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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: schmelzle t. Nat Cancer. 2024 Apr 2. doi: 10.1038/s43018-024-00754-9. Online ahead of print. Nat Cancer. 2024. PMID: 38565920
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: schmelzle t. 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. Among authors: schmelzle t. ChemMedChem. 2023 Jun 1;18(11):e202300051. doi: 10.1002/cmdc.202300051. Epub 2023 Apr 13. ChemMedChem. 2023. PMID: 36988034
Cancer lineage-specific regulation of YAP responsive elements revealed through large-scale functional epigenomic screens.
Barbosa IAM, Gopalakrishnan R, Mercan S, Mourikis TP, Martin T, Wengert S, Sheng C, Ji F, Lopes R, Knehr J, Altorfer M, Lindeman A, Russ C, Naumann U, Golji J, Sprouffske K, Barys L, Tordella L, Schübeler D, Schmelzle T, Galli GG. Barbosa IAM, et al. Among authors: schmelzle t. Nat Commun. 2023 Jul 3;14(1):3907. doi: 10.1038/s41467-023-39527-w. Nat Commun. 2023. PMID: 37400441 Free PMC article.
Effect of the acylation of TEAD4 on its interaction with co-activators YAP and TAZ.
Mesrouze Y, Meyerhofer M, Bokhovchuk F, Fontana P, Zimmermann C, Martin T, Delaunay C, Izaac A, Kallen J, Schmelzle T, Erdmann D, Chène P. Mesrouze Y, et al. Among authors: schmelzle t. Protein Sci. 2017 Dec;26(12):2399-2409. doi: 10.1002/pro.3312. Epub 2017 Nov 11. Protein Sci. 2017. PMID: 28960584 Free PMC article.
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