Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase
Angst, Daniela, Gessier, François, Janser, Philipp, Vulpetti, Anna, Wälchli, Rudolf, Beerli, Christian, Littlewood-Evans, Amanda, Dawson, Janet, Nuesslein-Hildesheim, Barbara, Wieczorek, Grazyna, Gutmann, Sascha, Scheufler, Clemens, Hinniger, Alexandra, Zimmerlin, Alfred, Funhoff, Enrico G, Pulz, Robert, Cenni, Bruno
Published in Journal of Medicinal Chemistry (28.05.2020)
Published in Journal of Medicinal Chemistry (28.05.2020)
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Journal Article
N‐terminal β‐strand in YAP is critical for stronger binding to scalloped relative to TEAD transcription factor
Fedir, Bokhovchuk, Yannick, Mesrouze, Marco, Meyerhofer, Patrizia, Fontana, Catherine, Zimmermann, Frédéric, Villard, Dirk, Erdmann, Joerg, Kallen, Clemens, Scheufler, Camilo, Velez‐Vega, Patrick, Chène
Published in Protein science (01.01.2023)
Published in Protein science (01.01.2023)
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Journal Article
A new perspective on the interaction between the Vg/VGLL1-3 proteins and the TEAD transcription factors
Mesrouze, Yannick, Aguilar, Gustavo, Bokhovchuk, Fedir, Martin, Typhaine, Delaunay, Clara, Villard, Frédéric, Meyerhofer, Marco, Zimmermann, Catherine, Fontana, Patrizia, Wille, Roman, Vorherr, Thomas, Erdmann, Dirk, Furet, Pascal, Scheufler, Clemens, Schmelzle, Tobias, Affolter, Markus, Chène, Patrick
Published in Scientific Reports (15.10.2020)
Published in Scientific Reports (15.10.2020)
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Journal Article
Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach
Chen, Chao, Zhu, Hugh, Stauffer, Frédéric, Caravatti, Giorgio, Vollmer, Susanne, Machauer, Rainer, Holzer, Philipp, Möbitz, Henrik, Scheufler, Clemens, Klumpp, Martin, Tiedt, Ralph, Beyer, Kim S, Calkins, Keith, Guthy, Daniel, Kiffe, Michael, Zhang, Jeff, Gaul, Christoph
Published in ACS Medicinal Chemistry Letters (11.08.2016)
Published in ACS Medicinal Chemistry Letters (11.08.2016)
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Journal Article
Optimization of a Fragment-Based Screening Hit toward Potent DOT1L Inhibitors Interacting in an Induced Binding Pocket
Scheufler, Clemens, Möbitz, Henrik, Gaul, Christoph, Ragot, Christian, Be, Céline, Fernández, César, Beyer, Kim S, Tiedt, Ralph, Stauffer, Frédéric
Published in ACS Medicinal Chemistry Letters (11.08.2016)
Published in ACS Medicinal Chemistry Letters (11.08.2016)
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Journal Article
Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach
Möbitz, Henrik, Machauer, Rainer, Holzer, Philipp, Vaupel, Andrea, Stauffer, Frédéric, Ragot, Christian, Caravatti, Giorgio, Scheufler, Clemens, Fernandez, Cesar, Hommel, Ulrich, Tiedt, Ralph, Beyer, Kim S, Chen, Chao, Zhu, Hugh, Gaul, Christoph
Published in ACS Medicinal Chemistry Letters (09.03.2017)
Published in ACS Medicinal Chemistry Letters (09.03.2017)
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Journal Article
Modulation of Activation-Loop Phosphorylation by JAK Inhibitors Is Binding Mode Dependent
Andraos, Rita, Qian, Zhiyan, Bonenfant, Débora, Rubert, Joëlle, Vangrevelinghe, Eric, Scheufler, Clemens, Marque, Fanny, Régnier, Catherine H, De Pover, Alain, Ryckelynck, Hugues, Bhagwat, Neha, Koppikar, Priya, Goel, Aviva, Wyder, Lorenza, Tavares, Gisele, Baffert, Fabienne, Pissot-Soldermann, Carole, Manley, Paul W, Gaul, Christoph, Voshol, Hans, Levine, Ross L, Sellers, William R, Hofmann, Francesco, Radimerski, Thomas
Published in Cancer Discovery (01.06.2012)
Published in Cancer Discovery (01.06.2012)
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Large Scale Meta-Analysis of Fragment-Based Screening Campaigns: Privileged Fragments and Complementary Technologies
Kutchukian, Peter S., Wassermann, Anne Mai, Lindvall, Mika K., Wright, S. Kirk, Ottl, Johannes, Jacob, Jaison, Scheufler, Clemens, Marzinzik, Andreas, Brooijmans, Natasja, Glick, Meir
Published in Journal of biomolecular screening (01.06.2015)
Published in Journal of biomolecular screening (01.06.2015)
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Journal Article
Identification of a Novel Allosteric Inhibitory Site on Tryptophan Hydroxylase 1 Enabling Unprecedented Selectivity Over all Related Hydroxylases
Petrassi, Mike, Barber, Rob, Be, Celine, Beach, Sarah, Cox, Brian, D'Souza, Anne-Marie, Duggan, Nick, Hussey, Martin, Fox, Roy, Hunt, Peter, Jarai, Gabor, Kosaka, Takatoshi, Oakley, Paul, Patel, Viral, Press, Neil, Rowlands, David, Scheufler, Clemens, Schmidt, Oliver, Srinivas, Honnappa, Turner, Mary, Turner, Rob, Westwick, John, Wolfreys, Alison, Pathan, Nuzhat, Watson, Simon, Thomas, Matthew
Published in Frontiers in pharmacology (05.05.2017)
Published in Frontiers in pharmacology (05.05.2017)
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Journal Article
Blockade of activin type II receptors with a dual anti-ActRIIA/IIB antibody is critical to promote maximal skeletal muscle hypertrophy
Morvan, Frederic, Rondeau, Jean-Michel, Zou, Chao, Minetti, Giulia, Scheufler, Clemens, Scharenberg, Meike, Jacobi, Carsten, Brebbia, Pascale, Ritter, Veronique, Toussaint, Gauthier, Koelbing, Claudia, Leber, Xavier, Schilb, Alain, Witte, Florian, Lehmann, Sylvie, Koch, Elke, Geisse, Sabine, Glass, David J., Lach-Trifilieff, Estelle
Published in Proceedings of the National Academy of Sciences - PNAS (21.11.2017)
Published in Proceedings of the National Academy of Sciences - PNAS (21.11.2017)
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Journal Article
Identification of FAM181A and FAM181B as new interactors with the TEAD transcription factors
Bokhovchuk, Fedir, Mesrouze, Yannick, Delaunay, Clara, Martin, Typhaine, Villard, Frédéric, Meyerhofer, Marco, Fontana, Patrizia, Zimmermann, Catherine, Erdmann, Dirk, Furet, Pascal, Scheufler, Clemens, Schmelzle, Tobias, Chène, Patrick
Published in Protein science (01.02.2020)
Published in Protein science (01.02.2020)
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Journal Article
Discovery of WRN inhibitor HRO761 with synthetic lethality in MSI cancers
Ferretti, Stephane, Hamon, Jacques, de Kanter, Ruben, Scheufler, Clemens, Andraos-Rey, Rita, Barbe, Stephanie, Bechter, Elisabeth, Blank, Jutta, Bordas, Vincent, Dammassa, Ernesta, Decker, Andrea, Di Nanni, Noemi, Dourdoigne, Marion, Gavioli, Elena, Hattenberger, Marc, Heuser, Alisa, Hemmerlin, Christelle, Hinrichs, Jürgen, Kerr, Grainne, Laborde, Laurent, Jaco, Isabel, Núñez, Eloísa Jiménez, Martus, Hans-Joerg, Quadt, Cornelia, Reschke, Markus, Romanet, Vincent, Schaeffer, Fanny, Schoepfer, Joseph, Schrapp, Maxime, Strang, Ross, Voshol, Hans, Wartmann, Markus, Welly, Sarah, Zécri, Frédéric, Hofmann, Francesco, Möbitz, Henrik, Cortés-Cros, Marta
Published in Nature (09.05.2024)
Published in Nature (09.05.2024)
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Journal Article
Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies
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
Published in Journal of medicinal chemistry (14.04.2022)
Published in Journal of medicinal chemistry (14.04.2022)
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Journal Article
The First Class of Small Molecules Potently Disrupting the YAP‐TEAD Interaction by Direct Competition
Furet, Pascal, Bordas, Vincent, Le Douget, Mickaël, Salem, Bahaa, Mesrouze, Yannick, Imbach‐Weese, Patricia, Sellner, Holger, Voegtle, Markus, Soldermann, Nicolas, Chapeau, Emilie, Wartmann, Markus, Scheufler, Clemens, Fernandez, Cesar, Kallen, Joerg, Guagnano, Vito, Chène, Patrick, Schmelzle, Tobias
Published in ChemMedChem (06.10.2022)
Published in ChemMedChem (06.10.2022)
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Journal Article
Discovery and In Vivo Exploration of 1,3,4-Oxadiazole and α‑Fluoroacrylate Containing IL-17 Inhibitors
Velcicky, Juraj, Bauer, Matthias R., Schlapbach, Achim, Lapointe, Guillaume, Meyer, Arndt, Vögtle, Markus, Blum, Ernst, Ngo, Estelle, Rolando, Catherine, Nimsgern, Pierre, Teixeira-Fouchard, Sylvie, Lehmann, Hansjoerg, Furet, Pascal, Berst, Frédéric, Schümann, Jens, Stringer, Rowan, Larger, Patrice, Schmid, Cindy, Prendergast, Catriona T., Riek, Simone, Schmutz, Patrick, Lehmann, Sylvie, Berghausen, Jörg, Scheufler, Clemens, Rondeau, Jean-Michel, Burkhart, Christoph, Knoepfel, Thomas, Gommermann, Nina
Published in Journal of medicinal chemistry (26.09.2024)
Published in Journal of medicinal chemistry (26.09.2024)
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Journal Article
Biochemical and Structural Characterization of a Peptidic Inhibitor of the YAP:TEAD Interaction That Binds to the α‑Helix Pocket on TEAD
Mesrouze, Yannick, Gubler, Hanspeter, Villard, Frédéric, Boesch, Ralf, Ottl, Johannes, Kallen, Joerg, Reid, Patrick C., Scheufler, Clemens, Marzinzik, Andreas L., Chène, Patrick
Published in ACS chemical biology (17.03.2023)
Published in ACS chemical biology (17.03.2023)
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Journal Article
Crystal structure of human bone morphogenetic protein-2 at 2.7 Å resolution 1 1Edited by R. Huber
Scheufler, Clemens, Sebald, Walter, Hülsmeyer, Martin
Published in Journal of Molecular Biology (01.03.1999)
Published in Journal of Molecular Biology (01.03.1999)
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