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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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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Discovery of Umibecestat (CNP520): A Potent, Selective, and Efficacious beta-Secretase (BACE1) Inhibitor for the Prevention of Alzheimer's Disease
Machauer, Rainer, Lueoend, Rainer, Hurth, Konstanze, Veenstra, Siem J., Rueeger, Heinrich, Voegtle, Markus, Tintelnot-Blomley, Marina, Rondeau, Jean-Michel, Jacobson, Laura H., Laue, Grit, Beltz, Karen, Neumann, Ulf
Published in Journal of medicinal chemistry (28.10.2021)
Published in Journal of medicinal chemistry (28.10.2021)
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JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors
Lorthiois, Edwige, Gerspacher, Marc, Beyer, Kim S., Vaupel, Andrea, Leblanc, Catherine, Stringer, Rowan, Weiss, Andreas, Wilcken, Rainer, Guthy, Daniel A., Lingel, Andreas, Bomio-Confaglia, Claudio, Machauer, Rainer, Rigollier, Pascal, Ottl, Johannes, Arz, Dorothee, Bernet, Pascal, Desjonqueres, Gaëlle, Dussauge, Solene, Kazic-Legueux, Malika, Lozac’h, Marie-Anne, Mura, Christophe, Sorge, Mickaël, Todorov, Milen, Warin, Nicolas, Zink, Florence, Voshol, Hans, Zecri, Frederic J., Sedrani, Richard C., Ostermann, Nils, Brachmann, Saskia M., Cotesta, Simona
Published in Journal of medicinal chemistry (22.12.2022)
Published in Journal of medicinal chemistry (22.12.2022)
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Discovery of Cyclic Sulfone Hydroxyethylamines as Potent and Selective β-Site APP-Cleaving Enzyme 1 (BACE1) Inhibitors: Structure-Based Design and in Vivo Reduction of Amyloid β-Peptides
Rueeger, Heinrich, Lueoend, Rainer, Rogel, Olivier, Rondeau, Jean-Michel, Möbitz, Henrik, Machauer, Rainer, Jacobson, Laura, Staufenbiel, Matthias, Desrayaud, Sandrine, Neumann, Ulf
Published in Journal of medicinal chemistry (12.04.2012)
Published in Journal of medicinal chemistry (12.04.2012)
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Synthesis of the Potent, Selective, and Efficacious β‑Secretase (BACE1) Inhibitor NB-360
Rueeger, Heinrich, Lueoend, Rainer, Machauer, Rainer, Veenstra, Siem J, Holzer, Philipp, Hurth, Konstanze, Voegtle, Markus, Frederiksen, Mathias, Rondeau, Jean-Michel, Tintelnot-Blomley, Marina, Jacobson, Laura H, Staufenbiel, Matthias, Laue, Grit, Neumann, Ulf
Published in Journal of medicinal chemistry (22.04.2021)
Published in Journal of medicinal chemistry (22.04.2021)
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Discovery and Structural Characterization of ATP-Site Ligands for the Wild-Type and V617F Mutant JAK2 Pseudokinase Domain
McNally, Randall, Li, Qing, Li, Kunhua, Dekker, Carien, Vangrevelinghe, Eric, Jones, Matthew, Chène, Patrick, Machauer, Rainer, Radimerski, Thomas, Eck, Michael J
Published in ACS chemical biology (19.04.2019)
Published in ACS chemical biology (19.04.2019)
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A novel BACE inhibitor NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in APP transgenic mice
Neumann, Ulf, Rueeger, Heinrich, Machauer, Rainer, Veenstra, Siem Jacob, Lueoend, Rainer M, Tintelnot-Blomley, Marina, Laue, Grit, Beltz, Karen, Vogg, Barbara, Schmid, Peter, Frieauff, Wilfried, Shimshek, Derya R, Staufenbiel, Matthias, Jacobson, Laura H
Published in Molecular neurodegeneration (03.09.2015)
Published in Molecular neurodegeneration (03.09.2015)
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Pharmacological BACE1 and BACE2 inhibition induces hair depigmentation by inhibiting PMEL17 processing in mice
Shimshek, Derya R, Jacobson, Laura H, Kolly, Carine, Zamurovic, Natasa, Balavenkatraman, Kamal Kumar, Morawiec, Laurent, Kreutzer, Robert, Schelle, Juliane, Jucker, Mathias, Bertschi, Barbara, Theil, Diethilde, Heier, Annabelle, Bigot, Karine, Beltz, Karen, Machauer, Rainer, Brzak, Irena, Perrot, Ludovic, Neumann, Ulf
Published in Scientific reports (25.02.2016)
Published in Scientific reports (25.02.2016)
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NIBR-LTSi is a selective LATS kinase inhibitor activating YAP signaling and expanding tissue stem cells in vitro and in vivo
Namoto, Kenji, Baader, Clara, Orsini, Vanessa, Landshammer, Alexandro, Breuer, Eva, Dinh, Kieu Trinh, Ungricht, Rosemarie, Pikiolek, Monika, Laurent, Stephane, Lu, Bo, Aebi, Alexandra, Schönberger, Katharina, Vangrevelinghe, Eric, Evrova, Olivera, Sun, Tianliang, Annunziato, Stefano, Lachal, Julie, Redmond, Emily, Wang, Louis, Wetzel, Kristie, Capodieci, Paola, Turner, Jonathan, Schutzius, Gabi, Unterreiner, Vincent, Trunzer, Markus, Buschmann, Nicole, Behnke, Dirk, Machauer, Rainer, Scheufler, Clemens, Parker, Christian N., Ferro, Magali, Grevot, Armelle, Beyerbach, Armin, Lu, Wei-Yu, Forbes, Stuart J., Wagner, Jürgen, Bouwmeester, Tewis, Liu, Jun, Sohal, Bindi, Sahambi, Sukhdeep, Greenbaum, Linda E., Lohmann, Felix, Hoppe, Philipp, Cong, Feng, Sailer, Andreas W., Ruffner, Heinz, Glatthar, Ralf, Humar, Bostjan, Clavien, Pierre-Alain, Dill, Michael T., George, Elizabeth, Maibaum, Jürgen, Liberali, Prisca, Tchorz, Jan S.
Published in Cell stem cell (04.04.2024)
Published in Cell stem cell (04.04.2024)
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JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS G12C for the Treatment of Solid Tumors
Lorthiois, Edwige, Gerspacher, Marc, Beyer, Kim S, Vaupel, Andrea, Leblanc, Catherine, Stringer, Rowan, Weiss, Andreas, Wilcken, Rainer, Guthy, Daniel A, Lingel, Andreas, Bomio-Confaglia, Claudio, Machauer, Rainer, Rigollier, Pascal, Ottl, Johannes, Arz, Dorothee, Bernet, Pascal, Desjonqueres, Gaëlle, Dussauge, Solene, Kazic-Legueux, Malika, Lozac'h, Marie-Anne, Mura, Christophe, Sorge, Mickaël, Todorov, Milen, Warin, Nicolas, Zink, Florence, Voshol, Hans, Zecri, Frederic J, Sedrani, Richard C, Ostermann, Nils, Brachmann, Saskia M, Cotesta, Simona
Published in Journal of medicinal chemistry (22.12.2022)
Published in Journal of medicinal chemistry (22.12.2022)
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Discovery of amino-1,4-oxazines as potent BACE-1 inhibitors
Veenstra, Siem Jakob, Rueeger, Heinrich, Voegtle, Markus, Lueoend, Rainer, Holzer, Philipp, Hurth, Konstanze, Tintelnot-Blomley, Marina, Frederiksen, Mathias, Rondeau, Jean-Michel, Jacobson, Laura, Staufenbiel, Matthias, Neumann, Ulf, Machauer, Rainer
Published in Bioorganic & medicinal chemistry letters (01.07.2018)
Published in Bioorganic & medicinal chemistry letters (01.07.2018)
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Journal Article
Discovery of cyclic sulfoxide hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: Structure based design and in vivo reduction of amyloid β-peptides
Rueeger, Heinrich, Lueoend, Rainer, Machauer, Rainer, Veenstra, Siem Jacob, Jacobson, Laura Helen, Staufenbiel, Matthias, Desrayaud, Sandrine, Rondeau, Jean-Michel, Möbitz, Henrik, Neumann, Ulf
Published in Bioorganic & medicinal chemistry letters (01.10.2013)
Published in Bioorganic & medicinal chemistry letters (01.10.2013)
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KRAS 돌연변이 단백질의 억제제로서의 피라졸릴 유도체
WILCKEN RAINER, ZECRI FREDERIC, LORTHIOIS EDWIGE LILIANE JEANNE, VAUPEL ANDREA, BRACHMANN SASKIA MARIA, COTESTA SIMONA, RIGOLLIER PASCAL, STUTZ STEFAN, LEBLANC CATHERINE, LIMA FABIO, MACHAUER RAINER, MAH ROBERT, WARIN NICOLAS, BOMIO CONFAGLIA CLAUDIO, RACINE SOPHIE, GERSPACHER MARC
Year of Publication 26.02.2024
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Year of Publication 26.02.2024
Patent
KRAS G12C 억제제 화합물의 새로운 결정형
WILCKEN RAINER, XUE LIJUN, LORTHIOIS EDWIGE LILIANE JEANNE, VAUPEL ANDREA, COTESTA SIMONA, GE HENG, RIGOLLIER PASCAL, STUTZ STEFAN, MURA CHRISTOPHE, LEBLANC CATHERINE, MEISTER TANJA, MACHAUER RAINER, SCHNEIDER NADINE, MAH ROBERT, LIU BO, WARIN NICOLAS, GERSPACHER MARC
Year of Publication 03.07.2023
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Year of Publication 03.07.2023
Patent
KRAS G12C 저해제를 포함하는 약제학적 조합물 및 암의 치료를 위한 이의 용도
WILCKEN RAINER, LORTHIOIS EDWIGE LILIANE JEANNE, FARAGO ANNA, PRAHALLAD ANIRUDH CADAPA, BRACHMANN SASKIA MARIA, COTESTA SIMONA, STRINGER ROWAN, RIGOLLIER PASCAL, STUTZ STEFAN, MURA CHRISTOPHE, LEBLANC CATHERINE, KIM JAEYEON, CUI XIAOMING, MACHAUER RAINER, SCHNEIDER NADINE, MAH ROBERT, VAUPEL ANDREAS, DE KANTER RUBEN, GRAUS PORTA DIANA, WEISS ANDREAS, WARIN NICOLAS, GERSPACHER MARC
Year of Publication 26.02.2024
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Year of Publication 26.02.2024
Patent
Macrocyclic BACE-1 inhibitors acutely reduce Aβ in brain after po application
Lerchner, Andreas, Machauer, Rainer, Betschart, Claudia, Veenstra, Siem, Rueeger, Heinrich, McCarthy, Clive, Tintelnot-Blomley, Marina, Jaton, Anne-Lise, Rabe, Sabine, Desrayaud, Sandrine, Enz, Albert, Staufenbiel, Matthias, Paganetti, Paolo, Rondeau, Jean-Michel, Neumann, Ulf
Published in Bioorganic & medicinal chemistry letters (15.01.2010)
Published in Bioorganic & medicinal chemistry letters (15.01.2010)
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KRAS G12C 억제제를 포함하는 약제학적 조합물 및 암의치료를 위한 KRAS G12C 억제제의 용도
WILCKEN RAINER, ENGELMAN JEFFREY, LORTHIOIS EDWIGE LILIANE JEANNE, VAUPEL ANDREA, FARAGO ANNA, BRACHMANN SASKIA MARIA, COTESTA SIMONA, RIGOLLIER PASCAL, STUTZ STEFAN, MURA CHRISTOPHE, LEBLANC CATHERINE, CUI XIAOMING, MACHAUER RAINER, SCHNEIDER NADINE, MAH ROBERT, LIU BO, YERRAMILLI RAO PADMAJA, GRAUS PORTA DIANA, WEISS ANDREAS, WARIN NICOLAS, ASKOXYLAKIS VASILEIOS, GERSPACHER MARC
Year of Publication 31.08.2023
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Year of Publication 31.08.2023
Patent