Pharmacokinetic–pharmacodynamic guided optimisation of dose and schedule of CGM097, an HDM2 inhibitor, in preclinical and clinical studies von Bauer, Sebastian, Demetri, George D., Halilovic, Ensar, Dummer, Reinhard, Meille, Christophe, Tan, Daniel S. W., Guerreiro, Nelson, Jullion, Astrid, Ferretti, Stephane, Jeay, Sebastien, Van Bree, Laurence, Hourcade-Potelleret, Florence, Wuerthner, Jens U., Fabre, Claire, Cassier, Philippe A.

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Design of Dual EP2/EP4 Antagonists through Scaffold Merging of Selective Inhibitors von Corminboeuf, Olivier, Diethelm, Stefan, Zumbrunn, Cornelia, Lyothier, Isabelle, Niggli, Nadja, Gnerre, Carmela, Jeay, Sébastien, Lehembre, François, Boss, Christoph

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Combined ALK and MDM2 inhibition increases antitumor activity and overcomes resistance in human ALK mutant neuroblastoma cell lines and xenograft models von Wang, Hui Qin, Halilovic, Ensar, Li, Xiaoyan, Liang, Jinsheng, Cao, Yichen, Rakiec, Daniel P, Ruddy, David A, Jeay, Sebastien, Wuerthner, Jens U, Timple, Noelito, Kasibhatla, Shailaja, Li, Nanxin, Williams, Juliet A, Sellers, William R, Huang, Alan, Li, Fang

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Resistance mechanisms to TP53-MDM2 inhibition identified by in vivo piggyBac transposon mutagenesis screen in an Arf−/− mouse model von Chapeau, Emilie A., Gembarska, Agnieszka, Durand, Eric Y., Mandon, Emeline, Estadieu, Claire, Romanet, Vincent, Wiesmann, Marion, Tiedt, Ralph, Lehar, Joseph, deWeck, Antoine, Rad, Roland, Barys, Louise, Jeay, Sebastien, Ferretti, Stephane, Kauffmann, Audrey, Sutter, Esther, Grevot, Armelle, Moulin, Pierre, Murakami, Masato, Sellers, William R., Hofmann, Francesco, Jensen, Michael Rugaard

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Inhibition of Wild-Type p53-Expressing AML by the Novel Small Molecule HDM2 Inhibitor CGM097 von Weisberg, Ellen, Halilovic, Ensar, Cooke, Vesselina G, Nonami, Atsushi, Ren, Tao, Sanda, Takaomi, Simkin, Irene, Yuan, Jing, Antonakos, Brandon, Barys, Louise, Ito, Moriko, Stone, Richard, Galinsky, Ilene, Cowens, Kristen, Nelson, Erik, Sattler, Martin, Jeay, Sebastien, Wuerthner, Jens U, McDonough, Sean M, Wiesmann, Marion, Griffin, James D

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Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors von Holzer, Philipp, Masuya, Keiichi, Furet, Pascal, Kallen, Joerg, Valat-Stachyra, Therese, Ferretti, Stéphane, Berghausen, Joerg, Bouisset-Leonard, Michèle, Buschmann, Nicole, Pissot-Soldermann, Carole, Rynn, Caroline, Ruetz, Stephan, Stutz, Stefan, Chène, Patrick, Jeay, Sébastien, Gessier, Francois

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Dose and Schedule Determine Distinct Molecular Mechanisms Underlying the Efficacy of the p53-MDM2 Inhibitor HDM201 von Jeay, Sébastien, Ferretti, Stéphane, Holzer, Philipp, Fuchs, Jeanette, Chapeau, Emilie A, Wartmann, Markus, Sterker, Dario, Romanet, Vincent, Murakami, Masato, Kerr, Grainne, Durand, Eric Y, Gaulis, Swann, Cortes-Cros, Marta, Ruetz, Stephan, Stachyra, Therese-Marie, Kallen, Joerg, Furet, Pascal, Würthner, Jens, Guerreiro, Nelson, Halilovic, Ensar, Jullion, Astrid, Kauffmann, Audrey, Kuriakose, Emil, Wiesmann, Marion, Jensen, Michael R, Hofmann, Francesco, Sellers, William R

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Discovery of a novel class of highly potent inhibitors of the p53–MDM2 interaction by structure-based design starting from a conformational argument von Furet, Pascal, Masuya, Keiichi, Kallen, Joerg, Stachyra-Valat, Thérèse, Ruetz, Stephan, Guagnano, Vito, Holzer, Philipp, Mah, Robert, Stutz, Stefan, Vaupel, Andrea, Chène, Patrick, Jeay, Sébastien, Schlapbach, Achim

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Dependence of Wilms tumor cells on signaling through insulin-like growth factor 1 in an orthotopic xenograft model targetable by specific receptor inhibition von Bielen, Aleksandra, Box, Gary, Perryman, Lara, Bjerke, Lynn, Popov, Sergey, Jamin, Yann, Jury, Alexa, Valenti, Melanie, Brandon, Alexis de Haven, Martins, Vanessa, Romanet, Vincent, Jeay, Sebastien, Raynaud, Florence I, Hofmann, Francesco, Robinson, Simon P, Eccles, Suzanne A, Jones, Chris

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A distinct p53 target gene set predicts for response to the selective p53-HDM2 inhibitor NVP-CGM097 von Jeay, Sébastien, Gaulis, Swann, Ferretti, Stéphane, Bitter, Hans, Ito, Moriko, Valat, Thérèse, Murakami, Masato, Ruetz, Stephan, Guthy, Daniel A, Rynn, Caroline, Jensen, Michael R, Wiesmann, Marion, Kallen, Joerg, Furet, Pascal, Gessier, François, Holzer, Philipp, Masuya, Keiichi, Würthner, Jens, Halilovic, Ensar, Hofmann, Francesco, Sellers, William R, Graus Porta, Diana

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ARQ 197, a novel and selective inhibitor of the human c-Met receptor tyrosine kinase with antitumor activity von Munshi, Neru, Jeay, Sébastien, Li, Youzhi, Chen, Chang-Rung, France, Dennis S, Ashwell, Mark A, Hill, Jason, Moussa, Magdi M, Leggett, David S, Li, Chiang J

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Discovery of dihydroisoquinolinone derivatives as novel inhibitors of the p53–MDM2 interaction with a distinct binding mode von Gessier, François, Kallen, Joerg, Jacoby, Edgar, Chène, Patrick, Stachyra-Valat, Thérèse, Ruetz, Stephan, Jeay, Sébastien, Holzer, Philipp, Masuya, Keiichi, Furet, Pascal

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The tumor suppressor activity of the lysyl oxidase propeptide reverses the invasive phenotype of Her-2/neu-driven breast cancer von CHENGYIN MIN, KIRSCH, Kathrin H, YINGSHE ZHAO, JEAY, Sébastien, PALAMAKUMBURA, Amitha H, TRACKMAN, Philip C, SONENSHEIN, Gail E

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In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor von Vaupel, Andrea, Holzer, Philipp, Ferretti, Stephane, Guagnano, Vito, Kallen, Joerg, Mah, Robert, Masuya, Keiichi, Ruetz, Stephan, Rynn, Caroline, Schlapbach, Achim, Stachyra, Thérèse, Stutz, Stefan, Todorov, Milen, Jeay, Sébastien, Furet, Pascal

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Predictive Power of Time-Series Based Machine Learning Models for DMPK Measurements in Drug Discovery von von Korff, Modest, Corminboeuf, Olivier, Gatfield, John, Jeay, Sébastien, Reymond, Isabelle, Sander, Thomas

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High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells von Horn, Thomas, Ferretti, Stéphane, Ebel, Nicolas, Tam, Angela, Ho, Samuel, Harbinski, Fred, Farsidjani, Ali, Zubrowski, Matthew, Sellers, William R, Schlegel, Robert, Porter, Dale, Morris, Erick, Wuerthner, Jens, Jeay, Sébastien, Greshock, Joel, Halilovic, Ensar, Garraway, Levi A, Caponigro, Giordano, Lehár, Joseph

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The Propeptide Domain of Lysyl Oxidase Induces Phenotypic Reversion of Ras-transformed Cells von Palamakumbura, Amitha H., Jeay, Sébastien, Guo, Ying, Pischon, Nicole, Sommer, Pascal, Sonenshein, Gail E., Trackman, Philip C.

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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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Optimisation of a 5-[3-phenyl-(2-cyclic-ether)-methyl-ether]-4-aminopyrrolopyrimidine series of IGF-1R inhibitors von Fairhurst, Robin A., Marsilje, Thomas H., Stutz, Stefan, Boos, Andreas, Niklaus, Michel, Chen, Bei, Jiang, Songchun, Lu, Wenshuo, Furet, Pascal, McCarthy, Clive, Stauffer, Frédéric, Guagnano, Vito, Vaupel, Andrea, Michellys, Pierre-Yves, Schnell, Christian, Jeay, Sébastien

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c-Myc represses FOXO3a-mediated transcription of the gene encoding the p27(Kip1) cyclin dependent kinase inhibitor von Chandramohan, Vidyalakshmi, Mineva, Nora D, Burke, Brian, Jeay, Sébastien, Wu, Min, Shen, Jian, Yang, William, Hann, Stephen R, Sonenshein, Gail E

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