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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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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The design and implementation of a generic lipopeptide scanning platform to enable the identification of ‘locally acting’ agonists for the apelin receptor
McKeown, Stephen C., Zecri, Frederic J., Fortier, Eric, Taggart, Andrew, Sviridenko, Lilya, Adams, Christopher M., McAllister, Kathryn H., Pin, Sokhom S.
Published in Bioorganic & medicinal chemistry letters (15.10.2014)
Published in Bioorganic & medicinal chemistry letters (15.10.2014)
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Absorption and Disposition of the Sphingosine 1-Phosphate Receptor Modulator Fingolimod (FTY720) in Healthy Volunteers: A Case of Xenobiotic Biotransformation Following Endogenous Metabolic Pathways
ZOLLINGER, Markus, GSCHWIND, Hans-Peter, YI JIN, SAYER, Claudia, ZECRI, Frédéric, HARTMANN, Stefan
Published in Drug metabolism and disposition (01.02.2011)
Published in Drug metabolism and disposition (01.02.2011)
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A ROMPGEL-Supported N-Hydroxysuccinimide: A Host of Acylations with Minimal Purification
Barrett, Anthony G. M, Cramp, Susan M, Roberts, Richard S, Zecri, Frederic J
Published in Organic letters (10.02.2000)
Published in Organic letters (10.02.2000)
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Impurity annihilation; a strategy for solution phase combinatorial chemistry with minimal purification
Barrett, AGM, Smith, ML, Zecri, FJ
Published in Chemical communications (Cambridge, England) (07.11.1998)
Published in Chemical communications (Cambridge, England) (07.11.1998)
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Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C
Weiss, Andreas, Lorthiois, Edwige, Barys, Louise, Beyer, Kim S, Bomio-Confaglia, Claudio, Burks, Heather, Chen, Xueying, Cui, Xiaoming, de Kanter, Ruben, Dharmarajan, Lekshmi, Fedele, Carmine, Gerspacher, Marc, Guthy, Daniel Alexander, Head, Victoria, Jaeger, Ashley, Núñez, Eloísa Jiménez, Kearns, Jeffrey D, Leblanc, Catherine, Maira, Sauveur-Michel, Murphy, Jason, Oakman, Helen, Ostermann, Nils, Ottl, Johannes, Rigollier, Pascal, Roman, Danielle, Schnell, Christian, Sedrani, Richard, Shimizu, Toshio, Stringer, Rowan, Vaupel, Andrea, Voshol, Hans, Wessels, Peter, Widmer, Toni, Wilcken, Rainer, Xu, Kun, Zecri, Frederic, Farago, Anna F, Cotesta, Simona, Brachmann, Saskia M
Published in Cancer discovery (02.06.2022)
Published in Cancer discovery (02.06.2022)
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Medicinal Chemistry Profiling of Monocyclic 1,2‐Azaborines
Zhao, Peng, Nettleton, David O., Karki, Rajeshri G., Zécri, Frédéric J., Liu, Shih‐Yuan
Published in ChemMedChem (07.03.2017)
Published in ChemMedChem (07.03.2017)
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Water-Compatible Cycloadditions of Oligonucleotide-Conjugated Strained Allenes for DNA-Encoded Library Synthesis
Westphal, Matthias V, Hudson, Liam, Mason, Jeremy W, Pradeilles, Johan A, Zécri, Frédéric J, Briner, Karin, Schreiber, Stuart L
Published in Journal of the American Chemical Society (29.04.2020)
Published in Journal of the American Chemical Society (29.04.2020)
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Rational Screening for Cooperativity in Small-Molecule Inducers of Protein–Protein Associations
Liu, Shuang, Tong, Bingqi, Mason, Jeremy W., Ostrem, Jonathan M., Tutter, Antonin, Hua, Bruce K., Tang, Sunny A., Bonazzi, Simone, Briner, Karin, Berst, Frédéric, Zécri, Frédéric J., Schreiber, Stuart L.
Published in Journal of the American Chemical Society (25.10.2023)
Published in Journal of the American Chemical Society (25.10.2023)
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A Phenotypic Screen Identifies Calcium Overload as a Key Mechanism of β-Cell Glucolipotoxicity
Vogel, Jennifer, Yin, Jianning, Su, Liansheng, Wang, Sharon X, Zessis, Richard, Fowler, Sena, Chiu, Chun-Hao, Wilson, Aaron C, Chen, Amy, Zecri, Frederic, Turner, Gordon, Smith, Thomas M, DeChristopher, Brian, Xing, Heming, Rothman, Deborah M, Cai, Xinming, Berdichevsky, Alina
Published in Diabetes (New York, N.Y.) (01.05.2020)
Published in Diabetes (New York, N.Y.) (01.05.2020)
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Abstract P124: JDQ443, a covalent irreversible inhibitor of KRAS G12C, exhibits a novel binding mode and demonstrates potent anti-tumor activity and favorable pharmacokinetic properties in preclinical models
Brachmann, Saskia M., Weiss, Andreas, Guthy, Daniel A., Beyer, Kim, Voshol, Johannes, Maira, Michel, Prahallad, Anirudh, Porta, Diana Graus, Schnell, Christian, Ostermann, Nils, Vaupel, Andrea, Gerspacher, Marc, Leblanc, Catherine, Erdmann, Dirk, Sterker, Dario, Kerr, Grainne, Jerome, Giovannoni, Head, Victoria, Stringer, Rowan, De Kanter, Ruben, Jeff, Kearns, Roman, Danielle, Widmer, Toni, Wessels, Peter, Nunez, Eloisa Jimenez, Sedrani, Richard, Zecri, Frederic, Hofmann, Francesco, Engleman, Jeff, Lorthiois, Edwige, Cotesta, Simona
Published in Molecular cancer therapeutics (01.12.2021)
Published in Molecular cancer therapeutics (01.12.2021)
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DNA-encoded library-enabled discovery of proximity-inducing small molecules
Mason, Jeremy W, Chow, Yuen Ting, Hudson, Liam, Tutter, Antonin, Michaud, Gregory, Westphal, Matthias V, Shu, Wei, Ma, Xiaolei, Tan, Zher Yin, Coley, Connor W, Clemons, Paul A, Bonazzi, Simone, Berst, Frédéric, Briner, Karin, Liu, Shuang, Zécri, Frédéric J, Schreiber, Stuart L
Published in Nature chemical biology (01.02.2024)
Published in Nature chemical biology (01.02.2024)
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Discovery and characterization of a selective IKZF2 glue degrader for cancer immunotherapy
Bonazzi, Simone, d’Hennezel, Eva, Beckwith, Rohan E.J., Xu, Lei, Fazal, Aleem, Magracheva, Anna, Ramesh, Radha, Cernijenko, Artiom, Antonakos, Brandon, Bhang, Hyo-eun C., Caro, Roxana García, Cobb, Jennifer S., Ornelas, Elizabeth, Ma, Xiaolei, Wartchow, Charles A., Clifton, Matthew C., Forseth, Ry R., Fortnam, Bethany Hughes, Lu, Hongbo, Csibi, Alfredo, Tullai, Jennifer, Carbonneau, Seth, Thomsen, Noel M., Larrow, Jay, Chie-Leon, Barbara, Hainzl, Dominik, Gu, Yi, Lu, Darlene, Meyer, Matthew J., Alexander, Dylan, Kinyamu-Akunda, Jacqueline, Sabatos-Peyton, Catherine A., Dales, Natalie A., Zécri, Frédéric J., Jain, Rishi K., Shulok, Janine, Wang, Y. Karen, Briner, Karin, Porter, Jeffery A., Tallarico, John A., Engelman, Jeffrey A., Dranoff, Glenn, Bradner, James E., Visser, Michael, Solomon, Jonathan M.
Published in Cell chemical biology (16.03.2023)
Published in Cell chemical biology (16.03.2023)
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Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors
Hoegenauer, Klemens, Soldermann, Nicolas, Zécri, Frédéric, Strang, Ross S, Graveleau, Nadege, Wolf, Romain M, Cooke, Nigel G, Smith, Alexander B, Hollingworth, Gregory J, Blanz, Joachim, Gutmann, Sascha, Rummel, Gabriele, Littlewood-Evans, Amanda, Burkhart, Christoph
Published in ACS medicinal chemistry letters (14.09.2017)
Published in ACS medicinal chemistry letters (14.09.2017)
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