstract 4700: A novel selective EZH2 inhibitor exhibits anti-tumor activity in lymphoma with EZH2 activating mutations von Creasy, Caretha L., McCabe, Michael T., Korenchuk, Susan, Diaz, Elsie, Ott, Heidi, Thompson, Christine S., Ganji, Gopi, Gorman, Shelby A., LaFrance, Louis V., Brandt, Martin, McHugh, Charles, Verma, Sharad K., Tummino, Peter J.

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Abstract 2939: Discovery and synthesis of highly potent and selective small molecule inhibitors of the histone methyltransferase EZH2 von Verma, Sharad K., LaFrance, Louis V., Tian, Xinrong, Newlander, Ken, Duquenne, Céline, Suarez, Dominic, Knight, Steven D., Burgess, Joelle, Brackley, James, Johnson, Neil W., Graves, Alan P., Mellinger, Mark, Romeril, Stuart, Grant, Seth W., Scherzer, Daryl, Shu, Art, Creasy, Caretha L., Kruger, Ryan, Diaz, Elsie, Le, Baochau, Thompson, Christine, Morgan-Ott, Heidi, McCabe, Michael T., McHugh, Charles F., Miller, William H., Tummino, Peter, Dhanak, Dash

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Comment établir les salaires de demain? Avantages et fonctionnement d'un système de salaires à primes d'activité (devis Rowan) par L. Danty-Lafrance von Danty-Lafrance, Louis

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Tetrasubstituted pyridines as potent and selective AKT inhibitors: Reduced CYP450 and hERG inhibition of aminopyridines von Lin, Hong, Yamashita, Dennis S., Xie, Ren, Zeng, Jin, Wang, Wenyong, Leber, Jack, Safonov, Igor G., Verma, Sharad, Li, Mei, LaFrance, Louis, Venslavsky, Joseph, Takata, Dennis, Luengo, Juan I., Kahana, Jason A., Zhang, Shuyun, Robell, Kimberly A., Levy, Dana, Kumar, Rakesh, Choudhry, Anthony E., Schaber, Michael, Lai, Zhihong, Brown, Barry S., Donovan, Brian T., Minthorn, Elisabeth A., Brown, Kristin K., Heerding, Dirk A.

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Identification of 4-(2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3 S )-3-piperidinylmethyl]oxy}-1 H -imidazo[4,5- c ]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a Novel Inhi... von Heerding, Dirk A., Rhodes, Nelson, Leber, Jack D., Clark, Tammy J., Keenan, Richard M., Lafrance, Louis V., Li, Mei, Safonov, Igor G., Takata, Dennis T., Venslavsky, Joseph W., Yamashita, Dennis S., Choudhry, Anthony E., Copeland, Robert A., Lai, Zhihong, Schaber, Michael D., Tummino, Peter J., Strum, Susan L., Wood, Edgar R., Duckett, Derek R., Eberwein, Derek, Knick, Victoria B., Lansing, Timothy J., McConnell, Randy T., Zhang, ShuYun, Minthorn, Elisabeth A., Concha, Nestor O., Warren, Gregory L., Kumar, Rakesh

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MRGX2 ANTAGONISTS von PAONE, Daniel, YING, Maben, LAFRANCE, Louis, COLLINS, Jon, BRNARDIC, Edward

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