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Page 1
The First Class of Small Molecules Potently Disrupting the YAP-TEAD Interaction by Direct Competition.
Furet P, Bordas V, Le Douget M, Salem B, Mesrouze Y, Imbach-Weese P, Sellner H, Voegtle M, Soldermann N, Chapeau E, Wartmann M, Scheufler C, Fernandez C, Kallen J, Guagnano V, Chène P, Schmelzle T. Furet P, et al. Among authors: sellner h. ChemMedChem. 2022 Oct 6;17(19):e202200303. doi: 10.1002/cmdc.202200303. Epub 2022 Sep 2. ChemMedChem. 2022. PMID: 35950546
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. ChemMedChem. 2023 Jun 1;18(11):e202300051. doi: 10.1002/cmdc.202300051. Epub 2023 Apr 13. ChemMedChem. 2023. PMID: 36988034
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: sellner h. Nat Cancer. 2024 Apr 2. doi: 10.1038/s43018-024-00754-9. Online ahead of print. Nat Cancer. 2024. PMID: 38565920
The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches.
Lorthiois E, Breitenstein W, Cumin F, Ehrhardt C, Francotte E, Jacoby E, Ostermann N, Sellner H, Kosaka T, Webb RL, Rigel DF, Hassiepen U, Richert P, Wagner T, Maibaum J. Lorthiois E, et al. Among authors: sellner h. J Med Chem. 2013 Mar 28;56(6):2207-17. doi: 10.1021/jm3017078. Epub 2013 Mar 15. J Med Chem. 2013. PMID: 23425156
Small-molecule factor B inhibitor for the treatment of complement-mediated diseases.
Schubart A, Anderson K, Mainolfi N, Sellner H, Ehara T, Adams CM, Mac Sweeney A, Liao SM, Crowley M, Littlewood-Evans A, Sarret S, Wieczorek G, Perrot L, Dubost V, Flandre T, Zhang Y, Smith RJH, Risitano AM, Karki RG, Zhang C, Valeur E, Sirockin F, Gerhartz B, Erbel P, Hughes N, Smith TM, Cumin F, Argikar UA, Haraldsson B, Mogi M, Sedrani R, Wiesmann C, Jaffee B, Maibaum J, Flohr S, Harrison R, Eder J. Schubart A, et al. Among authors: sellner h. Proc Natl Acad Sci U S A. 2019 Apr 16;116(16):7926-7931. doi: 10.1073/pnas.1820892116. Epub 2019 Mar 29. Proc Natl Acad Sci U S A. 2019. PMID: 30926668 Free PMC article.
Structure-based design and synthesis of macrocyclic human rhinovirus 3C protease inhibitors.
Namoto K, Sirockin F, Sellner H, Wiesmann C, Villard F, Moreau RJ, Valeur E, Paulding SC, Schleeger S, Schipp K, Loup J, Andrews L, Swale R, Robinson M, Farady CJ. Namoto K, et al. Among authors: sellner h. Bioorg Med Chem Lett. 2018 Mar 1;28(5):906-909. doi: 10.1016/j.bmcl.2018.01.064. Epub 2018 Feb 1. Bioorg Med Chem Lett. 2018. PMID: 29433930
Discovery of 4-((2S,4S)-4-Ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases.
Mainolfi N, Ehara T, Karki RG, Anderson K, Mac Sweeney A, Liao SM, Argikar UA, Jendza K, Zhang C, Powers J, Klosowski DW, Crowley M, Kawanami T, Ding J, April M, Forster C, Serrano-Wu M, Capparelli M, Ramqaj R, Solovay C, Cumin F, Smith TM, Ferrara L, Lee W, Long D, Prentiss M, De Erkenez A, Yang L, Liu F, Sellner H, Sirockin F, Valeur E, Erbel P, Ostermeier D, Ramage P, Gerhartz B, Schubart A, Flohr S, Gradoux N, Feifel R, Vogg B, Wiesmann C, Maibaum J, Eder J, Sedrani R, Harrison RA, Mogi M, Jaffee BD, Adams CM. Mainolfi N, et al. Among authors: sellner h. J Med Chem. 2020 Jun 11;63(11):5697-5722. doi: 10.1021/acs.jmedchem.9b01870. Epub 2020 Feb 19. J Med Chem. 2020. PMID: 32073845
Complement factor B is critical for sub-RPE deposit accumulation in a model of Doyne honeycomb retinal dystrophy with features of age-related macular degeneration.
Crowley MA, Garland DL, Sellner H, Banks A, Fan L, Rejtar T, Buchanan N, Delgado O, Xu YY, Jose S, Adams CM, Mogi M, Wang K, Bigelow CE, Poor S, Anderson K, Jaffee BD, Prasanna G, Grosskreutz C, Fernandez-Godino R, Pierce EA, Dryja TP, Liao SM. Crowley MA, et al. Among authors: sellner h. Hum Mol Genet. 2023 Jan 6;32(2):204-217. doi: 10.1093/hmg/ddac187. Hum Mol Genet. 2023. PMID: 35943778 Free PMC article.
14 results