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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Journal Article
Retinoic-acid-orphan-receptor-C inhibition suppresses Th17 cells and induces thymic aberrations
Guntermann, Christine, Piaia, Alessandro, Hamel, Marie-Laure, Theil, Diethilde, Rubic-Schneider, Tina, Del Rio-Espinola, Alberto, Dong, Linda, Billich, Andreas, Kaupmann, Klemens, Dawson, Janet, Hoegenauer, Klemens, Orain, David, Hintermann, Samuel, Stringer, Rowan, Patel, Dhavalkumar D, Doelemeyer, Arno, Deurinck, Mark, Schümann, Jens
Published in JCI insight (09.03.2017)
Published in JCI insight (09.03.2017)
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Journal Article
Structural States of RORγt: X‐ray Elucidation of Molecular Mechanisms and Binding Interactions for Natural and Synthetic Compounds
Kallen, Joerg, Izaac, Aude, Be, Celine, Arista, Luca, Orain, David, Kaupmann, Klemens, Guntermann, Christine, Hoegenauer, Klemens, Hintermann, Samuel
Published in ChemMedChem (06.07.2017)
Published in ChemMedChem (06.07.2017)
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Journal Article
Paradoxical Increase of Permeability and Lipophilicity with the Increasing Topological Polar Surface Area within a Series of PRMT5 Inhibitors
Argikar, Upendra, Blatter, Markus, Bednarczyk, Dallas, Chen, Zhuoliang, Cho, Young Shin, Doré, Michaël, Dumouchel, Jennifer L., Ho, Samuel, Hoegenauer, Klemens, Kawanami, Toshio, Mathieu, Simon, Meredith, Erik, Möbitz, Henrik, Murphy, Stephen K., Parthasarathy, Saravanan, Soldermann, Carole Pissot, Santos, Jobette, Silver, Serena, Skolnik, Suzanne, Stojanovic, Aleksandar
Published in Journal of medicinal chemistry (22.09.2022)
Published in Journal of medicinal chemistry (22.09.2022)
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Journal Article
G‑Protein-Coupled Bile Acid Receptor 1 (GPBAR1, TGR5) Agonists Reduce the Production of Proinflammatory Cytokines and Stabilize the Alternative Macrophage Phenotype
Högenauer, Klemens, Arista, Luca, Schmiedeberg, Niko, Werner, Gudrun, Jaksche, Herbert, Bouhelal, Rochdi, Nguyen, Deborah G, Bhat, B. Ganesh, Raad, Layla, Rauld, Celine, Carballido, José M
Published in Journal of medicinal chemistry (26.12.2014)
Published in Journal of medicinal chemistry (26.12.2014)
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Journal Article
Structure-Based and Property-Driven Optimization of N‑Aryl Imidazoles toward Potent and Selective Oral RORγt Inhibitors
Hoegenauer, Klemens, Kallen, Joerg, Jiménez-Núñez, Eloísa, Strang, Ross, Ertl, Peter, Cooke, Nigel G, Hintermann, Samuel, Voegtle, Markus, Betschart, Claudia, McKay, Daniel J. J, Wagner, Juergen, Ottl, Johannes, Beerli, Christian, Billich, Andreas, Dawson, Janet, Kaupmann, Klemens, Streiff, Markus, Gobeau, Nathalie, Harlfinger, Stephanie, Stringer, Rowan, Guntermann, Christine
Published in Journal of medicinal chemistry (12.12.2019)
Published in Journal of medicinal chemistry (12.12.2019)
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Journal Article
Optimizing a Weakly Binding Fragment into a Potent RORγt Inverse Agonist with Efficacy in an in Vivo Inflammation Model
Carcache, David A, Vulpetti, Anna, Kallen, Joerg, Mattes, Henri, Orain, David, Stringer, Rowan, Vangrevelinghe, Eric, Wolf, Romain M, Kaupmann, Klemens, Ottl, Johannes, Dawson, Janet, Cooke, Nigel G, Hoegenauer, Klemens, Billich, Andreas, Wagner, Juergen, Guntermann, Christine, Hintermann, Samuel
Published in Journal of medicinal chemistry (09.08.2018)
Published in Journal of medicinal chemistry (09.08.2018)
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Journal Article
Discovery of novel pyrrolidineoxy-substituted heteroaromatics as potent and selective PI3K delta inhibitors with improved physicochemical properties
Hoegenauer, Klemens, Soldermann, Nicolas, Hebach, Christina, Hollingworth, Gregory J., Lewis, Ian, von Matt, Anette, Smith, Alexander B., Wolf, Romain M., Wilcken, Rainer, Haasen, Dorothea, Burkhart, Christoph, Zécri, Frédéric
Published in Bioorganic & medicinal chemistry letters (01.12.2016)
Published in Bioorganic & medicinal chemistry letters (01.12.2016)
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Journal Article
The 2nd Alpine Winter Conference on Medicinal and Synthetic Chemistry
Ciulli, Alessio, Hamann, Lawrence, Jahnke, Wolfgang, Kalgutkar, Amit S., Magauer, Thomas, Ritter, Tobias, Steadman, Vicky, Williams, Scott D., Winter, Georg, Hoegenauer, Klemens, Krawinkler, Karl Heinz, Stepan, Antonia F.
Published in ChemMedChem (05.08.2021)
Published in ChemMedChem (05.08.2021)
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Journal Article
The 2 nd Alpine Winter Conference on Medicinal and Synthetic Chemistry
Ciulli, Alessio, Hamann, Lawrence, Jahnke, Wolfgang, Kalgutkar, Amit S, Magauer, Thomas, Ritter, Tobias, Steadman, Vicky, Williams, Scott D, Winter, Georg, Hoegenauer, Klemens, Krawinkler, Karl Heinz, Stepan, Antonia F
Published in ChemMedChem (05.08.2021)
Published in ChemMedChem (05.08.2021)
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Journal Article
Discovery of Ligands for TRIM58, a Novel Tissue-Selective E3 Ligase
Hoegenauer, Klemens, An, Shaojian, Axford, Jake, Benander, Christina, Bergsdorf, Christian, Botsch, Josephine, Chau, Suzanne, Fernández, César, Gleim, Scott, Hassiepen, Ulrich, Hunziker, Juerg, Joly, Emilie, Keller, Aramis, Lopez Romero, Sandra, Maher, Robert, Mangold, Anne-Sophie, Mickanin, Craig, Mihalic, Manuel, Neuner, Philippe, Patterson, Andrew W., Perruccio, Francesca, Roggo, Silvio, Scesa, Julien, Schröder, Martin, Shkoza, Dojna, Thai, Binh, Vulpetti, Anna, Renatus, Martin, Reece-Hoyes, John S.
Published in ACS medicinal chemistry letters (14.12.2023)
Published in ACS medicinal chemistry letters (14.12.2023)
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Journal Article
Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors
Hoegenauer, Klemens, Soldermann, Nicolas, Stauffer, Frédéric, Furet, Pascal, Graveleau, Nadege, Smith, Alexander B, Hebach, Christina, Hollingworth, Gregory J, Lewis, Ian, Gutmann, Sascha, Rummel, Gabriele, Knapp, Mark, Wolf, Romain M, Blanz, Joachim, Feifel, Roland, Burkhart, Christoph, Zécri, 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
Structural States of ROR[gamma]t: X-ray Elucidation of Molecular Mechanisms and Binding Interactions for Natural and Synthetic Compounds
Kallen, Joerg, Izaac, Aude, Be, Celine, Arista, Luca, Orain, David, Kaupmann, Klemens, Guntermann, Christine, Hoegenauer, Klemens, Hintermann, Samuel
Published in ChemMedChem (01.07.2017)
Published in ChemMedChem (01.07.2017)
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Journal Article
S1P receptor mediated activity of FTY720 phosphate mimics
Högenauer, Klemens, Hinterding, Klaus, Nussbaumer, Peter
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
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Journal Article
Total Synthesis of Five Thapsigargins: Guaianolide Natural Products Exhibiting Sub-Nanomolar SERCA Inhibition
Andrews, Stephen P., Ball, Matthew, Wierschem, Frank, Cleator, Ed, Oliver, Steven, Högenauer, Klemens, Simic, Oliver, Antonello, Alessandra, Hünger, Udo, Smith, Martin D., Ley, Steven V.
Published in Chemistry : a European journal (06.07.2007)
Published in Chemistry : a European journal (06.07.2007)
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Journal Article
Synthesis of the thapsigargins
Ley, S.V, Antonello, A, Balskus, E.P, Booth, D.T, Christensen, S.B, Cleator, E, Gold, H, Hogenauer, K, Hunger, U, Myers, R.M
Published in Proceedings of the National Academy of Sciences - PNAS (17.08.2004)
Published in Proceedings of the National Academy of Sciences - PNAS (17.08.2004)
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Journal Article
DIHYDRO-BENZO-OXAZINE AND DIHYDRO-PYRIDO-OXAZINE DERIVATIVES
ZECRI FREDERIC, SOLDERMANN NICOLAS, WOLF ROMAIN, FURET PASCAL, CHAMOIN SYLVIE, HOEGENAUER KLEMENS, SMITH ALEXANDER BAXTER, KALIS CHRISTOPH, LEWIS IAN, CARAVATTI GIORGIO, HURTH KONSTANZE, KAMMERTOENS KAREN, MOEBITZ HENRIK
Year of Publication 04.09.2014
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Year of Publication 04.09.2014
Patent
USE OF INHIBITORS OF THE ACTIVITY OR FUNCTION OF PI3K
ZECRI FREDERIC, STAUFFER FREDERIC, SOLDERMANN NICOLAS, WOLF ROMAIN, FURET PASCAL, HOEGENAUER KLEMENS, SMITH ALEXANDER BAXTER, KALIS CHRISTOPH, HEBACH CHRISTINA, LEWIS IAN, STOWASSER FRANK, TUFILLI NICOLA, STRANG ROSS, VON MATT ANETTE, FERNANDES GOMES DOS SANTOS PAULO ANTONIO, COOKE NIGEL GRAHAM, HOLLINGWORTH GREGORY
Year of Publication 04.09.2014
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Year of Publication 04.09.2014
Patent