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Retinoic-acid-orphan-receptor-C inhibition suppresses Th17 cells and induces thymic aberrations.
Guntermann C, Piaia A, Hamel ML, Theil D, Rubic-Schneider T, Del Rio-Espinola A, Dong L, Billich A, Kaupmann K, Dawson J, Hoegenauer K, Orain D, Hintermann S, Stringer R, Patel DD, Doelemeyer A, Deurinck M, Schümann J. Guntermann C, et al. Among authors: kaupmann k. JCI Insight. 2017 Mar 9;2(5):e91127. doi: 10.1172/jci.insight.91127. JCI Insight. 2017. PMID: 28289717 Free PMC article.
Structure-Based and Property-Driven Optimization of N-Aryl Imidazoles toward Potent and Selective Oral RORγt Inhibitors.
Hoegenauer K, Kallen J, Jiménez-Núñez E, Strang R, Ertl P, Cooke NG, Hintermann S, Voegtle M, Betschart C, McKay DJJ, Wagner J, Ottl J, Beerli C, Billich A, Dawson J, Kaupmann K, Streiff M, Gobeau N, Harlfinger S, Stringer R, Guntermann C. Hoegenauer K, et al. Among authors: kaupmann k. J Med Chem. 2019 Dec 12;62(23):10816-10832. doi: 10.1021/acs.jmedchem.9b01291. Epub 2019 Dec 3. J Med Chem. 2019. PMID: 31729873
Optimizing a Weakly Binding Fragment into a Potent RORγt Inverse Agonist with Efficacy in an in Vivo Inflammation Model.
Carcache DA, Vulpetti A, Kallen J, Mattes H, Orain D, Stringer R, Vangrevelinghe E, Wolf RM, Kaupmann K, Ottl J, Dawson J, Cooke NG, Hoegenauer K, Billich A, Wagner J, Guntermann C, Hintermann S. Carcache DA, et al. Among authors: kaupmann k. J Med Chem. 2018 Aug 9;61(15):6724-6735. doi: 10.1021/acs.jmedchem.8b00529. Epub 2018 Jul 24. J Med Chem. 2018. PMID: 29990434
Discovery and Optimization of Novel SUCNR1 Inhibitors: Design of Zwitterionic Derivatives with a Salt Bridge for the Improvement of Oral Exposure.
Velcicky J, Wilcken R, Cotesta S, Janser P, Schlapbach A, Wagner T, Piechon P, Villard F, Bouhelal R, Piller F, Harlfinger S, Stringer R, Fehlmann D, Kaupmann K, Littlewood-Evans A, Haffke M, Gommermann N. Velcicky J, et al. Among authors: kaupmann k. J Med Chem. 2020 Sep 10;63(17):9856-9875. doi: 10.1021/acs.jmedchem.0c01020. Epub 2020 Aug 28. J Med Chem. 2020. PMID: 32856916
LRRK2 protein levels are determined by kinase function and are crucial for kidney and lung homeostasis in mice.
Herzig MC, Kolly C, Persohn E, Theil D, Schweizer T, Hafner T, Stemmelen C, Troxler TJ, Schmid P, Danner S, Schnell CR, Mueller M, Kinzel B, Grevot A, Bolognani F, Stirn M, Kuhn RR, Kaupmann K, van der Putten PH, Rovelli G, Shimshek DR. Herzig MC, et al. Among authors: kaupmann k. Hum Mol Genet. 2011 Nov 1;20(21):4209-23. doi: 10.1093/hmg/ddr348. Epub 2011 Aug 9. Hum Mol Genet. 2011. PMID: 21828077 Free PMC article.
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