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

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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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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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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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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 o... von HEERDING, Dirk A, RHODES, Nelson, YAMASHITA, Dennis S, CHOUDHRY, Anthony E, COPELAND, Robert A, ZHIHONG LAI, SCHABER, Michael D, TUMMINO, Peter J, STRUM, Susan L, WOOD, Edgar R, DUCKETT, Derek R, EBERWEIN, Derek, LEBER, Jack D, KNICK, Victoria B, LANSING, Timothy J, MCCONNELL, Randy T, SHUYUN ZHANG, MINTHORN, Elisabeth A, CONCHA, Nestor O, WARREN, Gregory L, KUMAR, Rakesh, CLARK, Tammy J, KEENAN, Richard M, LAFRANCE, Louis V, MEI LI, SAFONOV, Igor G, TAKATA, Dennis T, VENSLAVSKY, Joseph W

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Research Article: Substituted 1,4-Benzodiazepine-2,5-diones as alpha -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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ChemInform Abstract: A Facile Method for the Synthesis of Substituted Pyrazolo[3,4-c]pyridines von Verma, Sharad K., LaFrance, Louis V.

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POTENCIADOR DE INHIBIDORES DEL HOMÓLOGO DE ZESTE von XINRONG TIAN, STEVEN DAVID KNIGHT, JIRI KASPAREC, KENNETH ALLEN NEWLANDER, DAI-SHI SU, MARK SCHULZ, JOELLE LORRAINE BURGESS, STUART PAUL ROMERIL, WILLIAM HENRY MILLER, CHARLES WILLIAM BLACKLEDGE, JR, LOUIS V. LAFRANCE III, NEIL W. JOHNSON, JUAN I. LUENGO

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Potenciador de inhibidores del homólogo de Zeste 2 von MILLER, William Henry, KASPAREC, Jiri, BLACKLEDGE, JR, LUENGO, Juan I, JOHNSON, Neil W, ROMERIL, Stuart Paul, NEWLANDER, Kenneth Allen, BURGESS, Joelle Lorraine, KNIGHT, Steven David, SU, Dai-Shi, LAFRANCE III, Louis V, SCHULZ, Mark, TIAN, Xinrong

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ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS von ROMERIL, STUART PAUL, LUENGO, JUAN I, NEWLANDER, KENNETH ALLEN, JOHNSON, NEIL W, BURGESS, JOELLE LORRAINE, KASPAREC, JIRI, SU, DAI-SHI, KNIGHT, STEVEN DAVID, BLACKLEDGE, CHARLES WILLIAM, JR, MILLER, WILLIAM HENRY, LAFRANCE, LOUIS V., III, TIAN, XINRONG, SCHULZ, MARK

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ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS von MILLER, William Henry, KASPAREC, Jiri, LUENGO, Juan I, JOHNSON, Neil W, ROMERIL, Stuart Paul, NEWLANDER, Kenneth Allen, BLACKLEDGE, JR., Charles William, BURGESS, Joelle Lorraine, KNIGHT, Steven David, SU, Dai-Shi, LAFRANCE III, Louis V, SCHULZ, Mark, TIAN, Xinrong

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