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Page 1
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: scheufler c. ChemMedChem. 2024 Dec 23:e202400851. doi: 10.1002/cmdc.202400851. Online ahead of print. ChemMedChem. 2024. PMID: 39715021
Identification of TAK-756, A Potent TAK1 Inhibitor for the Treatment of Osteoarthritis through Intra-Articular Administration.
Langlois JB, Brenneisen S, Rodde S, Vangrevelinghe E, Rose G, Lerch P, Sorge M, Ullrich T, Patora-Komisarska K, Quancard J, Larger P, Gianola L, Textor C, Chenal G, Rubic-Schneider T, Simkova K, Masmanidou O, Scheufler C, Lammens A, Bouzan A, Demirci S, Flotte L, Rivet H, Hartmann L, Guezel D, Flueckiger M, Schilb A, Schuepbach E, Kettle R, Jacobi C, Pearson D, Richards PJ, Minetti GC. Langlois JB, et al. Among authors: scheufler c. J Med Chem. 2024 Dec 12;67(23):21163-21185. doi: 10.1021/acs.jmedchem.4c01938. Epub 2024 Nov 22. J Med Chem. 2024. PMID: 39576936
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: scheufler c. 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
Author Correction: Direct and selective pharmacological disruption of the YAP-TEAD interface by IAG933 inhibits Hippo-dependent and RAS-MAPK-altered cancers.
Chapeau EA, Sansregret L, Galli GG, Chène P, Wartmann M, Mourikis TP, Jaaks P, Baltschukat S, Barbosa IAM, Bauer D, Brachmann SM, Delaunay C, Estadieu C, Faris JE, Furet P, Harlfinger S, Hueber A, Jiménez Núñez E, Kodack DP, Mandon E, Martin T, Mesrouze Y, Romanet V, Scheufler C, Sellner H, Stamm C, Sterker D, Tordella L, Hofmann F, Soldermann N, Schmelzle T. Chapeau EA, et al. Among authors: scheufler c. Nat Cancer. 2024 Jul;5(7):1130. doi: 10.1038/s43018-024-00797-y. Nat Cancer. 2024. PMID: 38886525 Free PMC article. No abstract available.
Discovery of WRN inhibitor HRO761 with synthetic lethality in MSI cancers.
Ferretti S, Hamon J, de Kanter R, Scheufler C, Andraos-Rey R, Barbe S, Bechter E, Blank J, Bordas V, Dammassa E, Decker A, Di Nanni N, Dourdoigne M, Gavioli E, Hattenberger M, Heuser A, Hemmerlin C, Hinrichs J, Kerr G, Laborde L, Jaco I, Núñez EJ, Martus HJ, Quadt C, Reschke M, Romanet V, Schaeffer F, Schoepfer J, Schrapp M, Strang R, Voshol H, Wartmann M, Welly S, Zécri F, Hofmann F, Möbitz H, Cortés-Cros M. Ferretti S, et al. Among authors: scheufler c. Nature. 2024 May;629(8011):443-449. doi: 10.1038/s41586-024-07350-y. Epub 2024 Apr 24. Nature. 2024. PMID: 38658754 Free PMC article.
NIBR-LTSi is a selective LATS kinase inhibitor activating YAP signaling and expanding tissue stem cells in vitro and in vivo.
Namoto K, Baader C, Orsini V, Landshammer A, Breuer E, Dinh KT, Ungricht R, Pikiolek M, Laurent S, Lu B, Aebi A, Schönberger K, Vangrevelinghe E, Evrova O, Sun T, Annunziato S, Lachal J, Redmond E, Wang L, Wetzel K, Capodieci P, Turner J, Schutzius G, Unterreiner V, Trunzer M, Buschmann N, Behnke D, Machauer R, Scheufler C, Parker CN, Ferro M, Grevot A, Beyerbach A, Lu WY, Forbes SJ, Wagner J, Bouwmeester T, Liu J, Sohal B, Sahambi S, Greenbaum LE, Lohmann F, Hoppe P, Cong F, Sailer AW, Ruffner H, Glatthar R, Humar B, Clavien PA, Dill MT, George E, Maibaum J, Liberali P, Tchorz JS. Namoto K, et al. Among authors: scheufler c. Cell Stem Cell. 2024 Apr 4;31(4):554-569.e17. doi: 10.1016/j.stem.2024.03.003. Cell Stem Cell. 2024. PMID: 38579685
Direct and selective pharmacological disruption of the YAP-TEAD interface by IAG933 inhibits Hippo-dependent and RAS-MAPK-altered cancers.
Chapeau EA, Sansregret L, Galli GG, Chène P, Wartmann M, Mourikis TP, Jaaks P, Baltschukat S, Barbosa IAM, Bauer D, Brachmann SM, Delaunay C, Estadieu C, Faris JE, Furet P, Harlfinger S, Hueber A, Jiménez Núñez E, Kodack DP, Mandon E, Martin T, Mesrouze Y, Romanet V, Scheufler C, Sellner H, Stamm C, Sterker D, Tordella L, Hofmann F, Soldermann N, Schmelzle T. Chapeau EA, et al. Among authors: scheufler c. Nat Cancer. 2024 Jul;5(7):1102-1120. doi: 10.1038/s43018-024-00754-9. Epub 2024 Apr 2. Nat Cancer. 2024. PMID: 38565920 Free PMC article.
Optimization of a Class of Dihydrobenzofurane Analogs toward Orally Efficacious YAP-TEAD Protein-Protein Interaction Inhibitors.
Sellner H, Chapeau E, Furet P, Voegtle M, Salem B, Le Douget M, Bordas V, Groell JM, Le Goff AL, Rouzet C, Wietlisbach T, Zimmermann T, McKenna J, Brocklehurst CE, Chène P, Wartmann M, Scheufler C, Kallen J, Williams G, Harlfinger S, Traebert M, Dumotier BM, Schmelzle T, Soldermann N. Sellner H, et al. Among authors: scheufler c. ChemMedChem. 2023 Jun 1;18(11):e202300051. doi: 10.1002/cmdc.202300051. Epub 2023 Apr 13. ChemMedChem. 2023. PMID: 36988034
40 results