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Page 1
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: stringer r. 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
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: stringer r. 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: stringer r. 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
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: stringer r. 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
JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors.
Lorthiois E, Gerspacher M, Beyer KS, Vaupel A, Leblanc C, Stringer R, Weiss A, Wilcken R, Guthy DA, Lingel A, Bomio-Confaglia C, Machauer R, Rigollier P, Ottl J, Arz D, Bernet P, Desjonqueres G, Dussauge S, Kazic-Legueux M, Lozac'h MA, Mura C, Sorge M, Todorov M, Warin N, Zink F, Voshol H, Zecri FJ, Sedrani RC, Ostermann N, Brachmann SM, Cotesta S. Lorthiois E, et al. Among authors: stringer r. J Med Chem. 2022 Dec 22;65(24):16173-16203. doi: 10.1021/acs.jmedchem.2c01438. Epub 2022 Nov 18. J Med Chem. 2022. PMID: 36399068
Optimization of Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for Duration of Action, as an Inhaled Therapy for Lung Remodeling in Pulmonary Arterial Hypertension.
Shaw DE, Baig F, Bruce I, Chamoin S, Collingwood SP, Cross S, Dayal S, Drückes P, Furet P, Furminger V, Haggart D, Hussey M, Konstantinova I, Loren JC, Molteni V, Roberts S, Reilly J, Saunders AM, Stringer R, Sviridenko L, Thomas M, Thomson CG, Tomlins C, Wen B, Yeh V, Pearce AC. Shaw DE, et al. Among authors: stringer r. J Med Chem. 2016 Sep 8;59(17):7901-14. doi: 10.1021/acs.jmedchem.6b00703. Epub 2016 Aug 19. J Med Chem. 2016. PMID: 27502700
Discovery and In Vivo Exploration of 1,3,4-Oxadiazole and α-Fluoroacrylate Containing IL-17 Inhibitors.
Velcicky J, Bauer MR, Schlapbach A, Lapointe G, Meyer A, Vögtle M, Blum E, Ngo E, Rolando C, Nimsgern P, Teixeira-Fouchard S, Lehmann H, Furet P, Berst F, Schümann J, Stringer R, Larger P, Schmid C, Prendergast CT, Riek S, Schmutz P, Lehmann S, Berghausen J, Scheufler C, Rondeau JM, Burkhart C, Knoepfel T, Gommermann N. Velcicky J, et al. Among authors: stringer r. J Med Chem. 2024 Sep 26;67(18):16692-16711. doi: 10.1021/acs.jmedchem.4c01520. Epub 2024 Sep 14. J Med Chem. 2024. PMID: 39276085
Thiazole-Based IL-17 Inhibitors Discovered by Scaffold Morphing.
Velcicky J, Ngo E, Bauer MR, Meyer A, Schlapbach A, Racine S, Orain D, Pflieger D, Teixeira-Fouchard S, Dubois C, Goetz A, Steiner R, Palmieri M, Bussenault A, Stringer R, Larger P, Riek S, Schmutz P, Lehmann S, Scheufler C, Rondeau JM, Burkhart C, Knoepfel T, Gommermann N. Velcicky J, et al. Among authors: stringer r. ChemMedChem. 2024 Dec 23:e202400851. doi: 10.1002/cmdc.202400851. Online ahead of print. ChemMedChem. 2024. PMID: 39715021
Discovery, optimization, and biological evaluation of 5-(2-(trifluoromethyl)phenyl)indazoles as a novel class of transient receptor potential A1 (TRPA1) antagonists.
Rooney L, Vidal A, D'Souza AM, Devereux N, Masick B, Boissel V, West R, Head V, Stringer R, Lao J, Petrus MJ, Patapoutian A, Nash M, Stoakley N, Panesar M, Verkuyl JM, Schumacher AM, Petrassi HM, Tully DC. Rooney L, et al. Among authors: stringer r. J Med Chem. 2014 Jun 26;57(12):5129-40. doi: 10.1021/jm401986p. Epub 2014 Jun 13. J Med Chem. 2014. PMID: 24884675
256 results