Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase von Lingel, Andreas, Sendzik, Martin, Huang, Ying, Shultz, Michael D, Cantwell, John, Dillon, Michael P, Fu, Xingnian, Fuller, John, Gabriel, Tobias, Gu, Justin, Jiang, Xiangqing, Li, Ling, Liang, Fang, McKenna, Maureen, Qi, Wei, Rao, Weijun, Sheng, Xijun, Shu, Wei, Sutton, James, Taft, Benjamin, Wang, Long, Zeng, Jue, Zhang, Hailong, Zhang, Maya, Zhao, Kehao, Lindvall, Mika, Bussiere, Dirksen E

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6‑Amino-3-methylpyrimidinones as Potent, Selective, and Orally Efficacious SHP2 Inhibitors von Sarver, Patrick, Acker, Michael, Bagdanoff, Jeffrey T, Chen, Zhouliang, Chen, Ying-Nan, Chan, Homan, Firestone, Brant, Fodor, Michelle, Fortanet, Jorge, Hao, Huaixiang, Hentemann, Murphy, Kato, Mitsunori, Koenig, Robert, LaBonte, Laura R, Liu, Gang, Liu, Shumei, Liu, Chen, McNeill, Eric, Mohseni, Morvarid, Sendzik, Martin, Stams, Travis, Spence, Stan, Tamez, Victoriano, Tichkule, Ritesh, Towler, Christopher, Wang, Hongyun, Wang, Ping, Williams, Sarah L, Yu, Bing, LaMarche, Matthew J

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Optimization of Fused Bicyclic Allosteric SHP2 Inhibitors von Bagdanoff, Jeffrey T, Chen, Zhouliang, Acker, Michael, Chen, Ying-Nan, Chan, Homan, Dore, Michael, Firestone, Brant, Fodor, Michelle, Fortanet, Jorge, Hentemann, Murphy, Kato, Mitsunori, Koenig, Robert, LaBonte, Laura R, Liu, Shumei, Mohseni, Movarid, Ntaganda, Rukundo, Sarver, Patrick, Smith, Troy, Sendzik, Martin, Stams, Travis, Spence, Stan, Towler, Christopher, Wang, Hongyun, Wang, Ping, Williams, Sarah L, LaMarche, Matthew J

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Dual Allosteric Inhibition of SHP2 Phosphatase von Fodor, Michelle, Price, Edmund, Wang, Ping, Lu, Hengyu, Argintaru, Andreea, Chen, Zhouliang, Glick, Meir, Hao, Huai-Xiang, Kato, Mitsunori, Koenig, Robert, LaRochelle, Jonathan R, Liu, Gang, McNeill, Eric, Majumdar, Dyuti, Nishiguchi, Gisele A, Perez, Lawrence B, Paris, Gregory, Quinn, Christopher M, Ramsey, Timothy, Sendzik, Martin, Shultz, Michael David, Williams, Sarah L, Stams, Travis, Blacklow, Stephen C, Acker, Michael G, LaMarche, Matthew J

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Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies von Huang, Ying, Sendzik, Martin, Zhang, Jeff, Gao, Zhenting, Sun, Yongfeng, Wang, Long, Gu, Justin, Zhao, Kehao, Yu, Zhengtian, Zhang, Lijun, Zhang, Qiong, Blanz, Joachim, Chen, Zijun, Dubost, Valérie, Fang, Douglas, Feng, Lijian, Fu, Xingnian, Kiffe, Michael, Li, Ling, Luo, Fangjun, Luo, Xiao, Mi, Yuan, Mistry, Prakash, Pearson, David, Piaia, Alessandro, Scheufler, Clemens, Terranova, Remi, Weiss, Andreas, Zeng, Jue, Zhang, Hailong, Zhang, Jiangwei, Zhao, Mengxi, Dillon, Michael P, Jeay, Sebastien, Qi, Wei, Moggs, Jonathan, Pissot-Soldermann, Carole, Li, En, Atadja, Peter, Lingel, Andreas, Oyang, Counde

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CRA-026440: a potent, broad-spectrum, hydroxamic histone deacetylase inhibitor with antiproliferative and antiangiogenic activity in vitro and in vivo von Cao, Z Alexander, Bass, Kathryn E, Balasubramanian, Sriram, Liu, Liang, Schultz, Brian, Verner, Erik, Dai, Yuqin, Molina, Rafael A, Davis, Jack R, Misialek, Shawn, Sendzik, Martin, Orr, Christine J, Leung, Ling, Callan, Ondine, Young, Peter, Dalrymple, Stacie A, Buggy, Joseph J

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Discovery and Evaluation of Clinical Candidate IDH305, a Brain Penetrant Mutant IDH1 Inhibitor von Cho, Young Shin, Levell, Julian R, Liu, Gang, Caferro, Thomas, Sutton, James, Shafer, Cynthia M, Costales, Abran, Manning, James R, Zhao, Qian, Sendzik, Martin, Shultz, Michael, Chenail, Gregg, Dooley, Julia, Villalba, Brian, Farsidjani, Ali, Chen, Jinyun, Kulathila, Raviraj, Xie, Xiaoling, Dodd, Stephanie, Gould, Ty, Liang, Guiqing, Heimbach, Tycho, Slocum, Kelly, Firestone, Brant, Pu, Minying, Pagliarini, Raymond, Growney, Joseph D

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Evaluation of antitumor properties of novel saframycin analogs in vitro and in vivo von Spencer, Jeffrey R., Sendzik, Martin, Oeh, Jason, Sabbatini, Peter, Dalrymple, Stacie A., Magill, Catherine, Kim, Hyunjin M., Zhang, Penglie, Squires, Neil, Moss, Katherine G., Sukbuntherng, Juthamas, Graupe, Doris, Eksterowicz, John, Young, Peter R., Myers, Andrew G., Green, Michael J.

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Abstract LB-005: Allosteric SHP2 phosphatase inhibition: Multiple mechanisms and chemotypes von LaMarche, Matthew J., Bagdanoff, Jeff, Acker, Mike, Chen, Ying-Nan, Chan, Homan, Dore, Michael, Firestone, Brant, Fodor, Michelle, Garcia-Fortanet, Jorge, Hentemann, Murphy, Kato, Mitsunori, Koenig, Robert, Bonte, Laura La, Liu, Shumei, Mohseni, Movarid, Ntaganda, Rukundo, Sarver, Patrick, Smith, Troy, Sendzik, Martin, Stams, Travis, Spence, Stan, Towler, Chris, Wang, Hongyun, Wang, Ping, Williams, Sarah, Chen, Zhouliang, Hao, Huaixiang, Liu, Gang, Liu, Chen, McNeill, Eric, Yu, Bing

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Correction to Optimization of Fused Bicyclic Allosteric SHP2 Inhibitors von Bagdanoff, Jeffrey T, Chen, Zhouliang, Acker, Michael, Chen, Ying-Nan, Chan, Homan, Dore, Michael, Firestone, Brant, Fodor, Michelle, Fortanet, Jorge, Hentemann, Murphy, Kato, Mitsunori, Koenig, Robert, LaBonte, Laura R, Liu, Shumei, Mohseni, Movarid, Ntaganda, Rukundo, Sarver, Patrick, Shultz, Michael D, Smith, Troy, Sendzik, Martin, Stams, Travis, Spence, Stan, Towler, Christopher, Wang, Hongyun, Wang, Ping, Williams, Sarah L, LaMarche, Matthew J

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Abstract 2808: Simultaneous inhibition of SHP2 phosphatase at two allosteric sites von Fodor, Michelle, Price, Edmund, Wang, Ping, Lu, Hengyu, Argintaru, Andreea, Chen, Zhouliang, Glick, Meir, Hao, Huai-Xiang, Kato, Mitsunori, Koenig, Robert, LaRochelle, Jonathan R., Liu, Gang, McNeill, Eric, Majumdar, Dyuti, Nishiguchi, Gisele, Perez, Lawrence, Paris, Greg, Quinn, Christopher, Ramsey, Timothy, Sendzik, Martin, Shultz, Michael, Williams, Sarah, Stams, Travis, Blacklow, Stephen C., LaMarche, Matthew J., Acker, Michael G.

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Correction to 6‑Amino-3-methylpyrimidinones as Potent, Selective, and Orally Efficacious SHP2 Inhibitors von Sarver, Patrick, Acker, Michael, Bagdanoff, Jeffrey T, Chen, Zhouliang, Chen, Ying-Nan, Chan, Homan, Firestone, Brant, Fodor, Michelle, Fortanet, Jorge, Hao, Huaixiang, Hentemann, Murphy, Jouk, Andriana, Kato, Mitsunori, Koenig, Robert, LaBonte, Laura R, Liu, Gang, Liu, Shumei, Liu, Chen, McNeill, Eric, Mohseni, Morvarid, Shultz, Michael D, Sendzik, Martin, Stams, Travis, Spence, Stan, Tamez, Victoriano, Tichkule, Ritesh, Towler, Christopher, Wang, Hongyun, Wang, Ping, Williams, Sarah L, Yu, Bing, LaMarche, Matthew J

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Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase von Lingel, Andreas, Sendzik, Martin, Huang, Ying, Shultz, Michael D., Cantwell, John, Dillon, Michael P., Fu, Xingnian, Fuller, John, Gabriel, Tobias, Gu, Justin, Jiang, Xiangqing, Li, Ling, Liang, Fang, McKenna, Maureen, Qi, Wei, Rao, Weijun, Sheng, Xijun, Shu, Wei, Sutton, James, Taft, Benjamin, Wang, Long, Zeng, Jue, Zhang, Hailong, Zhang, Maya, Zhao, Kehao, Lindvall, Mika, Bussiere, Dirksen E.

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Optimization of 3‑Pyrimidin-4-yl-oxazolidin-2-ones as Orally Bioavailable and Brain Penetrant Mutant IDH1 Inhibitors von Zhao, Qian, Manning, James R., Sutton, James, Costales, Abran, Sendzik, Martin, Shafer, Cynthia M., Levell, Julian R., Liu, Gang, Caferro, Thomas, Cho, Young Shin, Palermo, Mark, Chenail, Gregg, Dooley, Julia, Villalba, Brian, Farsidjani, Ali, Chen, Jinyun, Dodd, Stephanie, Gould, Ty, Liang, Guiqing, Slocum, Kelly, Pu, Minying, Firestone, Brant, Growney, Joseph, Heimbach, Tycho, Pagliarini, Raymond

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A New Synthetic Approach to the C Ring of Known as Well as Novel Bryostatin Analogues von Wender, Paul A, Koehler, Michael F. T, Sendzik, Martin

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Environmentally friendly and efficient: iron-mediated reduction of 3-methyl-5-aryl-1,2,4-oxadiazoles to benzamidines von Sendzik, Martin, Hui, Hon C

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Discovery of 5-(4-hydroxy-6-methyl-2-oxo-2 H-pyran-3-yl)-7-phenyl-( E)-2,3,6,7-tetrahydro-1,4-thiazepines as a new series of apoptosis inducers using a cell- and caspase-based HTS... von Drewe, John, Kasibhatla, Shailaja, Tseng, Ben, Shelton, Emma, Sperandio, David, Yee, Robert M., Litvak, Joane, Sendzik, Martin, Spencer, Jeffrey R., Cai, Sui Xiong

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Elaborate Manifold of Short Hydrogen Bond Arrays Mediating Binding of Active Site-directed Serine Protease Inhibitors von Katz, Bradley A., Elrod, Kyle, Verner, Erik, Mackman, Richard L., Luong, Christine, Shrader, William D., Sendzik, Martin, Spencer, Jeffrey R., Sprengeler, Paul A., Kolesnikov, Aleks, Tai, Vincent W.-F., Hui, Hon C., Guy Breitenbucher, J., Allen, Darin, Janc, James W.

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Design and synthesis of β-amino-α-hydroxy amide derivatives as inhibitors of MetAP2 and HUVEC growth von SENDZIK, Martin, JANC, James W, CABUSLAY, Ronnel, HONIGBERG, Lee, MACKMAN, Richard L, MAGILL, Catherine, SQUIRES, Neil, WALDECK, Nancy

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Design and synthesis of β-amino-α-hydroxy amide derivatives as inhibitors of MetAP2 and HUVEC growth von Sendzik, Martin, Janc, James W., Cabuslay, Ronnel, Honigberg, Lee, Mackman, Richard L., Magill, Catherine, Squires, Neil, Waldeck, Nancy

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