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Page 1
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: wartmann m. Nat Cancer. 2024 Apr 2. doi: 10.1038/s43018-024-00754-9. Online ahead of print. Nat Cancer. 2024. PMID: 38565920
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: wartmann m. ChemMedChem. 2023 Jun 1;18(11):e202300051. doi: 10.1002/cmdc.202300051. Epub 2023 Apr 13. ChemMedChem. 2023. PMID: 36988034
INPP5A phosphatase is a synthetic lethal target in GNAQ and GNA11-mutant melanomas.
Elbatsh AMO, Amin-Mansour A, Haberkorn A, Textor C, Ebel N, Renard E, Koch LM, Groenveld FC, Piquet M, Naumann U, Ruddy DA, Romanet V, Martínez Gómez JM, Shirley MD, Wipfli P, Schnell C, Wartmann M, Rausch M, Jager MJ, Levesque MP, Maira SM, Manchado E. Elbatsh AMO, et al. Among authors: wartmann m. Nat Cancer. 2024 Mar;5(3):481-499. doi: 10.1038/s43018-023-00710-z. Epub 2024 Jan 17. Nat Cancer. 2024. PMID: 38233483 Free PMC article.
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: wartmann m. 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.
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: wartmann m. ChemMedChem. 2022 Oct 6;17(19):e202200303. doi: 10.1002/cmdc.202200303. Epub 2022 Sep 2. ChemMedChem. 2022. PMID: 35950546
Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor.
Fairhurst RA, Furet P, Imbach-Weese P, Stauffer F, Rueeger H, McCarthy C, Ripoche S, Oswald S, Arnaud B, Jary A, Maira M, Schnell C, Guthy DA, Wartmann M, Kiffe M, Desrayaud S, Blasco F, Widmer T, Seiler F, Gutmann S, Knapp M, Caravatti G. Fairhurst RA, et al. Among authors: wartmann m. J Med Chem. 2022 Jun 23;65(12):8345-8379. doi: 10.1021/acs.jmedchem.2c00267. Epub 2022 May 2. J Med Chem. 2022. PMID: 35500094
Discovery of Potent, Highly Selective, and In Vivo Efficacious, Allosteric MALT1 Inhibitors by Iterative Scaffold Morphing.
Pissot Soldermann C, Simic O, Renatus M, Erbel P, Melkko S, Wartmann M, Bigaud M, Weiss A, McSheehy P, Endres R, Santos P, Blank J, Schuffenhauer A, Bold G, Buschmann N, Zoller T, Altmann E, Manley PW, Dix I, Buchdunger E, Scesa J, Quancard J, Schlapbach A, Bornancin F, Radimerski T, Régnier CH. Pissot Soldermann C, et al. Among authors: wartmann m. J Med Chem. 2020 Dec 10;63(23):14576-14593. doi: 10.1021/acs.jmedchem.0c01245. Epub 2020 Nov 30. J Med Chem. 2020. PMID: 33252239
Optimization of the In Vivo Potency of Pyrazolopyrimidine MALT1 Protease Inhibitors by Reducing Metabolism and Increasing Potency in Whole Blood.
Quancard J, Simic O, Pissot Soldermann C, Aichholz R, Blatter M, Renatus M, Erbel P, Melkko S, Endres R, Sorge M, Kieffer L, Wagner T, Beltz K, Mcsheehy P, Wartmann M, Régnier CH, Calzascia T, Radimerski T, Bigaud M, Weiss A, Bornancin F, Schlapbach A. Quancard J, et al. Among authors: wartmann m. J Med Chem. 2020 Dec 10;63(23):14594-14608. doi: 10.1021/acs.jmedchem.0c01246. Epub 2020 Nov 20. J Med Chem. 2020. PMID: 33216547
78 results